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BI 2536 is a novel, highly selective, potent dual PLK1 and BRD4 inhibitor with IC50s of 0.83 and 25 nM, respectively. BI 2536 causes HeLa cells to accumulate with a 4N DNA content, indicative of a cell-cycle block in either G2 phase or mitosis. In addition to HeLa cells, BI 2536 potently inhibits the proliferation of a panel of 32 human cancer cell lines, representing diverse organ derivations (including carcinomas of the breast, colon, lung, pancreas, and prostate, melanomas, and hematopoietic cancers) and varied patterns of tumor suppressor or oncogene mutations (including RB1, TP53, PTEN, andKRAS status).
In vivo, BI 2536 (40-50 mg/kg, i.v.) blocks the growth of human cancer xenografts in immunodeficient, nu/nu mice. Consecutive cycles of 40-50 mg/kg BI 2536 given i.v. once or twice per week are found to be highly efficacious in diverse xenograft models, such as the HCT 116 colon cancer with complete tumor suppression with the twice per week schedule (treated versus the control (T/C) value 0.3%) and a T/C value of 16% with once per week treatment.
J Virol. 2024 Apr 24.
Japanese encephalitis virus NS1 and NS1’ proteins induce vimentin rearrangement via the CDK1-PLK1 axis to promote viral replication
BI 2536 purchased from AbMole
Oncogene. 2018 Mar 22.
HIPK2 and extrachromosomal histone H2B are separately recruited by Aurora-B for cytokinesis
BI 2536 purchased from AbMole
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Source | Oncogene (2018). Figure 2. Bi 2536 (AbMole BioScience) |
| Method | The kinase activity assay | |
| Cell Lines | HeLa cells | |
| Concentrations | 1 μM | |
| Incubation Time | 20 min | |
| Results | To avoid earlystage effects on central spindle formation, PLK1 and Aurora-B were inhibited by BI 2536 and Hesperadin, respectively, in temporally controlled modes. |
| Cell Experiment | |
|---|---|
| Cell lines | HeLa, A43, SKOV-3, HT-29, K562, A549, Saos-2, MCF7, HCT116, COLO 205, Hep G2, Raji and PC-3 cells line |
| Preparation method | cell viability were quantified by Alamar Blue assay, 72 hr after initiation of BI 2536 treatment or the vehicle control. The bar chart summarizes the mean values for half-maximal growth inhibition for each cell line (EC50 values; [nM]) on a logarithmic scale. |
| Concentrations | 1~100nM |
| Incubation time | 72 hr |
| Animal Experiment | |
|---|---|
| Animal models | Nude mice bearing established HCT 116 tumors xenograft model |
| Formulation | unknown |
| Dosages | 50mg/kg once or twice weekly |
| Administration | i.v. |
| Molecular Weight | 521.66 |
| Formula | C28H39N7O3 |
| CAS Number | 755038-02-9 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage | 2-8°C, protect from light, sealed |
| Related PLK Products |
|---|
| (1E)-CFI-400437 dihydrochloride
(1E)-CFI-400437 dihydrochloride is a potent PLK4 (IC50= 0.6 nM) inhibitor and selective against other members of the PLK family (>10 μM). |
| 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. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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