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Isoforms Recommended: MAP3K7/TAK1
Results for "

TAK1

" in MedChemExpress (MCE) Product Catalog:

38

Inhibitors & Agonists

3

Peptides

10

Natural
Products

3

Recombinant Proteins

6

Antibodies

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-132172
    TAK1-IN-2

    		MAP3K Cancer
    TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM [1].
    TAK1-IN-2
  • HY-115743
    TAK1-IN-3

    		MAP3K Cancer
    TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.
    TAK1-IN-3
  • HY-122642
    TAK1-IN-4

    		MAP3K Inflammation/Immunology
    TAK1-IN-4 (Compound 14) is a TAK1 inhibitor [1].
    TAK1-IN-4
  • 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-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 [1].
    (R)-STU104
  • 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 [1].
    PF-05381941
  • HY-15434
    NG25
    Maximum Cited Publications
    24 Publications Verification

    		 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-157871
    TAK1-IN-5

    		MAP3K Cancer
    TAK1-IN-5 (Compound 26) is an inhibitor of the transforming growth factor-β activated kinase (TAK1) with an IC50 value of 55 nM. TAK1-IN-5 can inhibit the growth of MPC-11 and H929 cells with a GI50 lower than 30 nM. TAK1-IN-5 can be used in the study of multiple myeloma [1].
    TAK1-IN-5
  • HY-153320
    AZ-TAK1

    		MAP3K Cancer
    AZ-TAK1, an ATP-competitive small molecule inhibitor of TAK1, dephosphorylates TAK1, p38, and IκB-α in lymphoma cell lines [1].
    AZ-TAK1
  • HY-169949
    TAK-756

    		MAP3K Inflammation/Immunology
    TAK-756 is a TAK1 inhibitor with good selectivity for IRAK1/4 and excellent intra-articular pharmacokinetic properties. TAK1 is a potential molecular target for osteoarthritis (OA) with complementary anti-catabolic and anti-inflammatory effects [1].
    TAK-756
  • HY-N2435
    [8]-Shogaol
    3 Publications Verification

    		 COX Apoptosis Cancer
    [8]-Shogaol, a kind of stimulating compound in ginger, has antiplatelet (IC50=5 μM), anti-cancer and anti-inflammatory activity. [8]-Shogaol inhibited COX-2 (IC50=17.5 μM), which led to the decline of human leukemia cells. 8-Shogaol Selective direction TAK1 sum TAK1-TAB1 (IC50=5 μM), suppress IKK, Akt sum MAPK signal pathway, and reverse synovitis synovial sum Air dampness (RA) [1] .
    [8]-Shogaol
  • HY-147141
    HS-276

    		IRAK TNF Receptor Casein Kinase 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 can be used for rheumatoid arthritis (RA) research [1].
    HS-276
  • HY-N2435R
    [8]-Shogaol (Standard)

    		COX Apoptosis Cancer
    -Shogaol (Standard) is the analytical standard of -Shogaol. This product is intended for research and analytical applications. -Shogaol, a kind of stimulating compound in ginger, has antiplatelet (IC50=5 μM), anti-cancer and anti-inflammatory activity. -Shogaol inhibited COX-2 (IC50=17.5 μM), which led to the decline of human leukemia cells. 8-Shogaol Selective direction TAK1 sum TAK1-TAB1 (IC50=5 μM), suppress IKK, Akt sum MAPK signal pathway, and reverse synovitis synovial sum Air dampness (RA) [1] .
    [8]-Shogaol (Standard)
  • HY-12686
    5Z-7-Oxozeaenol
    20+ 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-103490
    Takinib
    20+ 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) [1] .
    Takinib
  • HY-N15315
    Triptriolide

    		Apoptosis MAP3K NF-κB Others
    Triptriolide inhibits Puromycin aminonucleoside PAN (HY-15695)-induced apoptosis in mouse podocytes through regulation of Bcl-2 family proteins and inhibition of Caspase-3. Triptriolide promotes the cell survival, protects and restores the podocyte function through activation of TAK1-NF-κB signaling pathway and upregulation of podocin [1].
    Triptriolide
  • HY-15434A
    NG25 trihydrochloride

