Home Transmembrane Transporters ATPase inhibitor (-)-Blebbistatin

(-)-Blebbistatin

Catalog No.S7099 Synonyms: (S)-(-)-Blebbistatin

For research use only.

(-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase with IC50 of ~2 μM in cell-free assays, does not inhibit myosin light chain kinase, inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly.

(-)-Blebbistatin Chemical Structure

CAS No. 856925-71-8

Selleck's (-)-Blebbistatin has been cited by 34 publications

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Biological Activity

Description (-)-Blebbistatin ((S)-(-)-Blebbistatin) is a cell-permeable inhibitor for non muscle myosin II ATPase with IC50 of ~2 μM in cell-free assays, does not inhibit myosin light chain kinase, inhibits contraction of the cleavage furrow without disrupting mitosis or contractile ring assembly.
Targets
non-muscle myosin II ATPases [2]
(Cell-free assay)
0.5 μM-5 μM
In vitro

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[1] 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. [2] 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. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Rh41 NF3GO2RyUFSVIHHzd4F6 MXvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFQyKGOnbHzz MmHJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC NFTtb|NyUFSVIHHzd4F6 MkLudWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MkHQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 M1T4cJFJXFNiYYPzZZk> MljZdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= NGjVU5E9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot PY epitopes / vinculin / paxillin ; paxillin / pY31 paxillin / pY397FAK / FAK ; talin 1 / vinculin / paxillin 20308429
Growth inhibition assay Cell death ; Cell viability 26733241
Glycerol/urea gel electrophoresis RLC phosphorylation ; RLC phosphorylation ; RLC phosphorylation 18701651
DIC image Traction force of a palladin KD (Palld4) cell 27353427
Immunofluorescence talin 1 / FAK / β1 integrin / zyxin / vinculin / α-actinin / paxillin ; PY epitopes / paxillin ; PY epitopes / actin ; VE-cadherin / F-actin ; actin / NMIIA / tubulin ; GCs morphology 20308429 22090347 25598228

Protocol (from reference)

Solubility (25°C)

In vitro

 DMSO 58 mg/mL
(198.4 mM)
Water Insoluble
Ethanol Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

 5mg/mL

Chemical Information

Molecular Weight 292.33
Formula

C18H16N2O2
CAS No. 856925-71-8
Storage 3 years -20°C(in the dark) powder
2 years -80°C(in the dark) in solvent
Smiles CC1=CC2=C(C=C1)N=C3C(C2=O)(CCN3C4=CC=CC=C4)O

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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