2. Search Result
Search Result
Results for "

dual inhibition

" in MedChemExpress (MCE) Product Catalog:

53

Inhibitors & Agonists

1

Inhibitory Antibodies

1

Isotope-Labeled Compounds

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-129496
    NP-313

    		Thrombin Cardiovascular Disease
    NP-313 is a potent antithrombotic agent that inhibits platelet aggregation and activation. NP-313 has dual inhibition of thromboxane A 2 synthesis and selective inhibition of SOCC-mediated Ca 2+ inward flow .
    NP-313
  • HY-U00177
    GDP366
    1 Publications Verification

    		 Survivin Cancer
    GDP366, a dual inhibitor of survivin and Op18, induces cell growth inhibition, cellular senescence and mitotic catastrophe in human cancer cells.
    GDP366
  • HY-P99940
    Remtolumab

    ABT-122

    		 TNF Receptor Interleukin Related Inflammation/Immunology
    Remtolumab (ABT-122) is a dual-variable domain immunoglobulin that neutralises both tumor necrosis factor α (TNFα) and IL-17A. Remtolumab shows dual inhibition of TNFα and IL-17A. Remtolumab can be used for rheumatoid arthritis (RA) research .
    Remtolumab
  • HY-12299
    WH-4-023
    4 Publications Verification

    dual LCK/SRC inhibitor

    		 Src Cancer
    WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
    WH-4-023
  • HY-174366
    JMC14

    		c-Fms PI3K Cancer
    JMC14 is a selective and orally active PI3Kδ and CSF1R inhibitor with IC50 values of 12 nM and 143 nM, respectively. JMC14 preferentially inhibits PI3Kδ-mediated signaling at the cellular level. JMC14 demonstrates potent antitumor activity against B-cell lymphomas and triple-negative breast cancer (TNBC) in both in vitro and vivo studies. JMC14 can be used for the study of antitumor immunity .
    JMC14
  • HY-157290
    HL403

    		Epigenetic Reader Domain Src Cancer
    HL403 is a potent and dual BRD4/Src inhibitor. HL403 has IC50 values of 133 nM for BRD4 inhibition and 4.5 nM for Src inhibition. HL403 shows anti-cancer activity .
    HL403
  • HY-19876
    PL37

    Debio-0827

    		 Opioid Receptor Aminopeptidase Neprilysin Neurological Disease Metabolic Disease
    PL37 (Debio-0827) is an orally active Enkephalinase dual inhibitor (dual inhibition refers to the simultaneous inhibition of Neutral Endopeptidase and Aminopeptidase N activities). PL37 exerts its anti-hyperalgesic effects by activating μ-opioid receptors (µ-opioid receptors), with an ED50 value of 13.4 mg/kg for analgesic effects in mice. PL37 can be used to study diabetic neuropathic pain .
    PL37
  • HY-158763
    MPI8

    TG0205221

    		 SARS-CoV Cathepsin Virus Protease Infection
    MPI8 (TG0205221) is an inhibitor of the major protease of SARS-CoV-2 (MPro) with high antiviral activity. MPI8 exerts its antiviral effect by dual and selective inhibition of SARS-CoV-2 MPro and host cell cysteine protease L (cathepsin L). This dual inhibition enhanced the overall antiviral potency and effect of MPI8. MPI8 can be used in clinical studies of COVID-19 .
    MPI8
  • HY-117761
    MHY908

    		PPAR Metabolic Disease Cancer
    MHY908 is a potent dual agonist of PPARα and PPARγ . MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity .
    MHY908
  • HY-163755
    GPER activator 1

    		Estrogen Receptor/ERR Inflammation/Immunology
    GPER activator 1 (compound 6-26) is a GPER-selective compound without cytotoxicity. GPER activator 1 exhibits dual inhibition of TNFα- and IL-6-induced inflammation .
    GPER activator 1
  • HY-141864
    ITK/TRKA-IN-1

