|(S)-3a-羟基-6-甲基-1-苯基-3,3a-二氢-1H-吡咯[2,3-b]喹啉-4(2H)-酮|CsnPharm

CAS No.: 856925-71-8

(-)-Blebbistatin/(-)-布雷他汀 Catalog No. CSN17147

Synonyms: (S)-(-)-Blebbistatin;(-)-Blebbistatin(-)-Blebbistatin(-)-Blebbistatin;(–)-Blebbistatin

(-)-Blebbistatin is a selective cell-permeable inhibitor of non-muscle myosin II ATPases and the active enantiomer of (+)-blebbistatin. It rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50 = 0.5-5 µM), while poorly inhibiting smooth muscle myosin (IC50 = 80 µM).

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Myosin IIA (non-muscle)

IC50:0.5-5µM Myosin IIB (non-muscle)

IC50:0.5-5µM
描述Non muscle myosin II ATPase provides contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly during the cell division completion process of cytokinesis. (-)-Blebbistatin is a cell-permeable non muscle myosin II ATPase inhibitor with IC50 of 2μM, which does not inhibit myosin light chain kinase. (-)-Blebbistatin is shown to inhibit the enzymatic activities of HMM fragments of nonmuscle myosin IIA, nonmuscle myosin IIB and of rabbit skeletal muscle myosin S1, but not smooth muscle myosin. (-)-Blebbistatin potently inhibited the activity of fast rabbit skeletal muscle S1 with a half maximal inhibition at 0.5μM concentration while Porcine b-cardiac myosin S1 and scallop striated muscle S1 were inhibited with slightly higher IC50 values of 1.2 and 2.3μM, respectively. The IC50 values for non muscle myosin IIA and IIB HMM fragments were 5.1 and 1.8 μM, respectively. In contrast, the actin activated MgATPase required considerably higher (-)-blebbistatin concentrations for inhibition (IC50 of about 80μM). No inhibition was observed with rat myosin Ib, mouse myosin Va S1 and bovine myosin X S1 at 100μM. For skeletal myosin (S1), the acto-S1 ATPase activity was almost totally inhibited with half-maximal inhibition at 0.4 ± 0.1 μM. Nevertheless, actin activated the low inhibited basal S1 ATPase even in 50μM to a maximum of 0.45±0.02 /s (about 2% of the uninhibited activity). At low concentrations, the onset of the blebbistatin-inhibited steady-state of the acto-S1 ATPase was preceded by a slow exponential phase whose observed rate constant fell between 0.02 and 0.07/s with the concentration range of 0.5–4μM, and indicated that the blebbistatin off-rate constant from S1 during ATP turnover is below. Besides, blebbistatin will bind to a nucleotide bound S1 ATPase intermediate slowly but with high affinity (Kd = 3.1± 0.8 μM) which is accompanied by a quench in both tryptophan and mant fluorescence. The inhibitor preferentially binds to the ATPase intermediate with ADP and phosphate bound at the active site, and it slows down phosphate release.
作用机制Blebbistatin blocked myosin II–dependent cell processes by blocking cell blebbing rapidly and reversibly as well as rapidly disrupted directed cell migration and cytokinesis in vertebrate cells.
动物研究
剂量
Mice: min = 1 mg/kg^[3]

给药途径
i.p.
参考文献

动物研究
剂量	Mice: min = 1 mg/kg^[3]
给药途径	i.p.

[1] Kovacs M, Toth J, et al. Mechanism of blebbistatin inhibition of myosin II. J Biol Chem. 2004 Aug 20;279(34):35557-63.
[2] Straight AF, Cheung A, et al. Dissecting temporal and spatial control of cytokinesis with a myosin II Inhibitor. Science. 2003 Mar 14;299(5613):1743-7.
[3] Zhang Y, Li L, et al. The Myosin II Inhibitor, Blebbistatin, Ameliorates FeCl3-induced Arterial Thrombosis via the GSK3β-NF-κB Pathway. Int J Biol Sci. 2017;13(5):630-639.

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
- 3.4208 mL
- 17.1040 mL
- 34.2079 mL
- 5 mM
- 0.6842 mL
- 3.4208 mL
- 6.8416 mL
- 10 mM
- 0.3421 mL
- 1.7104 mL
- 3.4208 mL

技术信息

CAS号

856925-71-8

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H16N2O2

运输

蓝冰

分子量

292.33

别名

(S)-(-)-Blebbistatin;(-)-Blebbistatin(-)-Blebbistatin(-)-Blebbistatin;(–)-Blebbistatin;(S)-Blebbistatin;Blebbistatin

溶解度

DMSO	46.0 mg/mL (157.4 mM)
Water	insoluble

动物实验配方

2% DMSO+40% PEG 300+5% Tween 80+water

5 mg/mL

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

靶点	Description	IC50
Myosin IIA (non-muscle)		IC50:0.5-5µM
Myosin IIB (non-muscle)		IC50:0.5-5µM

(-)-Blebbistatin/(-)-布雷他汀 Catalog No. CSN17147

靶点选择性

请登录您的专属账户

确认信息