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(diMF，H-1152P)Rho激酶抑制剂19121878899上海睿安生物Merck-Sigma-Roche-Millipore官方正式授权代理商- ￥9223.65
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- 文献和实验
- 技术资料
- 库存：
100⁺瓶
- 英文名：
H-1152，H-1152P，2HCl
- CAS号：
871543-07-6
- 保质期：
1年
- 供应商：
上海睿安生物19121878899
- 保存条件：
2-8°C
- 规格：
5mg/瓶
Sigma-Millipore货号555550二甲基法舒地尔(diMF，H-1152P)Rho激酶抑制剂19121878899上海睿安生物Merck-Sigma-Roche-Millipore官方正式授权代理商
Rho激酶抑制剂
The Rho kinase inhibitor,CAS 872543-07-6,is a cell-permeable,highly specific,reversible,potent,and ATP-competitive inhibitor of Rho-associated kinase(ROCK;Ki=1.6nM).
别名:Rho激酶抑制剂，H-1152，H-1152P，(S)-(+)-2-甲基-1-[(4-甲基-5-异喹(kuí)啉)磺酰基]高哌嗪，2HCl，ROCK抑制剂，二甲基法舒地尔(diMF，H-1152P)
Sigma-Millipore货号555550-1mg，目录价¥4387.76元
Sigma-Millipore货号555550-5mg，目录价¥9223.65元
说明
一般描述
一种细胞可渗透性氯硝(xiāo)基苯甲酰胺化合物，可作为G蛋白Rho相关激酶(ROCK；Ki=1.6nM)的高度特异性、可逆、有效和ATP竞争性抑制剂。对其他丝氨酸/苏氨酸激酶的亲和力要弱得多(PKA的Ki=630nm，PKC的Ki=9.27μM，MLCK的Ki=10.1μM)。在NT-2细胞(IC50=2.5μM)中，显示出选择性阻断溶血磷脂酸诱导的、但不是PDBu诱导的豆蔻酰化富含丙氨酸的C激酶底物的磷酸化。据报道比Y-27632(目录号688000和688001)更具效力和选择性。主靶极光激酶A，诱导急性巨核细胞白血病细胞(AMKL)多倍体化。也可提供10mM(500µg/128µlRho激酶抑制剂(目录号555552)的H2O溶液。
生化/生理作用
主要靶标
ROCK
ROCK
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标Ki：对G蛋白Rho相关激酶为1.6 nM
包装:用惰性气体包装
制备说明:复溶后，等分并冷冻保存(-20°C)。贮备溶液在-20°C下可稳定保存至多6个月。
其他说明
Wen,Qiang,et al.2012.Cell150,575.
Ikenoya,M.,et al.2002.J. Neurochem.81,9.
Sasaki,Y.,et al.2002.Pharmacol.Ther.93,225.
Ikenoya,M.,et al.2002.J. Neurochem.81,9.
Sasaki,Y.,et al.2002.Pharmacol.Ther.93,225.
法律信息:CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明:毒性:有害(C)
同行评审论文(部分:文献)
Myosin II Reactivation and Cytoskeletal Remodeling as a Hallmark and a Vulnerability in Melanoma Therapy Resistance.
Jose L Orgaz et al.
Cancer cell, 37(1), 85-103 (2020-01-15)
Despite substantial clinical benefit of targeted and immune checkpoint blockade-based therapies in melanoma, resistance inevitably develops. We show cytoskeletal remodeling and changes in expression and activity of ROCK-myosin II pathway during acquisition of resistance to MAPK inhibitors. MAPK regulates myosin
Ap_ical Restriction of the Planar Cell Polarity Component VANGL in Pancreatic Ducts Is Required to Maintain Epithelial Integrity.
Lydie Flasse et al.
Cell reports, 31(8), 107677-107677 (2020-05-28)
Cell polarity is essential for the architecture and function of numerous epithelial tissues. Here, we show that ap_ical restriction of planar cell polarity (PCP) components is necessary for the maintenance of epithelial integrity. Using the mammalian pancreas as a model
Rho-associated kinase and zipper-interacting protein kinase, but not myosin light chain kinase, are involved in the regulation of myosin phosphorylation in serum-stimulated human arterial smooth muscle cells.
Jing-Ti Deng et al.
PloS one, 14(12), e0226406-e0226406 (2019-12-14)
Myosin regulatory light chain (LC20) phosphorylation plays an important role in vascular smooth muscle contraction and cell migration. Ca2+/calmodulin-dependent myosin light chain kinase (MLCK) phosphorylates LC20 (its only known substrate) exclusively at S19. Rho-associated kinase (ROCK) and zipper-interacting protein kinase
Expression of E-cadherin by CD8+ T cells promotes their invasion into biliary epithelial cells.
Scott P Davies et al.
Nature communications, 15(1), 853-853 (2024-01-30)
The presence of CD8+ T cells in the cytoplasm of biliary epithelial cells (BEC) has been correlated with biliary damage associated with primary biliary cholangitis (PBC). Here, we characterise the mechanism of CD8+ T cell invasion into BEC. CD8+ T
Publicly Available hiPSC Lines with Extreme Polygenic Risk Scores for Modeling Schizophrenia.
Kristina Do_brindt et al.
