Chemical Structure : BCL6 inhibitor YK01
CAS No.:
3034883-70-7
BCL6 inhibitor YK01
Catalog No.: PC-25337Not For Human Use, Lab Use Only.
BCL6 inhibitor YK01 is a potent, specific small molecule inhibitor of BCL6-BTB with binding IC50 of 11.7 nM, directly binds to BCL6BTB with SPR KD of 148 nM, inhibits BCL6 transcriptional activity.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
BCL6 inhibitor YK01 is a potent, specific small molecule inhibitor of BCL6-BTB with binding IC50 of 11.7 nM, directly binds to BCL6BTB with SPR KD of 148 nM, inhibits BCL6 transcriptional activity.
YK01 inhibited BCL6-BTB domain repression but did not affect the BTB domains associated with the Kaiso and PLZF proteins.
YK01 inhibits the proliferation of glioma cells with high BCL6 expression in vitro (U87-MG, IC50=0.66 uM).
YK01 reactivates BCL6 downstream genes and induces apoptosis in GBM cells. YK01 induces the degradation of BCL6 and inhibits the activation of AKT and ERK and promotes the enhancement of the DNA damage response by blocking the ability of BCL6 to inhibit cell proliferation.
YK01 (12.5 mg/kg/d) inhibits tumor growth in U87-MG xenograft mouse models.
YK01 combined with temozolomide (TMZ) can synergically inhibit glioblastoma multiforme growth.
Physicochemical Properties
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M.Wt
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498.34
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Formula
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C21H20BrN7O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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2-bromo-N-(1-(7-((2-oxo-2H-chromen-6-yl)amino)-[1,2,4]triazolo[1,5-a]pyrimidin-5-yl)piperidin-3-yl)acetamide
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References
1. Wu M, et al. Genes Dis. 2025 Apr 15;12(6):101644.
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