BI-3802 (BI3802) | BCL6 inhibitor | Probechem Biochemicals

Chemical Structure : BI-3802

CAS No.: 2166387-65-9

BI-3802 (BI3802, BI 3802)

Catalog No.: PC-60949Not For Human Use, Lab Use Only.

BI-3802 (BI3802) is a highly potent and efficacious BCL6 degrader that potently inhibits the interaction of the BTB/POZ domain of BCL6 with several co-repressors in vitro with IC50 of <3 nM.

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5 mg	$328	In stock
10 mg	$528	In stock
25 mg	$898	In stock
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Biological Activity

BI-3802 (BI 3802) is a small molecule B cell lymphoma 6 (BCL6) degrader, binds the Broad complex/Tramtrack/Bric-a-brac (BTB) domain and induces BCL6 degradation.

BI-3802 induced degradation of the full-length BCL6 reporter, while the inhibitor, BI-3812, did not alter stability of the reporter, which can be attenuated by chemical inhibition of the 26S proteasome with MG132 or inhibition of the ubiquitin activating enzyme UBA1 by MLN7243 (TAK-243).

BI-3802 induces cellular BCL6 foci and BCL6 polymerization.

Mutation of Y58 to alanine in BCL6 prevents BI-3802 binding in vitro.

The non-cullin E3 ubiquitin ligase SIAH1 is involved in degradation of polymerized BCL6, BI-3802 increased the interaction between BCL6 and SIAH1 (EC50=64 nM) both in vitro and in cells.

Physicochemical Properties

M.Wt	484.985
Formula	C24H29ClN6O3
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	2-((6-((5-chloro-2-((3S,5R)-3,5-dimethylpiperidin-1-yl)pyrimidin-4-yl)amino)-1-methyl-2-oxo-1,2-dihydroquinolin-3-yl)oxy)-N-methylacetamide

References

1. Kerres N, et al. Cell Rep. 2017 Sep 19;20(12):2860-2875.
2. Mikołaj Słabicki, et al. Nature. 2020 Dec;588(7836):164-168.

BI-3802 (BI3802, BI 3802)

Biological Activity

Physicochemical Properties

References

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