    		MAP3K MAP4K Cancer
    NG25 trihydrochloride is a dual TAK1 and MAP4K2 inhibitor (IC50: 149 nM and 21.7 nM respectively). NG25 sensitizes the breast cancer cells to Doxorubicin (HY-15142A), and enhances apoptosis. NG25 trihydrochloride can be used for research of various cancers [1] .
    NG25 trihydrochloride
  • HY-W995241
    BPD

    		COX NF-κB Inflammation/Immunology
    BPD is a COX-2 and TAK1-NF-κB inhibitor, with an IC50 of 18.5 μM for COX-2. BPD inhibits the expression of iNOS, TNF-α, IL-6 and IL-1β at the transcriptional level. BPD has anti-inflammatory activity. BPD can inhibit Carrageenan-induced paw oedema and LPS-induced septic death [1].
    BPD
  • HY-114454
    INH14
    3 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 [1].
    INH14
  • HY-115630
    cRIPGBM chloride

    		RIP kinase Caspase Apoptosis Cancer
    cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models [1].
    cRIPGBM chloride
  • HY-134911
    HS-243

    		IRAK CDK Inflammation/Immunology Cancer
    HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity [1].
    HS-243
  • HY-151363
    IRAK4-IN-21

    		IRAK Inflammation/Immunology
    IRAK4-IN-21 (compound 17) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 5 and 56 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.17 μM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis [1].
    IRAK4-IN-21
  • HY-151365
    IRAK4-IN-22

    		IRAK Inflammation/Immunology
    IRAK4-IN-22 (compound 18) is an orally active, potent and selective IRAK4 inhibitor with IC50 values of 3 and 17 nM for IRAK4 and TAK1, respectively. IRAK4-IN-21 effectively inhibits IL-23 production (IC50=0.10 µM) and can be used in studies of autoimmune diseases such as plaque psoriasis and psoriatic arthritis [1].
    IRAK4-IN-22
  • HY-N1904
    4′-Hydroxywogonin

    8-Methoxyapigenin

    		 IKK NF-κB p38 MAPK PI3K Akt Reactive Oxygen Species 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 [1] .
    4′-Hydroxywogonin
  • HY-W011121
    2-Oleoylglycerol

    2-OG

    		 GPR119 NF-κB TGF-beta/Smad GLP Receptor Metabolic Disease
    2-Oleoylglycerol (2-OG) is a lipid found in the diet. It is a GPR119 agonist, with an EC50 value of 2.5 μM in activating hGPR119 in transiently transfected COS-7 cells. 2-Oleoylglycerol enhances the inflammatory response of macrophages and promotes fibrosis by activating the GPR119/TAK1/NF-κB/TGF-β1 signaling pathway. It also stimulates glucagon-like peptide 1 (GLP-1) secretion in vivo. 2-Oleoylglycerol is expected to be used in the research of non-alcoholic steatohepatitis (NASH) [1] .
    2-Oleoylglycerol
  • HY-D0885
    Phosphocreatine
    1 Publications Verification

    Creatine phosphate; Creatinephosphoric acid

    		 Endogenous Metabolite MAP3K Akt Mitochondrial Metabolism ERK Apoptosis ROS Kinase Metabolic Disease
    Phosphocreatine (creatine phosphate) is an organic compound found in vertebrate skeletal muscles. Phosphocreatine enhances antioxidant activity, and activates the TAK1 pathway to protect the heart. Phosphocreatine normalizing mitochondrial function and reducing oxidative stress via Akt mediated Nrf2/HO-1 pathway. Phosphocreatine provides renal protection by suppressing Apoptosis and ROS (Reactive Oxygen Species) generation through ERK mediated mediated Nrf-2/HO-1 pathway. [1] .
    Phosphocreatine
  • HY-D0885C
    Phosphocreatine dipotassium

