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  3. (-)-Blebbistatin (GMP)

(-)-Blebbistatin (GMP) is (-)-Blebbistatin (HY-13441) produced by using GMP guidelines. (-)-Blebbistatin (GMP) is a selective inhibitor of the ATPase activity of non-muscle myosin II.

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(-)-Blebbistatin (GMP) Chemical Structure

(-)-Blebbistatin (GMP) Chemical Structure

CAS No. : 856925-71-8

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Description

(-)-Blebbistatin (GMP) is (-)-Blebbistatin (HY-13441) produced by using GMP guidelines. (-)-Blebbistatin (GMP) is a selective inhibitor of the ATPase activity of non-muscle myosin II[1][2].

In Vitro

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)[1]. 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[2]. 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 Ca2+ release. It promotes wound-induced cell migration[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

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[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

292.33

Formula

C18H16N2O2

CAS No.
SMILES

CC1=CC=C(N=C(N(C2=CC=CC=C2)CC3)[C@]3(O)C4=O)C4=C1

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
(-)-Blebbistatin (GMP)
Cat. No.:
HY-13441G
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