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BI8622

Chemical Structure : BI8622

CAS No.: 1875036-74-0

BI8622 (BI-8622;BI 8622)

Catalog No.: PC-63514Not For Human Use, Lab Use Only.

BI8622 (BI-8622) is a specific small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 3.1 uM, does not inhibit the activity of other HECT-domain ubiquitin ligases (HECW2, NEDD4,UBA1 and UbcH5b).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BI8622 (BI-8622) is a specific small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 3.1 uM, does not inhibit the activity of other HECT-domain ubiquitin ligases (HECW2, NEDD4,UBA1 and UbcH5b).
BI8622 abolishes ubiquitination of MCL1 induced by ectopically expressed HUWE1 in HeLa cells with IC50 of 6.8 uM, suppresses colony formation of Ls174T cells with IC50 of 8.4 uM.
BI8622 inhibits MYC-dependent transactivation in colorectal cancer cells, but not in stem and normal colon epithelial cells.
BI8622 stabilizes MYC-associated protein MIZ1.

Physicochemical Properties

M.Wt 426.524
Formula C25H26N6O
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

N-(4-(aminomethyl)phenyl)-6-(4-cyano-4-phenylpiperidin-1-yl)-5-methylpyrimidine-4-carboxamide

References

1. Peter S, et al. EMBO Mol Med. 2014 Dec;6(12):1525-41.

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