    Creatine phosphate dipotassium; Creatinephosphoric acid dipotassium

    		 Endogenous Metabolite MAP3K Akt Mitochondrial Metabolism ERK Apoptosis ROS Kinase Metabolic Disease
    Phosphocreatine (creatine phosphate) is an organic compound found in vertebrate skeletal muscles. Phosphocreatine enhances antioxidant activity, and activates the TAK1 pathway to protect the heart. Phosphocreatine normalizing mitochondrial function and reducing oxidative stress via Akt mediated Nrf2/HO-1 pathway. Phosphocreatine provides renal protection by suppressing Apoptosis and ROS (Reactive Oxygen Species) generation through ERK mediated mediated Nrf-2/HO-1 pathway. [1] .
    Phosphocreatine dipotassium
  • HY-N6969A
    Dicentrine hydrochloride

    		Adrenergic Receptor Cancer
    Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 [1].
    Dicentrine hydrochloride
  • HY-145015
    Tuspetinib

    HM43239

    		 FLT3 Apoptosis Cancer
    Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells [1] .
    Tuspetinib
  • HY-145015A
    Tuspetinib hydrate

    HM43239 hydrate

    		 FLT3 Apoptosis Cancer
    Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells [1] .
    Tuspetinib hydrate
  • HY-15504A
    RGB-286638 free base
    2 Publications Verification

    		 CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
    RGB-286638 free base
  • HY-136848
    SM1-71

    		MAP3K Src FGFR Ribosomal S6 Kinase (RSK) LIM Kinase (LIMK) Cancer
    SM1-71 (compound 5) is a potent TAK1 inhibitor, with a Ki of 160 nM, it also can covalently inhibit MKNK2, MAP2K1/2/3/4/6/7, GAK, AAK1, BMP2K, MAP3K7, MAPKAPK5, GSK3A/B, MAPK1/3, SRC, YES1, FGFR1, ZAK (MLTK), MAP3K1, LIMK1 and RSK2. SM1-71 can inhibit proliferation of multiple cancer cell lines [1] .
    SM1-71
  • HY-15504
    RGB-286638
    2 Publications Verification

    		 CDK GSK-3 MEK JAK Cancer
    RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
    RGB-286638
  • HY-N10156
    1,3,5-Trihydroxy-4-prenylxanthone

    		Na+/H+ Exchanger (NHE) Phosphodiesterase (PDE) NO Synthase Inflammation/Immunology
    1,3,5-Trihydroxy-4-prenylxanthone is a Na +/H + exchange system (Na+/H+ Exchanger (NHE)) inhibitor with a minimum inhibitory concentration of 10 μg/mL [1]. 1,3,5-Trihydroxy-4-prenylxanthone is a phosphodiesterase type 5 (PDE5) (Phosphodiesterase (PDE)) inhibitor with an IC50 value of 3.0 μM . 1,3,5-Trihydroxy-4-prenylxanthone inhibits Lipopolysaccharide (LPS) (Lipopolysaccharides (HY-D1056))-induced NO production in RAW264.7 macrophages, and has anti-inflammatory activities .
    1,3,5-Trihydroxy-4-prenylxanthone
  • HY-10456
    TAK-715
    10+ Cited Publications

    		 p38 MAPK Casein Kinase 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 [1] .
    TAK-715
  • HY-P2161B
    TAK-683 acetate
    1 Publications Verification

    		 Kisspeptin Receptor Cancer
    TAK-683 acetate is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 acetate is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively [1]. TAK-683 acetate depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer [1] .
    TAK-683 acetate
  • HY-P2161
    TAK-683

    		Kisspeptin Receptor Cancer
    TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively [1]. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer [1] .
    TAK-683
  • HY-P2161A
    TAK-683 TFA

    		Kisspeptin Receptor Cancer
    TAK-683 TFA is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 TFA is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively [1]. TAK-683 TFA depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer [1] .
    TAK-683 TFA

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