555550
Rho Kinase Inhibitor
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 = 1.6 nM).
동의어(들):
Rho Kinase Inhibitor, H-1152, H-1152P, (S)-(+)-2-Methyl-1-[(4-methyl-5-isoquinolinyl)sulfonyl]homopiperazine, 2HCl, ROCK Inhibitor, Dimethylfasudil (diMF, H-1152P)
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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C16H21N3O2S · 2HCl
CAS 번호:
Molecular Weight:
392.34
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.54
SMILES string
[S](=O)(=O)(N3[C@H](CNCCC3)C)c1c2c(cncc2C)ccc1.Cl.Cl
InChI
1S/C16H21N3O2S.2ClH/c1-12-9-18-11-14-5-3-6-15(16(12)14)22(20,21)19-8-4-7-17-10-13(19)2;;/h3,5-6,9,11,13,17H,4,7-8,10H2,1-2H3;2*1H/t13-;;/m0../s1
InChI key
BFOPDSJOLUQULZ-GXKRWWSZSA-N
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, desiccated (hygroscopic), protect from light
color
white
solubility
methanol: 5 mg/mL, water: 5 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable isoquinolinesulfonamide compound that acts as a highly specific, reversible, potent, and ATP-competitive inhibitor of G-protein Rho-associated kinase (ROCK; Ki = 1.6 nM). Exhibits a much weaker affinity for other serine/threonine kinases (Ki = 630 nM for PKA, 9.27 μM for PKC, and 10.1 μM for MLCK). Shown to selectively block lysophosphatidic acid-induced, but not PDBu-induced, phosphorylation of myristoylated alanine-rich C kinase substrate MARCKS (IC50 = 2.5 μM) in NT-2 cells. Reported to be more potent and selective than Y-27632 (Cat. Nos. 688000 and 688001). Mainly targets Aurora Kinase A, and induces polyploidization of acute megakaryocytic leukemia cells (AMKL). At 10 mM (500 µg/128 µl) solution of Rho Kinase Inhibitor (Cat. No. 555552) in H2O is also available.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
ROCK
ROCK
Product competes with ATP.
Reversible: yes
Target Ki: 1.6 nM against G-protein Rho-associated kinase
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Harmful (C)
저장 등급
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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
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 apical restriction of planar cell polarity (PCP) components is necessary for the maintenance of epithelial integrity. Using the mammalian pancreas as a model
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
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
Kristina Dobrindt 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
관련 콘텐츠
국제 무역 품목 번호
| SKU | GTIN |
|---|---|
| 555550-5MGCN | 04055977268409 |
| 555550-1MGCN | 04055977268393 |
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