货号:A156190 同义名: GS-4997;GS-4977
Selonsertib (GS-4997) 是一种口服可用和选择性的凋亡信号调节激酶 1 (ASK1) 抑制剂,pIC50 为 8.3,已被研究作为治疗糖尿病肾病和肾纤维化的潜在药物。
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产品名称 | MEK ↓ ↑ | MEK1 ↓ ↑ | MEK1/2 ↓ ↑ | MEK2 ↓ ↑ | MEK5 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Honokiol | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Mirdametinib |
++++
MEK, IC50: 0.33 nM |
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Binimetinib |
+++
MEK, IC50: 12 nM |
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BI-847325 |
++
MEK1, IC50: 25 nM |
+++
MEK2, IC50: 4 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
U0126-EtOH |
+
MEK1, IC50: 0.07 μM |
++
MEK2, IC50: 0.06 μM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
GDC-0623 |
++++
MEK1, IC50: 0.13 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
TAK-733 |
++++
MEK1, IC50: 3.2 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Trametinib |
++++
MEK1, IC50: 0.92 nM |
++++
MEK2, IC50: 1.8 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Selumetinib |
+++
MEK1, Kd: 99 nM MEK1, IC50: 14 nM |
+
MEK2, Kd: 530 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
CI-1040 |
++
MEK1, IC50: 17 nM |
++
MEK2, IC50: 17 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Myricetin | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Refametinib |
++
MEK1, IC50: 19 nM |
++
MEK2, IC50: 47 nM |
{[allProObj[0].p_purity_real_show]} | ||||||||||||||||
Cobimetinib |
+++
MEK1, IC50: 4.2 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
PD98059 |
+
MEK1, IC50: 2 μM |
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SL327 |
+
MEK1, IC50: 0.18 μM |
+
MEK2, IC50: 0.22 μM |
AP-1 | {[allProObj[0].p_purity_real_show]} | |||||||||||||||
PD318088 | ✔ | {[allProObj[0].p_purity_real_show]} | |||||||||||||||||
AZD8330 |
+++
MEK1/2, IC50: 7 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Pimasertib | {[allProObj[0].p_purity_real_show]} | ||||||||||||||||||
(E/Z)-BIX02189 |
++++
MEK5, IC50: 1.5 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
(E/Z)-BIX02188 |
+++
MEK5, IC50: 4.3 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Selonsertib (GS-4997) is identified as an ASK1 inhibitor under clinical evaluation, proposed as a novel therapeutic for diabetic nephropathy and kidney fibrosis[1]. Selonsertib (GS-4997) is characterized as a highly selective and potent ASK1 inhibitor that operates through competitive inhibition with ATP within the catalytic kinase domain of ASK1, offering potential therapeutic benefits when administered once daily orally[2]. |
体外研究 | Selonsertib (GS-4997) is identified as an ASK1 inhibitor under clinical evaluation, proposed as a novel therapeutic for diabetic nephropathy and kidney fibrosis[1]. Selonsertib (GS-4997) is characterized as a highly selective and potent ASK1 inhibitor that operates through competitive inhibition with ATP within the catalytic kinase domain of ASK1, offering potential therapeutic benefits when administered once daily orally[2]. |
作用机制 | GS-4997 binds to the catalytic domain of ASK1 in an ATP-competitive manner thus preventing phosphorylation and activation. |
Dose | Mice: 30 mg/kg[3] (p.o.), 15 mg/kg[4] (p.o.) |
Administration | p.o. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.24mL 0.45mL 0.22mL |
11.22mL 2.24mL 1.12mL |
22.45mL 4.49mL 2.24mL |
CAS号 | 1448428-04-3 |
分子式 | C24H24FN7O |
分子量 | 445.492 |
别名 | GS-4997;GS-4977 |
运输 | 蓝冰 |
存储条件 |
粉末 Sealed in dry,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 30 mg/mL(67.34 mM),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 |
IP 2% DMSO+2% Tween80+40% PEG300+water 1 mg/mL clear PO 0.5% CMC-Na 60 mg/mL suspension |