MAP3K Inhibitor

MAP3K Inhibitors (40):

Cat. No.	Product Name	Effect	Purity

HY-103490

Takinib	Inhibitor	98.92%
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 (K_D(app) of 0.46 μM).

HY-12686

5Z-7-Oxozeaenol	Inhibitor	99.60%
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.

HY-18938

Selonsertib	Inhibitor	99.05%
Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC₅₀ of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.

HY-112136

TAO Kinase inhibitor 1	Inhibitor	99.46%
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC₅₀s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.

HY-163752

CS17919	Inhibitor
CS17919 is a potent, selective and orally active ASK1 inhibitor with an IC₅₀ of 22.52 nM. CS17919 shows anti-inflammatory and antifibrotic effects. CS17919 can be used for the study of metabolic-related kidney and liver diseases.

HY-136848

SM1-71	Inhibitor
SM1-71 (compound 5) is a potent TAK1 inhibitor, with a K_i 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.

HY-12947

GNE-3511	Inhibitor	99.07%
GNE-3511 is an orally active bioavailable and brain-penetrant dual leucine zipper kinase (DLK) inhibitor with a K_i of 0.5 nM. GNE-3511 can cross the blood-brain-barrier and can be used for the research of neurodegenerative diseases.

HY-100844

GS-444217	Inhibitor	99.67%
GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC₅₀ of 2.87 nM.

HY-15434

NG25	Inhibitor	99.35%
NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC₅₀s of 149 nM and 21.7 nM, respectively.

HY-12358

Tpl2 Kinase Inhibitor 1	Inhibitor	99.22%
Tpl2 Kinase Inhibitor 1 is a 3-pyridylmethylamino analog, and is a selective Tpl2 inhibitor (IC₅₀=50 nM). Tpl2 consists of COT kinase and MAP3K8. Tpl2 Kinase Inhibitor 1 plays an important role in the regulation of the inflammatory response and the progression of some cancers.

HY-32018

Cot inhibitor-2	Inhibitor	99.22%
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC₅₀ of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC₅₀ of 0.3 μM.

HY-124953

7,3',4'-Trihydroxyisoflavone	Inhibitor	99.98%
7,3',4'-Trihydroxyisoflavone, a major metabolite of Daidzein, is an ATP-competitive inhibitor of Cot (Tpl2/MAP3K8) and MKK4. 7,3',4'-Trihydroxyisoflavone has anticancer, anti-angiogenic, chemoprotective, and free radical scavenging activities.

HY-19566

NQDI-1	Inhibitor	98.11%
NQDI-1 inhibits apoptosis signal-regulating kinase 1 (ASK1) with a K_i of 500 nM and an IC₅₀ of 3 μM.

HY-132172

TAK1-IN-2	Inhibitor	98.75%
TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC_50> of 2 nM.

HY-32015

Cot inhibitor-1	Inhibitor	98.45%
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC₅₀ of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC₅₀ of 5.7 nM.

HY-114332

GNE-8505	Inhibitor	99.86%
GNE-8505 is an orally available inhibitor of Dual leucine zipper kinase (DLK).

HY-77251

TAK1/MAP4K2 inhibitor 1	Inhibitor	99.90%
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.

HY-120823

PF-05381941	Inhibitor	99.73%
PF-05381941 is a potent dual inhibitor of TAK1/p38α, with IC₅₀s of 156 and186 nM, respectively.

HY-131969

ASK1-IN-2	Inhibitor	99.55%
ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC₅₀ of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.

HY-115743

TAK1-IN-3	Inhibitor	98.88%
TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.

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