产品说明书

MLS000532223

Print
Chemical Structure| 16616-39-0 同义名 : -
CAS号 : 16616-39-0
货号 : A1352007
分子式 : C15H9NO3
纯度 : 99%+
分子量 : 251.237
MDL号 : MFCD00560016
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(199.02 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
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.98mL

0.80mL

0.40mL

19.90mL

3.98mL

1.99mL

39.80mL

7.96mL

3.98mL
参考文献

[1]Surviladze Z, Waller A, Wu Y, et al. Identification of a small GTPase inhibitor using a high-throughput flow cytometry bead-based multiplex assay. J Biomol Screen. 2010;15(1):10-20.

[2]Mutsuki Amano et al. Rho-kinase/ROCK: A key regulator of the cytoskeleton and cell polarity. Cytoskeleton (Hoboken). 2010 Sep;67(9):545-54.

[3]Jia-yin Han,et al. Research progress of Rho/ROCK signal pathway. Yao Xue Xue Bao. 2016 Jun;51(6):853-9.

[4]Shunsuke Tawara,et al. Progress of the study of rho-kinase and future perspective of the inhibitor. Yakugaku Zasshi. 2007 Mar;127(3):501-14.

[5] Zurab Surviladze, et al. Identification of a Small GTPase Inhibitor Using a High-Throughput Flow Cytometry Bead-Based Multiplex Assay. J Biomol Screen. 2010 Jan;15(1):10-20.