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Phosphorylation Blocker

" in MedChemExpress (MCE) Product Catalog:

134

Inhibitors & Agonists

2

Screening Libraries

1

Fluorescent Dye

1

Biochemical Assay Reagents

10

Peptides

6

Inhibitory Antibodies

19

Natural
Products

2

Isotope-Labeled Compounds

1

Click Chemistry

2

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-103471
    Y11

    		FAK Cancer
    Y11 inhibits FAK1 autophosphorylation by blocking phosphorylation of Y397 and decreases tumor growth .
    Y11
  • HY-122198
    ML367

    		Checkpoint Kinase (Chk) Cancer
    ML367 is a potent inhibitor of ATPase family AAA domain-containing protein 5 (ATAD5) stabilization, acts as a probe molecule that has low micromolar inhibitory activity. ML367 blocks DNA repair pathways, suppresses general DNA damage responses including RPA32-phosphorylation and CHK1-phosphorylation in response to UV irradiation .
    ML367
  • HY-118922
    IW927

    		TNF Receptor Inflammation/Immunology
    IW927 is a potent small molecule antagonist that blocks the binding of TNF-α to TNFRc1 with an IC50 value of 50 nM and disrupts TNFα-induced IκB phosphorylation with an IC50 value of 600 nM .
    IW927
  • HY-162092
    Multi-target Pt

    		NF-κB IKK Cancer
    Multi-target Pt (IV), an antitumor agent, suppresses the IKKβ phosphorylation, IκBα phosphorylation and NF-κB p65 phosphorylation and nuclear translocation, leading to blocked the NF-kB signal pathway .
    Multi-target Pt
  • HY-P10119
    PDGFR Y1021 peptide (non-phosphorylation)

    		PDGFR Mitosis Others
    PDGFR Y1021 peptide (non-phosphorylation) is the non-phosphorylated fragment of platelet-derived growth factor receptor (PDGFR). PDGFR Y1021 peptide (non-phosphorylation) blocks the PLCγ association to PDGFR through PLCγSH2 domain, and thus inhibits mitogenic response .
    PDGFR Y1021 peptide (non-phosphorylation)
  • HY-139741
    cyclo(Phe-Ala-Gly-Arg-Arg-Arg-Gly-AEEAc)

    		DNA/RNA Synthesis Others
    cyclo(Phe-Ala-Gly-Arg-Arg-Arg-Gly-AEEAc) provides an avenue for developing a nonhormonal male contraceptive by blocking of GRTH/DDX25 phosphorylation.
    cyclo(Phe-Ala-Gly-Arg-Arg-Arg-Gly-AEEAc)
  • HY-120542
    SR 1824

    		PPAR Metabolic Disease
    SR 1824 is a non-agonist PPARγ ligand that blocks Cdk5-mediated phosphorylation. SR 1824 has anti-diabetic effects .
    SR 1824
  • HY-176407
    ZYH-23

    		Necroptosis Inflammation/Immunology Cancer
    ZYH-23 is a potent necroptosis inhibitor. ZYH-23 blocks necroptosis by inhibiting RIPK1, RIPK3, and MLKL phosphorylation via HSP90 targeting .
    ZYH-23
  • HY-108554
    Q94 hydrochloride

    		Protease Activated Receptor (PAR) Others
    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 .
    Q94 hydrochloride
  • HY-158178
    EGFR T790M/L858R-IN-7

    		EGFR Cancer
    EGFR T790M/L858R-IN-7 (Compound 72) is a novel pyrimidine compound that inhibits the EGFR T790M and L858R mutation with a high efficacy (93% inhibition rate at 0.05 μM). EGFR T790M/L858R-IN-7 functions by specifically binding to the kinase domain of EGFR, thereby inhibiting its phosphorylation activity .
    EGFR T790M/L858R-IN-7
  • HY-N1987
    Cucurbitacin IIb
    2 Publications Verification

    		 Apoptosis Inflammation/Immunology
    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 .
    Cucurbitacin IIb
  • HY-110335
    OXA-06 hydrochloride

    		ROCK Cancer
    OXA-06 hydrochloride is an ATP-competitive ROCK inhibitor that blocks anchorage-dependent growth and invasion of non-small cell lung cancer cell lines. OXA-06 hydrochloride inhibits cofilin phosphorylation but does not stimulate apoptosis .
    OXA-06 hydrochloride
  • HY-107593
    PS-1145 dihydrochloride

    		IKK Inflammation/Immunology
    PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats .
    PS-1145 dihydrochloride
  • HY-N6782
    Oligomycin
    Maximum Cited Publications
    67 Publications Verification

