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TAK inhibitor

" in MedChemExpress (MCE) Product Catalog:

119

Inhibitors & Agonists

1

Biochemical Assay Reagents

5

Peptides

7

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. 상품명 Target 연구분야 Chemical Structure
  • HY-11109
    Resatorvid
    Maximum Cited Publications
    494 Publications Verification

    TAK-242; CLI-095

    		 Toll-like Receptor (TLR) TNF Receptor Interleukin Related Autophagy Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Resatorvid (TAK-242) is a selective Toll-like receptor 4 (TLR4) inhibitor. Resatorvid inhibits NO, TNF-α and IL-6 production with IC50s of 1.8 nM, 1.9 nM and 1.3 nM, respectively. Resatorvid downregulates expression of TLR4 downstream signaling molecules MyD88 and TRIF. Resatorvid inhibits autophagy and plays pivotal role in various inflammatory diseases .
    Resatorvid
  • HY-111789
    Subasumstat
    30+ Cited Publications

    TAK-981

    		 E1/E2/E3 Enzyme Inflammation/Immunology Cancer
    Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities .
    Subasumstat
  • HY-100487
    TAK-243
    80+ Cited Publications

    MLN7243

    		 E1/E2/E3 Enzyme NF-κB Apoptosis Cancer
    TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis .
    TAK-243
  • HY-13328
    Sapanisertib
    50+ Cited Publications

    INK-128; MLN0128; TAK-228

    		 mTOR Autophagy Cancer
    Sapanisertib (INK-128; MLN0128; TAK-228) is an orally available, ATP-dependent mTOR1/2 inhibitor with an IC50 of 1 nM for mTOR kinase.
    Sapanisertib
  • HY-103490
    Takinib
    25+ Cited Publications

    EDHS-206

    		 MAP3K Apoptosis Infection Inflammation/Immunology Cancer
    Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
    Takinib
  • HY-15246
    Tovorafenib
    5+ Cited Publications

    TAK-580; MLN 2480; BIIB-024

    		 Raf Cancer
    Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase. Tovorafenib can be used for the study of glioma .
    Tovorafenib
  • HY-14882
    Cenicriviroc
    5+ Cited Publications

    TAK-652; TBR-652

    		 CCR HIV Infection Endocrinology
    Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity .
    Cenicriviroc
  • HY-12686
    5Z-7-Oxozeaenol
    25+ Cited Publications

    FR148083; L783279; LL-Z 1640-2

    		 MAP3K VEGFR Antibiotic Infection Inflammation/Immunology
    5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.
    5Z-7-Oxozeaenol
  • HY-15295
    Vonoprazan Fumarate
    5+ Cited Publications

    TAK-438

    		 Proton Pump Metabolic Disease Cancer
    Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease .
    Vonoprazan Fumarate
  • HY-147141
    HS-276
    2 Publications Verification

    		 IRAK TNF Receptor Casein Kinase Interleukin Related Inflammation/Immunology
    HS-276 is an orally active, potent and highly selective TAK1 inhibitor, with a Ki of 2.5 nM. HS-276 shows significant inhibition of TAK1, CLK2, GCK, ULK2, MAP4K5, IRAK1, NUAK, CSNK1G2, CAMKKβ-1, and MLK1, with IC50 values of 8.25, 29, 33, 63, 125, 264, 270, 810, 1280, and 5585 nM, respectively. HS-276 reduces the expression of TNF, IL-6, and IL-1β. HS-276 can be used for rheumatoid arthritis (RA) research .
    HS-276
  • HY-15160
    TAK-960
    2 Publications Verification

    		 Polo-like Kinase (PLK) Cancer
    TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts .
    TAK-960
  • HY-135815
    Mobocertinib
    10+ Cited Publications

    TAK-788; AP32788

    		 EGFR Cancer
    Mobocertinib (TAK-788) is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib can be used in NSCLC research .
    Mobocertinib
  • HY-13406
    TAK-779
    10+ Cited Publications

    TAKeda 779

    		 CCR HIV CXCR Infection Inflammation/Immunology Endocrinology
    TAK-779 is a potent and selective nonpeptide antagonist of CCR5 and CXCR3, with a Ki of 1.1 nM for CCR5, and effectively and selectively inhibits R5 HIV-1, with EC50 and EC90 of 1.2 nM and 5.7 nM, respectively, in MAGI-CCR5 cells.
    TAK-779
  • HY-100007
    Vonoprazan
    5+ Cited Publications

