map3k

Cot inhibitor-1 is a selective inhibitor of Cot protein kinase (also known as Tpl2 or MAP3K8) (IC50 at 28 nM). Cot inhibitor-1 inhibited TNF-alpha production in human whole blood with IC50 of 5.7 nM. Cot is involved in a variety of cellular signaling pathways, particularly those involved in inflammation and immune responses. Cot inactivate-1 inhibits Cot activity and may have potential therapeutic effects on rheumatoid arthritis, inflammatory bowel disease and some types of cancer.

Cot inhibitor-2 is a cot (Tpl2/MAP3K8) inhibitor (IC50: 1.6 nM) with potency, selectivity and oral activity. cot inhibitor-2 inhibits LPS-stimulated TNF-α production in human whole blood with an IC50 of 0.3 μM.

TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1)(IC50 of 14 nM).

5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM.

TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death. TAO Kinase inhibitor 1 is a selective and ATP-competitive thousand-and-one amino acid kinases inhibitor (IC50s: 11 to 15 nM for TAOK1 and 2, respectively).

NQDI-1 (NQDI 1) is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1, MAP3K5) (IC50/Ki: 3 μM/500 nM).

Selonsertib (GS-4997) is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities.

SM1-71 is a potent multi-targeted acrylamide-modified TAK1 inhibitor that inhibits 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 be used as a kinase probe with anticancer activity and inhibits the proliferation of various cancer cell lines.

GNE-3511 is a potent and selective dual leucine zipper kinase inhibitors.

Takinib (EDHS-206) is a specific and effective TAK1 inhibitor(IC50= 9.5 nM).

GS-444217 is a selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1, IC50: 2.87 nM).

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

HS220 is an inhibitor of TAK1 which plays a key role in the signaling pathways of inflammation and cell survival.

ASK1-IN-2 is a potent, orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. It has potential therapeutic applications for ulcerative colitis[1].

TAK-756 is a TAK1 inhibitor that selectively targets IRAK1/4 and exhibits excellent intra-articular pharmacokinetic properties. TAK1 is a potential molecular target for osteoarthritis (OA) due to its complementary anti-catabolic and anti-inflammatory effects.

PROTAC LZK-IN-1 (Compound 21A) is a PROTAC molecule that targets the degradation of LZK (leucine zipper kinase, encoded by MAP3K13). At a concentration of 10 μM, PROTAC LZK-IN-1 facilitates the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. This compound is applicable in anticancer research.

KAI-11101 is an inhibitor of dual leucine zipper kinase (DLK, MAP3K12) with a Ki of 0.7 nM. It effectively suppresses paclitaxel-induced cJun phosphorylation (IC50=95 nM), thereby inhibiting the activation of the MAPK pathway. KAI-11101 exhibits blood-brain barrier permeability, allowing for further exploration of its neuroprotective properties.

Anti-inflammatory agent 102 (Compound 11a) is an orally effective anti-inflammatory compound. It exerts its effects by inhibiting the activation of the ASK1/p38 MAPKs/NF-κB signaling pathway. This agent displays significant anti-inflammatory activity by suppressing the release of NO, ROS, and inflammatory cytokines such as IL-6, TNF-α, and IL-1β. Anti-inflammatory agent 102 is applicable in research concerning inflammatory diseases, including ulcerative colitis (UC).

PF-05381941 is a selective and potent dual inhibitor of TAK1 and p38α with IC 50 =156 nM/186nM that inhibits the kinase activity of TAK1 by binding to its active site.

CBP-501 acetate is a cell-permeable calmodulin-binding peptide and a candidate G2 phase checkpoint abrogator. It inhibits several Ser216-specific kinases, including 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 acetate is applicable to various cancer research studies.

Cot inhibitor-1 hydrochloride is an inhibitor of tumor progression loci-2 kinase (IC50 = 28 nM) and inhibits the production of TNF-α in human whole blood (IC50 = 5.7 nM).

Cot-IN-4 (compound 32) is a potent inhibitor of cancer Osaka thyroid (COT) kinase, with an IC50 value of 6 nM. It effectively inhibits the phosphorylation of ERK (IC50: 60 nM) and suppresses the release of TNFα (IC50: 60 nM). Additionally, Cot-IN-4 reduces the production of the pro-inflammatory cytokine IL-1β in macrophages stimulated by uric acid (IC50: 0.2 μM). This compound is applicable for research in inflammatory diseases.

Cot-IN-5 (compound 1) is a potent ATP-competitive inhibitor of cancer Osaka thyroid (COT). It effectively blocks the autophosphorylation of the COT kinase.

MAP3K14-IN-173 is a potent MAP3K14 kinase inhibitor.