货号:A204681 同义名: Y-39983 Dihydrochloride;Y-33075 Dihydrochloride
Y-33075 2HCl具有选择性作为 ROCK 抑制剂,IC50 为 3.6 nM。
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产品名称 | ROCK ↓ ↑ | ROCK1 ↓ ↑ | ROCK2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Thiazovivin |
+
ROCK, IC50: ~0.5 μM |
98% | |||||||||||||||||
Netarsudil hydrochloride |
++++
ROCK, Ki: 2 nM |
99%+ | |||||||||||||||||
Y-33075 2HCl |
++++
ROCK, IC50: 3.6 nM |
99%+ | |||||||||||||||||
ROCK1-IN-1 |
++
ROCK, Ki: 17nM |
95% | |||||||||||||||||
GSK429286A |
+++
ROCK1, IC50: 14 nM |
++
ROCK2, IC50: 63 nM |
99%+ | ||||||||||||||||
Ripasudil |
++
ROCK1, IC50: 51 nM |
++
ROCK2, IC50: 19 nM |
99%+ | ||||||||||||||||
Belumosudil |
++
ROCK2, IC50: 60 nM ROCK2, Ki: 41 nM |
99%+ | |||||||||||||||||
Y-27632 dihydrochloride |
++
ROCK1, Ki: 140 nM |
+
ROCK2, Ki: 300 nM |
99%+ | ||||||||||||||||
Fasudil HCl |
+
ROCK2, Ki: 330 nM |
PKG,Rho | 98% | ||||||||||||||||
Chroman 1 |
++++
ROCK1, IC50: 52 pM |
++++
ROCK2, IC50: 1 pM |
99% | ||||||||||||||||
BAY-549 |
++++
ROCK1, IC50: 0.6 nM |
++++
ROCK2, IC50: 1.1 nM |
99%+ | ||||||||||||||||
AT13148 |
+++
ROCK1, IC50: 6 nM |
+++
ROCK2, IC50: 4 nM |
PKA | 98+% | |||||||||||||||
RKI-1447 |
+++
ROCK1, IC50: 14.5 nM |
+++
ROCK2, IC50: 6.2 nM |
99%+ | ||||||||||||||||
Hydroxyfasudil HCl |
+
ROCK1, IC50: 0.73 μM |
+
ROCK2, IC50: 0.72 μM |
PKA | 98% | |||||||||||||||
H-1152 2HCl |
+++
ROCK2, IC50: 0.0120 μM |
PKG | 99% | ||||||||||||||||
GSK269962A HCl |
++++
ROCK1, IC50: 1.6 nM |
+++
ROCK2, IC50: 4 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 | Rho-associated kinases (ROCK1 and ROCK2) are serine/threonine kinases that are downstream targets of the small GTPases RhoA, RhoBm and RhoC. ROCKs are involved in diverse cellular activities and irregular ROCK activities could lead to cardiovascular diseases[3]. Y-33075 is a potent and selective ROCK family inhibitor, with an IC50 of 3.6 nM. Y-33075 also inhibits PKC and CaMKII, with IC50 0.42μM and 0.81 μM, respectively[4]. Y-33075 (1 μM) inhibits the contraction of rabbit ciliary artery segments evoked by histamine in Ca2+-free solutions[5]. It also inhibits demyelination and reduces the incidence of relapse episodes in a mouse model of chronic relapsing experimental autoimmune encephalomyelitis (EAE)[6]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.83mL 0.57mL 0.28mL |
14.15mL 2.83mL 1.42mL |
28.31mL 5.66mL 2.83mL |
CAS号 | 173897-44-4 |
分子式 | C16H18Cl2N4O |
分子量 | 353.246 |
别名 | Y-39983 Dihydrochloride;Y-33075 Dihydrochloride |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Inert atmosphere,Room Temperature |
溶解度 |
DMSO: 105 mg/mL(297.24 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 H2O: 50 mg/mL(141.54 mM),配合低频超声助溶 |
动物实验配方 |