Search Result
Results for "
ERK phosphorylation
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P3751
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-
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- HY-114436
-
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Ras
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Cancer
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MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
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- HY-124097
-
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Insulin Receptor
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Metabolic Disease
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HNMPA-(AM)3 is a cell-permeable and selective insulin receptor tyrosine kinase inhibitor analog of HNMPA. HNMPA-(AM)3 greatly inhibits the ability of prothoracicotropic hormone (PTTH) to activate ERK phosphorylation and stimulate ecdysteroidogenesis. HNMPA-(AM)3 is also effective in inhibiting ecdysteroid production (IC50=14.2 μM) and insulin receptor activity (IC50 is 14.2 μM and 200 μM in mosquitoes and mammals, respectively) .
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- HY-113592
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ERK
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Cancer
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ERK-IN-4 is an ERK inhibitor binds preferentially to ERK2 with a Kd of 5 μM. ERK-IN-4 specificity inhibits ERK Rsk-1 and Elk-1 phosphorylation. ERK-IN-4 has little effect on ERK protein phosphorylation by its upstream activator MEK1/2 .
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- HY-157787
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LPL Receptor
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Neurological Disease
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Ginkgolic acid 2-phosphate is a potent sphingosine 1-phosphate agonist. Ginkgolic acid 2-phosphate induces ERK phosphorylation. Ginkgolic acid 2-phosphate interactes with S1P1 .
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- HY-146319
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-
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- HY-114436S
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Isotope-Labeled Compounds
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Cancer
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MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
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- HY-18849
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ERK
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Cancer
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ERK2-IN-3 (compound 2) is a inhibitor of ERK2, and inhibits Erk2 WT and Erk2 DS1 activation loop phosphorylation, with IC50 of 5 μM and 42 nM, respectively .
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- HY-P5977
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Ste-MPKKKPTPIQLNP-NH₂; ERK Activation Inhibitor Peptide
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ERK
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Cancer
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STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH ) is a cell permeable ERK1/2 inhibitor (IC50: 13-30 μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
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- HY-W838814
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ERK
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Cancer
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ERK1/2 inhibitor 12 (compound 76.3) is a ERK1/2 inhibitor which inhibits ERK-mediated phosphorylation of caspase-9 and the p90Rsk-1 kinase. ERK1/2 inhibitor 12 exhibits anti-cancer activity and can be utilized in cancer research .
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- HY-N9725
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16ξ-Hydroxycleroda-3,13-dien-15,16-olide
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Dipeptidyl Peptidase
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Metabolic Disease
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16-Hydroxycleroda-3,13-dien-15,16-olide (16ξ-Hydroxycleroda-3,13-dien-15,16-olide; HCD), a clerodane diterpene, is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. 16-Hydroxycleroda-3,13-dien-15,16-olide exhibits hypolipidemic, hepatoprotective, hypoglycemic efficacy .
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- HY-122246
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GPR55
PKC
ERK
Arrestin
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Metabolic Disease
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ML192 is a selective ligand antagonist of GPR55. ML192 inhibits the β-arrestin trafficking, ERK1/2 phosphorylation and PKCβII translocation .
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- HY-124740
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Melanocortin Receptor
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Cancer
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ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity .
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- HY-50706
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Selumetinib
Maximum Cited Publications
65 Publications Verification
AZD6244; ARRY-142886
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MEK
Apoptosis
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Cancer
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Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
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- HY-50706A
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AZD6244 sulfate; ARRY-142886 sulfate
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MEK
Apoptosis
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Cancer
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Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
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- HY-108330
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AG126
2 Publications Verification
Tyrphostin AG126
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ERK
Mitosis
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Inflammation/Immunology
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AG126 is a tyrosine kinase inhibitor, can inhibit the phosphorylation of ERK1 and ERK2 at 25-50 μM. AG126 can be used in meiosis, mitosis, and postmitotic research .
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- HY-162460
-
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ERK
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Cancer
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ERK1/2 inhibitor 10 (Compound 36c) is a potent ERK1 and ERK2 inhibitor (IC50: 0.11 and 0.08 nM respectively). ERK1/2 inhibitor 10 inhibits ERK1/2 and blocks the phosphorylation expression of their downstream substrates p90RSK and c-Myc. ERK1/2 inhibitor 10 induces cell apoptosis and incomplete autophagy-related cell death. ERK1/2 inhibitor 10 shows potent antitumor efficacy against triple-negative breast cancer and colorectal cancer models harboring BRAF and RAS mutations .
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- HY-N2858
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Apoptosis
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Cancer
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Alpinumisoflavone acetate is a anticancer agent. Alpinumisoflavone acetate shows antiproliferative activity. Alpinumisoflavone acetate decreases the expression of phosphorylation of ERK1/2. Alpinumisoflavone acetate induces mitochondrial dysfunction and mitochondria-mediated Apoptosis. Alpinumisoflavone acetate has the potential for the research of HCC .
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- HY-13241
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LY2228820 dimesylate
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p38 MAPK
Autophagy
Apoptosis
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Inflammation/Immunology
Cancer
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Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
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- HY-N1987
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Apoptosis
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Inflammation/Immunology
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Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
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- HY-150700
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ERK
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Metabolic Disease
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RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .
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- HY-13241A
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LY2228820
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p38 MAPK
Autophagy
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Inflammation/Immunology
Cancer
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Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .
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- HY-12960
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FLT3-IN-1
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FLT3
c-Kit
Apoptosis
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Cancer
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SKLB4771 is a potent and selective Flt3 inhibitor with an IC50 value of 10 nM. SKLB4771 downregulates the phosphorylation of FLT3/STAT5/ERK, blocks cell proliferation, and induces apoptosis in tumor tissue .
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- HY-76474A
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Apoptosis
Syk
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Inflammation/Immunology
Cancer
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BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
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- HY-153445
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ERK
MEK
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Cancer
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MEK-IN-6 (Example 69) is a MEK inhibitor. MEK-IN-6 inhibits ERK1/2 (Thr202/Tyr204) phosphorylation in A375 cells (IC50: 2 nM). MEK-IN-6 can be used for research of cancer .
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- HY-76474
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Syk
Apoptosis
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Inflammation/Immunology
Cancer
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BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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- HY-14985
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Syk
Apoptosis
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Inflammation/Immunology
Cancer
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BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
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- HY-P1342
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Orphan Receptor
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Neurological Disease
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Prosaptide Tx14(A), a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) increases both ERK1 and ERK2 phosphorylation in Schwann cells .
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- HY-N1966
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p38 MAPK
JNK
ERK
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Neurological Disease
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(E)-Osmundacetone is the isomer of Osmundacetone. Osmundacetone significantly suppresses the phosphorylation of MAPKs, including JNK, ERK, and p38 kinases. Osmundacetone has a neuroprotective effect against oxidative stress .
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- HY-170916
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ERK
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Inflammation/Immunology
Cancer
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Angiogenesis inhibitor 7 (compound BT2) ia a potent inhibitor of angiogenesis. Angiogenesis inhibitor 7 inhibits ERK phosphorylation, FosB/ΔFosB and VCAM-1 expression .
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- HY-N2270
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p38 MAPK
ERK
IKK
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Inflammation/Immunology
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Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity .
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- HY-147301
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AP1189
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Melanocortin Receptor
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Metabolic Disease
Inflammation/Immunology
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Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research .
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- HY-155533
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SHP2
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Cancer
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YF704 (compound 4w) is a selective allosteric inhibitor of SHP2 (IC50=0.25 μM). YF704 shows antiproliferative activity and induces apoptosis in cancer cells. YF704 also downregulates Erk1/2 and Akt phosphorylation levels in cancer cells .
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- HY-P1342A
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ERK
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Neurological Disease
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Prosaptide Tx14(A) TFA, a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells .
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- HY-147301A
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AP1189 acetate
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Melanocortin Receptor
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Metabolic Disease
Inflammation/Immunology
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Resomelagon (AP1189) acetate is a potent, orally active melanocortin receptor (MR) agonist about MC1 and MC3. Resomelagon acetate induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon acetate has anti-inflammatory activity. Resomelagon acetate can be used for obesity and chronic inflammation research .
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- HY-N1987R
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Apoptosis
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Inflammation/Immunology
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Cucurbitacin IIb (Standard) is the analytical standard of Cucurbitacin IIb. This product is intended for research and analytical applications. Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
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- HY-N2362R
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Endogenous Metabolite
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Metabolic Disease
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Cucurbitacin IIb (Standard) is the analytical standard of Cucurbitacin IIb. This product is intended for research and analytical applications. Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
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- HY-100403
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mGluR
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Cancer
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Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
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- HY-P5986
-
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ERK
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Others
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mSIRK (L9A) is a cell-permeable, N-myristoylated G-Protein Binding Peptide (mSIRK). mSIRK (L9A) contains a single point mutation (Leu9 to Ala). mSIRK (L9A) cannot enhance ERK1/2 phosphorylation. mSIRK (L9A) can be used as a control peptide .
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- HY-110318
-
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CXCR
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Inflammation/Immunology
Cancer
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VUF11207 fumarate is a CXCR7 agonist that binds specifically to CXCR7. VUF11207 fumarate reduces CXCL12-mediated osteoclastogenesis and bone resorption by inhibiting ERK phosphorylation .
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- HY-107640
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MMP
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Cancer
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WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC50 of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer research .
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- HY-P3750
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-
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- HY-124404A
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ERK
DNA/RNA Synthesis
p38 MAPK
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Cancer
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12(S)-HETE is the 12-lipoxygenase metabolite of arachidonic acid and has a mitogenic effect on cancer cell proliferation. 12(S)-HETE induces tyrosine phosphorylation of cellular proteins, promotes ERK and P38 MAPK phosphorylation, increases DNA synthesis, and stimulates the proliferation of pancreatic cancer cells .
