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WK369

Chemical Structure : WK369

CAS No.:

WK369 (WK 369, WK-369)

Catalog No.: PC-21609Not For Human Use, Lab Use Only.

WK369 (WK-369) is a specific small molecule inhibitor of BCL6, directly binds to the BCL6-BTB domain (SPR KD=2.24 uM) and blocks the interaction between BCL6 and SMRT with IC50 of 0.32 uM in HTRF assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

WK369 (WK-369) is a specific small molecule inhibitor of BCL6, directly binds to the BCL6-BTB domain (SPR KD=2.24 uM) and blocks the interaction between BCL6 and SMRT with IC50 of 0.32 uM in HTRF assays.
WK369 exhibits excellent binding affinities to BCL6-BTB domain with IC50 of <2 uM in HTRF assays, 120 times higher potent than that of FX1 (Cat# PC-60927).
WK369 inhibits the transcriptional repressor activity of BCL6-BTB in a dose dependent manner in vitro and in vivo, but without any effect on the other BTB zinc finger repressors (Kaiso and PLZF).
WK369 significantly reactivates multiple BCL6-target genes including ATR, CD69, p53 and CDKN1A.
WK369 inhibits ovarian cancer cell growth, migration and induces apoptosis.
WK369 prevents ovarian cancer growth, suppresses ovarian cancer intra-abdominal metastasis in vivo.
WK369 sensitizes ovarian cancer to chemotherapy on SKOV3 xenograft mouse models, inhibits AKT and MEK/ERK signaling pathway by targeting BCL6.

Physicochemical Properties

M.Wt 369.40
Formula C19H20FN5O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-((2-((3S,5R)-3,5-dimethylpiperazin-1-yl)-5-fluoropyrimidin-4-yl)amino)-2H-chromen-2-one

References

1. Min Wu, et al. Int J Biol Sci. 2024 Jan 1;20(2):486-501.

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