MAP3K

Selonsertib (GS-4997) (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.

NG25 is a potent and cell-permeable inhibitor of transforming growth factor-β-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2), with IC 50 values of 149nM and 21.7nM, respectively.

TAK1 mitogen-activated protein kinase kinase kinase (MAPKKK) inhibitor

ASK1 inhibitor

A selective inhibitor of ASK1

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

GNE-3511 is a dual leucine zipper kinase (DLK) inhibitor with a Ki of 0.5 nM.

DLK-IN-1 is a selective, orally active inhibitor of dual leucine zipper kinase (DLK, MAP3K12), with a Ki of 3 nM.

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-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.

Phosphocreatine is a high-energy phosphate compound that is abundant in muscle and brain.

Compound 43 TAO kinase inhibitor is an ATP-competitive inhibitor of the thousand-and-one amino acid kinases TAOK1 and TAOK2 (IC50s = 11 and 15 nM, respectively).

Tpl2 Kinase Inhibitor (TKI) is a cell-permeable naphthyridine compound that acts as a potent reversible and ATP-competitive inhibitor of Tpl2 kinase.

A Tpl2 inhibitor

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM.

TAK1-IN-2 is a potent and selective TAK1 inhibitor, with an IC50> of 2 nM.

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

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

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

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

(E/Z)-ASK1-IN-4 is an isomer of ASK1-IN-4.

TAO Kinase-IN-3 is a potent pan- TAOK ( Thousand-And-One Kinase ) inhibitor that specifically binds to and inhibits the kinase activities of TAOK1, TAOK2 and TAOK3 with K d values of <0.17 nM, 0.34 nM, and 0.17 nM, respectively.