    		 Oxidative Phosphorylation ATP Synthase Fungal Antibiotic Infection Cancer
    Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells .
    Oligomycin
  • HY-163432
    YGL-12

    		PPAR Metabolic Disease
    YGL-12 is a potent PPARγ modulator with good binding affinity and an IC50 value of 0.85 μM. YGL-12 effectively blocks PPARγ Ser273 phosphorylation and can be used in diabetes research .
    YGL-12
  • HY-150700
    RLX-33

    		ERK Metabolic Disease
    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 .
    RLX-33
  • HY-P3695
    VSPPLTLGQLLS

    		FGFR Cancer
    VSPPLTLGQLLS is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation .
    VSPPLTLGQLLS
  • HY-12960
    SKLB4771

    FLT3-​IN-​1

    		 FLT3 c-Kit Apoptosis Cancer
    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 .
    SKLB4771
  • HY-151776
    Cy3 methyltetrazine

    TZ-Cy3

    		 Fluorescent Dye Others
    Cy3 methyltetrazine (TZ-Cy3) is a click chemistry reagent with methyltetrazine building blocks that is highly reactive towards cyclooctene. Cy3 methyltetrazine is also a tetrazine-modified fluorescent probe that can be used to analyze protein phosphorylation in solution and living cells .
    Cy3 methyltetrazine
  • HY-P10359
    TAT-QFNP12

    		TGF-beta/Smad MMP Neurological Disease
    TAT-QFNP12 is a peptide that blocks the NDRG2-PPM1A binding and reduces Smad2/3 phosphorylation, decreases astrocytic MMP-9 production and BBB disruption after subarachnoid hemorrhage (SAH) .
    TAT-QFNP12
  • HY-P3695A
    VSPPLTLGQLLS TFA

    		FGFR Cancer
    VSPPLTLGQLLS TFA is a small peptide FGFR3 inhibitor, peptide P3, inhibits FGFR3 phosphorylation. VSPPLTLGQLLS TFA inhibits 9-cisRA-induced tracheal lymphangiogenesis and blocks lymphatic endothelial cell (LEC) proliferation, migration, and tubule formation .
    VSPPLTLGQLLS TFA
  • HY-100830
    NCB-0846
    4 Publications Verification

    		 Wnt MAP4K TGF-beta/Smad Cancer
    NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation .
    NCB-0846
  • HY-15597
    Salinomycin
    35+ Cited Publications

    Procoxacin

    		 Bacterial Wnt β-catenin Mitophagy Autophagy Apoptosis Antibiotic Parasite Cancer
    Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin shows selective activity against human cancer stem cells .
    Salinomycin
  • HY-108559
    L-161982

    		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 .
    L-161982
  • HY-P2282
    APTSTAT3-9R
    1 Publications Verification

    		 STAT Cancer
    APTSTAT3-9R, a specific STAT3-binding peptide, inhibits STAT3 activation and downstream signaling by specifically blocking STAT3 phosphorylation. APTSTAT3-9R exerts antiproliferative effects and antitumor activity .
    APTSTAT3-9R
  • HY-N1987R
    Cucurbitacin IIb (Standard)

    		Reference Standards Apoptosis Inflammation/Immunology
    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 .
    Cucurbitacin IIb (Standard)
  • HY-N2362R
    DL-Alanine (Standard)

    DL-2-Aminopropionic acid (Standard)

    		 Reference Standards Endogenous Metabolite Metabolic Disease
    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 .
    DL-Alanine (Standard)
  • HY-118052
    BPKDi

    		PKD HDAC Cardiovascular Disease
    BPKDi is an inhibitor of PKD. BPKDi inhibits three members of the PKD family, PKD1, PKD2, and PKD3, with IC50 values of 1 nM, 9 nM, and 1 nM, respectively. BPKDi blocks signal-dependent phosphorylation and nuclear export of class IIa HDACs in cardiomyocytes and concomitantly suppresses hypertrophy of these cells .
    BPKDi
  • HY-144012A
    DPPE-PEG350

    16:0 PEG350 PE; 1,2-Dipalmitoyl-sn-glycero-3-phosphoethanolamine-N-[methoxy(polyethylene glycol)-350] ammonium

    		 Liposome CD1 Others
    DPPE-PEG350 is a CD1d-dependent lipid antagonist thus blocking the ERK phosphorylation pathway in iNKT cells . DPPE-PEG350 is a PEG lipid functional end group used in the synthesis of liposomes (LPs) for the design of conjugated polymer nanoparticles.
    DPPE-PEG350
  • HY-139833
    Anti-inflammatory agent 6

