GS-444217

SKU: orb1226648

Description

GS-444217 (GS444217) is a potent, selective, ATP-competitive, orally available inhibitor of ASK1 with Kd/IC50 of 4.1/2.87 nM; displays >53-fold selectivity over DYRK1A and 104-fold over RSK4 in a panel of 442 kinases; strongly suppresses the activation of ASK1, p38, and JNK in the kidney resulting in decreased death of parenchymal cells, inflammation, and fibrosis;abrogates p38 MAPK activation in diabetic kidneys but has no effect upon hypertension in Nos3(-/-) mice; dose dependently reduced pulmonary arterial pressure and reduced RV hypertrophy in pulmonary arterial hypertension (PAH) models; also reduces the progressive inflammation and fibrosis in the kidney and halted decline of glomerular filtration rate in models of kidney disease, causes regression of fibrosis combined with RAS inhibitor enalapril.

Key Properties

• CAS Number: 1262041-49-5
• MW: 411.469
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₁N₇O
• SMILES: O=C(NC1=CC=CC(C2=NN=CN2C3CC3)=C1)C4=NC=CC(N5C=C(C6CC6)N=C5)=C4
• Target: MEK
• Solubility: DMSO: 13 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GS444217

Quick Database Links

Gene Symbol

MEK