    		Itk Inflammation/Immunology
    ITK/TRKA-IN-1 is a dual inhibitor of IL-2-inducible T-cell kinase (ITK) and tropomyosin receptor kinase A (TRKA) with an IC50 value of 1.0 nM and 96 % inhibition, respectively.
    ITK/TRKA-IN-1
  • HY-161515
    BRD4/NAMPT-IN-1

    		NAMPT Epigenetic Reader Domain Cancer
    BRD4/NAMPT-IN-1 (Compound A2) shows strong inhibitory effects on NAMPT and BRD4 (IC50=35 nM (NAMPT) and 58 nM (BRD4)). BRD4/NAMPT-IN-1 inhibits the growth and migration of hepatocellular carcinoma cells and promotes apoptosis. BRD4/NAMPT-IN-1 also shows potent anticancer effects in HCCLM3 xenograft mouse model, with no obvious toxic effects .
    BRD4/NAMPT-IN-1
  • HY-141543
    YW2065

    		β-catenin Cancer
    YW2065 is an Axin-1 stabilizer. Axin-1 is a scaffolding protein that regulates proteasome degradation of β-catenin. YW2065 exhibits anti-colorectal cancer effects via dual activities of wnt/β-catenin signaling inhibition and AMPK activation .
    YW2065
  • HY-162228
    VI-60

    		COX Phospholipase Inflammation/Immunology
    VI-60 is a dual, orally active inhibitor of cPLA2 and COX-2, which reveals an anti-inflammtory efficacy through the inhibition of p38 MAPK/cPLA2/COX-2/PGE2 pathway .
    VI-60
  • HY-160682
    EGFR/HER2-IN-12

    		EGFR Others
    EGFR/HER2-IN-12 (compound 14b) is a dual inhibitor of EGFR and HER2 with 81% and 51% inhibition at 10 μM. The toxicity of EGFR/HER2-IN-12 to cancer cells A431 and MDA-MB-361 was not significant .
    EGFR/HER2-IN-12
  • HY-15838
    ID-8
    5 Publications Verification

    		 DYRK Cancer
    ID-8 is an inhibitor of dual-specificity tyrosine phosphorylation-regulated kinase (DYRK). ID-8 sustains embryonic stem cell (ESC) self-renewal and pluripotency. ID-8 enhances Wnt-mediated hESC survival and proliferation via inhibition of DYRKs .
    ID-8
  • HY-121736
    AGI-12026

    AGI-026

    		 Isocitrate Dehydrogenase (IDH) Neurological Disease
    AGI-12026 is brain-penetrant dual inhibitor of mutant IDH1 and 2. AGI-12026 shows partial inhibition of the IDH1-R132H homodimer as allosteric modulators. AGI-12026 has the potential for research of glioma .
    AGI-12026
  • HY-106720
    Amosulalol

    YM 09538

    		 Adrenergic Receptor Cardiovascular Disease
    Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
    Amosulalol
  • HY-106720A
    Amosulalol hydrochloride

    YM 09538 hydrochloride

    		 Adrenergic Receptor Cardiovascular Disease
    Amosulalol (YM 09538) hydrochloride is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol hydrochloride exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol hydrochloride decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
    Amosulalol hydrochloride
  • HY-146806
    YL93

    		MDM-2/p53 Cancer
    YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. YL93 induces cell-cycle arrest and apoptosis. YL93 shows p53-dependent cell growth inhibition .
    YL93
  • HY-157087
    AChE/MAO-B-IN-4

    		Cholinesterase (ChE) Monoamine Oxidase Neurological Disease
    AChE/MAO-B-IN-4 (compound 4a) is a selective dual AChE and MAO-B inhibitor. AChE/MAO-B-IN-4 shows no significant inhibition activity against BChE and h-MAO-A. AChE/MAO-B-IN-4 can be used for the Alzheimer’s disease (AD) research .
    AChE/MAO-B-IN-4
  • HY-112293
    GW2974