    TAK-438 free base

    		 Proton Pump Bacterial Endocrinology Cancer
    Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease. Vonoprazan can be used for eradication of Helicobacter pylori .
    Vonoprazan
  • HY-10456
    TAK-715
    10+ Cited Publications

    		 p38 MAPK Casein Kinase Wnt Inflammation/Immunology
    TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
    TAK-715
  • HY-13449
    TAK-733
    5+ Cited Publications

    		 MEK Cancer
    TAK-733 is a potent and selective MEK allosteric site inhibitor with an IC50 of 3.2 nM.
    TAK-733
  • HY-13501
    Mubritinib
    5+ Cited Publications

    TAK-165

    		 EGFR Cancer
    Mubritinib (TAK-165) is a potent and selective EGFR2/HER2 inhibitor with an IC50 of 6 nM.
    Mubritinib
  • HY-100888
    Simurosertib
    10+ Cited Publications

    TAK-931

    		 CDK Cancer
    Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM. Simurosertib has anti-cancer activity .
    Simurosertib
  • HY-16274
    Lapaquistat acetate
    1 Publications Verification

    TAK-475

    		 Farnesyl Transferase Metabolic Disease
    Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway . Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research .
    Lapaquistat acetate
  • HY-15196
    TAK-285
    3 Publications Verification

    		 EGFR Cancer
    TAK-285 is a potent, selective, ATP-competitive and orally active HER2 and EGFR(HER1) inhibitor with IC50 of 17 nM and 23 nM, respectively. TAK-285 is >10-fold selectivity for HER1/2 than HER4, and less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc. TAK-285 has effective antitumor activity . TAK-285 can cross the blood-brain barrier (BBB) .
    TAK-285
  • HY-109123
    Soticlestat

    TAK-935; OV935

    		 Cytochrome P450 Neurological Disease
    Soticlestat (TAK-935; OV935) is a first-in-class, potent, selective, and orally active cholesterol 24-hydroxylase (CH24H) inhibitor. Soticlestat has the potential for epilepsy syndromes research .
    Soticlestat
  • HY-12472
    Balipodect
    2 Publications Verification

    TAK-063

    		 Phosphodiesterase (PDE) Infection Neurological Disease Cancer
    Balipodect (TAK-063) is a selective, brain-penetrant and orally active PDE10A inhibitor with an IC50 of 0.30 nM. Balipodect shows >15000-fold selectivity over other PDEs. Balipodect elevates striatal cAMP and cGMP levels in mice. Balipodect can be used for the study of schizophrenia[1].
    Balipodect
  • HY-15434
    NG25
    20+ Cited Publications

    		 MAP4K MAP3K Inflammation/Immunology Cancer
    NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
    NG25
  • HY-14882A
    Cenicriviroc Mesylate
    5+ Cited Publications

    TAK-652 Mesylate; TBR-652 Mesylate

    		 CCR HIV Infection Inflammation/Immunology Endocrinology
    Cenicriviroc Mesylate (TAK-652 Mesylate) is a dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity.
    Cenicriviroc Mesylate
  • HY-12201
    TAK-901
    5 Publications Verification

    		 Aurora Kinase Cancer
    TAK-901 is a multi-targeted aurora inhibitor with IC50s of 21 and 15 nM for aurora A and B, respectively.
    TAK-901
  • HY-15767
    TAK-632
    4 Publications Verification

    		 Raf Aurora Kinase Cancer
    TAK-632 is a potent pan-RAF inhibitor with IC50 of 1.4, 2.4 and 8.3 nM for CRAF, BRAF V600E, BRAF WT, respectively.
    TAK-632
  • HY-100867A
    Mivavotinib monohydrochloride

    TAK-659 monohydrochloride; CB-659 monohydrochloride

    		 Syk FLT3 Cancer
    TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
    Mivavotinib monohydrochloride
  • HY-15506
    TAK-593
    1 Publications Verification

    		 PDGFR VEGFR Cancer
    TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
    TAK-593
  • HY-114454
    INH14
    5 Publications Verification

    		 IKK Inflammation/Immunology Cancer
    INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity .
    INH14
  • HY-N0894
    Octahydrocurcumin
    1 Publications Verification

