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- Kei K Ito, .et al. Cep57 and Cep57L1 maintain centriole engagement in interphase to ensure centriole duplication cycle, J Cell Biol, 2021, Mar 1;220(3):e202005153 PMID: 33492359
- Ryuzaburo Yuki, .et al. The tyrosine kinase v-Src modifies cytotoxicities of anticancer drugs targeting cell division, J Cell Mol Med, 2021, Feb;25(3):1677-1687 PMID: 33465289
- Yamagishi A, .et al. Targeting Insulin-Like Growth Factor 1 Receptor Delays M-Phase Progression and Synergizes with Aurora B Inhibition to Suppress Cell Proliferation, Int J Mol Sci, 2020, Feb 5;21(3) PMID: 32033461
- Bucko PJ, .et al. Subcellular drug targeting illuminates local kinase action, Elife, 2019, Dec 24;8. pii: e52220 PMID: 31872801
- Watanabe K, .et al. The Cep57-pericentrin module organizes PCM expansion and centriole engagement, Nat Commun, 2019, Feb 25;10(1):931 PMID: 30804344
- Valérian Pasche, .et al. Screening a repurposing library, the Medicines for Malaria Venture Stasis Box, against Schistosoma mansoni, Parasit Vectors, 2018, 11: 298 PMID: 29764454
- Takeshi Wakida, .et al. The CDK-PLK1 axis targets the DNA damage checkpoint sensor protein RAD9 to promote cell proliferation and tolerance to genotoxic stress, eLife, 2017, 6: e29953 PMID: 29254517
- Majid Momeny, .et al. Dacomitinib, a pan-inhibitor of ErbB receptors, suppresses growth and invasive capacity of chemoresistant ovarian carcinoma cells, Sci Rep, 2017, 7: 4204 PMID: 28646172
- Ifuji A, .et al. A novel immunofluorescence method to visualize microtubules in the antiparallel overlaps of microtubule-plus ends in the anaphase and telophase midzone, Exp Cell Res, 2017, Nov 15;360(2):347-357 PMID: 28942021
Biological Activity
BI 2536 is a selective inhibitor of Plk1, which inhibits Plk1 enzyme activity at low nanomolar concentrations.
Targets
| Target | Value |
|---|---|
| PLK1 | IC50: 0.83nM |
| PLK2 | IC50: 3.5nM |
| PLK3 | IC50: 9.0nM |
| PI3Kα | IC50: 2.407μM |
| Met | IC50: 4.754μM |
| Tie-2 | IC50: 6.549μM |
| HGFR | IC50: 9.5μM |
| ErbB4 | IC50: 9.908μM |
| Abl | IC50: >10μM |
| Axl | IC50: >10μM |
| AMPK | IC50: >10μM |
| AuroraA | IC50: >10μM |
| AuroraB | IC50: >10μM |
| βIRK | IC50: >10μM |
| B-Raf | IC50: >10μM |
| BTK | IC50: >10μM |
| CDK1/CyclinB1 | IC50: >10μM |
| CDK2/CyclinE | IC50: >10μM |
| Chk1 | IC50: >10μM |
| CK1 | IC50: >10μM |
| CK2 | IC50: >10μM |
| C-Raf | IC50: >10μM |
| CSK | IC50: >10μM |
| DYRK1A | IC50: >10μM |
| ECK | IC50: >10μM |
| ERK2 | IC50: >10μM |
| FGFR1 | IC50: >10μM |
| FGFR3 | IC50: >10μM |
| FLT1 | IC50: >10μM |
| FLT3 | IC50: >10μM |
| GSK-3β | IC50: >10μM |
| Hek | IC50: >10μM |
| HER2 | IC50: >10μM |
| ITK | IC50: >10μM |
| JAK2 | IC50: >10μM |
| JAK3 | IC50: >10μM |
| JNK1 | IC50: >10μM |
| LCK | IC50: >10μM |
| Lyn | IC50: >10μM |
| MAPKAPK2 | IC50: >10μM |
| MEK1 | IC50: >10μM |
| MSK1 | IC50: >10μM |
| MKK1 | IC50: >10μM |
| NEK6 | IC50: >10μM |
| p38α | IC50: >10μM |
| p38β | IC50: >10μM |
| p38γ | IC50: >10μM |
| p38δ | IC50: >10μM |
| PAK2 | IC50: >10μM |
| PDGFRα | IC50: >10μM |
| PDGFRβ | IC50: >10μM |
| PDK-1 | IC50: >10μM |
| PKA | IC50: >10μM |
| PKBα | IC50: >10μM |
| PKBβ | IC50: >10μM |
| PKCα | IC50: >10μM |
| PRAK | IC50: >10μM |
| RET | IC50: >10μM |
| ROCK2 | IC50: >10μM |
| RON | IC50: >10μM |
| S6K | IC50: >10μM |
| SGK | IC50: >10μM |
| Src | IC50: >10μM |
| Syk | IC50: >10μM |
| In vitro (25°C) | DMSO | 21 mg/mL (40.25 mM) | |
| Water | Insoluble | ||
| Ethanol | 98 mg/mL (187.86 mM) | ||
| In vivo | 30% PEG 400+0.5% Tween 80+5% Propylene glycol | 14 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 19.17 mL | 95.84 mL | 191.68 mL |
| 0.5 mM | 3.83 mL | 19.17 mL | 38.34 mL |
| 1 mM | 1.92 mL | 9.58 mL | 19.17 mL |
| 5 mM | 0.38 mL | 1.92 mL | 3.83 mL |
*The above data is based on the productmolecular weight 521.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10134 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 755038-02-9 |
| Formula | C28H39N7O3 |
| M. Wt | 521.7 |
| Purity | >98% |
| Synonyms | BI2536, BI-2536 |
| SMILES | CC[[email protected]@H]1C(=O)N(C2=CN=C(N=C2N1C3CCCC3)NC4=C(C=C(C=C4)C(=O)NC5CCN(CC5)C)OC)C |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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