| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
(+)-Blebbistatin is the inactive isomer/enantiomer of (–)-Blebbistatin, which is a potent, selective and cell-permeable small molecule inhibitor for non muscle myosin II ATPase with IC50 of around 2 μM in cell-free assays. As a cell-permeable molecule with high affinity and selectivity toward the myosin II contractile molecule, (-)-Blebbistatin preferentially binds to the myosin-ADP-Pi complex to slow down phosphate release. The inhibitor completely eliminate contraction of activity of actin-activated Mg-ATPase and motility of myosins II for several species in vitro (IC50 = 0.5-5.0 μM), but it has poor effects on smooth muscle myosin II (IC50 =80 μM) and myosins I,V, and X.
| Targets |
Inactive R-isomer/enantiomer of (–)-Blebbistatin; Myosin II
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|---|---|
| ln Vitro |
Blebbistatin is a small molecule inhibitor discovered in a screen for inhibitors of nonmuscle myosin IIA. We have examined the specificity and potency of the drug by assaying its effects on the actin-activated MgATPase assay of diverse members of the myosin superfamily. 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 microM. Interestingly, smooth muscle which is highly homologous to vertebrate nonmuscle myosin is only poorly inhibited (IC50=80 microM). The drug potently inhibits Dictyostelium myosin II, but poorly inhibits Acanthamoeba myosin II. Blebbistatin did not inhibit representative myosin superfamily members from classes I, V, and X[2].
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| References |
[1]. Science. 2003 Mar 14;299(5613):1743-7; |
| Additional Infomation |
(R)-blebbistatin is the (R)-enantiomer of blebbistatin. It is a blebbistatin and a tertiary α-hydroxy ketone.
The completion of cell division during cytokinesis requires temporally and spatially regulated communication between the microtubule cytoskeleton, the actin cytoskeleton, and the cell membrane. We have discovered a non-muscle myosin II specific inhibitor, blebbistatin, that inhibits the contraction of the cleavage groove without interfering with the assembly of mitotic or contractile loops. Using blebbistatin and other drugs, we have found that the exit from the cytokinesis phase of the cell cycle depends on ubiquitin-mediated proteolysis. Continuous microtubule signaling is crucial for maintaining the position of the cleavage groove, and these signals control the localization of myosin II independently of other cleavage groove components. [1] |
| Molecular Formula |
C18H16N2O2
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|---|---|
| Molecular Weight |
292.33184
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| Exact Mass |
292.121
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| Elemental Analysis |
C, 73.95; H, 5.52; N, 9.58; O, 10.95
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| CAS # |
1177356-70-5
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| Related CAS # |
(-)-Blebbistatin; 856925-71-8; Blebbistatin; 674289-55-5; (+)-Blebbistatin; 1177356-70-5
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| PubChem CID |
6604910
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
507.3±60.0 °C at 760 mmHg
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| Flash Point |
260.6±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.681
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| LogP |
1.62
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
22
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| Complexity |
497
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CC1=CC2=C(C=C1)N=C3[C@](CCN3C4=CC=CC=C4)(C2=O)O
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| InChi Key |
LZAXPYOBKSJSEX-SFHVURJKSA-N
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| 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-/m0/s1
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| Chemical Name |
(3aR)-3a-hydroxy-6-methyl-1-phenyl-2,3-dihydropyrrolo[2,3-b]quinolin-4-one
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| Synonyms |
(+)-Blebbistatin; 1177356-70-5; (R)-(+)-Blebbistatin; Blebbistatin, (+)-; UNII-XWG1958E8I; XWG1958E8I; (3aR)-3a-hydroxy-6-methyl-1-phenyl-2,3-dihydropyrrolo[2,3-b]quinolin-4-one; CHEBI:75387;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~120 mg/mL (~410.5 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6 mg/mL (20.52 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (60.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 6 mg/mL (20.52 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (60.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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