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CAS No.: 1262041-49-5

GS-444217 Catalog No. CSN18896

Synonyms: ASK1-IN-1

ASK1-IN-1 is an apoptosis signal regulating kinase 1 (ASK1) inhibitor.

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技术信息

生物活性

描述ASK1 (Apoptosis signal-regulating kinase 1) is one of the upstream kinases in the p38 MAPK-signaling pathway, which is activated by inflammation and oxidative stress and regarded as an important target for renal disease. GS-444217 is a selective ASK1 inhibitor with IC50 value of 2.9nM. Administration of GS-444217 through chow at 0.1% (w/w) reduced renal inflammation and fibrosis independent of blood pressure control in diabetic Nos3^-/- mice, as well as abrogated p38 MAPK activation in diabetic kidneys. GS-444217 inhibited ASK1 activity, shown by decreased level of autophosphorylation of ASK1 at Thr838, in a dose-dependent manner at concentration ranging in 3nM-1μM post 2h, and in a time-dependent manner at concentration of 1μM at 5-240min post treatment in HEK293T cells with adenoviral overexpression of human ASK1. Meanwhile, a decreased phosphorylatio level of MKK3/6 and MKK4, two ASK1 substrates, and their downstream substrates p38 and JNK could be observed. GS-444217 showed similar effect on MAPK pathway in vivo. Administration of GS-444217 through chow at 0.3% (w/w) for 8 weeks reduced progressive inflammation and fibrosis in the kidney and halted glomerular filtration rate decline of db/db eNOS^–/– mice.
作用机制GS-444217 is an ATP-competitive ASK1 inhibitor.^[2]
动物研究
剂量
Rat: 10 mg/kg, 30 mg/kg^[2] (p.o.) Mice: 55 mg/kg^[1] (i.p.)

给药途径
p.o., i.p.
参考文献

动物研究
剂量	Rat: 10 mg/kg, 30 mg/kg^[2] (p.o.) Mice: 55 mg/kg^[1] (i.p.)
给药途径	p.o., i.p.

[1] Tesch GH, Ma FY, et al. ASK1 Inhibitor Halts Progression of Diabetic Nephropathy in Nos3-Deficient Mice. Diabetes. 2015 Nov;64(11):3903-13.
[2] Liles JT, Corkey BK, et al. ASK1 contributes to fibrosis and dysfunction in models of kidney disease. J Clin Invest. 2018 Oct 1;128(10):4485-4500.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4304 mL
- 12.1519 mL
- 24.3038 mL
- 5 mM
- 0.4861 mL
- 2.4304 mL
- 4.8608 mL
- 10 mM
- 0.2430 mL
- 1.2152 mL
- 2.4304 mL

技术信息

CAS号

1262041-49-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H21N7O

运输

蓝冰

分子量

411.46

别名

ASK1-IN-1

溶解度

DMSO	60.0 mg/mL (145.8 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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