    		NF-κB IKK Inflammation/Immunology
    Anti-inflammatory agent 6 blocks the phosphorylation of I kappa b kinase α/β (IKKα/β), IκBα, and nuclear factor kB p65 (NF-κB p65) which is a key controller of inflammation, thereby showing anti-inflammatory potential.
    Anti-inflammatory agent 6
  • HY-18758
    IN-1130
    1 Publications Verification

    		 TGF-β Receptor Inflammation/Immunology Cancer
    IN-1130 is a highly selective transforming growth factor-β type I receptor kinase (ALK5) inhibitor with an IC50 of 5.3 nM for ALK5-mediated Smad3 phosphorylation. IN-1130 inhibits ALK5 phosphorylation of casein (IC50=36 nM) and p38α mitogen-activated protein kinase (IC50=4.3 μM). IN-1130 suppresses renal fibrosis in obstructive nephropathy and blocks breast cancer lung metastasis .
    IN-1130
  • HY-N0811
    Anemarsaponin B

    		NO Synthase COX NF-κB MEK Inflammation/Immunology
    Anemarsaponin B is a steroidal saponin. Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
    Anemarsaponin B
  • HY-17439
    Salinomycin sodium salt
    35+ Cited Publications

    Salinomycin sodium; Sodium salinomycin

    		 Wnt β-catenin Bacterial Autophagy Apoptosis Antibiotic Parasite Cancer
    Salinomycin sodium salt (Salinomycin sodium), an antibiotic potassium ionophore, is a potent inhibitor of Wnt/β-catenin signaling. Salinomycin sodium salt acts on the Wnt/Fzd/LRP complex, blocks Wnt-induced LRP6 phosphorylation, and causes degradation of the LRP6 protein. Salinomycin sodium salt shows selective activity against human cancer stem cells .
    Salinomycin sodium salt
  • HY-155555
    SCAL-266

    		Oxidative Phosphorylation Mitochondrial Metabolism Cancer
    SCAL-266 is a potent mitochondrial complex I (CI) inhibitor with IC50 of 0.83 μM. SCAL-266 blocks mitochondrial function, inhibits OCR, induces ROS production, and reduces MMP. SCAL-266 displays a considerable antiproliferation effect against oxidative phosphorylation (OXPHOS)-dependent cancer cells .
    SCAL-266
  • HY-110198
    ONO-8130

    		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 .
    ONO-8130
  • HY-112700
    SHIP2-IN-1

    		Phosphatase Neurological Disease
    SHIP2-IN-1 is a potent SHIP2 inhibitor, inhibits SHIP2 activity, with an IC50 of 2 μM. SHIP2-IN-1 blocks GSK3β activation by phosphorylation at the Ser9 residue. SHIP2-IN-1 is used in the research of Alzheimer’s disease .
    SHIP2-IN-1
  • HY-147905
    CDK9-IN-18

    		CDK Apoptosis Cancer
    CDK9-IN-18 is a potent CDK9 inhibitor. CDK9-IN-18 blocks the phosphorylation function of kinase CDK9. CDK9-IN-18 exhibits both good anticancer activity and low cellular activity. CDK9-IN-18 induces apoptosis.
    CDK9-IN-18
  • HY-136882
    TM-1

    		PDHK Cancer
    TM-1 is a potent inhibitor of pyruvate dehydrogenase kinase (PDHK1). TM-1 inhibits PDHK1 and PDHK2 with IC50s of 2.97 μM and 5.2 μM, respectively. TM-1 blocks pyruvate dehydrogenase complex (PDHC) phosphorylation, and inhibits cell proliferation .
    TM-1
  • HY-170837
    STAT5-IN-3

    		STAT Cancer
    STAT5-IN-3 (Compound 14a) is a STAT5 inhibitor with anticancer activity. STAT5-IN-3 blocks the tyrosine phosphorylation of STAT5A/5B at the Y694/699 sites and significantly reduces the expression of STAT5B protein, thereby inhibiting downstream gene transcription and blocking the proliferation and survival of leukemia cells. Additionally, STAT5-IN-3 holds significant value in overcoming chemotherapy resistance .
    STAT5-IN-3
  • HY-U00462
    D-Mannoheptulose

    		Hexokinase Metabolic Disease Cancer
    D-Mannoheptulose is a 7-carbon keto sugar found in avocado. D-mannoheptulose is a specific inhibitor of D-glucose phosphorylation by hexokinase isoenzymes. D-Mannoheptulose can block insulin release and utilization of carbohydrate in rat. D-Mannoheptulose has various functions as anti-oxidants, anticancer effects and energy sources .
    D-Mannoheptulose
  • HY-12283
    Rostafuroxin
    1 Publications Verification