    		EGFR Cancer
    GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research .
    GW2974
  • HY-163352
    Chitinase-IN-6

    		Insecticide Infection
    Chitinase-IN-6 (Compound 4h) is a potent dual-Chitinase inhibitor, with Ki values of 1.82 and 2.00 μM against OfChtI and OfChi-h, respectively. Chitinase-IN-6 exhibits certain growth inhibition effects against Ostrinia furnacalis. Chitinase-IN-6 is a potential novel insecticide candidate friendly to nontarget organisms .
    Chitinase-IN-6
  • HY-163272
    GPX4/CDK-IN-1

    		Glutathione Peroxidase CDK Cancer
    GPX4/CDK-IN-1 (Compound B9) is a dual inhibitor of GPX4 and CDK, with IC50 values of 542.5 nM, 191.2 nM and 68.1 nM for GPX4, CDK4 and CDK6, reapectively. GPX4/CDK-IN-1 shows strong cancer cell growth inhibition in vivo .
    GPX4/CDK-IN-1
  • HY-170812
    BET/Aurora kinase-IN-1

    		Aurora Kinase Cancer
    BET/Aurora kinase-IN-1 (Compound 38) is a dual BET/Aurora kinase inhibitor. BET/Aurora kinase-IN-1 shows antiproliferative activities on diverse cancer cell lines and favorable antitumor efficacy in renal cell cancer and colon cancer xenograft models with tumor growth inhibition (TGI) of 45.99% and 53.06%, respectively .
    BET/Aurora kinase-IN-1
  • HY-123538
    GRK2 Inhibitor 1

    		Dopamine Receptor G Protein-coupled Receptor Kinase (GRK) Cardiovascular Disease
    GRK2 Inhibitor 1 (methyl 5-[2-(5-nitro-2-furyl)vinyl]-2-furoate) is a dual GRK2/β-ARK1 inhibitor that induces dopamine (DA) inhibition reversal (DIR). GRK2 Inhibitor 1 can also block serotonin-induced or neurotensin-induced DIR reversal. Note: DIR refers to the phenomenon in which neurons in addiction-related brain pathways become less sensitive to DA inhibition when exposed to moderate concentrations of DA for a long time .
    GRK2 Inhibitor 1
  • HY-160481
    MG-1102

    		Tau Protein MicroRNA Neurological Disease
    MG-1102 is first-in-class dual binder of monomeric tau and pre-miRNA-146a. MG-1102 shows specific inhibition of miRNA146a with IC50s of 0.21 mM and 0.36 mM specific inhibition of doublelabeled pre-miRNA146a and mono-labeled pre-miRNA146a, respectively. MG-1102 interacts with tau monomers with a Kd of 3.21 mM by surface plasmon resonance (SPR). MG-1102 is a potential multi-target-directed ligands (MTDLs) for Alzheimer’s disease (AD) .
    MG-1102
  • HY-144315
    CYD19

    Snail/HDAC-IN-1

    		 HDAC Cancer
    CYD19 is a potent Snail/HDAC dual target inhibitor. CYD19 displays potent inhibitory activity against HDAC1 with an IC50 of 0.405 μM and potent inhibition against Snail with a Kd of 0.18 μM. CYD19 increases histone H4 acetylation in HCT-116 cells and decreases the expression of Snail protein to induce cell apoptosis .
    CYD19
  • HY-145406
    IHCH-3064

    		Adenosine Receptor HDAC Inflammation/Immunology Cancer
    IHCH-3064 is a dual-acting compounds targeting Adenosine A2A Receptor and HDAC. IHCH-3064 exhibits potent binding to A2AR (Ki=2.2 nM) and selective inhibition of HDAC1 (IC50=80.2 nM), with good antiproliferative activity against tumor cell lines in vitro. IHCH-3064 is a tumor immunotherapeutic agent.
    IHCH-3064
  • HY-162940
    MerTK/Axl-IN-1