Complex psychiatry, 6(3-4), 68-82 (2021-12-10)
Schizophrenia (SZ) is a common and debilitating psychiatric disorder with limited effective treatment options. Although highly heritable, risk for this polygenic disorder depends on the complex interplay of hundreds of common and rare variants. Translating the growing list of genetic
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文献和实验该产品被引用文献
Sigma-Millipore货号555550二甲基法舒地尔(diMF，H-1152P)Rho激酶抑制剂19121878899上海睿安生物Merck-Sigma-Roche-Millipore官方正式授权代理商
Rho激酶抑制剂
The Rho kinase inhibitor,CAS 872543-07-6,is a cell-permeable,highly specific,reversible,potent,and ATP-competitive inhibitor of Rho-associated kinase(ROCK;Ki=1.6nM).
别名:Rho激酶抑制剂，H-1152，H-1152P，(S)-(+)-2-甲基-1-[(4-甲基-5-异喹(kuí)啉)磺酰基]高哌嗪，2HCl，ROCK抑制剂，二甲基法舒地尔(diMF，H-1152P)
Sigma-Millipore货号555550-1mg，目录价¥4387.76元
Sigma-Millipore货号555550-5mg，目录价¥9223.65元
说明
一般描述
一种细胞可渗透性氯硝(xiāo)基苯甲酰胺化合物，可作为G蛋白Rho相关激酶(ROCK；Ki=1.6nM)的高度特异性、可逆、有效和ATP竞争性抑制剂。对其他丝氨酸/苏氨酸激酶的亲和力要弱得多(PKA的Ki=630nm，PKC的Ki=9.27μM，MLCK的Ki=10.1μM)。在NT-2细胞(IC50=2.5μM)中，显示出选择性阻断溶血磷脂酸诱导的、但不是PDBu诱导的豆蔻酰化富含丙氨酸的C激酶底物的磷酸化。据报道比Y-27632(目录号688000和688001)更具效力和选择性。主靶极光激酶A，诱导急性巨核细胞白血病细胞(AMKL)多倍体化。也可提供10mM(500µg/128µlRho激酶抑制剂(目录号555552)的H2O溶液。
生化/生理作用
主要靶标
ROCK
ROCK
产物与ATP竞争。
可逆性：是
细胞可渗透性：是
靶标Ki：对G蛋白Rho相关激酶为1.6 nM
包装:用惰性气体包装
制备说明:复溶后，等分并冷冻保存(-20°C)。贮备溶液在-20°C下可稳定保存至多6个月。
其他说明
Wen,Qiang,et al.2012.Cell150,575.
Ikenoya,M.,et al.2002.J. Neurochem.81,9.
Sasaki,Y.,et al.2002.Pharmacol.Ther.93,225.
Ikenoya,M.,et al.2002.J. Neurochem.81,9.
Sasaki,Y.,et al.2002.Pharmacol.Ther.93,225.
法律信息:CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明:毒性:有害(C)
同行评审论文(部分:文献)
Myosin II Reactivation and Cytoskeletal Remodeling as a Hallmark and a Vulnerability in Melanoma Therapy Resistance.
Jose L Orgaz et al.
Cancer cell, 37(1), 85-103 (2020-01-15)
Despite substantial clinical benefit of targeted and immune checkpoint blockade-based therapies in melanoma, resistance inevitably develops. We show cytoskeletal remodeling and changes in expression and activity of ROCK-myosin II pathway during acquisition of resistance to MAPK inhibitors. MAPK regulates myosin
Ap_ical Restriction of the Planar Cell Polarity Component VANGL in Pancreatic Ducts Is Required to Maintain Epithelial Integrity.
Lydie Flasse et al.
Cell reports, 31(8), 107677-107677 (2020-05-28)
Cell polarity is essential for the architecture and function of numerous epithelial tissues. Here, we show that ap_ical restriction of planar cell polarity (PCP) components is necessary for the maintenance of epithelial integrity. Using the mammalian pancreas as a model
Rho-associated kinase and zipper-interacting protein kinase, but not myosin light chain kinase, are involved in the regulation of myosin phosphorylation in serum-stimulated human arterial smooth muscle cells.
Jing-Ti Deng et al.
PloS one, 14(12), e0226406-e0226406 (2019-12-14)
Myosin regulatory light chain (LC20) phosphorylation plays an important role in vascular smooth muscle contraction and cell migration. Ca2+/calmodulin-dependent myosin light chain kinase (MLCK) phosphorylates LC20 (its only known substrate) exclusively at S19. Rho-associated kinase (ROCK) and zipper-interacting protein kinase
Expression of E-cadherin by CD8+ T cells promotes their invasion into biliary epithelial cells.
Scott P Davies et al.
Nature communications, 15(1), 853-853 (2024-01-30)
The presence of CD8+ T cells in the cytoplasm of biliary epithelial cells (BEC) has been correlated with biliary damage associated with primary biliary cholangitis (PBC). Here, we characterise the mechanism of CD8+ T cell invasion into BEC. CD8+ T
Publicly Available hiPSC Lines with Extreme Polygenic Risk Scores for Modeling Schizophrenia.
Kristina Do_brindt et al.
Complex psychiatry, 6(3-4), 68-82 (2021-12-10)
Schizophrenia (SZ) is a common and debilitating psychiatric disorder with limited effective treatment options. Although highly heritable, risk for this polygenic disorder depends on the complex interplay of hundreds of common and rare variants. Translating the growing list of genetic
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Sigma-Millipore货号555550二甲基法舒地尔(diMF，H-1152P)Rho激酶抑制剂19121878899上海睿安生物Merck-Sigma-Roche-Millipore官方正式授权代理商
￥9223.65
