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WK692

Chemical Structure : WK692

CAS No.: 2694055-38-2

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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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Purity & Documentation Purity: >98% (HPLC)

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.

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