    		TAM Receptor Inflammation/Immunology Cancer
    MerTK/Axl-IN-1 (Compound A-910) is a potent and selective dual MerTK/Axl inhibitor, with IC50s of 4.2 and 8.8 nM in Ba/F3, and 0.2 and 0.9 nM in HTRF. MerTK/Axl-IN-1 results in pMerTK inhibition in vivo. MerTK/Axl-IN-1 has long half-life, high oral exposure and bioavailability .
    MerTK/Axl-IN-1
  • HY-138215
    ADTL-EI1712

    		ERK Cancer
    ADTL-EI1712 is a potent, orally active, and selective dual-target inhibitor of ERK1 and ERK5, inhibition rates of ERK1/5 at 1 μM are 93.54% and 89.35%, respectively. ADTL-EI1712 can induce regulated cell death, a form of cell death that relies on the activation of genetically encoded machinery, to overcome compensatory mechanism in specific cancer cells in vitro and in vivo .
    ADTL-EI1712
  • HY-149819
    CDK/HDAC-IN-3

    		HDAC CDK Cancer
    CDK/HDAC-IN-3 is an orally active HDACs/CDKs dual inhibitor. CDK/HDAC-IN-3 has potent and selective inhibition of CDK9, CDK12, CDK13, HDAC1, HDAC2 and HDAC3 with IC50 values of 98.32 nM, 98.85 nM, 100 nM, 62.12 nM, 93.28nM and 82.87 nM. CDK/HDAC-IN-3 can be used for the acute myeloid leukemia (AML) .
    CDK/HDAC-IN-3
  • HY-144825
    Chol-CTPP

    		Apoptosis Reactive Oxygen Species (ROS) Cancer
    Chol-CTPP is a ligand with dual targeting effect on blood-brain barrier (BBB) and glioma cells. Lip-CTPP can be gained by Chol-CTPP and another mitochondria targeting ligand (Chol-TPP). Lip-CTPP is a promising potential carrier to exert the anti-glioma effect of doxorubicin (DOX) and lonidamine (LND) collaboratively. Lip-CTPP elevates the inhibition rate of tumor cell proliferation, migration and invasion, promote apoptosis and necrosis, and interfere with mitochondrial function .
    Chol-CTPP
  • HY-156523
    TNIK&MAP4K4-IN-1

    		MAP4K Cancer
    TNIK&MAP4K4-IN-1 (compound A-39) is a dual inhibitor of TNIK and MAP4K4/HGK with IC50s of 1.29 nM and <10 nM，respectively，in human hepaticstellate cell LX-2. TNIK&MAP4K4-IN-1 can be used for cancer and fibrosis inhibition .
    TNIK&MAP4K4-IN-1
  • HY-143402
    Topoisomerase I/II inhibitor 2

    		Topoisomerase Cancer
    Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
    Topoisomerase I/II inhibitor 2
  • HY-103160A
    EHNA hydrochloride
    4 Publications Verification

    		 Adenosine Deaminase Phosphodiesterase (PDE) Influenza Virus Infection Cardiovascular Disease Neurological Disease Cancer
    EHNA hydrochloride is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA hydrochloride exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA hydrochloride play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
    EHNA hydrochloride
  • HY-50878A
    Crizotinib hydrochloride
    Maximum Cited Publications
    70 Publications Verification

    PF-02341066 hydrochloride

    		 Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy Cancer
    Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
    Crizotinib hydrochloride
  • HY-103160B
    EHNA

