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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 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
Binimetinib |
+++
MEK, IC50: 12 nM |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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 |
{[allProObj[0].p_purity_real_show]} | |||||||||||||||||
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。 |
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]. |
Animal study | GS-444217 mitigates oxidative stress (OS)-triggered ASK1 signaling in the kidneys and prevents acute injury to renal tubules in rats. Administered at a dose of 30 mg/kg, GS-444217 suppresses the activation of ASK1, p38, and JNK in the rat kidney. In vivo, GS-444217 achieves an EC50 of around 1.6 μM for the inhibition of the ASK1 pathway in rodent kidneys[1]. |
计算器 | ||||
存储液制备 | 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 |
CAS号 | 1262041-49-5 |
分子式 | C23H21N7O |
分子量 | 411.459 |
别名 | ASK1-IN-1 |
运输 | 蓝冰 |
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 |