WK692 | BCL6 inhibitor | Probechem Biochemicals

Chemical Structure : WK692

WK692 (WK-692)

Catalog No.: PC-23130Not For Human Use, Lab Use Only.

WK692 is a specific small molecule BCL6 inhibitor, directly binds to BCL6 BTB domain (SPR, KD=324 nM), disrupts BCL6BTB/SMRT interaction (IC50=16 nM) and activates the expression of BCL6 downstream genes in cancer cells.

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Biological Activity

WK692 is a specific small molecule BCL6 inhibitor, directly binds to BCL6 BTB domain (SPR, KD=324 nM), disrupts BCL6BTB/SMRT interaction (IC50=16 nM) and activates the expression of BCL6 downstream genes in cancer cells.

WK692 is specific for BCL6 rather than other BTB-zinc finger proteins, attenuates BCL6-mediated transcriptional repression but had minimal impact on other BTB proteins.

WK692 disrupts BCL6BTB/SMRT complex formation and activates BCL6 downstream genes expression.

WK692 inhibits cells proliferation at IC50 1-5 µM for GCB-DLBCL cell lines including SUDHL4, SUDHL6, OCI-LY7, Farage and DOHH2.

WK692 abrogates germinal center formation in vivo, effectively inhibits lymphoma growth with no toxic side effects in vivo

WK692 inhibits the DLBCL growth without toxic effects in vivo and synergizes with the EZH2 and PRMT5 inhibitors.

Physicochemical Properties

M.Wt	692.37
Formula	C26H28Br2N8O5
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	(R)-(1-(7-((3-(2-(2-bromoacetamido)ethoxy)-1-methyl-2-oxo-1,2-dihydroquinolin-6-yl)amino)-[1,2,4]triazolo[1,5-a]pyrimidin-5-yl)pyrrolidin-2-yl)methyl 2-bromoacetate

References

1. Xing Y, et al. Mol Cancer Ther. 2024 Oct 10. doi: 10.1158/1535-7163.MCT-23-0830.

WK692 (WK-692)

Biological Activity

Physicochemical Properties

References

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