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Merck
CN

SML3148

BI8622

≥98% (HPLC)

Synonym(s):

BI 8622, BI-8622, N-[4-(Aminomethyl)phenyl]-6-(4-cyano-4-phenyl-1-piperidinyl)-5-methyl-4-pyrimidinecarboxamide

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About This Item

Empirical Formula (Hill Notation):
C25H26N6O
CAS Number:
Molecular Weight:
426.51
UNSPSC Code:
12352107
NACRES:
NA.77
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

SMILES string

N#CC1(CCN(CC1)C2=C(C)C(C(NC3=CC=C(CN)C=C3)=O)=NC=N2)C4=CC=CC=C4

InChI

1S/C25H26N6O/c1-18-22(24(32)30-21-9-7-19(15-26)8-10-21)28-17-29-23(18)31-13-11-25(16-27,12-14-31)20-5-3-2-4-6-20/h2-10,17H,11-15,26H2,1H3,(H,30,32)

InChI key

IJHAXMJRQQTBPL-UHFFFAOYSA-N

Biochem/physiol Actions

BI8622 is a selective HUWE1 (HECTH9; MULE; ARF-BP1) inhibitor (IC50 = 3.2 μM by HUWE1 HECT-domain auto-ubiquitination assay; IC50 >50 μM against other HECT-domain Ub ligases tested). BI8622 inhibits the degradation of HUWE1 target proteiins, including MCL1 (IC50 = 6.8 μM; UV irradiated HeLa MCL1 transfectants), MIZ1 (10 μM; Ls174T), and TopBP1. BI8622 suppresses Ls174T colony formation (IC50 = 8.4 μM in 5 days) and the growth of three colon carcinoma cell lines (20 μM for 5 days; HCT116, HT29, SW480).
Selective HUWE1 (HECTH9; MULE; ARF-BP1) inhibitor against HUWE1-mediated degration of target proteins.


Storage Class

11 - Combustible Solids

wgk

WGK 3



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