(-)-Blebbistatin (Synonyms: (S)Blebbistatin) |
| Catalog No.GC13430 |
(-)-Blebbistatin은 외상혼합물 (±)- Blebbistatin (카타로그 번호 GC12341)의 구성 중 하나이며 활성 형태이다. (-)-Blebbistatin은 세포를 통과할 수 있는 비근육 myosins II ATPase로 다양한 줄무늬 근육 myosins과 포유류 비근육 myosins을 효과적으로 억제하고 IC50 값이 0.5-5μM 범위 내에 있고 평활근 myosins (IC50=80μM)의 억제 작용은 약한다.
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Cas No.: 856925-71-8
Sample solution is provided at 25 µL, 10mM.
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(-)-Blebbistatin은 외상혼합물 (±)- Blebbistatin (카타로그 번호 GC12341)의 구성 중 하나이며 활성 형태이다. (-)-Blebbistatin은 세포를 통과할 수 있는 비근육 myosins II ATPase로 다양한 줄무늬 근육 myosins과 포유류 비근육 myosins을 효과적으로 억제하고 IC50 값이 0.5-5μM 범위 내에 있고 평활근 myosins (IC50=80μM)의 억제 작용은 약한다. (+)-Blebbistatin은 다양한 myosins II의 ATP아세이트 활동이나 평활근 세포의 셀 미그레이션에 영향을 미치지 않다 [3]. Blebbistatin은 암세포를 죽일 수 있는 잠재적인 포토다이내믹 에이전트이다. 488nm 미만의 파장의 UV 광에 노출하면 블레비스타틴의 급속한 억제도 유발된다 [4].
체외 실험에서 (-)-Blebbistatin (10-200μM)은 24시간 동안 F11-hTERT, U87, Du145, FEMX-I, LNCaP 등 다섯 가지 인간 세포라인을 처리하고 농도에 따라 세포 생존률을 억제했다. 가장 높은 농도인 200μM에서 F11-hTERT 세포의 생존률은 약 20%, U87 세포는 30%였고 Du145, FEMX-I, LNCaP 세포는 모두 10% 미만이었다[5]. 완전하고 가죽이 고립 된 쥐 심장 작은 끈, 완전한 쥐 심장 미세구 그리고 단일 토끼 엉덩이 섬유사에서 (-)-Blebbistatin (10μM) 처리는 삐걱임 힘과 세포 단축을 줄였고 완전한 막을 가진 작은 끈의 수축성을 낮추었지만 텐션에 의존하는 마이오필라멘트 ATP아세이트 활동에 영향을 미치지 않았다[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.
| 세포 실험 [1]: | |
세포 라인 | F11-hTERT、U87、Du145、FEMX-I、LNCaP세포 |
제조 방법 | 세포는 0-200µM의 (-)-Blebbistatin으로 3시간과 24시간 동안 처리되었고 세포 생존률이 측정되었습니다. |
반응 조건 | 0-200µM; 3、24h |
응용 분야 | 세포가 24시간 동안 배양될 때 (-)-Blebbistatin의 세포독성 효과는 농도에 따라 관찰되었습니다. 시험된 가장 높은 복용량 (24시간 동안 200μM)은 F11-hTERT 세포의 생존률이 약 20%, U87 세포가 30%, Du145, FEMX-I, LNCaP 세포는 모두 10% 미만으로 독성 효과를 생산했습니다. |
참고문헌: [1] 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. | |
| Cas No. | 856925-71-8 | SDF | |
| Synonyms | (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 |
| Solubility | ≥ 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 | |||
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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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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.
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Quality Control & SDS
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- Purity: >99.00%
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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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