BI8626( BI-8626 | BI 8626 )

Catalog No. M12906 CAS No. 1875036-75-1

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

BI8626
Note

Research use only, not for human use.
Brief Description

BI8626 (BI-8626) is a specific, small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 0.9 uM.
Description

BI8626 (BI-8626) is a specific, small molecule inhibitor of the HUWE1 ubiquitin ligase with IC50 of 0.9 uM, does not inhibit the activity of other HECT-domain ubiquitin ligases (HECW2, NEDD4,UBA1 and UbcH5b, IC50>50 uM); suppresses colony formation of Ls174T cells with IC50 of 0.7 uM; inhibits MYC-dependent transactivation in colorectal cancer cells, but not in stem and normal colon epithelial cells; stabilizes MYC-associated protein MIZ1.
In Vitro

Cell Cycle Analysis Cell Line:Ls174T cells Concentration:0 μM, 5 μM,10 μM, 15 μM, 20 μM Incubation Time:0-4 days Result:Retarded passage of Ls174T cells through all phases of the cell cycle, with the effect being strongest for G1.Western Blot Analysis Cell Line:U2OS cells Concentration:0 μM, 20 μM, 50 μM Incubation Time:0 hour,1 hour,2 hours,4 hours,6 hours Result:Retarded the degradation of MCL1 in response to UV irradiation in HeLa cells by inhibiting HUWE1 in U2OS cells.
In Vivo

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Synonyms

BI-8626 | BI 8626
Pathway

Proteasome/Ubiquitin
Target

E3 Ubiquitin Ligase
Recptor

E3 Ubiquitin Ligase
Research Area

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Indication

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CAS Number

1875036-75-1
Formula Weight

440.555
Molecular Formula

C25H28N8
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 83.33 mg/mL (189.15 mM)
SMILES

NCC1=CC(CNC2=C(N=CN=C3N4CCN(CC5=CC=CC=C5)CC4)C3=NC=N2)=CC=C1
Chemical Name

N-(3-(aminomethyl)benzyl)-8-(4-benzylpiperazin-1-yl)pyrimido[5,4-d]pyrimidin-4-amine

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

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