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- HY-113599
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EGFR
ERK
Akt
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Others
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Isoprocurcumenol is a guaiane type sesquiterpene, that can be isolated from Curcuma comosa. Isoprocurcumenol can activate EGFR signaling. Isoprocurcumenol increases the phosphorylation of ERK and AKT. Isoprocurcumenol promotes the proliferation of keratinocytes .
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- HY-146672
-
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Itk
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Cancer
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ITK inhibitor 6 (compound 43) is a potent and selective ITK inhibitor with IC50s of 4 nM, 133 nM, 320 nM, 2360 nM, 155 nM for ITK, BTK, JAK3, EGFR, LCK, respectively. ITK inhibitor 6 inhibits phosphorylation of PLCγ1 and ERK1/2. ITK inhibitor 6 shows antiproliferative activities .
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- HY-126477
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NNK
1 Publications Verification
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Endogenous Metabolite
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Cancer
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NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser 70 and c-Myc at Thr 58 and Ser 62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
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- HY-15496
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ER-806201
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MEK
FLT3
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Cancer
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E6201 (ER-806201) is an ATP-competitive dual kinase inhibitor of MEK1 and FLT3. E6201 inhibits MEK1- induced ERK2 phosphorylation with an IC50 value of 5.2 nM, MKK4-induced JNK phosphorylation with an IC50 value of 91 nM, and MKK6-induced p38 MAPK phosphorylation with an IC50 value of 19 nM. Anti-tumor and anti-psoriasis efficacy .
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-
- HY-163283
-
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Amyloid-β
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Neurological Disease
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6’-Methyl paeonol is a paeonol derivative, which inihibits abnormal depolarizations and reduces the Amyloid β-induced ERK phosphorylation. 6’-Methyl paeonol exhibits alleviating activity against Alzheimer’s Disease .
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- HY-155417
-
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ERK
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Neurological Disease
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GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680?μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
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- HY-16697
-
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GPR55
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Cancer
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CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca 2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function .
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- HY-N10047
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NF-κB
PPAR
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Cardiovascular Disease
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7,8-Didehydrocimigenol is an active triterpenoid that can be isolated from Cimicifugae rhizoma. 7,8-Didehydrocimigenol inhibits TNF-α-induced VCAM-1 expression, inhibits NF-kB activity and phosphorylation of ERK1/2 and Akt, increases PPAR-γ expression. 7,8-Didehydrocimigenol can be used for the research of cardiovascular disorders such as atherosclerosis .
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- HY-P0178
-
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Integrin
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Inflammation/Immunology
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LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
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- HY-13905
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HHGV678 mesylate
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Bcr-Abl
c-Kit
PDGFR
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Cancer
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Flumatinib (HHGV678) mesylate is an orally active and selective inhibitor of Bcr-Abl. Flumatinib mesylate inhibits c-Abl, PDGFRβ and c-Kit with IC50 values of 1.2, 307.6 and 665.5 nM, respectively. Flumatinib mesylate inhibits Bcr-Abl autophosphorylation and Stat5 and Erk1/2 phosphorylation. Flumatinib mesylate inhibits tumor growth in chronic myelogenous leukemia model .
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- HY-154985
-
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PPAR
Bombesin Receptor
ERK
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Metabolic Disease
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DSO-5a is a potent, selective, orally active BB3 agonist. DSO-5a is a representative DMAKO-00 derivative compound. DSO-5a upregulates ppar-γ activity through BB3 and activates ERK1/2 phosphorylation. DSO-5a can be used in diabetes-related research .
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- HY-P99183
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EMD 525797; DI17E6
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Integrin
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Cancer
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Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer .
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- HY-N0774
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ERK
COX
MMP
Toll-like Receptor (TLR)
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Inflammation/Immunology
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Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .
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- HY-162616
-
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HDAC
Apoptosis
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Cancer
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SelSA is a selective, orally active inhibitor for histone deacetylase 6 (HDAC6) with IC50 of 56.9 nM. SelSA inhibits the phosphorylation of ERK1/2. SelSA inhibits the proliferation of breast cancer cells and hepatocellular carcinoma cells with IC50 of 0.58-2.6 μM, inhibits cell migration and invasion of Huh7, and induces apoptosis. SelSA exhibits antitumor activity in mouse model .
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- HY-P0178A
-
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Integrin
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Inflammation/Immunology
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LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
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- HY-111083
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CID23612552
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GPR55
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Others
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ML-191 is an antagonist of GPR55. It inhibits GPR55 signaling induced by lysophosphatidylinositol (EC50=1.076 µM in U2OS cells overexpressing GPR55). ML-191 inhibits LPI-induced phosphorylation of ERK1/2 (IC50=328 nM) and receptor-dependent translocation of PKCβII when used at a concentration of 30 µM .
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- HY-147301B
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AP1189 methanesulfonate
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Melanocortin Receptor
ERK
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Inflammation/Immunology
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Resomelagon methanesulfonate (AP1189 methanesulfonate) is the methanesulfonate salt form of Resomelagon (HY-147301). Resomelagon methanesulfonate is an orally active melanocortin receptor (MR) agonist. Resomelagon methanesulfonate induces ERK1/2 phosphorylation and Ca 2+ mobilization. Resomelagon methanesulfonate exhibits anti-inflammatory activity in mouse peritonitis and peritonitis model. Resomelagon methanesulfonate can be used for obesity and chronic inflammation research .
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- HY-147259
-
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c-Met/HGFR
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Cancer
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Dalmelitinib is an orally active selective c-Met kinase inhibitor (IC50: 2.9 nM) that binds to the ATP-binding region of c-Met. Dalmelitinib induces the phosphorylation of MET, partially or completely inhibits the phosphorylation of AKT and ERK. Dalmelitinib potently inhibits cancer cell (c-Met oncogene amplification) proliferation, and is used for the research of cancers like human non-small cell lung cancer (NSCLC) .
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- HY-153606
-
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Ras
SOS1
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Cancer
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SOS1 agonist-1 (compound 79) is an agonist for the Son of sevenless homologue SOS1. SOS1 is a guanine nucleotide exchange factor that catalyzes the exchange of GDP to GTP on RAS and regulates RAS activation. SOS1 agonists increase nucleotide exchange on RAS, enhance cellular RAS-GTP levels, and trigger biphasic signaling changes in ERK1/2 phosphorylation. Play an anti-cancer role [1] .
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- HY-D0205A
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Carbocysteine
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NF-κB
PERK
Keap1-Nrf2
Apoptosis
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Infection
Inflammation/Immunology
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Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
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- HY-108554
-
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Protease Activated Receptor (PAR)
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Others
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Q94 hydrochloride, a selective PAR1 antagonist (IC50=916 nM), can selectively block PAR1/Gαq interaction and signalling. Q94 hydrochloride blocks PAR1-mediated increases in both CCL2 mRNA and protein levels in a dose-dependent manner. Q94 hydrochloride also completely blocks thrombin-induced ERK1/2 and MLC phosphorylation .
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- HY-130176
-
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Opioid Receptor
ERK
Adenylate Cyclase
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Neurological Disease
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UFP-512 is a selective and potent σ-opioid receptor (DOP receptor) peptidic agonist with antidepressant- and anxiolytic-like effects. UFP-512 exhibits as a potent agonist on adenylyl cyclase inhibition and Erk1/2 activation. UFP-512 induces phosphorylation of DOP receptors on Ser 363 with a low desensitization of the cAMP pathway. UFP-512 is promising for research of mood disorders .
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- HY-N1504
-
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PAI-1
Potassium Channel
ERK
JNK
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Metabolic Disease
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
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- HY-107426
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Muconomycin A
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Apoptosis
Reactive Oxygen Species
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Cancer
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Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53 .
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-
- HY-119460
-
|
ERK
|
Neurological Disease
|
Cuspin-1 is a upregulator of Survival of Motor Neuron protein (SMN). Cuspin-1 upregulates SMN expression post-transcriptionally, and increases the phosphorylation of Erk. Cuspin-1 can be used for research of neurodegenerative disease, such as spinal muscular atrophy (SMA) .
|
-
- HY-151379
-
|
Histone Methyltransferase
|
Cancer
|
EM127 (compound 11c) is a SMYD3 covalent inhibitor with high selectivity, high affinity (KD=13 μM) and site-specificity. EM127 effectively inhibits ERK1/2 phosphorylation and reduces transcriptional regulation of SMYD3 target genes. EM127 effectively and prolongedly impairs methyltransferase activity. EM127 can be used in cancer research, particularly in SMYD3 positive tumours .
|
-
- HY-117982
-
|
GnRH Receptor
ERK
|
Endocrinology
|
SKI2496 is an orally active GnRH receptor antagonist (IC50: 0.25 nM for hGnRHR, 13.2 nM for monkey GnRHR, 279.2 nM for rat GnRHR). SKI2496 blocks Ca 2+ flux with an IC50 value of 0.76 nM. SKI2496 inhibits ERK1/2 phosphorylation with an IC50 value of 2.6 nM. SKI2496 inhbits serum LH concentrations, and can be used for research of sex hormone-dependent disorders .
|
-
- HY-149759
-
|
SHP2
ERK
|
Cancer
|
SHP2-IN-23 (compound 30) is an orally active SHP2 inhibitor (IC50=38 nM) with excellent in vivo efficacy and pharmacokinetic profiles. SHP2-IN-23 inhibits ERK phosphorylation with IC50=5 nM .
|
-
- HY-161145
-
|
EGFR
Apoptosis
Microtubule/Tubulin
|
Cancer
|
EGFR/microtubule-IN-1 (Compound 10c) is a dual inhibitor targeting EGFR and tubulin. The IC50 for inhibiting EGFR is 10.66 nM. EGFR/microtubule-IN-1 can reduce the phosphorylation levels of EGFR, AKT and ERK, hinder tubulin polymerization, and induce apoptosis .
