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GS-444217

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Chemical Structure| 1262041-49-5 同义名 : ASK1-IN-1
CAS号 : 1262041-49-5
货号 : A203074
分子式 : C23H21N7O
纯度 : 99%+
分子量 : 411.459
MDL号 : MFCD30534397
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 15 mg/mL(36.46 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 GS-444217 is a potent, orally bioavailable, and selective ATP-competitive inhibitor targeting ASK1, with an IC50 of 2.87 nM. GS-444217 administration leads to a reduction in ASK1 phosphorylation and inhibits the phosphorylation of MKK3/6, MKK4, p38, and JNK at concentrations starting from 0.3 μM, achieving complete suppression of ASK1 activity at 1 μM. The introduction of GS-444217 at 1 μM to cell cultures decreases ASK1 activity within 5 minutes, with the peak effect at 30 minutes. Removing GS-444217 results in the reactivation of ASK1 autophosphorylation within 10 minutes, with a near-full recovery observed 2 hours post-drug removal[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.43mL

0.49mL

0.24mL

12.15mL

2.43mL

1.22mL

24.30mL

4.86mL

2.43mL
参考文献

[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.