1262041-49-5

1262041-49-5 structure

Name: GS-444217
Chemical Name: ASK1-IN-1
CAS Number: 1262041-49-5
Molecular Formula: C₂₃H₂₁N₇O
Molecular Weight: 411.46
Catalog: Signaling Pathways MAPK/ERK Pathway MAP3K
Create Date: 2018-06-18 13:50:06
Modify Date: 2024-01-13 13:55:30
GS-444217 is a potent and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87±0.85 nM[1].

Name	ASK1-IN-1

Description	GS-444217 is a potent and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87±0.85 nM[1].
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> MAP3K Research Areas >> Cancer
Target	ASK1:2.87 nM (IC50)
In Vitro	Treatment with GS-444217 reduces ASK1 phosphorylation and prevents the phosphorylation of MKK3/6, MKK4, p38, and JNK at concentrations of 0.3 μM and above with full suppression of ASK1 activity at 1 μM. GS-444217 (1 μM) reduces ASK1 activity within 5 minutes of addition to the cultures, reaching a maximum level of inhibition by 30 minutes. Removal of GS-444217 from the cultures results in reactivation of ASK1 autophosphorylation within 10 minutes and near-complete recovery 2 hours after drug washout[1].
In Vivo	GS-444217 reduces oxidative stress (OS)-induced ASK1 signaling in kidney and inhibits acute renal tubular injury in rats. GS-444217 (30 mg/kg) inhibits activation of ASK1, p38, and JNK in rat kidney. GS-444217 has an in vivo EC50 of approximately 1.6 μM for inhibiting the ASK1 pathway in rodent kidney[1].
References	[1]. Liles JT, et al. ASK1 contributes to fibrosis and dysfunction in models of kidney disease. J Clin Invest. 2018 Oct 1;128(10):4485-4500.