BDP5290 |
| Catalog No.GC32868 |
BDP5290은 ROCK과 MRCK의 강력한 억제제로 MRCKβ, ROCK1, ROCK2에 대한 IC50 값이 각각 17nM, 230nM, 123nM, 100nM 이다.
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Cas No.: 1817698-21-7
Sample solution is provided at 25 µL, 10mM.
BDP5290은 ROCK과 MRCK의 강력한 억제제로 MRCKβ, ROCK1, ROCK2에 대한 IC50 값이 각각 17nM, 230nM, 123nM, 100nM 이다.
BDP5290(2 µM, 24시간) 처리된 ATII 세포는 기본 TEER를 낮추고 β1 서브유닛에 의한 장벽 완성도 증가를 방지했다[2]. 3 µM BDP5290은 MRCKβ가 유도한 MLC인산화를 완전히 억제했지만 ROCK1이나 ROCK2가 유도한 것은 아니었다[1]. BDP5290은 다양한 농도의 기본 MDA-MB-231 유방암 세포를 처리하고 내원성 MRCK와 ROCK가 pMLC를 억제하는 EC50가 316 nM 보였다[1]. 0.5 µM BDP5290을 사용하여 MDA-MB-231 세포의 사이토플라즈마 및 코르텍스 pMLC 수준을 낮추었다[1]. BDP5290은 0.1 µM 농도부터 MDA-MB-231의 침입 능력을 줄였고 10 µM에서는 거의 완전하게 억제되었다[1]. 2-µM BDP5290은 인간 SCC12 민모세포암세포가 3D 콜라겐 행렬을침입하는 능력을 강력하게 억제했다[1].
References:
[1]. Unbekandt M, Croft D R, Crighton D, et al. A novel small-molecule MRCK inhibitor blocks cancer cell invasion[J]. Cell Communication and Signaling, 2014, 12(1): 1-15.
[2]. Bai H, Zhou R, Barravecchia M, et al. The Na+, K+-ATPase β1 subunit regulates epithelial tight junctions via MRCKα[J]. JCI insight, 2021, 6(4).
| 세포 실험 [1]: | |
세포 라인 | 폐엽상피II형 세포 (ATII) |
제조 방법 | ATII 세포는 분리 후 24시간에 플라스미드 (CMV-tet 및 Tet-β1)와 치료 고립하여 2 µM MRCKα 억제제 BDP5290으로 즉시 처리했습니다. 24시간 후에 전상피 전기 저항 (TEER)을 측정했습니다. |
반응 조건 | 2 µM , 24 시간 동안 |
응용 분야 | siRNA음소와 일치하게, MRCKα 억제 후 기본 TEER가 낮아졌습니다. BDP5290 처리는 β1 서브유닛에 의한 장벽의 완성도 증가를 방지했습니다. |
참고문헌: [1]: Bai H, Zhou R, Barravecchia M, et al. The Na+, K+-ATPase β1 subunit regulates epithelial tight junctions via MRCKα[J]. JCI insight, 2021, 6(4). | |
| Cas No. | 1817698-21-7 | SDF | |
| Canonical SMILES | ClC(C(C(NC1=CNN=C1C2=NC=CC=C2)=O)=N3)=CN3C4CCNCC4 | ||
| Formula | C17H18ClN7O | M.Wt | 371.82 |
| Solubility | DMSO : 12.5 mg/mL (33.62 mM) | Storage | Store at -20°C |
| 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 | 2.6895 mL | 13.4474 mL | 26.8947 mL |
| 5 mM | 0.5379 mL | 2.6895 mL | 5.3789 mL |
| 10 mM | 0.2689 mL | 1.3447 mL | 2.6895 mL |
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Quality Control & SDS
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- Purity: >98.50%
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Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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