ASK1-IN-1是一种能够穿透中枢神经系统的 ASK1(凋亡信号调节激酶 1)抑制剂,具有良好的效力(细胞 IC50 = 138 nM;生化 IC50 = 21 nM)。
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产品名称 | MEK ↓ ↑ | MEK1 ↓ ↑ | MEK1/2 ↓ ↑ | MEK2 ↓ ↑ | MEK5 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Honokiol | ✔ | 98% | |||||||||||||||||
Mirdametinib |
++++
MEK, IC50: 0.33 nM |
99%+ | |||||||||||||||||
Binimetinib |
+++
MEK, IC50: 12 nM |
99%+ | |||||||||||||||||
BI-847325 |
++
MEK1, IC50: 25 nM |
+++
MEK2, IC50: 4 nM |
99%+ | ||||||||||||||||
U0126-EtOH |
+
MEK1, IC50: 0.07 μM |
++
MEK2, IC50: 0.06 μM |
98% | ||||||||||||||||
GDC-0623 |
++++
MEK1, IC50: 0.13 nM |
99%+ | |||||||||||||||||
TAK-733 |
++++
MEK1, IC50: 3.2 nM |
99%+ | |||||||||||||||||
Trametinib |
++++
MEK1, IC50: 0.92 nM |
++++
MEK2, IC50: 1.8 nM |
99%+ | ||||||||||||||||
Selumetinib |
+++
MEK1, IC50: 14 nM MEK1, Kd: 99 nM |
+
MEK2, Kd: 530 nM |
99%+ | ||||||||||||||||
CI-1040 |
++
MEK1, IC50: 17 nM |
++
MEK2, IC50: 17 nM |
99%+ | ||||||||||||||||
Myricetin | ✔ | 98% | |||||||||||||||||
Refametinib |
++
MEK1, IC50: 19 nM |
++
MEK2, IC50: 47 nM |
99%+ | ||||||||||||||||
Cobimetinib |
+++
MEK1, IC50: 4.2 nM |
99%+ | |||||||||||||||||
PD98059 |
+
MEK1, IC50: 2 μM |
99%+ | |||||||||||||||||
SL327 |
+
MEK1, IC50: 0.18 μM |
+
MEK2, IC50: 0.22 μM |
AP-1 | 98+% | |||||||||||||||
PD318088 | ✔ | 99% | |||||||||||||||||
AZD8330 |
+++
MEK1/2, IC50: 7 nM |
99%+ | |||||||||||||||||
Pimasertib | 98% | ||||||||||||||||||
(E/Z)-BIX02189 |
++++
MEK5, IC50: 1.5 nM |
99%+ | |||||||||||||||||
(E/Z)-BIX02188 |
+++
MEK5, IC50: 4.3 nM |
99%+ | |||||||||||||||||
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 | ASK1-IN-1 is a CNS-penetrant inhibitor of ASK1 (apoptosis signal-regulating kinase 1), exhibiting strong potency with a cellular IC50 of 138 nM and a biochemical IC50 of 21 nM[1]. |
体内研究 | ASK1-IN-1 (10 mg/kg; pO.) maintains brain concentrations above the cellular IC50/IC70/IC90 for 12 hours, with trough levels of 50/115/435 mg/kg respectively. It demonstrates strong biochemical and cellular potency, low clearance, and effective brain penetration in rodents[1]. |
体外研究 | ASK1-IN-1 features an excellent CYP inhibition profile and shows no activity in a hERG assay. It was evaluated for kinase selectivity against a panel of 468 kinases and is found to be moderately selective[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.47mL 0.49mL 0.25mL |
12.33mL 2.47mL 1.23mL |
24.67mL 4.93mL 2.47mL |
CAS号 | 2411382-24-4 |
分子式 | C19H19N9O2 |
分子量 | 405.41 |
SMILES Code | O=C(NC1=NC(=CC=C1)C2=NN=CN2C(C)C)C3=CN(N=C3OC)C4=NC=CN=C4 |
MDL No. | N/A |
别名 | CAY10756 |
运输 | 蓝冰 |
InChI Key | FTPVMITWJIXRGQ-UHFFFAOYSA-N |
Pubchem ID | 146027049 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Sealed in dry,2-8°C |
溶解方案 |
DMF: 4 mg/mL(9.87 mM),配合低频超声助溶 |