    		Adenosine Deaminase Phosphodiesterase (PDE) Influenza Virus Infection Cardiovascular Disease Neurological Disease Cancer
    EHNA is a potent and selective dual inhibitor of cyclic nucleotide phosphodiesterase 2 (PDE2)(IC50=4 μM) and adenosine deaminase (ADA). EHNA exerts a concentration inhibition of the cGMP-stimulated PDE II (cGs-PDE)(IC50:0.8 μM (human), 2 μM (porcine myocardium)), but has smaller inhibitory effect on the unstimulated PDE2 activity. EHNA play roles in mediating diverse pharmacological responses, including antiviral, antitumour and antiarrhythmic effects .
    EHNA
  • HY-162578
    PPARα/γ agonist 4

    		PPAR Metabolic Disease
    PPARα/γ agonist 4 (Compound (S)-7) is an orally active dual potent agonist of PPARα and PPARγ, with EC50 values of 0.061 μM and 1.42 μM respectively. PPARα/γ agonist 4 acts through an insulin-independent mechanism and exhibits mitochondrial pyruvate carrier inhibition and anti-diabetic properties. PPARα/γ agonist 4 is expected to be used in research for dyslipidemic type 2 diabetes .
    PPARα/γ agonist 4
  • HY-164445
    STAT3-IN-32

    		STAT Cancer
    STAT3-IN-32 (compound 2p) is an orally active, potent STAT3 dual phosphorylation inhibitor with an indole-containing tetra-aromatic heterocycle scaffold. STAT3-IN-32 exhibits STAT3 luciferase inhibition activity using HEK293T cells with an IC50 of 5.3 nM and ATP production inhibition activity using BxPC-3 cells with an IC50 of 4.2 nM. STAT3-IN-32 significantly blocks p-Tyr705 and p-Ser727 and causes the abrogation of the corresponding nuclear transcription and mitochondrial oxidative phosphorylation functions of STAT3 by targeting the STAT3 SH2 domain (KD=21.3 nM). STAT3-IN-32 exhibits significant suppressive effects in a pancreatic cancer xenograft model .
    STAT3-IN-32
  • HY-108347
    CP-100356 hydrochloride
    5+ Cited Publications

    		 P-glycoprotein BCRP Metabolic Disease
    CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) .
    CP-100356 hydrochloride
  • HY-170940
    Dyrk1A-IN-12

    		DYRK Enterovirus Infection
    Dyrk1A-IN-12 (compound S43) is a Dyrk (Dual specificity tyrosine phosphorylation regulated kinase 1A inhibitor. Dyrk1A-IN-12 inhibits Dyrk1A with a IC50 of 95 nM. Dyrk1A-IN-12 shows anti-EV-A71 activity with an EC50 of 4.4 μM, CC50 of 12.8 μM and SI of 2.9. Dyrk1A-IN-12 shows potent inhibition against herpes simplex virus (HSV) .
    Dyrk1A-IN-12
  • HY-50878AS
    Crizotinib-d9 hydrochloride

    PF-02341066-d9 hydrochloride

    		 c-Met/HGFR Autophagy Anaplastic lymphoma kinase (ALK) ROS Kinase Isotope-Labeled Compounds Cancer
    Crizotinib-d9 hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition .
    Crizotinib-d9 hydrochloride
  • HY-120826
    A2AAR/hMAO-B-IN-1

    		Monoamine Oxidase Adenosine Receptor Neurological Disease
    A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
    A2AAR/hMAO-B-IN-1
  • HY-158138
    TOPOI/PARP-1-IN-1

    		PARP Topoisomerase Apoptosis Cancer
    TOPOI/PARP-1-IN-1 (Compound B6) is an orally active, low cytotoxic TOPOI/PARP dual inhibitor with an IC50 value of 0.09 μM for PARP1. TOPOI/PARP-1-IN-1 can effectively inhibit the proliferation and migration of cancer cells. TOPOI/PARP-1-IN-1 also causes cell cycle arrest in the G0/G1 phase and induces apoptosis. The tumor growth inhibition rate (TGI) of TOPOI/PARP-1-IN-1 in mice is 75.4% .
    TOPOI/PARP-1-IN-1
  • HY-159966
    Top/HDAC-IN-3

