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CAS No.: 16616-39-0

MLS000532223 Catalog No. CSN27587

MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 ranging from 16 μM to 120 μM. Small GTPases are key regulators of cellular activity .

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技术信息

生物活性

描述Rho GTPases comprise a family of molecular switches that control signal transduction pathways in eukaryotic cells. A conformational change induced upon binding GTP promotes an interaction with target (effector) proteins to generate a cellular response{{Alan Hall. Rho family GTPases. Biochem Soc Trans . 2012 Dec 1;40(6):1378-82. |https://pubmed.ncbi.nlm.nih.gov/23176484/}}.Rho-associated kinase (Rho-kinase/ROCK/ROK) is an effector of the small GTPase Rho and belongs to the AGC family of kinases. Rho-kinase has pleiotropic functions including the regulation of cellular contraction, motility, morphology, polarity, cell division, and gene expression^[2].Rho/ROCK signal pathway induces cytoskeletal reorganization, cell migration and stress fiber formation, affects endothelial permeability, tissue constriction and growth, involves in diabetic nephropathy, eye disease, cancer, heart disease, nerve injury disease, hypertension, radiation injury and leukemia^[3]. The expression of Rho-kinase itself is mediated by the protein kinase C/NF-kappaB pathway with an inhibitory and stimulatory modulation by estrogen and nicotine, respectively. At the cellular level, Rho-kinase mediates VSMC contraction, stimulates VSMC proliferation and migration, and enhances inflammatory cell motility^[4].MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 values ranging from 16 μM to 120 μM. MLS000532223 prevents GTP binding to several GTPases. It prevents GTP binding to several GTPases in a dose-dependent manner,and modulates Rho-family GTP-binding kinetics.MLS000532223 is active in cell-based assays and inhibits EGF-stimulated Rac 1 activation.MLS000532223 inhibits actin rearrangements and changes in cell morphology that are downstream of Rho family GTPase activation.MLS000532223 (10 μM) modulates actin remodeling in mast cells.MLS000532223 (10 μM) inhibits ligand-stimulated β-hexosaminidase secretion of RBL cells^[5].
参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9803 mL
- 19.9015 mL
- 39.8031 mL
- 5 mM
- 0.7961 mL
- 3.9803 mL
- 7.9606 mL
- 10 mM
- 0.3980 mL
- 1.9902 mL
- 3.9803 mL

技术信息

CAS号	16616-39-0	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C15H9NO3	运输	蓝冰
分子量	251.24	别名

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