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Y-27632 dihydrochloride

Y-27632 dihydrochloride

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商品描述
Y-27632 dihydrochloride,HY-10583,MCE:
Description

Y-27632 dihydrochloride is a cell-permeable, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively.

IC50 & Target

ROCK-I

220 nM (Ki)

ROCK-II

300 nM (Ki)

Citron kinase

5.3 μM (Ki)

PKN

3.1 μM (Ki)

PKCα

73 μM (Ki)

PKA

25 μM (Ki)

In Vitro

Y-27632 inhibits the ROCK family of kinases 100 times more potently than other kinases including protein kinase C, cAMP-dependent kinase and myosin light chain kinase. Y-27632 prolongs the lag time and delays the appearance of BrdU-labeled cells in a concentration-dependent manner, delays of about 1 and 4 h are noticed in the Swiss 3T3 cells treated with 10 and 100 μM Y-27632, respectively. Y-27632 promotes neuronal differentiation of adipose tissue-derived stem cells (ADSCs). Compared to 1.0 and 2.5 μM Y-27632 induced groups, percentages of neuroal-like cells achieved a peak in the 5.0 μM Y-27632 induced group.

In Vivo

Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of myoclonic jerks when compare with saline group. Y-27632 (5 and 10 mg/kg) significantly prolongs the onset time of clonic convulsions when compare with saline group. Treatment with Dimethylnitrosamine (DMN) causes a significant decrease in rat body and liver weight (DMN-S group) compared with control animals (S-S group). Oral Y27632 (30 mg/kg) essentially prevents this DMN-induced rat body and liver weight loss (DMN-Y group).

Solvent & Solubility
In Vitro: 

H2O : ≥ 124 mg/mL (387.19 mM)

DMSO : ≥ 32 mg/mL (99.92 mM)

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1225 mL 15.6123 mL 31.2246 mL
5 mM 0.6245 mL 3.1225 mL 6.2449 mL
10 mM 0.3122 mL 1.5612 mL 3.1225 mL
*Please refer to the solubility information to select the appropriate solvent.

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