    		Topoisomerase HDAC Reactive Oxygen Species (ROS) Apoptosis Cancer
    Top/HDAC-IN-3 (Compound 31) is an orally active dual inhibitor of Topoisomerase and HDAC. Top/HDAC-IN-3 increases reactive oxygen species (ROS) levels, leading to DNA damage, thereby inhibiting cancer cell colony formation and migration, inducing cancer cell Apoptosis, and causing cell cycle arrest. In the NSCLC model, Top/HDAC-IN-3 exhibited significant antitumor effects, with a tumor growth inhibition (TGI) of 77.5% at 100 mg/kg, surpassing the efficacy of the HDAC inhibitor SAHA (HY-10221) and the combination of SAHA (HY-10221) with the topoisomerase inhibitor Irinotecan (HY-16562) .
    Top/HDAC-IN-3
  • HY-155066
    FD274

    		PI3K mTOR Cancer
    FD274 is a highly potent PI3K/mTOR dual inhibitor with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
    FD274
  • HY-162910
    HDAC-IN-79

    		Xanthine Oxidase HDAC Autophagy Apoptosis Metabolic Disease Inflammation/Immunology Cancer
    HDAC-IN-79 (compound 4) is an orally active dual xanthine oxidase-HDAC inhibitor (Xanthine oxidase: IC50=6.6 nM; HDAC1: IC50=134 nM; HDAC2: IC50=284 nM; HDAC3: IC50=173 nM; HDAC6: IC50=1.32 nM;), with significant in vivo anti-hyperuricemia and anti-tumor activities. HDAC-IN-79 is the most potent cell growth inhibitor (IC50=0.706 μM) of leukemia HL60 cells, induces apoptosis and autophagy, and can regulate the expression levels of signature biomarkers associated with intracellular HDAC inhibition .
    HDAC-IN-79
  • HY-114796
    tHGA

    		Lipoxygenase Inflammation/Immunology
    tHGA is a compound with anti-inflammatory activity and has the activity to inhibit soybean 15-LOX. tHGA showed significant inhibitory effects in experiments on human leukocytes, with an IC50 value of 0.42 μM, which is close to the effect of commonly used standard NDGA. tHGA concentration-dependently inhibits the synthesis of 5-LOX products, especially the cysteine leukotriene LTC(4), with an IC50 value of 1.80 μM. and showed no cytotoxicity. The anti-inflammatory effects of tHGA do not appear to be through redox or metal chelation mechanisms, as the compound was negative in these bioactivity tests. tHGA works through a dual LOX/COX inhibition mechanism and has higher selectivity for 5-LOX and COX-2, with an IC50 value of 0.40 μM .
    tHGA
  • HY-104042
    Vorasidenib
    4 Publications Verification

    AG-881

    		 Isocitrate Dehydrogenase (IDH) Cancer
    Vorasidenib (AG-881) is an orally available, brain penetrant second-generation dual mutant isocitrate dehydrogenases 1 and 2 (mIDH1/2) inhibitor. Vorasidenib (AG-881) exhibits nanomolar inhibition of (D)-2-hydroxyglutarate (D-2-HG), and the IC50 ranges of 0.04~22 nM against IDH1 R132C, IDH1 R132G, IDH1 R132H and IDH1 R132S and 7~14 nM against IDH2 R140Q and 130 nM against IDH2 R172K. Vorasidenib can be used for the study of grade 2 astrocytoma or oligodendroglioma with a susceptible IDH1/2 mutation .
    Vorasidenib

Inquiry Online

Your information is safe with us. * Required Fields.

Salutation

  

Country or Region *

Applicant Name *

 

Organization Name *

Department *

     

Email Address *

 

Product Name *

Cat. No.

  

Requested quantity *

Phone Number *

     

Remarks

Inquiry Online

Inquiry Information

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent: