GS-444217
产品说明书
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同义名 : | ASK1-IN-1 |
| CAS号 : | 1262041-49-5 | |
| 货号 : | A203074 | |
| 分子式 : | C23H21N7O | |
| 纯度 : | 99%+ | |
| 分子量 : | 411.46 | |
| MDL号 : | MFCD30534397 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 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]. | ||
| 作用机制 | GS-444217 is an ATP-competitive ASK1 inhibitor.[2] | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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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 |
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