minus-Blebbistatin-S-minus-Blebbistatin-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE(-)-BlebbistatinCat. No.: HY-13441CAS No.: 856925-71-8Synonyms: (S)-(-)-Blebbistatin分式: CHNO分量: 292.33作靶點: Myosin作通路: Cytoskeleton儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 5.2 mg/mL (

2、17.79 mM; Need ultrasonic and warming)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 1 mg/mL (3.42 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 1 mg/mL (3.42 mM); Suspended solution; Need ultrasonic1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑：

3、10% DMSO 90% corn oilSolubility: 1 mg/mL (3.42 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 (-)-Blebbistatin布雷他汀的S對映體。 Blebbistatin 有效且選擇性的 myosin II 抑制劑，IC50 范 為0.55M。IC50 & Target IC50: 0.5 to 5 M (myosin II) 1體外研究 Blebbistatin potently inhibits several striated muscle myosins as well as vertebrate n

4、onmuscle myosin IIA andIIB with IC50 values ranging from 0.5 to 5 M. Smooth muscle myosin is only poorly inhibited (IC50=80 M)1. Blebbistatin does not compete with nucleotide binding to the skeletal muscle myosin subfragment-1. Theinhibitor preferentially binds to the ATPase intermediate with ADP an

5、d phosphate bound at the active site,and it slows down phosphate release. It blocks the myosin heads in a products complex with low actin affinity2. In culture-activated hepatic stellate cells, blebbistatin is found to change both cell morphology andfunction. Stellate cells become smaller, acquire a

6、 dendritic morphology and have less myosin IIA-containingstress fibres and vinculin-containing focal adhesions. Blebbistatin impairs silicone wrinkle formation, reducescollagen gel contraction and blocks endothelin-1-induced intracellular Ca2+ release. It promotes wound-induced cell migration 3.體內(nèi)研究

7、 Blebbistatin dose-dependently and completely relax both KCl- and carbachol-induced rat detrusor andendothelin-1-induced human bladder contraction. Pre-incubation with 10 M blebbistatin attenuatescarbachol responsiveness by 65% while blocking electrical field stimulation-induced bladder contractionr

8、eaching 50% inhibition at 32 Hz 4.PROTOCOLCell Assay 3 Freshly isolated HSCs are replated on 96-well plate. At day 3, medium is replaced by serum-free mediumand cells are starved overnight, treated with or without blebbistatin (25 M) for 2 h followed by stimulationwith platelet-derived growth factor

9、-BB (20 ng/mL). After an overnight incubation, the WST-1 cell proliferationassay are performed 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Theranostics. 2019 Apr 13;9(9):2555-2571. Anal Chem. 2017 Oct 17;89(20):10841-10849. Nanomedicin

10、e (Lond). 2019 Mar;14(5):613-626. Colloid Surface B. 2019 Jun 28.See more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEREFERENCES1. Limouze J, et al. Specificity of blebbistatin, an inhibitor of myosin II. J Muscle Res Cell Motil. 2004;25(4-5):337-

11、41.2. Kovcs M, et al. Mechanism of blebbistatin inhibition of myosin II. J Biol Chem. 2004 Aug 20;279(34):35557-63.3. Liu Z, et al. Blebbistatin inhibits contraction and accelerates migration in mouse hepatic stellate cells. Br J Pharmacol. 2010 Jan1;159(2):304-15.4. Zhang X, et al. In vitro and in vivo relaxation of urinary bladder smooth muscle by the selective myosin IIinhibitor, blebbistatin. BJU Int.2011 Jan;107(2):310-7.McePdfHeightCaution: Product h