MAPK Signaling

MNK1 inhibitor, specific and selective

PF-4708671, is a novel cell-permeable inhibitor of S6K1, specifically inhibits the S6K1 isoform with a Ki of 20 nM and IC50 of 160 nM.

A potent and orally bioavailable pan-Akt inhibitor

XMD8-92 is a BMK1 kinase inhibitor, with an IC 50 of 1.5μM and a dissociation constant (Kd) of 80nM.

A signal-specific JNK/p38 pathway and TAK 1 inhibitor

inhibitor of p38α-mediated MK2a phosphorylation

ML-264 is a novel selective Krüppel-like factor 5 (KLF5) inhibitor.

A protein kinase inhibitor

reversible ERK1/2 inhibitor

BIRB 796 (Doramapimod) (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM.

JNK inhibitor

Anisomycin, an antibiotic isolated from Streptomyces griseus, is also a JNK activator.

C-1 is a potent protein kinase inhibitor, with IC50s of 4 μM, 8 μM, 12 μM and 240 μM for cGMP-dependent protein kinase (PKG), cAMP-dependent protein kinase (PKA), protein kinase C (PKC) and MLC-kinase, respectively. C-1 also used as a ROCK inhibitor.

p38 MAPK inhibitor

An oral pan-Raf kinase inhibitor

Pexmetinib (ARRY-614) is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.

p38 MAPK inhibitor

GDC-0994 (GDC-0994) is an orally active ERK kinase inhibitor with an IC50 of 6.1 nM and 3.1 nM for ERK1 and ERK2, respectively.

LY2584702 is a selective ATP competitive inhibitor of p70S6K with an IC50 of 4 nM. In S6K1 enzyme assay, the IC50 of LY-2584702 is 2 nM.

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.

T-LAK-cell-originated protein kinase (TOPK) inhibitor

Selective MEK5 inhibitor