(-)-Blebbistatin (Synonyms: (S)Blebbistatin) |
| رقم الكتالوجGC13430 |
(-) - Blebbistatin هو مثبط انتقائي لنشاط ATPase للميوسين غير العضلي II
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 856925-71-8
Sample solution is provided at 25 µL, 10mM.
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(-)-Blebbistatin is one of the configurations of the racemic mixture (±)-Blebbistatin (Cat. No. GC12341) and is the active form. (-)-Blebbistatin is a cell-permeable inhibitor of non-muscle myosin II ATPase, which effectively inhibits multiple striated muscle myosins as well as vertebrate non-muscle myosins with IC50 values ranging from 0.5-5μM, and only slightly inhibits smooth muscle myosin (IC50=80μM) [1, 2]. (+)-Blebbistatinb has no effect on the ATPase activity of various myosin IIs or cell migration in cultured smooth muscle[3]. Blebbistatin is a potential photodynamic agent that can kill cancer cells. Exposure to UV light with a wavelength below 488nm can also lead to rapid inhibition of Blebbistatin [4].
In vitro, (-)-Blebbistatin (10-200μM) was used to treat five human cell lines, including F11-hTERT, U87, Du145, FEMX-I, and LNCaP, for 24h, which inhibited cell viability in a concentration-dependent manner. At the highest dose of 200μM, the survival rates of F11-hTERT cells were approximately 20%, U87 cells were 30%, and Du145, FEMX-I, and LNCaP cells were all below 10%[5]. Treatment with (-)-Blebbistatin (10μM) on intact and skinned isolated rat heart trabeculae, intact rat cardiomyocytes, and single rabbit psoas myofibrils reduced twitch force and cell shortening, decreased the contractility of trabeculae with intact membranes, without affecting tension-dependent myofilament ATPase activity[6].
References:
[1] Lucas‐Lopez C, Patterson S, Blum T, et al. Absolute Stereochemical Assignment and Fluorescence Tuning of the Small Molecule Tool,(–)‐Blebbistatin[J]. 2005.
[2] Limouze J, Straight A F, Mitchison T, et al. Specificity of blebbistatin, an inhibitor of myosin II[J]. Journal of Muscle Research & Cell Motility, 2004, 25: 337-341.
[3] Watanabe M, Yumoto M, Tanaka H, et al. Blebbistatin, a myosin II inhibitor, suppresses contraction and disrupts contractile filaments organization of skinned taenia cecum from guinea pig[J]. American Journal of Physiology-Cell Physiology, 2010, 298(5): C1118-C1126.
[4] Sakamoto T, Limouze J, Combs C A, et al. Blebbistatin, a myosin II inhibitor, is photoinactivated by blue light[J]. Biochemistry, 2005, 44(2): 584-588.
[5] Mikulich A, Kavaliauskiene S, Juzenas P. Blebbistatin, a myosin inhibitor, is phototoxic to human cancer cells under exposure to blue light[J]. Biochimica et Biophysica Acta (BBA)-General Subjects, 2012, 1820(7): 870-877.
[6] Farman G P, Tachampa K, Mateja R, et al. Blebbistatin: use as inhibitor of muscle contraction[J]. Pflügers Archiv-European Journal of Physiology, 2008, 455(6): 995-1005.
| Cell experiment [1]: | |
Cell lines | F11-hTERT、U87、Du145、FEMX-I、LNCaP cells |
Preparation Method | Cells were treated with 0-200µM of (-)-Blebbistatin for 3h and 24h, and cell viability was measured. |
Reaction Conditions | 0-200µM; 3、24h |
Applications | The cytotoxic effect of (-)-Blebbistatin was observed in a concentration-dependent manner when the cells were incubated for 24h. The highest dose tested (200μM for 24h) produced toxic effect with the cell viability being about 20% for the F11-hTERT cells, 30% for the U87 cells, and below 10% for the Du145, FEMX-I and LNCaP cells. |
References: | |
| Cas No. | 856925-71-8 | SDF | |
| المرادفات | (S)Blebbistatin | ||
| Chemical Name | (S)-3a-hydroxy-6-methyl-1-phenyl-3,3a-dihydro-1H-pyrrolo[2,3-b]quinolin-4(2H)-one | ||
| Canonical SMILES | O[C@@]12CCN(C3=CC=CC=C3)C1=NC4=CC=C(C)C=C4C2=O | ||
| Formula | C18H16N2O2 | M.Wt | 292.33 |
| الذوبان | ≥ 14.6 mg/mL in DMSO | Storage | Store at -20°C,unstable in solution, ready to use. |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.4208 mL | 17.104 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 |
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- Purity: >99.00%
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