erk2 in-1

ERK2 IN-1, a selective ERK2 inhibitor, exhibits an IC50 of 7 nM.

ERK2 allosteric-IN-1 (compound 1) acts as a selective allosteric inhibitor of ERK2, exhibiting an IC 50 value of 11 μM [1].

ERK2 p38α MAPK-IN-1 (Compound 1, In silico Hit-2), a selective inhibitor of ERK2 and p38α MAPK, exhibits potent activity with an IC 50 of 82 μM against ERK2. It uniquely binds to the allosteric sites of both ERK2 and p38α MAPK. This compound is utilized for type 2 diabetes research [1].

Mps1-IN-1 is a potent, selective, and ATP-competitive inhibitor of Mps1 kinase (IC50: 367 nM).

Rineterkib (ERK-IN-1) is an inhibitor of RAF and ERK1 2 activating mutations in the MAPK pathway.

CHIR-99021 HCl (Laduviglusib HCl) is a highly potent and selective inhibitor of GSK-3α β, with IC50 values of 10 nM and 6.7 nM respectively. It demonstrates remarkable selectivity for GSK-3, with over 500-fold selectivity over CDC2, ERK2, and other protein kinases. Additionally, CHIR-99021 HCl serves as a robust activator of the Wnt β-catenin signaling pathway. Moreover, it exhibits the ability to enhance self-renewal in both mouse and human embryonic stem cells. Furthermore, CHIR-99021 HCl induces autophagy [1] [2] [3].

ERK-IN-2, an ERK2 inhibitor, exhibits an IC50 value of 1.8 nM. At doses greater than 10 μM, it may induce off-target toxicity and or activity [1].

ADTL-EI1712 is a dual inhibitor of ERK1 and ERK5 (IC50s = 40.43 and 64.5 nM, respectively).1It reduces ERK1 and ERK5 activity by 93.5% and 89.4%, respectively, but also inhibits ERK2 activity by 92.7%, in a panel of 100 kinases at 1 μM. ADTL-EI1712 inhibits proliferation of HL-60 and MKN74, but not HeLa, cancer cells (IC50s = 1.26, 2.55, and >50 μM, respectively). It reduces tumor growth and intratumor phosphorylation of ERK1/2 and ERK5 in an MKN74 mouse xenograft model when administered at a dose of 50 mg/kg per day. 1.Wang, G., Zhao, Y., Liu, Y., et al.Discovery of a novel dual-target inhibitor of ERK1 and ERK5 that induces regulated cell death to overcome compensatory mechanism in specific tumor typesJ. Med. Chem.63(8)3976-3995(2020)

1. Corynoxeine is a potent ERK1 2 inhibitor of key PDGF-BB-induced VSMC proliferation and may be useful in the prevention and treatment of vascular diseases and restenosis after angioplasty.

E6201 (ER-806201) is a potent dual kinase inhibitor targeting MEK1 and FLT3, inhibiting their activities in an ATP-competitive manner. It effectively suppresses MEK1-induced ERK2 phosphorylation (IC50 = 5.2 nM), MKK4-induced JNK phosphorylation (IC50 = 91 nM), and MKK6-induced p38 MAPK phosphorylation (IC50 = 19 nM). E6201 exhibits anti-tumor and anti-psoriasis effects [1] [2].

TAT-MEK1, an inhibitor of ERK2, comprises TAT and MEK1 (N-terminal). The TAT component (YGRKKRRQRRR) is a cell-penetrating peptide derived from the human immunodeficiency (HIV-1) transcriptional trans activator (TAT). TAT-MEK1 has an IC50 of 29 μM for ERK2 in vitro [1] [2].

Prosaptide Tx14(A) TFA is a prosaposin-derived peptide and a potent agonist of both GPR37L1 and GPR37, exhibiting EC50 values of 5 nM and 7 nM, respectively. In Schwann cells, this compound enhances phosphorylation of both ERK1 and ERK2 [1] [2].

MEK1 Derived Peptide Inhibitor 1, a peptide inhibitor, prevents the in vitro activation of ERK2 by MEK1, exhibiting an inhibitory concentration (IC 50) of 30 μM. It is utilized in the study of cell-permeable [1].