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Y-27632 dihydrochloride

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Chemical Structure| 129830-38-2 同义名 : Y-27632 (hydrochloride);Y-27632 2HCl
CAS号 : 129830-38-2
货号 : A101744
分子式 : C14H23Cl2N3O
纯度 : 99%+
分子量 : 320.258
MDL号 : MFCD03490488
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(109.29 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: 100 mg/mL(312.25 mM)，配合低频超声助溶
动物实验配方：

PO 0.5% CMC-Na 40 mg/mL clear

生物活性
靶点

  • ROCK1

    ROCK1 (p160ROCK), Ki:140 nM

  • ROCK2

    ROCK2, Ki:300 nM

  • ROCK1

    ROCK1, Ki:140 nM
描述 Y-27632 is a specific inhibitor of Rho-associated kinases[1]. Y-27632 2HCl is the dihydrochloride form of Y-27632 with much higher solubility than Y-27632. It is usually used for ES cell maintance[2], cell reprogramming[3],improving cell suviving after thawing[4], as well as facilitates cell proliferation and migration[5].
作用机制 Y-27632 2HCl can inhibit ROCK1 and ROCK2 in an ATP-competition manner.[1]
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
C2C12 10 μM Function Assay 6 h Prevents the serine phosphorylation of IRS-1 induced by insulin and/or TNF-α 16267124
CCL39 30 μM Function Assay 30 min Completely abolishes activation of Na-H exchanger NHE1 by integrins 9693382
Cynomolgus monkey embryonic stem cells 20 µM Cytotoxic Assay 24 h Promotes cyES cell survival 18940855
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.12mL

0.62mL

0.31mL

15.61mL

3.12mL

1.56mL

31.22mL

6.24mL

3.12mL
参考文献

[1]Ishizaki T, Uehata M, et al. Pharmacological properties of Y-27632, a specific inhibitor of rho-associated kinases. Mol Pharmacol. 2000 May;57(5):976-83.

[2]Li X, Meng G, et al. The ROCK inhibitor Y-27632 enhances the survival rate of human embryonic stem cells following cryopreservation. Stem Cells Dev. 2008 Dec;17(6):1079-85.

[3]Zhao Y, Zhao T, et al. A XEN-like State Bridges Somatic Cells to Pluripotency during Chemical Reprogramming. Cell. 2015 Dec 17;163(7):1678-91.

[4]Gauthaman K, Fong CY, et al. ROCK inhibitor Y-27632 increases thaw-survival rates and preserves stemness and differentiation potential of human Wharton's jelly stem cells after cryopreservation. Stem Cell Rev. 2010 Dec;6(4):665-76.

[5]Wang T, Kang W, et al. Rho-kinase inhibitor Y-27632 facilitates the proliferation, migration and pluripotency of human periodontal ligament stem cells. J Cell Mol Med. 2017 Nov;21(11):3100-3112.

[6]Osei-Owusu P, Knutsen RH, et al. Altered reactivity of resistance vasculature contributes to hypertension in elastin insufficiency. Am J Physiol Heart Circ Physiol. 2014;306(5):H654-66.

[7]Mavria G, Vercoulen Y, et al. ERK-MAPK signaling opposes Rho-kinase to promote endothelial cell survival and sprouting during angiogenesis. Cancer Cell. 2006;9(1):33-44.