Chemical Structure : MCC1019
货号: PC-20477Not For Human Use, Lab Use Only.
MCC1019 is a selective inhibitor of PLK1, targets PLK1 Polo box domain (PBD) with binding IC50 of 16.4 uM, 2.75-fold over PLK2-PBD (IC50=44.1 uM) and > 6-fold higher specificity over PLK3 PBD (IC50 >100 uM).
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MCC1019 is a selective inhibitor of PLK1, targets PLK1 Polo box domain (PBD) with binding IC50 of 16.4 uM, 2.75-fold over PLK2-PBD (IC50=44.1 uM) and > 6-fold higher specificity over PLK3 PBD (IC50 >100 uM).
MCC1019 exerted profound cytotoxicity across a panel of cancer cell lines, hematologic malignancies (CCRF-CEM, K562 and CEM/ADR5000) were more sensitive to MCC1019 (IC50s <2 uM).
MCC1019 inhibit downstream effector proteins of PLK1 (BUBR1, p-AKT, p-FOXO1 and HIF-1α), induced M phase cell cycle arrest, and apoptosis and necroptosis.
MCC1019 (20 and 40 mg/kg) significantly inhibited tumor growth in LLC-1 lung tumor bearing mice and RM-1 prostate tumor bearing mice models.
分子量 | 283.12 | |
分子式 | C12H11BrO3 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
1. Abdelfatah S, et al. Acta Pharm Sin B. 2019 Sep;9(5):1021-1034.
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