HTH-01-015 is a selective NUAK1 inhibitor, but not NUAK2, with IC50 of 100 nM, suppressing NUAK1-mediated MYPT1 phosphorylation.
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产品名称 | AMPK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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WZ4003 |
++++
NUAK2, IC50: 100 nM NUAK1, IC50: 20 nM |
98+% | |||||||||||||||||
Dorsomorphin |
++
AMPK, Ki: 109 nM |
99% | |||||||||||||||||
HTH-01-015 |
+++
NUAK1 , IC50: 100 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。 |
靶点 |
|
描述 | HTH-01-015 is a selective NUAK1 inhibitor with IC50 value of 100nM. HTH-01-015 at 10μM inhibited the phosphorylation of the only well-characterized substrate, MYPT1 (myosin phosphate-targeting subunit 1) that is phosphorylated by NUAK1 at Ser-445. HTH-01-015 significantly inhibited MEFs proliferation and migration in a wound-healing assay. HTH-01-015 inhibited the proliferation and impaired the invasive potential of U2OS cells in a 3D cell invasion assay. The 195 site of NUAK1 is important for the inactivation effect of HTH-01-015 for a mutation (A195T) renders NUAK1 ∼50-fold resistant to HTH-01-015[2]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.13mL 0.43mL 0.21mL |
10.67mL 2.13mL 1.07mL |
21.34mL 4.27mL 2.13mL |
CAS号 | 1613724-42-7 |
分子式 | C26H28N8O |
分子量 | 468.553 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(224.09 mM),配合低频超声助溶,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 |