|
-
- HY-N11439
-
|
CDK
Akt
ERK
Apoptosis
Bacterial
|
Infection
Neurological Disease
Cancer
|
Albanol B is an arylbenzofuran derivative which can be isolated from mulberries. Albanol B exhibits anti-Alzheimer's disease, anti-bacterial and antioxidant activities. Albanol B inhibits cancer cells proliferation, down-regulates CDK1 expression. Albanol B also induces cell cycle arrest at G2/M and apoptosis. And Albanol B induces mitochondrial ROS production and increases the phosphorylation levels of AKT and ERK1/2 .
|
-
- HY-N2484
-
Astrapterocarpan
|
PDGFR
ERK
|
Cardiovascular Disease
|
Methylnissolin (Astrapterocarpan), isolated from Astragalus membranaceus, inhibits platelet-derived growth factor (PDGF)-BB-induced cell proliferation with an IC50 of 10 μM. Methylnissolin inhibits PDGF-BB-induced phosphorylation of extracellular signal-regulated kinase 1/2 (ERIC1/2) mitogen-activated protein (MAP) kinase. Methylnissolin inhibits PDGF-BB-induced vascular smooth muscle cell proliferation by inhibition of the ERK1/2 MAP kinase cascade .
|
-
- HY-126477R
-
|
Endogenous Metabolite
|
Cancer
|
NNK (Standard) is the analytical standard of NNK. This product is intended for research and analytical applications. NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser70 and c-Myc at Thr58 and Ser62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
|
-
- HY-153864
-
|
PROTACs
MEK
ERK
|
Cancer
|
PROTAC MEK1 Degrader-1 is a PROTAC targeting MEK1 with a pIC50 value of 7.0. PROTAC MEK1 Degrader-1 consists of a MEK1 inhibitor and a von Hippel-Lindau ligand. PROTAC MEK1 Degrader-1 can inhibit ERK1/2 phosphorylation. PROTAC MEK1 Degrader-1 shows an antiproliferative activity against A375 cells .
|
-
- HY-108559
-
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
L-161982 is a selective EP4 receptor antagonist. L-161982 completely blocks PGE2-induced ERK phosphorylation and cell proliferation of HCA-7 cells. L-161982 alleviates collagen-induced arthritis in mice .
|
-
- HY-N9866
-
|
Others
|
Inflammation/Immunology
|
It is a bioactive compound with anti-inflammatory activity that inhibits LPS-induced NO production in RAW 264.7 cells and acts by inhibiting the phosphorylation of MAPK (ERK, JNK and p38) and NF-κB p65. Grasshopper ketone, as an ingredient, has shown its potential in anti-inflammatory inhibition .
|
-
- HY-101246
-
|
RET
|
Cancer
|
RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .
|
-
- HY-149710
-
|
ICMT
ERK
|
Cancer
|
POP-3MB (compound 1b) is an ICMT inhibitor (IC50: 2.5 μM). POP-3MB changes the subcellular localization of K-Ras and inhibits Ras activation. POP-3MB also inhibits Erk phosphorylation .
|
-
- HY-17600
-
ACP-196
|
Btk
|
Cancer
|
Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17600S
-
ACP-196-d4
|
Btk
|
Cancer
|
Acalabrutinib-d4 is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor . Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-17600R
-
|
Btk
|
Cancer
|
Acalabrutinib (Standard) is the analytical standard of Acalabrutinib. This product is intended for research and analytical applications. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor. Acalabrutinib binds covalently to Cys481 in the ATP-binding pocket of BTK. Acalabrutinib demonstrates potent on-target effects and efficacy in mouse models of chronic lymphocytic leukemia (CLL) . Acalabrutinib is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N0774R
-
|
ERK
COX
MMP
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
Isofraxidin (Standard) is the analytical standard of Isofraxidin. This product is intended for research and analytical applications. Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .
|
-
- HY-D0205AS2
-
Carbocysteine-d3
|
Isotope-Labeled Compounds
|
Infection
Inflammation/Immunology
|
Carbocisteine-d3 (Carbocysteine-d3) is deuterium labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-N12561
-
|
ERK
p38 MAPK
JNK
|
Others
|
Pestanoid A is a rearranged pimarane diterpenoid osteoclastogenesis inhibitor with an IC50 of 4.2 μM. Pestanoid A can be isolated from the marine mesophotic zone chalinidae sponge-associated fungus, Pestalotiopsis sp. NBUF145. Pestanoid A inhibits the receptor activator of NF-kB ligand-induced MAPK and NF-κB signaling by suppressing the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and NF-κB nuclear translocation. Pestanoid A can be used for the study of osteoporosis .
|
-
- HY-129636A
-
GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
|
-
- HY-18318
-
|
Raf
VEGFR
PERK
|
Cancer
|
Takeda-6D (compound 6d) is an orally active and potent BRAF/VEGFR2 inhibitor, with IC50 values of 7.0 and 2.2 nM, respectively. Takeda-6D shows antiangiogenesis by suppressing the VEGFR2 pathway in 293/KDR and VEGF-stimulated HUVEC cells.Takeda-6D shows significant suppression of ERK1/2 phosphorylation. Takeda-6D shows antitumor activity .
|
-
- HY-116461
-
CID2440433
|
GPR55
|
Neurological Disease
|
ML-184 (CID244033) is a selective GPR55 agonist with an EC50 of 250 nM, more than 100-fold selectivity for GPR55 over GPR35, CB1, and CB2. ML-184 induces ERK1/2 phosphorylation and PKCβII translocation to the plasma membrane via activation of GPR55. ML-184 (CID2440433) increases the proliferation of neural stem cells and promotes neuronal differentiation in vitro .
|
-
- HY-164551
-
|
VEGFR
STAT
ERK
Apoptosis
|
Cancer
|
YLL545 is a type of vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor. YLL545 can inhibit VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling factors (like phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). YLL545 can suppress the proliferation, migration, invasion, and angiogenesis of HUVEC. YLL545 can induce apoptosis in breast cancer mice and inhibit tumor growth .
|
-
- HY-N7140
-
γ-Linolenic acid
|
Endogenous Metabolite
Apoptosis
NF-κB
ERK
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Gamma-linolenic acid (γ-Linolenic acid) is an orally active unsaturated fatty acid. Gamma-linolenic acid exerts anti-inflammatory effects by inhibiting the NF-κB pathway and the phosphorylation of ERK1/2 and JNK. At the same time, it exerts anticancer effects by inducing apoptosis (Apoptosis) in cancer cells. Additionally, Gamma-linolenic acid also has antioxidant and memory-improving effects. It holds promise for research in the fields of inflammation, neurology, and cancer diseases .
|
-
- HY-P99768
-
TTAC-0001
|
VEGFR
|
Cancer
|
Olinvacimab (TTAC-0001) is a fully human anti-VEGFR2 monoclonal antibody. Olinvacimab inhibits VEGF binds to KDR with a Kd value of 0.23 nM. Olinvacimab has antiangiogenic activity. Olinvacimab can be used for the research of recurrent glioblastoma and breast cancer .
|
-
- HY-N6670
-
|
Antibiotic
Raf
ERK
Ras
MEK
Bacterial
|
Infection
|
Cefotetan is a binding agent that targets human Raf1 kinase inhibitor protein (hRKIP). Cefotetan binds to hRKIP, reduces the binding space between hRKIP and Raf1 kinase, relieves hRKIP's inhibition of the Ras/Raf1/MEK/ERK signaling pathway, and enhances ERK phosphorylation. Cefotetan can be used to study diseases associated with dysregulated Ras/Raf1/MEK/ERK signaling pathways. Cefotetan is also a broad-spectrum antibacterial agent that disrupts cell wall synthesis by binding to bacterial penicillin-binding proteins (PBPs). It is used to study bacterial infections such as bone, skin, urinary tract, and lower respiratory tract .
|
-
- HY-N0103A
-
|
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MEK
ERK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Sophocarpine monohydrate is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine monohydrate upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine monohydrate inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine monohydrate can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine monohydrate has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage .
|
-
- HY-N0103
-
|
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MEK
ERK
PTEN
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage .
|
-
- HY-N2208
-
|
p38 MAPK
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
4-Hydroxylonchocarpin is a chalcone compound from an extract of Psoralea corylifolia. 4-Hydroxylonchocarpin increases phosphorylation of p38 MAPK, JNK and ERK. 4-Hydroxylonchocarpin has diverse pharmacological activities, including antibacterial, antifungal, anticancer, antireverse transcriptase, antitubercular, antimalarial, anti-inflammatory and antioxidant activities .
|
-
- HY-N0809
-
-
- HY-145384
-
|
Phospholipase
|
Inflammation/Immunology
|
ROC-0929 (compound 13a) is a potent and selective inhibitor of secreted phospholipases A2 (sPLA2s) with an IC50 of 80 nM, specially targeting hGX. ROC-0929 inhibits the phosphorylation of ERK1/2 and p-38. Secreted phospholipases A2 (sPLA2s) are a family of disulfide-rich, Ca 2+-dependent enzymes that hydrolyze the sn-2 position of glycero-phospholipids to release a fatty acid and a lysophospholipid. ROC-0929 has the potential for researching inflammation related diseases .
|
-
- HY-P10941A
-
|
Integrin
FAK
ERK
|
Inflammation/Immunology
Cancer
|
VSLRGDTRG acetate is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG acetate promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG acetate can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
|
-
- HY-12927
-
|
CXCR
|
Inflammation/Immunology
|
SX-517 is a dual CXCR2/1 antagonist, containing boronic acid. SX-517 inhibits CXCL1-induced Ca 2+ flux (IC50=38 nM), and antagonizes CXCL8-induced [(35)S]GTPγS binding (IC50=60 nM) and ERK1/2 phosphorylation. SX-517 has significant ability for inflammation suppression, in both humanized polymorphonuclear (PMN) cells and in murine model .
|
-
- HY-P10941
-
|
Integrin
FAK
ERK
|
Inflammation/Immunology
Cancer
|
VSLRGDTRG is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
|
-
- HY-108626
-
NCGC84
|
Neuropeptide S Receptor
|
Neurological Disease
|
ML154 (NCGC84) is a selective, brain-penetrant and non-peptide neuropeptide S receptor (NPSR) antagonist with a pA2 of 9.98. ML154 potently inhibits NPS-stimulated cellular calcium, cAMP, and ERK phosphorylation responses with IC50 values of 36.5 nM, 22.1 nM, and 9.3 nM, respectively .
|
-
- HY-100851A
-
|
5-HT Receptor
|
Cardiovascular Disease
|
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats .
|
-
- HY-157888
-
|
SHP2
Phosphatase
|
Cancer
|
SHP2-IN-26 (Compound 4b) is a highly selective SHP2 allosteric inhibitor with a IC50 value of 3.2 nM. SHP2-IN-26 inhibits the phosphorylation of ERK and AKT in NCI-H358 cells. SHP2-IN-26 has antitumor activity .
|
-
- HY-N0366
-
|
PDGFR
|
Inflammation/Immunology
|
Sennoside B is a potent and orally active platelet-derived growth factor (PDGF) inhibitor. Sennoside B inhibits cell proliferation and the expression of phosphorylation of PDGFR-β, STAT-5, AKT and ERK induced by PDGF-BB. Sennoside B shows gastroprotective activities. Sennoside B has the potential for the research of gastritis .
|
-
- HY-100851
-
|
5-HT Receptor
|
Cardiovascular Disease
|
LY-272015 is an orally active, specific 5-HT2B receptor antagonist. LY-272015 completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats .
|
-
- HY-110198
-
|
Prostaglandin Receptor
PERK
|
Inflammation/Immunology
|
ONO-8130 is an orally active and selective prostanoid EP1 receptor antagonist. ONO-8130 blocks phosphorylation of ERK in the L6 spinal cord. ONO-8130 relieves bladder pain in mice with cyclophosphamide-induced cystitis. ONO-8130 can be used for interstitial cystitis research .
|
-
- HY-B0916
-
|
Insecticide
Cholinesterase (ChE)
MMP
Reactive Oxygen Species
ERK
Keap1-Nrf2
|
Infection
Neurological Disease
Cancer
|
Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
|
-
- HY-N0103R
-
|
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MEK
ERK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Sophocarpine (Standard) is the analytical standard of Sophocarpine (HY-N0103). This product is intended for research and analytical applications. Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage .
|
-
- HY-164389
-
|
Ras
|
Cancer
|
SML-10-70-1 is a ligand for RAS, which covalently modifies the K-Ras G12C mutant protein, and inhibits the phosphorylation of ERK and Akt. SML-10-70-1 inhibits the proliferation of cancer cells H23, H358 and A549 with IC50 of 26.6-47.6 μM .
|
-
- HY-N13294
-
TMJ-105
|
Apoptosis
JAK
STAT
p38 MAPK
JNK
ERK
|
Cancer
|
Cernuumolide J (TMJ-105) is an JAK2/STAT3 inhibitor. Cernuumolide J induces G2/M phase arrest and apoptosis in HEL leukemia cells by downregulating the phosphorylation of JAK2, STAT3, and Erk, and activating the phosphorylation of JNK and p38 MAPK. Cernuumolide J inhibits HEL leukemia cell growth in a time- and concentration-dependent manner, with an IC50 value of 1.79 μM. Cernuumolide J can be used for research in the field of anti-cancer therapy .
|
-
- HY-13404A
-
INC280 dihydrochloride; INCB28060 dihydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404C
-
INC280 dihydrochloride hydrate; INCB-28060 dihydrochloride hydrate
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) dihydrochloride hydrate is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib dihydrochloride hydrate can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib dihydrochloride hydrate potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib dihydrochloride hydrate is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-13404
-
INC280; INCB28060
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-D0205AS1
-
Carbocysteine-13C3-1
|
Isotope-Labeled Compounds
Keap1-Nrf2
NF-κB
PERK
Apoptosis
|
Infection
Inflammation/Immunology
|
Carbocisteine- 13C3-1 (Carbocysteine- 13C3-1) is 13C labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-13404B
-
INC280 hydrochloride; INCB-28060 hydrochloride
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (INC280; INCB28060) hydrochloride is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib hydrochloride can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib hydrochloride potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib hydrochloride is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-104066A
-
Xiliertinib tartrate; HMPL-309 tartrate
|
EGFR
|
Cancer
|
Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-105226B
-
PD134308 hemihydrate
|
Cholecystokinin Receptor
|
Neurological Disease
Cancer
|
CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects .
|
-
- HY-105226
-
PD134308
|
Cholecystokinin Receptor
|
Neurological Disease
Cancer
|
CI-988 (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects .
|
-
- HY-104066
-
Xiliertinib; HMPL-309
|
EGFR
|
Cancer
|
Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N9541
-
|
Others
|
Inflammation/Immunology
|
Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
|
-
- HY-N1504R
-
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
Loureirin B (Standard) is the analytical standard of Loureirin B. This product is intended for research and analytical applications. Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-156420
-
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
Cancer
|
ATUX-1215 is an activator of protein phosphatase 2A (PP2A). ATUX-1215 reduced the phosphorylation of ERK, p38, JNK, and Akt and the secretion of IL-12p70, GM-CSF, and IL1α in BLM-treated animals. ATUX-1215 can slow the progression of lung fibrosis .
|
-
- HY-168442
-
|
Ras
PERK
|
Cancer
|
KRAS inhibitor-40 (Compound 41) is a KRAS inhibitor that interferes with the KRAS G12C-BRAF complex. KRAS inhibitor-40 inhibits the ERK phosphorylation of KRAS downstream signaling pathway. KRAS inhibitor-40 can inhibit the proliferation of tumor cells with different KRAS mutation types and has antitumor activity .
|
-
- HY-151431
-
|
Keap1-Nrf2
Reactive Oxygen Species
ERK
Akt
JNK
|
Neurological Disease
|
Nrf2/HO-1 activator 2 (compound 13m), difluoro-substituted derivative, is a potent Nrf2/HO-1 activator. Nrf2/HO-1 activator 2 has neuroprotective and antioxidant effects through the Nrf2/HO-1 pathway mediated by phosphorylation of ERK1/2, JNK, or Akt in PC12 cells. Nrf2/HO-1 activator 2 can be used in the research of Parkinson's disease (PD) .
|
-
- HY-168438
-
|
EGFR
Akt
ERK
|
Cardiovascular Disease
|
ERBB agonist-1 (Compound EF-1) is an agonist for ERBB4, that activates the ERBB4 signaling pathway by inducing dimerization of the ERBB4 receptor with an EC50 of 10.5 μM. ERBB agonist-1 induces phosphorylation of Akt and ERK1/2, reduces the collagen expression in cardiac fibroblasts, inhibits H2O2-induced cardiomyocyte death and Ang II (HY-13948)-induced cardiomyocyte hypertrophy. ERBB agonist-1 prevents fibrosis and exhibits cardioprotective efficacy in mouse models .
|
-
- HY-N0809R
-
-
- HY-115605
-
|
EGFR
p38 MAPK
ERK
Phosphatase
|
Cancer
|
CN009543V is an epidermal growth factor receptor (EGFR) agonist. CN009543V enhances tyrosine phosphorylation of EGFR at Tyr1068 and Tyr1173, thereby activating the MAPK/ERK cascade. CN009543V inhibits the activity of PTP-1B in MDA MB468 cells. CN009543V can be used in cancer research .
|
-
- HY-B0916S
-
|
Isotope-Labeled Compounds
Insecticide
Cholinesterase (ChE)
MMP
Reactive Oxygen Species
ERK
Keap1-Nrf2
|
Infection
Neurological Disease
Cancer
|
Propoxur-d3 is the deuterated form of Propoxur (HY-B0916). Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
|
-
- HY-B0916R
-
|
Reference Standards
MMP
Insecticide
Cholinesterase (ChE)
Reactive Oxygen Species
ERK
Keap1-Nrf2
|
Infection
Neurological Disease
Cancer
|
Propoxue (Standard) is the analytical standard of Propoxue (HY-B0916). This product is intended for research and analytical applications. Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
|
-
- HY-129636
-
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
|
-
- HY-168493
-
|
FLT3
VEGFR
HDAC
STAT
PERK
|
Cancer
|
FLT3/VEGFR2-IN-1 (Compound 26) is a FLT3/VEGFR2/HDAC inhibitor with IC50 values of 14.5 nM, 3.9 nM, and 30.8 nM for FLT3, VEGFR2, and HDAC1, respectively. FLT3/VEGFR2-IN-1 can inhibit the phosphorylation of STAT3 and ERK1/2 and the proliferation of leukemia cells. FLT3/VEGFR2-IN-1 has anti-tumor activity and can be used for the research of acute myeloid leukemia .
|
-
- HY-168013
-
|
Ras
|
Cancer
|
KRASG12C IN-14 (compound 15) is an inhibitor targeting the KRAS G12C mutation. KRASG12C IN-14 inhibits CYPA-dependent KRAS-BRAF with an IC50 of 0.002 μM. KRASG12C IN-14 inhibits ERK phosphorylation in NCI-H358 cells with an IC50 of 0.002 μM .
|
-
- HY-P99275
-
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
-
- HY-172221
-
|
SOS1
Ras
ERK
|
Cancer
|
SOS1-IN-18 (Compound 8) is the inhibitor for Son of Sevenless 1 protein (SOS1) with a KD of 2.6 nM, and inhibits SOS1-KRAS G12C interaction with an IC50 of 3.4 nM. SOS1-IN-18 inhibits the phosphorylation of ERK in H358 with an IC50 of 31 nM, inhibits the proliferation of H358 with an IC50 of 5 nM .
|
-
- HY-138842
-
|
Insulin Receptor
Akt
ERK
|
Metabolic Disease
|
DDN is a selective insulin receptor (Insulin Receptor) activator, an insulin sensitizer, and a glucose-lowering insulin mimetic with oral bioavailability. DDN can directly bind to the receptor kinase domain and induce Akt and ERK phosphorylation, and it can also enhance insulin's effect on glucose uptake. DDN significantly reduces blood glucose levels in wild-type and diabetic ob/ob and db/db mice .
|
-
- HY-101798
-
|
PI3K
|
Cancer
|
MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .
|
-
- HY-134811
-
|
Ras
|
Cancer
|
KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation . KRAS G12D inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-134000
-
NSC624610
|
p38 MAPK
NF-κB
ERK
JNK
VEGFR
MMP
|
Cancer
|
Emodic acid (NSC624610) is an anthraquinone compound isolated from A. microcarpus, which can inhibit the proliferation of cancer cells by inhibiting the activity of NF-κB. Emodic acid can also inhibit the phosphorylation of p38, ERK and JNK, the secretion of tumor-promoting cytokines IL-1β and IL-6, and the expression of VEGF and MMP, thereby inhibiting the invasion and migration potential of cancer cells .
|
-
- HY-173153
-
|
JNK
PERK
MEK
NO Synthase
|
Inflammation/Immunology
Cancer
|
BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3 and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM and 0.009 μM, respectively. BRAFV600E/JNK-IN-1 can inhibit the phosphorylation of MEK1/2 and ERK1/2. In addition, BRAFV600E/JNK-IN-1 can inhibit tumor cell proliferation, NO release and PGE2 production, and has anti-tumor and anti-inflammatory activities .
|
-
- HY-13404R
-
|
c-Met/HGFR
Apoptosis
|
Cancer
|
Capmatinib (Standard) is the analytical standard of Capmatinib. This product is intended for research and analytical applications. Capmatinib (INC280; INCB28060) is a potent, orally active, selective, and ATP competitive c-Met kinase inhibitor (IC50=0.13 nM). Capmatinib can inhibit phosphorylation of c-MET as well as c-MET pathway downstream effectors such as ERK1/2, AKT, FAK, GAB1, and STAT3/5. Capmatinib potently inhibits c-MET-dependent tumor cell proliferation and migration and effectively induces apoptosis. Antitumor activity. Capmatinib is largely metabolized by CYP3A4 and aldehyde oxidase .
|
-
- HY-103211
-
L748337
1 Publications Verification
|
Adrenergic Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
L748337 is a potent β3-adrenergic receptor antagonist and displays selectivity over β1 and β2 receptors. The Ki values of L748337 for β3-, β2- and β1-adrenoceptors are 4.0 nM, 204 nM and 390 nM, respectively . L748337 couples predominantly to Gi to activate MAPK signaling and increases phosphorylation of Erk1/2 with pEC50 value of 11.6 . L748337 can be used for the research of cancer, nonalcoholic fatty liver disease (NAFLD), and cardiovascular related diseases .
|
-
- HY-113308
-
|
Calcium Channel
Endogenous Metabolite
|
Others
|
Taurolithocholic acid is a bile acid that has the activity of increasing cell viability, inducing the S phase of the cell cycle, and promoting DNA synthesis in a concentration-dependent manner in the intrahepatic cholangiocarcinoma cell line RMCCA-1. It can also increase the phosphorylation of EGFR and ERK 1/2 and the expression of cyclin D1 in RMCCA-1 cells, and its induced RMCCA-1 cell growth can be inhibited by specific antagonists and inhibitors.
|
-
- HY-B1092A
-
D-Gluconic acid sodium salt; Sodium D-gluconate; D-Gluconate sodium salt
|
Endogenous Metabolite
NO Synthase
Interleukin Related
ERK
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
Gluconate sodium (D-Gluconic acid sodium salt) is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury .
|
-
- HY-W010983
-
SC-236
1 Publications Verification
|
COX
PPAR
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
SC-236 is an orally active COX-2 specific inhibitor (IC50 = 10 nM) and a PPARγ agonist. SC-236 suppresses activator protein-1 (AP-1) through c-Jun NH2-terminal kinase. SC-236 exerts anti-inflammatory effects by suppressing phosphorylation of ERK in a murine model .
|
-
- HY-W060074
-
|
Endogenous Metabolite
Bacterial
Tyrosinase
PERK
|
Infection
Endocrinology
|
1-Acetyl-β-carboline is a metabolite of Streptomyces kasugaensis and antibacterial agent. 1-Acetyl-β-carboline increases tyrosinase activity, reduces ERK phosphorylation. 1-Acetyl-β-carboline exhibits antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) strains with MICs ranging from 128 to 256 ug/mL. 1-Acetyl-β-carboline increases the melanin .
|
-
- HY-N5083
-
-
- HY-112701
-
|
CCR
|
Inflammation/Immunology
Endocrinology
Cancer
|
CCR6 inhibitor 1 is a potent and selective CCR6 inhibitor, with IC50s of 0.45 and 6 nM for monkey and human CCR6, much more selective at CCR6 over human CCR1 (IC50, > 30000 nM), and CCR7 (IC50, 9400 nM). CCR6 inhibitor 1 markedly blocks ERK phosphorylation. CCR6 inhibitor 1 is used in the research of autoimmune diseases and cancer .
|
-
- HY-W745090
-
|
Formyl Peptide Receptor (FPR)
Src
ERK
Akt
p38 MAPK
|
Others
|
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
-
- HY-162888
-
|
PDGFR
ERK
|
Cardiovascular Disease
|
WQ-C-401 is an orally active platelet-derived growth factor receptor (PDGFR) inhibitor. WQ-C-401 inhibits cell proliferation by blocking PDGFR autophosphorylation in a concentration-dependent manner, with EC50 values of 3.5 nM for PDGFRα Y849 and 5.8 nM for PDGFRβ Y1021. Additionally, WQ-C-401 can inhibit PASMCs proliferation and migration by blocking PDGF-BB-induced ERK1/2 phosphorylation, reducing collagen I synthesis, and increasing α-SMA expression, thereby preventing pulmonary vascular remodeling. WQ-C-401 holds promise for research in the field of pulmonary arterial hypertension .
|
-
- HY-W744699
-
(+)-Larixol
|
Src
ERK
Akt
|
Inflammation/Immunology
|
Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
-
- HY-116504
-
|
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
|
-
- HY-N0619
-
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
|
-
- HY-118140
-
|
Cannabinoid Receptor
|
Neurological Disease
Inflammation/Immunology
|
ZCZ011 is a potent and brain penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
|
-
- HY-111671
-
SOS1 activator 1
|
SOS1
Ras
PERK
Ligands for Target Protein for PROTAC
|
Cancer
|
VUBI1 (SOS1 activator 1) is a benzimidazole derivative and SOS1 activator with a Kd of 44 nM. VUBI1 can significantly activate RAS-GTP and regulate the phosphorylation of ERK. VUBI1 also can serve as a target ligand for synthesizing PROTACs, such as PROTAC SOS1 degrader-1 (HY-145737), to induce SOS1 degradation. VUBI1 can be used in the study of cancer .
|
-
- HY-143293
-
|
VEGFR
Apoptosis
|
Cancer
|
VEGFR-IN-3 (compound 3f) is a VEGFR inhibitor. VEGFR-IN-3 inhibits OVCAR-4 and MDA-MB-468 cancer cells growth with IC50s of 0.29 and 0.35 μM, respectively. VEGFR-IN-3 can be used for the research of cancer .
|
-
- HY-168895
-
|
AP-1
ERK
Apoptosis
|
Cancer
|
c-Fos-IN-1 (Compound P16) is a c-Jun inhibitor, and decreases mRNA levels and protein levels of c-Fos. c-Fos-IN-1 also inhibits the phosphorylation activity of ERK and the transcriptional activity of AP-1. c-Fos-IN-1 shows anticancer activity by inhibiting ERK/c-Fos/Jun pathway. c-Fos-IN-1 inhibits the proliferation and migration of gastric cancer cells (IC50: 2.31 μM for MGC-803 cell). c-Fos-IN-1 arrests cell cycle at G2/M phase and induces cancer cell apoptosis. c-Fos-IN-1 inhibits gastric cancer tumor growth .
|
-
- HY-156041
-
Lyso-PE (egg); LPE (egg); L-α-lysophosphatidylethanolamine
|
Endogenous Metabolite
|
Metabolic Disease
|
Lysophosphatidylethanolamine (LPE) is a naturally-occurring lysophospholipid that can be generated via deacylation of phosphatidylethanolamine by phospholipase A2 (PLA2). It increases the phosphorylation of ERK1/2 in PC12 cells, an effect that can be blocked by the MEK inhibitors U-0126 (HY-12031A) and PD 98059 (HY-12028) and the EGFR inhibitor AG-1478 (HY-13524).1 LPE also increases neurite outgrowth and expression of neurofilament M in PC12 cells. LPE inhibits the activity of phospholipase D (PLD) partially purified from cabbage.3 This product contains lysophosphatidylethanolamine molecular species with variable fatty acyl chain lengths at the sn-1 position and a hydroxy group at the sn-2 position.
|
-
- HY-100035
-
|
ROCK
ERK
CDK
Apoptosis
|
Cancer
|
PT-262 is a potent ROCK inhibitor with an IC50 value of around 5 μM. PT-262 induces the loss of mitochondrial membrane potential and elevates the caspase-3 activation and apoptosis. PT-262 inhibits the ERK and CDC2 phosphorylation via a p53-independent pathway. PT-262 blocks cytoskeleton function and cell migration. PT-262 has anti-cancer activity .
|
-
- HY-145491
-
|
ERK
NF-κB
|
Inflammation/Immunology
|
Resolvin D5 is a prolytic mediator (SPM) with anti-inflammatory activity derived from oxidized lipids DHA. Resolvin D5 inhibits Th17 cell differentiation and promotes regulatory T cell differentiation, and inhibits CD4+ T cell proliferation. Resolvin D5 attenuates osteoclast differentiation and interferes with osteoclastogenesis. Resolvin D5 also regulates ERK phosphorylation and nuclear translocation of NF-kappaB. Resolvin D5 could be used in rheumatoid arthritis research .
|
-
- HY-170550
-
|
Ras
ERK
|
Cancer
|
KRAS G12C inhibitor 69 (Compound K09) is the inhibitor for mutant RAS protein KRASG12C with an IC50 of 4.36 nM. KRAS G12C inhibitor 69 inhibits the ERK phosphorylation in NCI-H358 and MIA-PACA-2 with an IC50 of 12 nM and 7 nM. KRAS G12C inhibitor 69 inhibits the proliferation of cancer cell NCI-H358 and MIA-PACA-2 with IC50 of 3.15 nM and 2.33 nM .
|
-
- HY-N0619A
-
Mulberroside D
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
|
-
- HY-B1092AR
-
D-Gluconic acid sodium salt (Standard); Sodium D-gluconate (Standard); D-Gluconate sodium salt (Standard)
|
Endogenous Metabolite
|
Others
Cancer
|
Gluconate (sodium) (Standard) is the analytical standard of Gluconate (sodium). This product is intended for research and analytical applications. Gluconate sodium (D-Gluconic acid sodium salt) is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury .
|
-
- HY-147183
-
|
EGFR
|
Cancer
|
JBJ-09-063 is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 can be used for researching EGFR-mutant lung cancer .
|
-
- HY-147183A
-
|
EGFR
|
Cancer
|
JBJ-09-063 TFA is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 TFA effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 TFA is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 TFA can be used for researching EGFR-mutant lung cancer .
|
-
- HY-147183B
-
|
EGFR
|
Cancer
|
JBJ-09-063 hydrochloride is a mutant-selective allosteric EGFR inhibitor with IC50s of 0.147 nM, 0.063 nM, 0.083 nM and 0.396 nM for EGFR L858R, EGFR L858R/T790M, EGFR L858R/T790M/C797S and EGFRLT/L747S. JBJ-09-063 hydrochloride effectively reduces EGFR, Akt and ERK1/2 phosphorylation. JBJ-09-063 hydrochloride is effective across EGFR tyrosine kinase inhibitor (TKI)-sensitive and resistant models. JBJ-09-063 hydrochloride can be used for researching EGFR-mutant lung cancer .
|
-
- HY-N0092R
-
|
Adenosine Receptor
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR . Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation . Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes . In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
|
-
- HY-N0619R
-
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
Mulberroside A (Standard) is the analytical standard of Mulberroside A. This product is intended for research and analytical applications. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) . Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
|
-
- HY-120200
-
|
VEGFR
|
Cardiovascular Disease
Cancer
|
YF-452 is a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR2). YF-452 remarkably inhibits the migration, invasion and tube-like structure formation of human umbilical vein endothelial cells (HUVECs) with little toxicity. YF-452 inhibits VEGF-induced phosphorylation of VEGFR2 kinase and the downstream protein kinases including extracellular signal regulated kinase (ERK), focal adhesion kinase (FAK) and Src. YF-452 is a potential antiangiogenic agent candidate for cancer research .
|
-
- HY-128634
-
|
Apoptosis
PI3K
MEK
|
Cancer
|
CML-IN-1 (compound 7) is a potent anticancer agent. CML-IN-1 displays very good induced-apoptosis effect for human chronic myeloid leukemia (CML) cell line K562. CML-IN-1 exerts its effect via a significantly reduced protein phosphorylation of PI3K/Akt signal pathway. CML-IN-1 (compound 4) also inhibits cell proliferation by suppressing the MEK/ERK signaling pathway in colorectal cancer .
|
-
- HY-123468
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-123468A
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-150026
-
|
VEGFR
PDGFR
FGFR
c-Kit
Akt
Src
Apoptosis
|
Cancer
|
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .
|
-
- HY-P1844
-
|
Chemerin Receptor
Akt
ERK
Reactive Oxygen Species
Amyloid-β
|
Inflammation/Immunology
|
Chemerin-9 (149-157) is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) has anti-inflammatory activity. Chemerin-9 (149-157) stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) regulates immune responses, adipocyte differentiation, and glucose metabolism .
|
-
- HY-N5083R
-
-
- HY-134813
-
|
Ras
|
Cancer
|
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
|
-
- HY-P1844A
-
|
Chemerin Receptor
Akt
ERK
Reactive Oxygen Species
Amyloid-β
|
Inflammation/Immunology
|
Chemerin-9 (149-157) TFA is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) TFA has anti-inflammatory activity. Chemerin-9 (149-157) TFA stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) TFA ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) TFA regulates immune responses, adipocyte differentiation, and glucose metabolism .
|
-
- HY-164350
-
|
Ras
ERK
p38 MAPK
|
Cancer
|
KRAS inhibitor-27 (Compound 15h) is the inhibitor for KRAS. KRAS inhibitor-27 inhibits KRAS G12D/G12V mutated cells AsPC-1, SW620 and KRAS wildtype cell HT-29 with IC50 of 378, 0.6 and 3230 nM, respectively. KRAS inhibitor-27 inhibits ERK phosphorylation (IC50 in cell AsPC-1 and SW620 is 0.6 nM and 1 nM), reduces the expression of DUSP4, thereby inhibiting MAPK signaling pathway .
|
-
- HY-112348
-
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-12624
-
ON123300
|
CDK
AMPK
PDGFR
|
Cancer
|
Narazaciclib (ON123300), a strong and brain-penetrant multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent Narazaciclib causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors . Narazaciclib inhibits CDK6 with an IC50 of 9.82 nM .
|
-
- HY-168716
-
|
SOS1
Ras
|
Cancer
|
SOS1-IN-17 (Compound 8d) is an orally active inhibitor for SOS1-KRASG12C interaction with an IC50 of 5.1 nM. SOS1-IN-17 inhibits ERK phosphorylation in DLD-1 cell with an IC50 of 18 nM. SOS1-IN-17 exhibits anti-proliferative activity in KRASG12C mutated Mia-Paca-2 cell with an IC50 of 0.11 μM. SOS1-IN-17 exhibits antitumor efficacy against pancreatic cancer in mouse model .
|
-
- HY-156498
-
|
Ras
ERK
Raf
Ribosomal S6 Kinase (RSK)
AMPK
Apoptosis
PARP
|
Cancer
|
RMC-7977 is an orally active triple-complex RAS inhibitor that can simultaneously bind to cyclophilin A (CYPA) (Kd = 195 nM) and KRAS (G12V) (Kd = 292 μM). It exhibits broad-spectrum inhibitory activity against KRAS, NRAS, and HRAS proteins and their various wild-type and mutant variants. RMC-7977 induces apoptosis by inhibiting the phosphorylation of ERK, CRAF, and RSK, as well as increasing PARP cleavage. This leads to tumor regression, reduces resistance in KRAS G12C cancer models, and demonstrates good tolerability across various RAS cancer models .
|
-
- HY-176192
-
|
Toll-like Receptor (TLR)
TNF Receptor
NF-κB
p38 MAPK
ERK
IKK
|
Inflammation/Immunology
|
SMU-14a is a TLR3 inhibitor (IC50: 0.18 µM). SMU-14a inhibits IL-6 secretion in mouse peritoneal macrophages and downregulates TNF-α in human peripheral blood monocytes. SMU-14a exerts anti-inflammatory effects by reducing the phosphorylation of p65, ERK, and TBK1 through NF-κB, MAPK, and IRF3 signaling pathways, and decreasing serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels. SMU-14a can be used in the study of acute hepatitis .
|
-
- HY-173047
-
|
Ras
ERK
|
Cancer
|
KRASG12C IN-15 (Compound 21) is the orally active inhibitor for KRAS G12C, and inhibits SOS1-mediated GDP/GTP exchange with an IC50 of 19 nM. KRASG12C IN-15 inhibits the phosphorylation of ERK with IC50 of 0.051 μM. KRASG12C IN-15 inhibits the cell viability of KRAS G12C mutated MIA PaCa-2 with IC50 of 0.023 μM. KRASG12C IN-15 exhibits antitumor effect in MIA PaCa-2 xenograft mouse models .
|
-
- HY-P1845
-
|
ERK
EGFR
Reactive Oxygen Species
Calcium Channel
|
Neurological Disease
|
PACAP-38 (31-38), human, mouse, rat is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat can be used for neurotrophic and neuroprotective research .
|
-
- HY-172916
-
|
SHP2
FGFR
p38 MAPK
ERK
|
Cancer
|
LC-SF-14 is a selective dual inhibitor of SHP2 and FGFR (IC50 values are 71.6 and 8.9 nM, respectively). LC-SF-14 inhibits FGFR2-FRS2α-SHP2-MAPK signaling and ERK phosphorylation. LC-SF-14 inhibits the proliferation of KATOIII cancer cells (IC50: 9.2 nM). LC-SF-14 has antitumor activity in the SNU-16 xenograft mouse model. LC-SF-14 can be used in FGFR2-driven gastric cancer research .
|
-
- HY-109041
-
AKB-9778
|
Phosphatase
Tie
|
Inflammation/Immunology
|
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM) .
|
-
- HY-N6576
-
|
p38 MAPK
ERK
JNK
IAP
PARP
Apoptosis
Caspase
|
Cancer
|
Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers .
|
-
- HY-P1845A
-
|
ERK
EGFR
Reactive Oxygen Species
Calcium Channel
|
Neurological Disease
|
PACAP-38 (31-38), human, mouse, rat TFA is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat TFA elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat TFA can be used for neurotrophic and neuroprotective research .
|
-
- HY-148098
-
|
Ras
|
Cancer
|
Pan KRas-IN-1 is a pan KRas inhibitor, can be used for agent resistance in cancer developed with KRas G12C inhibitors .
|
-
- HY-164529
-
|
Raf
Ras
MEK
ERK
VEGFR
Tie
c-Fms
|
Cancer
|
SJ-C1044 is an orally available pan-RAF inhibitor with immunomodulatory and anti-tumor activities. SJ-C1044 inhibits wild-type BRAF, wild-type CRAF, and BRAF (V600E) with IC50 values ??of 331, 257, and 187 nM, respectively. SJ-C1044 inhibits tumor cell proliferation by inhibiting kras activation and MEK-ERK phosphorylation. In addition, SJ-C1044 also has a certain inhibitory effect on VEGFR2, TIE2, and CSF1R, with IC50 values ??of 100, 23, and 235 nM, respectively. SJ-C1044 improves the tumor immune microenvironment by inhibiting angiogenesis and regulating macrophage function. SJ-C1044 can be used in the study of colorectal cancer .
|
-
- HY-N4205
-
|
Cytochrome P450
|
Cancer
|
Tetrahydropiperine is an orally effective, selective inhibitor of NF-κB and MAPKs<、b>, and an activator of the PI3K/Akt/mTOR<、b> pathway. Tetrahydropiperine reduces the production of pro-inflammatory cytokines such as TNF-α, IL-6, and nitric oxide (NO) by inhibiting the nuclear translocation of NF-κB and the phosphorylation of MAPKs such as ERK, JNK, and p38. At the same time, Tetrahydropiperine inhibits excessive autophagy by activating the PI3K/Akt/mTOR pathway, protecting neurons from oxidative damage. Tetrahydropiperine has anti-inflammatory, anti-apoptotic, and neuroprotective effects, and is mainly used in the study of inflammatory diseases (such as endotoxemia, arthritis) and neurological diseases such as ischemic stroke .
|
-
- HY-124858
-
|
STAT
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
SC99 is an orally active, selective STAT3 inhibitor targeting JAK2-STAT3 pathway. SC99 docks into the ATP-binding pocket of JAK2. SC99 inhibits phosphorylation of JAK2 and STAT3 with no effects on the other kinases associated with STAT3 signaling. SC99 inhibits platelet activation, aggregation and displays potent anti-myeloma, anti-thrombotic activities .
|
-
- HY-161923
-
|
EGFR
Apoptosis
Akt
ERK
|
Cancer
|
EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFR L858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFR WT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFR L858R/T790M/C797S with an IC50 of 0.052 μM .
|
-
- HY-161654
-
|
SOS1
PROTACs
Ras
|
Cancer
|
PROTAC SOS1 degrader-10 (Compound 11o) is a degrader for son of sevenless 1 (SOS1) in a CRBN and proteasome dependent manner. PROTAC SOS1 degrader-10 degrades SOS1 in KRAS mutant cancer cells SW620, A549 and DLD-1, with DC50s of 2.23, 1.85 and 7.53 nM, respectively. PROTAC SOS1 degrader-10 inhibits the proliferations of cells SW620, A549 and DLD-1, with IC50s of 36.7, 52.2 and 107 nM, respectively. PROTAC SOS1 degrader-10 inhibits phosphorylation of ERK. (Pink: SOS1 ligand (HY-161655); Black: linker (HY-161656); Blue: E3 ligase ligand (HY-W249500))
|
-
Cat. No. |
Product Name |
Type |
-
- HY-W745090
-
|
Biochemical Assay Reagents
|
Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3751
-
-
- HY-P1342
-
|
Orphan Receptor
|
Neurological Disease
|
Prosaptide Tx14(A), a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) increases both ERK1 and ERK2 phosphorylation in Schwann cells .
|
-
- HY-P0178
-
|
Integrin
|
Inflammation/Immunology
|
LXW7, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
|
-
- HY-P0178A
-
|
Integrin
|
Inflammation/Immunology
|
LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect .
|
-
- HY-P10941A
-
|
Integrin
FAK
ERK
|
Inflammation/Immunology
Cancer
|
VSLRGDTRG acetate is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG acetate promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG acetate can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
|
-
- HY-P5977
-
Ste-MPKKKPTPIQLNP-NH₂; ERK Activation Inhibitor Peptide
|
ERK
|
Cancer
|
STE-MEK1(13) (Ste-MPKKKPTPIQLNP-NH ) is a cell permeable ERK1/2 inhibitor (IC50: 13-30 μM). STE-MEK1(13) inhibits ERK1/2 phosphorylation .
|
-
- HY-P1342A
-
|
ERK
|
Neurological Disease
|
Prosaptide Tx14(A) TFA, a prosaposin-derived peptide, is a potent GPR37L1 and GPR37 agonist with EC50s of 5 and 7 nM, respectively. Prosaptide Tx14(A) TFA increases both ERK1 and ERK2 phosphorylation in Schwann cells .
|
-
- HY-P5986
-
|
ERK
|
Others
|
mSIRK (L9A) is a cell-permeable, N-myristoylated G-Protein Binding Peptide (mSIRK). mSIRK (L9A) contains a single point mutation (Leu9 to Ala). mSIRK (L9A) cannot enhance ERK1/2 phosphorylation. mSIRK (L9A) can be used as a control peptide .
|
-
- HY-P3750
-
-
- HY-P10941
-
|
Integrin
FAK
ERK
|
Inflammation/Immunology
Cancer
|
VSLRGDTRG is a synthetic peptide containing the RGD motif from cadherin 17 (CDH17), which binds to α2β1 integrin and activates its signaling pathway. VSLRGDTRG promotes the high-affinity conformational change of β1 integrin through the RGD motif, enhancing cell adhesion and phosphorylation of FAK and ERK1/2, thereby driving tumor proliferation and metastasis. VSLRGDTRG can be used in research on cancers expressing CDH17, such as colon cancer and pancreatic cancer .
|
-
- HY-P1844
-
|
Chemerin Receptor
Akt
ERK
Reactive Oxygen Species
Amyloid-β
|
Inflammation/Immunology
|
Chemerin-9 (149-157) is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) has anti-inflammatory activity. Chemerin-9 (149-157) stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) regulates immune responses, adipocyte differentiation, and glucose metabolism .
|
-
- HY-P1844A
-
|
Chemerin Receptor
Akt
ERK
Reactive Oxygen Species
Amyloid-β
|
Inflammation/Immunology
|
Chemerin-9 (149-157) TFA is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) TFA has anti-inflammatory activity. Chemerin-9 (149-157) TFA stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) TFA ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) TFA regulates immune responses, adipocyte differentiation, and glucose metabolism .
|
-
- HY-P1845
-
|
ERK
EGFR
Reactive Oxygen Species
Calcium Channel
|
Neurological Disease
|
PACAP-38 (31-38), human, mouse, rat is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat can be used for neurotrophic and neuroprotective research .
|
-
- HY-P1845A
-
|
ERK
EGFR
Reactive Oxygen Species
Calcium Channel
|
Neurological Disease
|
PACAP-38 (31-38), human, mouse, rat TFA is a PAC1 receptor activator and increases the α-secretase activity. PACAP-38 (31-38), human, mouse, rat TFA elevates cytosolic Ca 2+, increases proliferation and increases phosphorylation of extracellular regulates kinase (ERK) and the epidermal growth factor receptor (EGFR). PACAP-38 (31-38), human, mouse, rat TFA demonstrates potent, efficacious, and sustained stimulatory effects on sympathetic neuronal NPY and catecholamine production. PACAP-38 (31-38), human, mouse, rat TFA can be used for neurotrophic and neuroprotective research .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99183
-
EMD 525797; DI17E6
|
Integrin
|
Cancer
|
Abituzumab (DI17E6) is a humanised anti-integrin αV monoclonal antibody (IgG2 type). Abituzumab effectively reduces the phosphorylation of FAK, Akt and ERK. Abituzumab can be used in cancer research, particularly in prostate cancer .
|
-
- HY-P99768
-
TTAC-0001
|
VEGFR
|
Cancer
|
Olinvacimab (TTAC-0001) is a fully human anti-VEGFR2 monoclonal antibody. Olinvacimab inhibits VEGF binds to KDR with a Kd value of 0.23 nM. Olinvacimab has antiangiogenic activity. Olinvacimab can be used for the research of recurrent glioblastoma and breast cancer .
|
-
- HY-P99275
-
Human Anti-ERBB3 Recombinant Antibody
|
EGFR
Akt
ERK
PARP
Survivin
|
Cancer
|
Patritumab (Human Anti-ERBB3 Recombinant Antibody) is a neutralizing monoclonal antibody to ERBB3. Patritumab shows a synergy with Cetuximab (HY-P9905), potently inhibits the phosphorylation of EGFR, HER2, HER3, ERK, and AKT. Patritumab also induces cell apoptosis and suppresses the growth of pancreatic, non-small cell lung cancer, and colorectal cancer xenograft tumors .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N1987
-
-
-
- HY-N1966
-
-
-
- HY-N2270
-
-
-
- HY-113599
-
-
-
- HY-126477
-
-
-
- HY-N2858
-
-
-
- HY-N1987R
-
|
Triterpenes
Structural Classification
Terpenoids
Cucurbitaceae
Plants
Hemsleya amabilis Diels
|
Apoptosis
|
Cucurbitacin IIb (Standard) is the analytical standard of Cucurbitacin IIb. This product is intended for research and analytical applications. Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α .
|
-
-
- HY-N2362R
-
-
-
- HY-124404A
-
-
-
- HY-N10047
-
-
-
- HY-N0774
-
-
-
- HY-D0205A
-
-
-
- HY-N1504
-
-
-
- HY-N11439
-
-
-
- HY-N2484
-
-
-
- HY-126477R
-
-
-
- HY-N9866
-
-
-
- HY-N0774R
-
-
-
- HY-N12561
-
|
Structural Classification
Microorganisms
Terpenoids
Source classification
Diterpenoids
|
ERK
p38 MAPK
JNK
|
Pestanoid A is a rearranged pimarane diterpenoid osteoclastogenesis inhibitor with an IC50 of 4.2 μM. Pestanoid A can be isolated from the marine mesophotic zone chalinidae sponge-associated fungus, Pestalotiopsis sp. NBUF145. Pestanoid A inhibits the receptor activator of NF-kB ligand-induced MAPK and NF-κB signaling by suppressing the phosphorylation of ERK1/2-JNK1/2-p38 MAPKs and NF-κB nuclear translocation. Pestanoid A can be used for the study of osteoporosis .
|
-
-
- HY-N7140
-
-
-
- HY-N0103A
-
|
Infection
Alkaloids
Piperidine Alkaloids
Structural Classification
Classification of Application Fields
Leguminosae
Source classification
Sophora japonica L.
Plants
Inflammation/Immunology
Disease Research Fields
|
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MEK
ERK
|
Sophocarpine monohydrate is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine monohydrate upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine monohydrate inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine monohydrate can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine monohydrate has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage .
|
-
-
- HY-N0103
-
Sophocarpine
Maximum Cited Publications
6 Publications Verification
|
Infection
Alkaloids
Piperidine Alkaloids
Structural Classification
Classification of Application Fields
Leguminosae
Source classification
Sophora flavescens Aiton
Plants
Inflammation/Immunology
Disease Research Fields
|
Autophagy
Apoptosis
NF-κB
PI3K
Akt
MEK
ERK
PTEN
|
Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage .
|
-
-
- HY-N2208
-
-
-
- HY-N0809
-
-
-
- HY-N0366
-
-
-
- HY-N0103R
-
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Alkaloids
Piperidine Alkaloids
Structural Classification
Leguminosae
Source classification
Sophora flavescens Aiton
Plants
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Autophagy
Apoptosis
NF-κB
PI3K
Akt
MEK
ERK
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Sophocarpine (Standard) is the analytical standard of Sophocarpine (HY-N0103). This product is intended for research and analytical applications. Sophocarpine is a PTEN activator and an inhibitor of PI3K/Akt, MEK/ERK, and NF-κB signaling pathways. Sophocarpine upregulates PTEN expression and inhibits PI3K/Akt phosphorylation, arrests tumor cell cycle and induces apoptosis. Sophocarpine inhibits MEK/ERK phosphorylation and VEGF secretion, reducing tumor cell migration. Sophocarpine can also inhibit NF-κB activation and p38 and JNK phosphorylation, reduce the expression of inflammatory factors such as iNOS and COX-2, and activate the Nrf2/HO-1 pathway to reduce oxidative stress. Sophocarpine has anti-tumor, anti-inflammatory, antioxidant and anti-apoptotic effects, and can be used in the research of cancers such as glioblastoma and colorectal cancer, inflammation-related diseases, and Doxorubicin (HY-15142A)-induced cardiac damage .
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- HY-N13294
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- HY-N9541
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Structural Classification
Alkaloids
Microorganisms
Pyrrole Alkaloids
Source classification
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Others
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Chaetoglobosin Vb is a novel cytotoxic alkaloid with anti-inflammatory and antioxidant activities. Chaetoglobosin Vb can inhibit oxidative stress induced by LPS stimulation, reduce the production of reactive oxygen species and increase the expression of the antioxidant enzyme superoxide dismutase (SOD). Chaetoglobosin Vb significantly reduced the gene and protein expression of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2) induced by LPS, and alleviated the production of proinflammatory cytokines such as TNF-α, IL-6 and IL-1β. Chaetoglobosin Vb exerts its biological activity through the TLR4-mediated MyD88-dependent signaling pathway and the TRIF-dependent signaling pathway, which is specifically manifested by inhibiting the phosphorylation of p38, ERK, and JNK MAPK and the translocation of NF-κB p65 subunit to the nucleus. Chaetoglobosin Vb showed no cytotoxic effect in the concentration range of 25-100 μM and promoted SOD enzyme activity and phosphorylation of p38, ERK1/2 and JNK in a dose-dependent manner .
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- HY-N1504R
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- HY-N0809R
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- HY-134000
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- HY-B1092A
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- HY-W060074
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- HY-N5083
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- HY-W744699
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(+)-Larixol
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Larix decidua Miller
Structural Classification
Natural Products
Pinaceae
Source classification
Plants
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Src
ERK
Akt
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Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
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- HY-N0619
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- HY-145491
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Structural Classification
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
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ERK
NF-κB
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Resolvin D5 is a prolytic mediator (SPM) with anti-inflammatory activity derived from oxidized lipids DHA. Resolvin D5 inhibits Th17 cell differentiation and promotes regulatory T cell differentiation, and inhibits CD4+ T cell proliferation. Resolvin D5 attenuates osteoclast differentiation and interferes with osteoclastogenesis. Resolvin D5 also regulates ERK phosphorylation and nuclear translocation of NF-kappaB. Resolvin D5 could be used in rheumatoid arthritis research .
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- HY-N0619A
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- HY-B1092AR
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D-Gluconic acid sodium salt (Standard); Sodium D-gluconate (Standard); D-Gluconate sodium salt (Standard)
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Structural Classification
other families
Source classification
Plants
Endogenous metabolite
Saccharides
Monosaccharides
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Endogenous Metabolite
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Gluconate (sodium) (Standard) is the analytical standard of Gluconate (sodium). This product is intended for research and analytical applications. Gluconate sodium (D-Gluconic acid sodium salt) is an orally active glucose derivative. Gluconate sodium reduces nitric oxide and inflammatory cytokines (IL-1β and IL-6). Gluconate sodium inhibits ERK phosphorylation. Gluconate sodium has antioxidant and antiplatelet activation activities. Gluconate sodium has antitumor activity against colorectal cancer. Gluconate sodium improves osteoarthritis, intestinal damage and acute lung injury .
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- HY-N0092R
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Structural Classification
Natural Products
Human Gut Microbiota Metabolites
Microorganisms
Source classification
Endogenous metabolite
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Adenosine Receptor
Endogenous Metabolite
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Inosine (Standard) is the analytical standard of Inosine. This product is intended for research and analytical applications. Inosine is an endogenous purine nucleoside produced by catabolism of adenosine. Inosine has anti-inflammatory, antinociceptive, immunomodulatory and neuroprotective effects. Inosine is an agonist for adenosine A1 (A1R) and A2A (A2AR) receptors . In Vitro:Inosine dose-dependently stimulates cAMP production mediated through the A2AR . Inosine dose-dependently induces hA2AR-mediated ERK1/2 phosphorylation . Inosine (100 μM; 24 hours) reduces oxidative stress in MES 23.5 cells cultured with astrocytes . In Vivo:Inosine (10-100 mg/kg; i.p.) exhibits antinociceptive effect in mice .
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- HY-N0619R
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- HY-N5083R
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- HY-N6576
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Structural Classification
Animals
Classification of Application Fields
Source classification
Disease Research Fields
Steroids
Cancer
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p38 MAPK
ERK
JNK
IAP
PARP
Apoptosis
Caspase
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Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers .
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- HY-N4205
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Alkaloids
Piperidine Alkaloids
Structural Classification
Classification of Application Fields
Source classification
Piperaceae
Plants
Disease Research Fields
Piper nigrum Linn.
Cancer
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Cytochrome P450
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Tetrahydropiperine is an orally effective, selective inhibitor of NF-κB and MAPKs<、b>, and an activator of the PI3K/Akt/mTOR<、b> pathway. Tetrahydropiperine reduces the production of pro-inflammatory cytokines such as TNF-α, IL-6, and nitric oxide (NO) by inhibiting the nuclear translocation of NF-κB and the phosphorylation of MAPKs such as ERK, JNK, and p38. At the same time, Tetrahydropiperine inhibits excessive autophagy by activating the PI3K/Akt/mTOR pathway, protecting neurons from oxidative damage. Tetrahydropiperine has anti-inflammatory, anti-apoptotic, and neuroprotective effects, and is mainly used in the study of inflammatory diseases (such as endotoxemia, arthritis) and neurological diseases such as ischemic stroke .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-17600S
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Acalabrutinib-d4 is a deuterium labeled Acalabrutinib. Acalabrutinib (ACP-196) is an orally active, irreversible, and highly selective second-generation BTK inhibitor . Acalabrutinib-d4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-114436S
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MRTX-1257-d6 is the deuterium labeled MRTX-1257 (HY-114436). MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells .
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- HY-D0205AS2
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Carbocisteine-d3 (Carbocysteine-d3) is deuterium labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
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- HY-D0205AS1
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Carbocisteine- 13C3-1 (Carbocysteine- 13C3-1) is 13C labeled Carbocisteine. Carbocisteine is an orally active mucolytic agent. Carbocisteine attenuates the phosphorylation of NF-κB p65 and ERK1/2. Carbocisteine modulates Nrf2/HO-1 and NFκB interplay. Carbocisteine inhibits Apoptosis. Carbocisteine is used in chronic obstructive pulmonary disease (COPD) research .
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- HY-B0916S
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Propoxur-d3 is the deuterated form of Propoxur (HY-B0916). Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
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Cat. No. |
Product Name |
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Classification |
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- HY-104066
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Xiliertinib; HMPL-309
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Alkynes
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Theliatinib (Xiliertinib) is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-134811
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Alkynes
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KRAS G12D inhibitor 1 (example 243) is a KRAS G12D inhibitor, with an IC50 of 0.8 nM for KRAS G12D-mediated ERK phosphorylation . KRAS G12D inhibitor 1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-134813
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Alkynes
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MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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- HY-104066A
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Xiliertinib tartrate; HMPL-309 tartrate
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Alkynes
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Theliatinib (Xiliertinib) tartrate is a potent, ATP-competitive, orally active and highly selective EGFR inhibitor with a Ki of 0.05 nM and an IC50 of 3 nM. Theliatinib has an IC50 of 22 nM for EGFR T790M/L858R mutant. Theliatinib shows >50-fold selectivity for EGFR than other kinases . Theliatinib (tartrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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