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抑制剂/激活剂

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凋亡与自噬

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(-)-Blebbistatin

(-)-Blebbistatin (S-(-)-Blebbistatin)

(-)-Blebbistatin 是选择性的非肌肉肌球蛋白 II (myosin II) ATPase 活性的抑制剂。

货号：
TK0297
规格：

1mg

2mg

5mg

10mg
价格：
￥0.00

产品参数

CAS No.	856925-71-8
生物活性	(-)-Blebbistatin is a selective inhibitor of the ATPase activity of non-muscle myosin II.
分子式	C18H16N2O2
分子量	292.33
运输条件	Room temperature in continental US; may vary elsewhere.
储存条件	4°C, stored under nitrogen
溶解性数据	DMSO : 10 mg/mL (34.21 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)
体内研究	Blebbistatin dose-dependently and completely relax both KCl- and carbachol-induced rat detrusor and endothelin-1-induced human bladder contraction. Pre-incubation with 10 μM blebbistatin attenuates carbachol responsiveness by 65% while blocking electrical field stimulation-induced bladder contraction reaching 50% inhibition at 32 Hz.
体外研究	Blebbistatin potently inhibits several striated muscle myosins as well as vertebrate nonmuscle myosin IIA and IIB with IC50 values ranging from 0.5 to 5 μM. Smooth muscle myosin is only poorly inhibited (IC50=80 μM). Blebbistatin does not compete with nucleotide binding to the skeletal muscle myosin subfragment-1. The inhibitor preferentially binds to the ATPase intermediate with ADP and phosphate bound at the active site, and it slows down phosphate release. It blocks the myosin heads in a products complex with low actin affinity. In culture-activated hepatic stellate cells, blebbistatin is found to change both cell morphology and function. Stellate cells become smaller, acquire a dendritic morphology and have less myosin IIA-containing stress fibres and vinculin-containing focal adhesions. Blebbistatin impairs silicone wrinkle formation, reduces collagen gel contraction and blocks endothelin-1-induced intracellular Ca release. It promotes wound-induced cell migration.
文献	•Adv Sci (Weinh). 2020 Jun 17;7(15):1903583. •Theranostics. 2019 Apr 13;9(9):2555-2571. •J Cell Biol. 2021 Oct 4;220(10):e202010118. •Anal Chem. 2017 Oct 17;89(20):10841-10849. •Nanomedicine (Lond). 2019 Mar;14(5):613-626. •Colloids Surf B Biointerfaces. 2019 Oct 1;182:110332. •Am J Physiol Heart Circ Physiol. 2021 Jul 2. •Fundamental Research. 23 December 2021.
纯度及产品资料	98%

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