    Hexahydrobisdemethoxycurcumin

    		 Apoptosis MAP4K NF-κB COX Inflammation/Immunology Cancer
    Octahydrocurcumin (Hexahydrobisdemethoxycurcumin) is an orally active anticancer and anti-inflammatory agent, and is the final hydrogenated metabolite of Curcumin (HY-N0005) in vivo. Octahydrocurcumin exerts its anti-tumor and anti-inflammatory effects by inducing the mitochondrial apoptosis pathway and inhibiting the TAK1-NF-κB-COX-2 pathway, respectively .
    Octahydrocurcumin
  • HY-77251
    TAK1/MAP4K2 inhibitor 1
    1 Publications Verification

    		 MAP4K MAP3K Cancer
    TAK1/MAP4K2 inhibitor 1 is a potent dual TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2) inhibitor, with IC50s of 41.1 nM and 18.2 nM, respectively.
    TAK1/MAP4K2 inhibitor 1
  • HY-122642
    TAK1-IN-4

    		MAP3K Inflammation/Immunology
    TAK1-IN-4 (Compound 14) is a TAK1 inhibitor .
    TAK1-IN-4
  • HY-138830
    TAK-418
    2 Publications Verification

    		 Histone Demethylase Neurological Disease
    TAK-418 is a selective, orally active LSD1 (KDM1A) enzyme inhibitor with an IC50 of 2.9 nM. TAK-418 unlocks aberrant epigenetic machinery and improves autism symptoms in neurodevelopmental disorder models .
    TAK-418
  • HY-135815A
    Mobocertinib succinate
    10+ Cited Publications

    TAK-788 succinate; AP32788 succinate

    		 EGFR Cancer
    Mobocertinib (TAK-788) succinate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib succinate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib succinate can be used in NSCLC research .
    Mobocertinib succinate
  • HY-109183
    Luvadaxistat

    TAK-831

    		 Xanthine Oxidase Others
    Luvadaxistat (TAK-831) is an orally active, highly selective, potent D-amino acid oxidase (DAAO) inhibitor. Luvadaxistat inhibits oxidative deamination of D-serine via the human recombinant DAAO enzyme with an IC50 of 14 nM. Luvadaxistat significantly increases D-serine levels in the rodent brain, plasma, and cerebrospinal fluid. Luvadaxistat has the potential for schizophrenia research .
    Luvadaxistat
  • HY-B0189B
    Mosapride citrate dihydrate
    5+ Cited Publications

    TAK-370 citrate dihydrate; AS-4370 citrate dihydrate

    		 5-HT Receptor Potassium Channel Cytochrome P450 Metabolic Disease Cancer
    Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM . Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo .
    Mosapride citrate dihydrate
  • HY-W013636C
    2-Ketoglutaric acid potassium
    5+ Cited Publications

    Alpha-Ketoglutaric acid potassium

    		 Tyrosinase Endogenous Metabolite TNF Receptor Neurological Disease Metabolic Disease
    2-Ketoglutaric acid (Alpha-Ketoglutaric acid) (potassium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid potassium is a reversible and orally active inhibitor of tyrosinase with an IC50 value of 15 mM. 2-Ketoglutaric acid potassium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid potassium significantly suppresses abnormal intestinal permeability, delocalization of tight junction proteins from the intestinal cells, expression of TNFα in vitro and in vivo. 2-Ketoglutaric acid potassium directly binds to TAK1, and inhibits the TRAF6-TAK1 interaction. 2-Ketoglutaric acid potassium also alleviates inflammatory bowel disease (IBD) symptoms and gut microbiota dysbiosis, evident by the improvements in the intestine length .
    2-Ketoglutaric acid potassium
  • HY-19974
    TAK-220
    3 Publications Verification

    		 CCR HIV Infection Endocrinology
    TAK-220 is a selective and orally bioavailable CCR5 antagonist, with IC50s of 3.5 nM and 1.4 nM for inhibition on the binding of RANTES and MIP-1α to CCR5, respectively, but shows no effect on the binding to CCR1, CCR2b, CCR3, CCR4, or CCR7; TAK-220 also selectively inhibits HIV-1, with EC50s of 1.2 nM (HIV-1 KK), 0.72 nM (HIV-1 CTV), 1.7 nM (HIV-1 HKW), 1.7 nM (HIV-1 HNK), 0.93 nM (HIV-1 HTN), and 0.55 nM (HIV-1 HHA), and EC90s of 12 nM (HIV-1 KK), 5 nM (HIV-1 CTV), 12 nM (HIV-1 HKW), 28 nM (HIV-1 HNK), 15 nM (HIV-1 HTN), and 4 nM (HIV-1 HHA) in PBMCs.
    TAK-220
  • HY-115743
    TAK1-IN-3

