(S)-BI 2536
(S)-BI 2536 is the enantiomer of BI 2536 (HY-50698). (S)-BI 2536 acts as an inhibitor of the BRD4 bromodomain and PLK1 kinase, with a Ki value of 54 nM against BRD4 and a Ki value of 0.42 nM against PLK1 kinase. (S)-BI 2536 exhibits anticancer activity against acute myeloid leukemia. (S)-BI 2536 can be used for the research of acute myeloid leukemia.
For research use only. We do not sell to patients.
- CAS No.: 1241725-90-5
- Formula: C28H39N7O3
- Molecular Weight:521.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PLK1 0.42 nM (Ki) |
BRD4 54 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MV4-11 | GI50 |
0.019 μM
Compound: 39g
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Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay
Cytotoxicity against human MV4-11 cells after 24 hrs by CellTiter-Blue assay
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[PMID: 26191363] |
(S)-BI 2536 (Compound 39g) inhibits purified BRD4 protein with a Ki of 54 nM, exhibiting comparable BRD4 binding affinity to the parent compound BI-2536[1].
(S)-BI 2536 inhibits purified PLK1 protein with a Ki of 0.42 nM, showing 2-fold lower PLK1 binding affinity than the parent compound BI-2536[1].
(S)-BI 2536 inhibits the viability of MV4-11 acute myeloid leukemia cells with a GI50 of 0.019 μM, showing slightly reduced cell growth inhibitory activity compared to the parent compound BI-2536[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1241725-90-5
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Molecular Weight 521.65
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Formula C28H39N7O3
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SMILES
CC[C@@H]1N(C2CCCC2)C3=NC(NC4=C(C=C(C=C4)C(NC5CCN(CC5)C)=O)OC)=NC=C3N(C1=O)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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