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| Cas No.: | 1262041-49-5 |
| Chemical Name: | Ask1-IN-1 |
| Synonyms: | ASK1-IN-1;4-(4-cyclopropyl-1H-imidazol-1-yl)-N-(3-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)phenyl)picolinamide;4-(4-cyclopropyl-1H-imidazol-1-yl)-N-[3-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)phenyl]pyridine-2-carboxamide;4-(4-cyclopropylimidazol-1-yl)-N-[3-(4-cyclopropyl-1,2,4-triazol-3-yl)phenyl]pyridine-2-carboxamide;ASK1IN1;GTPL10430;BCP19368;S0L;GS-444217 |
| SMILES: | O=C(C1C([H])=C(C([H])=C([H])N=1)N1C([H])=NC(=C1[H])C1([H])C([H])([H])C1([H])[H])N([H])C1=C([H])C([H])=C([H])C(=C1[H])C1=NN=C([H])N1C1([H])C([H])([H])C1([H])[H] |
| Formula: | C23H21N7O |
| M.Wt: | 411.4591 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| 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]. |
| 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]. |
| 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]. |
| 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. |