SBE 13 hydrochloride is a selective inhibitor of PLK1 (IC50 values are 200 pM, 875 nM and 66 μM for PLK1, PLK3 and PLK2 respectively). Exhibits no effect on Aurora kinase A activity. Binds and stabilizes the inactive form of PLK1. Delays cell cycle progression, reduces cell proliferation and induces apoptosis in a range of human cancer cell lines. Transiently arrests cells cycle at G0/G1 in primary cells.
Molecular Weight | 479.4 |
Formula | C24H27ClN2O4.HCl |
CAS Number | 1052532-15-6 |
Solubility (25°C) | DMSO: ≥ 30 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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3MB-PP1
3MB-PP1 is a bulky purine analog and inhibitor of Polo-like kinase 1 (Plk1) that blocks mitotic progression and cytokinesis by targeting Plk1 in cells expressing the analog-sensitive Plk1 allele. 3MB-PP1 also specifically inhibits the activity of Leu93 mutant Zipper-interacting Ssn3 (Cdk8). 3MB-PP1 inhibits the activity of Leu93 mutant Zipper-interacting Ssn3 (Cdk8). In addition, 3MB-PP1 specifically inhibits the activity of analog-sensitive Ssn3 (Cdk8). 3MB-PP1 inhibits the Leu93 mutant Zipper-interacting protein kinase (Leu93-ZIPK; IC50=2 μM). 3MB-PP1 can be used in the mycelium of Candida albicans. 3MB-PP1 can be used in studies related to mycelium formation and cell division in Candida albicans. |
CYC-800
CYC-800 is a PLK1 inhibitor that can be used in tumor-related studies. |
SOL-686
SOL-686 is a PLK1 inhibitor that can be used in glioma-related studies. |
BAL0891
BAL0891 is a potential first-in-class PLK1/TTK inhibitor with antiproliferative activity for studies related to solid tumors. |
Plogosertib
Plogosertib is a selective, potent, orally active, ATP-competitive PLK1 inhibitor with an IC50 value of 3 nM.In addition, Plogosertib exhibits antiproliferative and anticancer activity and can be used in a variety of tumor studies. |
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