MAP3K

Heterocyclic compounds as covalent inhibitors of G12C mutant K-Ras protein useful for treating cancers.K-Ras G12C-IN-3 is a novel and irreversible inhibitor of mutant K-ras G12C.

K 259-3, a methyl ester of K 259-2, is an inhibitor of calmodulin-dependent cyclic nucleotide phosphodiesterase.

Cathepsin K Inhibitor 3, exhibiting an IC50 value of 0.5 nM, is a highly selective inhibitor of cathepsin K, featuring a favorable pharmacokinetic profile. It holds potential for use in studies of osteoarthritis (OA).

K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound comprising a ligand for the K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential for synthesizing PROTAC K-Ras Degrader-1, a potent degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

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

Compound 7, also known as 3′-O-Demethyl-4′-N-demethyl-4′-N-acetyl-4′-epi-staurosporine, serves as an inhibitor of protein kinases, displaying IC50 values of 0.092 μM for PKC-α, 0.26 μM for ROCK, and 0.77 μM for ASK1. Additionally, this compound exhibits significant cytotoxicity towards PC-3 cancer cells, with an IC50 of 0.16 μM [1].

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

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

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

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

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

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].

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).

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