ASK1-IN-1
ASK1-IN-1 Basic information
- Product Name:
- ASK1-IN-1
- Synonyms:
-
- ASK1-IN-1
- ASK1-IN-110
- 4-(4-cyclopropyl-1H-imidazol-1-yl)-N-(3-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)phenyl)picolinamide
- CS-2713
- GS-444217
- ASK1-IN-1/GS-444217
- ASK IN 1
- 2-Pyridinecarboxamide, 4-(4-cyclopropyl-1H-imidazol-1-yl)-N-[3-(4-cyclopropyl-4H-1,2,4-triazol-3-yl)phenyl]-
- CAS:
- 1262041-49-5
- MF:
- C23H21N7O
- MW:
- 411.46
- Mol File:
- 1262041-49-5.mol
ASK1-IN-1 Chemical Properties
- Density
- 1.50±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO:37.75(Max Conc. mg/mL);91.74(Max Conc. mM)
- form
- Solid
- pka
- 11.20±0.70(Predicted)
- color
- White to off-white
ASK1-IN-1 Usage And Synthesis
Uses
GS-444217 is a potent, orally available and selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 of 2.87 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].
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. DOI:10.1172/JCI99768
[2] Budas GR, et al. ASK1 Inhibition Halts Disease Progression in Preclinical Models of Pulmonary Arterial Hypertension. Am J Respir Crit Care Med. 2018 Feb 1;197(3):373-385. DOI:10.1164/rccm.201703-0502OC
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