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(-)-Blebbistatin
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(-)-Blebbistatin图片
CAS NO:856925-71-8
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)292.33
FormulaC18H16N2O2
CAS No.856925-71-8
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 58 mg/mL (198.4 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
SMILES CC1=CC=C(N=C(N(C2=CC=CC=C2)CC3)[C@]3(O)C4=O)C4=C1
Other info

Synonym: (S)-Blebbistatin; Blebbistatin.

Chemical Name: 1,2,3,3a-tetrahydro-3aS-hydroxy-6-methyl-1-phenyl-4H-Pyrrolo[2,3-b]quinolin-4-one

InChi Key: LZAXPYOBKSJSEX-GOSISDBHSA-N

InChi Code: InChI=1S/C18H16N2O2/c1-12-7-8-15-14(11-12)16(21)18(22)9-10-20(17(18)19-15)13-5-3-2-4-6-13/h2-8,11,22H,9-10H2,1H3/t18-/m1/s1

SMILES Code: O=C1[C@@]2(O)C(N(C3=CC=CC=C3)CC2)=NC4=C1C=C(C)C=C4

实验参考方法
In Vitro

In vitro activity: Blebbistatin, inhibits cytokinesis, alters the smooth movement of fish keratocytes and inhibits the spontaneous blebbing of a cell line lacking filamin. 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 rapidly and reversibly inhibits Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species, while poorly inhibiting smooth muscle myosin (IC50 = 80 μM). Blebbistatin potently inhibits Dictyostelium myosin II, but poorly inhibits Acanthamoeba myosin II. Blebbistatin does not inhibit representative myosin superfamily members from classes I, V, and X. 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. Blebbistatin interferes neither with binding of myosin to actin nor with ATP-induced actomyosin dissociation. Instead, it blocks the myosin heads in a products complex with low actin affinity.


Kinase Assay: Actin-activated MgATPase activity is measured using an NADH-coupled assay in a Beckman DU 640 spectrophotometer. Blebbistatin [a racemic mixture of the (+) and (-) enantiomers] is added from stocks dissolved in DMSO and the DMSO concentration is maintained at a constant concentration of 5% in all samples.


Cell Assay: Blebbistatin effectively inhibited actin-myosin interaction in mouse cardiac muscle through a mechanism independent on Ca2+ influx and activation systems. In addition, blebbistatin prevented thrombin-mediated inhibition of intercellular calcium wave propagation in bovine corneal endothelial cells.

In VivoBlebbistatin treatment induced zebrafish embryos cardia bifida in a dose-dependent manner.
Animal modelZebrafish embryos model
Formulation & Dosage5-25 μM
References

Science. 2003 Mar 14;299(5613):1743-7; J Muscle Res Cell Motil. 2004;25(4-5):337-41.