ASK1 Inhibitor 10 is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1). It is selective for ASK1 over ASK2 as well as MEKK1, TAK-1, IKKβ, ERK1, JNK1, p38α, GSK3β, PKCθ, and B-RAF. It inhibits streptozotocin-induced increases in JNK and p38 phosphorylation in INS-1 pancreatic β cells in a concentration-dependent manner.

Tpl2 Kinase Inhibitor 1 (Compound 1) is a potent and selective Tpl2 (COT kinase, MAP3K8) inhibitor that plays an important role in the regulation of the inflammatory response and the progression of some cancers[1].

PF-05381941是一种 TAK1/p38α 的双重抑制剂，IC50 分别为 156 和 186 nM。

Takinib（EDHS-206）是一种口服活性和选择性的TAK1抑制剂，IC50为9.5 nM。它在ATP结合口袋内非竞争性结合，在类风湿性关节炎和转移性乳腺癌细胞模型中，TNFα刺激后诱导凋亡，并以KD值为 0.46 μM抑制恶性疟原虫蛋白激酶 9（PfPK9）。

Cot inhibitor-2 is a COT/Tpl2 inhibitor.

Cot inhibitor-1 is a COT/Tpl2 inhibitor.

5Z-7-Oxozeaenol is a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC50s of 8 nM and 52 nM, respectively.

B-Raf inhibitor, a pyrazine and pyrrolo[2,3-b]pyridine derivative, is useful in the treatment of cancer and proliferative diseases.