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Merck

Y0503

Sigma-Aldrich

Y-27632 二盐酸盐

≥98% (HPLC)

别名:

Rock抑制剂y-27632, Y-27632 2HCl, (R)-(+)-反式-4-(1-氨基乙基)-N-(4-吡啶基)环己烷甲酰胺 二盐酸盐

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About This Item

经验公式(希尔记法):
C14H21N3O · 2HCl
分子量:
320.26
MDL號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

生物源

synthetic (organic)

品質等級

化驗

≥98% (HPLC)

形狀

powder

光學活性

[α]/D +3.0 to +5.0°, c = 1.0 in methanol

顏色

white to beige

溶解度

H2O: 14 mg/mL

儲存溫度

2-8°C

SMILES 字串

Cl.Cl.C[C@@H](N)[C@H]1CC[C@@H](CC1)C(=O)Nc2ccncc2

InChI

1S/C14H21N3O.2ClH/c1-10(15)11-2-4-12(5-3-11)14(18)17-13-6-8-16-9-7-13;;/h6-12H,2-5,15H2,1H3,(H,16,17,18);2*1H/t10-,11-,12-;;/m1../s1

InChI 密鑰

IDDDVXIUIXWAGJ-LJDSMOQUSA-N

基因資訊

一般說明

Y-27632二盐酸盐是一种有效的支气管扩张剂,可改善抗原和乙酰胆碱所诱导的肺耐药性(RL)。Y-27632可控制中性粒细胞迁移和肺水肿,并可能是治疗急性肺损伤的一种潜在药物。在人胚胎干细胞传代时,结合使用Y-27632二盐酸盐与Accutase消化酶或其他酶液,可增强细胞存活并大幅提高克隆效率。
Y-27632是一种Rho激酶抑制剂,可对抗兔和人阴茎海绵体的去甲肾上腺素能收缩。可松弛各种制备物中的血管和非血管平滑肌,可降低高血压大鼠的血压。此外,该抑制剂可引起细胞形状的可逆变化,使人小梁网(TM)细胞和施氏管细胞中的人肌动蛋白应力纤维、黏着斑和蛋白磷酸酪氨酸染色减少。Y-27632可同时体外抑制ROCK-I和ROCK-II激酶活性,这种抑制作用可被ATP彻底反转,说明它通过结合催化位点来抑制激酶。对于p160ROCK,Ki = 140 nM。

應用

Y-27632二盐酸盐用于:
  • 作为胰腺导管腺癌类器官培养中的培养基补充剂
  • 在小鼠胚胎干细胞中抑制Ras同源基因家族(Rho)激酶
  • 在人胚胎干细胞和诱导多能干细胞(iPSC)中抑制Rho相关蛋白激酶(ROCK)
  • Y-27632二盐酸盐可用作E8培养基补充剂,促进人多能干细胞的体外分化

生化/生理作用

Y-27632是一种高效的、细胞渗透性、选择性ROCK(Rho相关的卷曲螺旋形成蛋白丝氨酸/苏氨酸激酶)抑制剂。Ki = 140 nM用于p160ROCK.Y-27632还可同等高效的抑制ROCK-II。这种抑制对于ATP具有竞争性。

特點和優勢

该化合物是激酶磷酸酶生物学研究的特色产品。点击此处以发现更多的激酶磷酸酶生物学研究特色产品。可访问sigma.com/discover-bsm了解更多关于用于其他研究领域生物活性小分子。

法律資訊

经Mitsubishi Pharma Corporation许可销售

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable

個人防護裝備

dust mask type N95 (US), Eyeshields, Gloves


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Basement membrane destruction by pancreatic stellate cells leads to local invasion in pancreatic ductal adenocarcinoma
Koikawa K, et al.
Cancer Letters, 425, 65-77 (2018)
Naoki Okumura et al.
Investigative ophthalmology & visual science, 55(1), 318-329 (2013-10-10)
To investigate the molecular mechanism of Rho-associated kinase (ROCK) inhibitors Y-27632 and Y-39983 on corneal endothelial cell (CEC) proliferation and their wound-healing effect. The expression of G1 proteins of the cell cycle and expression of phosphorylated Akt in monkey CECs
Taisuke Kadoshima et al.
Proceedings of the National Academy of Sciences of the United States of America, 110(50), 20284-20289 (2013-11-28)
Here, using further optimized 3D culture that allows highly selective induction and long-term growth of human ES cell (hESC)-derived cortical neuroepithelium, we demonstrate unique aspects of self-organization in human neocorticogenesis. Self-organized cortical tissue spontaneously forms a polarity along the dorsocaudal-ventrorostral
Evaluation of Y-27632, a rho-kinase inhibitor, as a bronchodilator in guinea pigs
Iizuka K, et al.
European Journal of Pharmacology, 406(2), 273-279 (2000)
James L Hutchinson et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 28(1), 94-105 (2013-10-01)
Myometrial contraction is a central feature of labor. Although a link between infection and preterm labor is widely accepted, surprisingly little is known about the mechanisms coupling infection-induced inflammation to myocyte contractile machinery. This study explores the myocyte response to

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