(-)-Blebbistatin (Synonyms: (S)Blebbistatin) |
| カタログ番号GC13430 |
(-)-Blebbistatinはラセミック混合物の(±)-Blebbistatin(品目番号GC12341)の構成であり、しかも、活性形態である。(-)-Blebbistatinは細胞透過性非筋肉ミオシンII ATPaseの阻害剤であり、有効的に複数の横紋筋ミオシンおよび脊椎動物の非筋肉ミオシンを抑制でき、IC50値の範囲は0.5~5 μ Mであり、平滑筋ミオシンをわずかに抑制するだけである(IC50=80μM)。
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Cas No.: 856925-71-8
Sample solution is provided at 25 µL, 10mM.
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(-)-Blebbistatinはラセミック混合物の(±)-Blebbistatin(品目番号GC12341)の構成であり、しかも、活性形態である。(-)-Blebbistatinは細胞透過性非筋肉ミオシンII ATPaseの阻害剤であり、有効的に複数の横紋筋ミオシンおよび脊椎動物の非筋肉ミオシンを抑制でき、IC50値の範囲は0.5~5 μ Mであり、平滑筋ミオシンをわずかに抑制するだけである(IC50=80μM)[1, 2]。(+)-Blebbistatinbは、さまざまなミオシンIIのATPase活性あるいは培養平滑筋における細胞移動に影響しない[3]。Blebbistatinは潜在的な光ダイナミック剤であり、がん細胞を殺される。Blebbistatinは波長が488nm以下の紫外線において暴露すると、急速な阻害を引き起こすこともある。
体外で、(-)-BlebbistatinがF11-hTERT、U87、Du145、FEMX-I、LNCaPなど5種類の人の細胞株を24時間処理し、濃度依存の方法で細胞活性を抑制する。最高用量は200μMとうちゃくする時、それぞれの細胞の生存率は以下であり、F11-hTERTはおよそ20%であり、U87は30%でありDu145、FEMX-I、LNCaPはいずれも10%未満である[5]。(-)-Blebbistatinを使い、無傷および皮を剥がした体を離れたラット心臓小柱、無傷のラット心筋細胞、および単一のウサギの静脈筋線維を処理し、痙攣力と細胞短縮を減少でき、完全膜が持っている小柱の収縮性能を低下させるが、張力依存性ミオフィラメントATPase活性に影響しない[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.
| 細胞実験[1]: | |
細胞株 | F11-hTERT、U87、Du145、FEMX-I、LNCaP 細胞 |
準備方法 | 0-200μM の(-)-Blebbistatinで細胞を3時間と24時間処理し、細胞活性を観察する。 |
反応条件 | 0-200µM; 3、24h |
アプリケーション | 細胞を24時間孵化したとき、(-)-Blebbistatinのさいぼう毒作用濃度依存性が現れることが観察できる。てすとの最高用量毒作用（200 μ M、24時間）が現れ、それぞれの細胞の生存率は以下であり、F11-hTERTはおよそ20%であり、U87は30%でありDu145、FEMX-I、LNCaPはいずれも10%未満である。 |
| References:[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 | |
| 同義語 | (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 |
| 溶解度 | ≥ 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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Average Rating: 5 (Based on Reviews and 22 reference(s) in Google Scholar.)
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