    		MAP3K Cancer
    TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
    TAK1-IN-3
  • HY-169949
    TAK-756

    		MAP3K NF-κB MMP Leukotriene Receptor Inflammation/Immunology
    TAK-756 is a selective transforming growth factor β-activated kinase 1 (TAK1) inhibitor with a target pIC50 of 8.6. TAK-756 can inhibit TAK1 autophosphorylation and downstream NF-κB phosphorylation, suppress the production of inflammatory and catabolic factors such as MMP-3 and IL-6. TAK-756 exhibits anti-inflammatory effects in a rat joint inflammation model. TAK-756 can be used for the research of inflammatory joint disease, osteoarthritis .
    TAK-756
  • HY-132172
    TAK1-IN-2

    		MAP3K Cancer
    TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM .
    TAK1-IN-2
  • HY-103493
    TAK-915

    		Phosphodiesterase (PDE) Neurological Disease
    TAK-915 is a potent, selective, brain-penetrant and orally active phosphodiesterase 2A (PDE2A) inhibitor with an IC50 of 0.61 nM. TAK-915 is >4100-fold more selectivity for PDE2A than PDE1A. TAK-915 has the potential for neuropsychiatric and neurodegenerative disorders treatment .
    TAK-915
  • HY-132879
    TAK-020

    		Btk Inflammation/Immunology
    TAK-020 is a covalent Btk inhibitor, which becomes the clinical candidate.
    TAK-020
  • HY-100888A
    (R)-Simurosertib

    (R)-TAK-931

    		 CDK Others
    (R)-Simurosertib ((R)-TAK-931) is the (R)-enantiomer of Simurosertib. Simurosertib (TAK-931) is an orally active, selective and ATP-competitive cell division cycle 7 (CDC7) kinase inhibitor, with an IC50 of <0.3 nM .
    (R)-Simurosertib
  • HY-150612
    (R)-STU104

    		p38 MAPK Cancer
    (R)-STU104 is a potent and orally active TAK1-MKK3 interaction inhibitor with IC50s of 0.58 μM and 4.0 μM for TNF-α and MKK3 phosphorylation. (R)-STU104 suppresses the TAK1/MKK3/p38/MnK1/MK2/elF4E signal pathways through binding with MKK3 and disrupting the TAK1 phosphorylating MKK3. (R)-STU104 can be used for researching ulcerative colitis .
    (R)-STU104
  • HY-10505
    Orteronel
    2 Publications Verification

    TAK-700

    		 Cytochrome P450 Cancer
    Orteronel (TAK-700) is a highly selective inhibitor of human 17,20-lyase (CYP17) with IC50 of 38 nM, and exhibits >1000-fold selectivity over other CYPs such as 11-hydroxylase and CYP3A4 .
    Orteronel
  • HY-N1904
    4′-Hydroxywogonin

    8-Methoxyapigenin

    		 IKK NF-κB p38 MAPK PI3K Akt Reactive Oxygen Species (ROS) Interleukin Related TNF Receptor Apoptosis Caspase Bcl-2 Family Cardiovascular Disease Inflammation/Immunology Cancer
    4′-Hydroxywogonin (8-Methoxyapigenin), a flavonoid, could be isolated from a variety of plants including Scutellaria barbata and Verbena littoralis. 4′-Hydroxywogonin has anti-inflammatory activity via TAK1/IKK/NF-κB, MAPKs and PI3/AKT signaling pathways. 4′-Hydroxywogonin inhibits angiogenesis by disrupting PI3K/AKT signaling. 4′-Hydroxywogonin inhibits cell proliferation and induces apoptosis .
    4′-Hydroxywogonin
  • HY-117319
    Indolmycin

    TAK-083; PA-155A

    		 Antibiotic Bacterial Infection Inflammation/Immunology
    Indolmycin (TAK-083), an antibiotic, is a competitive inhibitor of prokaryotic tryptophanyl-tRNA synthetase (TrpS). Indolmycin (TAK-083) possesses both anti-viral and anti-bacterial activity .
    Indolmycin
  • HY-120823
    PF-05381941

    		MAP3K p38 MAPK Inflammation/Immunology
    PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC50s of 156 and186 nM, respectively .
    PF-05381941
  • HY-111789A
    (S)-Subasumstat

    (S)-TAK-981

    		 Drug Isomer Inflammation/Immunology Cancer
    (S)-Subasumstat is the isomer of Subasumstat (HY-111789). Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities .
    (S)-Subasumstat

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