    PST 2238

    		 Na+/K+ ATPase RSV Cardiovascular Disease
    Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na +,K +-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity .
    Rostafuroxin
  • HY-155805
    CAF-382

    		CDK Cancer
    CAF-382 (compound B1) is an analog of SNS-032 and a CDKL5 and pan-CDK inhibitor with a weak GSK3α/β affinity (>1.8 μM) and inhibitory activity. CAF-382 inhibits CDKL5 and blocks the phosphorylation of the CDKL5 E2 domain .
    CAF-382
  • HY-144043
    ALK5-IN-8

    		TGF-β Receptor Cancer
    ALK5-IN-8 is a potent inhibitor of TGFβRI (ALK5). ALK5-IN-8 Inhibits the phosphorylation of ALK5 on its downstream signaling proteins (Smad2 or Smad3) by blocking the binding of TGFβRI to ligands, thereby affecting or blocking TGF-β signaling. ALK5-IN-8 has the potential for the research of various ALK5-mediated related diseases (extracted from patent WO2021190425A1, compound 1) .
    ALK5-IN-8
  • HY-162317
    AMPK-IN-5

    		JAK p38 MAPK Infection
    AMPK-IN-5 (compound 7m) is a Osthole (HY-N0054) derivative, and blocks MAPK signal transduction by inhibiting the phosphorylation of JNK and p38, thereby inhibiting the release of inflammatory cytokines. AMPK-IN-5 reduce DSS-induced ulcerative colitis and LPS (HY-D1056)-induced acute lung injury .
    AMPK-IN-5
  • HY-P99161
    Tilvestamab

    BGB149

    		 TAM Receptor Cancer
    Tilvestamab (BGB149) is a humanized anti-AXL antibody that blocks AXL-mediated cell signaling. Tilvestamab significantly inhibits Gas6-induced AXL activation in 786-0-Luc RCC cells and inhibits downstream AKT phosphorylation. Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas .
    Tilvestamab
  • HY-149143
    JNJ-28583113
    2 Publications Verification

    		 TRP Channel Inflammation/Immunology
    JNJ-28583113 is an TRPM2 antagonist with brain permeability. JNJ-28583113 inhibits TRPM2 blocked phosphorylation of GSK3α and β subunits. JNJ-28583113 protects cells from oxidative stress induced cell death. JNJ-28583113 also suppresses cytokine release in response to pro-inflammatory stimuli in microglia .
    JNJ-28583113
  • HY-18938A
    Selonsertib hydrochloride

    GS-4997 hydrochloride

    		 Apoptosis MAP3K Cancer
    Selonsertib hydrochloride (GS-4997 hydrochloride) is an orally bioavailable enzyme inhibitor with potential anti-inflammatory, anti-tumor and anti-fibrotic activities. Selonsertib hydrochloride blocks ASK1 phosphorylation and activation by binding to the catalytic kinase domain. Selonsertib hydrochloride prevents the production of inflammatory cytokines and reduces the expression of genes associated with fibrosis. Selonsertib hydrochloride inhibits excessive apoptosis and limits cell proliferation .
    Selonsertib hydrochloride
  • HY-15597R
    Salinomycin (Standard)

    Procoxacin (Standard)

    		 Reference Standards Bacterial Wnt β-catenin Mitophagy Autophagy Apoptosis Antibiotic Parasite Cancer
    Salinomycin (Standard) is the analytical standard of Salinomycin. This product is intended for research and analytical applications. Salinomycin (Procoxacin), a polyether potassium ionophore antibiotic, selectively inhibits the growth of gram-positive bacteria. Salinomycin is a potent inhibitor of Wnt/β-catenin signaling, blocks Wnt-induced LRP6 phosphorylation. Salinomycin shows selective activity against human cancer stem cells[1][2][3].
    Salinomycin (Standard)
  • HY-125158
    HOI-07

    		Aurora Kinase Apoptosis Cancer
    HOI-07 is a selective Aurora B kinase inhibitor. HOI-07 blocks phosphorylation of histone H3 on Ser10 in lung cancer cells. HOI-07 induces cell-cycle arrest, and apoptosis. HOI-07 has antitumor activity, and suppresses the tumor growth of A549, 143B and KHOS xenografts .
    HOI-07
  • HY-100830A
    NCB-0970

    		Wnt MAP4K TGF-beta/Smad Inflammation/Immunology
    NCB-0970 is the negative control of NCB-0846 (HY-100830). NCB-0846 is an orally active, selective inhibitor for Wnt, that inhibits Traf2- and Nck-interacting kinase (TNIK) with an IC50 of 21 nM. NCB-0846 blocks TGF-β signaling pathway by inhibiting SMAD2/3 phosphorylation and nuclear translocation .
    NCB-0970

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