2253985-29-2
Chemical Structure
WK500B
- CAS No.: 2253985-29-2
- Formula:C22H23BrFN7O
- Molecular Weight:500.38
IUPAC Name: 6-bromo-N-(4-((2-((3S,5R)-3,5-dimethylpiperazin-1-yl)-5-fluoropyrimidin-4-yl)amino)phenyl)picolinamide
InChIKey: YJGYJPZYSQTACG-OKILXGFUSA-N
SMILES: N(C1=NC(=NC=C1F)N2C[C@H](C)N[C@H](C)C2)C3=CC=C(NC(=O)C=4N=C(Br)C=CC4)C=C3
Biological Activity: WK500B is a potent and orally active BCL6 inhibitor with a KD of 1.61 μM. WK500B engages intracellular BCL6 and disrupts BCL6‑corepressor interactions to reactivate BCL6 target genes. WK500B exerts cytotoxicity against diffuse large B‑cell lymphoma cells and induces apoptosis and cell cycle arrest. WK500B suppresses germinal center formation in C57BL/6 mice and DLBCL tumor growth in SCID xenograft models without observable toxicity. WK500B can be used for the study of diffuse large B‑cell lymphoma (DLBCL)[1].
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WK500B | WK500B is a potent and orally active BCL6 inhibitor with a KD of 1.61 μM. WK500B engages intracellular BCL6 and disrupts BCL6‑corepressor interactions to reactivate BCL6 target genes. WK500B exerts cytotoxicity against diffuse large B‑cell lymphoma cells and induces apoptosis and cell cycle arrest. WK500B suppresses germinal center formation in C57BL/6 mice and DLBCL tumor growth in SCID xenograft models without observable toxicity. WK500B can be used for the study of diffuse large B‑cell lymphoma (DLBCL). | |||||||||||||||||||||
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Keywords
