WK500B is a BCL6 inhibitor. WK500B engaged BCL6 inside cells, blocked BCL6 repression complexes, reactivated BCL6 target genes, killed DLBCL cells and caused apoptosis as well as cell cycle arrest. In animal models, WK500B inhibited germinal center (GC) formation and DLBCL tumour growth without toxic and side effects. Moreover, WK500B displayed strong efficacy and favourable pharmacokinetics and presented superior druggability.
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Name | WK500B |
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Iupac Chemical Name | 6-bromo-N-(4-((2-((3S,5R)-3,5-dimethylpiperazin-1-yl)-5-fluoropyrimidin-4-yl)amino)phenyl)picolinamide |
Synonyms | WK500B; WK 500B; WK-500B |
Molecular Formula | C22H23BrFN7O |
Molecular Weight | 500.37 |
Smile | C[C@H](N[C@H](C)C1)CN1C2=NC(NC(C=C3)=CC=C3NC(C4=CC=CC(Br)=N4)=O)=C(F)C=N2 |
InChiKey | YJGYJPZYSQTACG-OKILXGFUSA-N |
InChi | InChI=1S/C22H23BrFN7O/c1-13-11-31(12-14(2)26-13)22-25-10-17(24)20(30-22)27-15-6-8-16(9-7-15)28-21(32)18-4-3-5-19(23)29-18/h3-10,13-14,26H,11-12H2,1-2H3,(H,28,32)(H,25,27,30)/t13-,14+ |
CAS Number | 2253985-29-2 |
Related CAS |
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Formulation | Solid powder |
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Purity | 98% Min. |
Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
Solubility | Soluble in DMSO |
Handling | |
Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
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Xing Y, Guo W, Wu M, Xie J, Huang D, Hu P, Zhou M, Zhang L, Zhang Q, Wang P, Wang X, Wang G, Wu H, Zhou C, Chen Y, Liu M, Yi Z, Sun Z. An orally available small molecule BCL6 inhibitor effectively suppresses diffuse large B cell lymphoma cells growth in vitro and in vivo. Cancer Lett. 2022 Mar 31;529:100-111. doi: 10.1016/j.canlet.2021.12.035. Epub 2022 Jan 4. PMID: 34990752.