MAP3K Inhibitor

TAK1-IN-3 is a potent ATP-competitive TAK1 inhibitor.

Pelubiprofen is an orally active anti-inflammatory agent that inhibits COX enzyme activity (with IC₅₀ values of 10.66 and 2.88 μM for COX-1 and COX-2, respectively). Pelubiprofen has significant anti-inflammatory and analgesic effects.

DLK-IN-1 (Compound 14) is an orally active, blood-brain barrier-penetrable and selective inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a K_i value of 3 nM. DLK-IN-1 inhibits Flt3, PAK4, STK33 and TrkA. DLK-IN-1 reduces p-c-Jun. DLK-IN-1 can be used in Alzheimer's disease research.

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.

ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC₅₀=138 nM; Biochemical IC₅₀=21 nM).

TAK1-IN-4 (Compound 14) is a TAK1 inhibitor.

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.

GSK-114 is a highly selective, orally active TNNI3K inhibitor (IC₅₀= 25 nM). GSK-114 shows a 40-fold selectivity for TNNI3K over B-Raf kinase (IC₅₀= 1 μM). Cardiac troponin I-interacting kinase (TNNI3K or CARK) is a member of the tyrosine-like kinase family that is selectively expressed in heart tissue.

IACS-52825 is a potent and selective DLK inhibitor with K_d of 1.3 nM, useful for the study of chemotherapy-induced peripheral neuropathy.

TC ASK 10 (Compound 10) is a potent, selective and orally active apoptosis signal-regulating kinase 1 (ASK1) inhibitor with an IC₅₀ of 14 nM. The inhibitory activities of TC ASK 10 towards other representative panel of kinases are less than 50%, except for ASK2 (IC₅₀ of 0.51 μM).

TL13-68 is a biotin-tagged version of SM1-71, and it can be used to research the mechanism of SM1-71.

GSK329 is a potent and selective diarylurea inhibitor of the cardiac-specific kinase TNNI3K. GSK329 exhibits positive cardioprotective outcomes in the model of ischemia/reperfusion cardiac injury.

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

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.

CBP-501, a cell-permeable calmodulin-binding peptide and a G2-abrogating drug candidate, inhibits the activity of multiple Ser²¹⁶-specific kinases, such as MAPKAP-K2, C-Tak1, CHK1 and CHK2, with IC₅₀ values of 0.9 μM, 1.4 μM 3.4 μM and 6.5 μM, respectively. CBP-501 is used for various types of 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.

MAP3K14-IN-1 (Compound 173) is a MAP3K14 (NIK kinase) inhibitor with an IC₅₀ of 1.8 nM. MAP3K14-IN-1 inhibits the autophosphorylation of MAP3K14 kinase. MAP3K14-IN-1 reduces the level of phosphorylated IKKα in cancer cells. MAP3K14-IN-1 inhibits the proliferation of multiple myeloma cells. MAP3K14-IN-1 can be used in research related to multiple myeloma.

ASK1-IN-4 is an ASK1 inhibitor (IC₅₀ = 0.2 μM) that interacts with the ATP binding site of ASK1.

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.

SW-034538 is a TAO2 inhibitor, with an IC₅₀ of 300 nM.