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Purity: ≥98%
(-)-Blebbistatin is a potent, selective, reversible and cell-permeable small molecule inhibitor for non muscle myosin II ATPase with IC50 of around 2 μM in cell-free assays. It has been extensively used in research community to inhibit heart muscle myosin, non-muscle myosin II, and skeletal muscle myosin. 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.
| ln Vitro |
Blebbistatin, with IC50 values ranging from 0.5 to 5 μM, potently inhibits both vertebrate non-muscle myosins IIA and IIB and numerous striated muscle myosins. There is only a slight inhibition of smooth muscle myosin (IC50=80 μM)[1]. The nucleotide binding of blebbistatin to skeletal muscle myosin subfragment-1 is not competitive. The inhibitor inhibits the release of phosphate by preferentially binding to ATPase intermediates, ADP, and phosphate in the active site. It inhibits the myosin head group in complexes that have a low affinity for actin [2]. Blebbistatin was shown to modify the appearance and function of activated hepatic stellate cells in vitro. Star cells undergo dendritic morphology, shrink, and lose focal adhesions and stress fibers that contain vinculin and myosin IIA. Blebbistatin inhibits endothelin-1-induced intracellular Ca2+ release, decreases collagen gel contraction, and messes with the creation of silicone wrinkles. Wound-induced cell migration is facilitated by it [3].
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| ln Vivo |
In a dose-dependent manner, blebbistatin fully relaxes the rat detrusor triggered by KCl and carbachol as well as the human bladder contractions caused by endothelin-1. When 10 μM blebbistatin was preincubated, it reduced carbachol reactivity by 65% and inhibited bladder contraction induced by electric field stimulation, with 50% inhibition occurring at 32 Hz [4].
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| References |
[1]. Cristina Lucas‐Lopez, et al. Absolute Stereochemical Assignment and Fluorescence Tuning of the Small Molecule Tool, (–)‐Blebbistatin.
[2]. Ponsaerts R, et al. The myosin II ATPase inhibitor blebbistatin prevents thrombin-induced inhibition of intercellularcalcium wave propagation in corneal endothelial cells. Invest Ophthalmol Vis Sci. 2008 Nov;49(11):4816-27 |
| Molecular Formula |
C18H16N2O2
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|---|---|
| Molecular Weight |
292.33
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| CAS # |
856925-71-8
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| Related CAS # |
Blebbistatin;674289-55-5
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| SMILES |
CC1=CC=C(N=C(N(C2=CC=CC=C2)CC3)[C@]3(O)C4=O)C4=C1
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| InChi Key |
LZAXPYOBKSJSEX-GOSISDBHSA-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-/m1/s1
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| Chemical Name |
1,2,3,3a-tetrahydro-3aS-hydroxy-6-methyl-1-phenyl-4H-Pyrrolo[2,3-b]quinolin-4-one
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| Synonyms |
(S)-Blebbistatin; Blebbistatin.
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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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1 mg/mL (3.42 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 1 mg/mL (3.42 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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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