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SML3148

Sigma-Aldrich

BI8622

≥98% (HPLC)

Synonyme(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

Formule empirique (notation de Hill):
C25H26N6O
Numéro CAS:
1875036-74-0
Poids moléculaire :
426.51
Numéro MDL:
MFCD32062798
Code UNSPSC :
12352107
Nomenclature NACRES :
NA.77

Niveau de qualité

100

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

2-8°C

Chaîne SMILES 

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

Actions biochimiques/physiologiques

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).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

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Yu Guo et al.
The Journal of clinical investigation, 130(12), 6301-6316 (2020-10-27)
The mechanism by which inflammasome activation is modulated remains unclear. In this study, we identified an AIM2-interacting protein, the E3 ubiquitin ligase HUWE1, which was also found to interact with NLRP3 and NLRC4 through the HIN domain of AIM2 and
Aswini Krishnan et al.
Nature communications, 11(1), 2056-2056 (2020-04-30)
Papillary thyroid cancer (PTC) is the most common type of endocrine malignancy. By RNA-seq analysis, we identify a RET rearrangement in the tumour material of a patient who does not harbour any known RAS or BRAF mutations. This new gene
Stefanie Peter et al.
EMBO molecular medicine, 6(12), 1525-1541 (2014-09-26)
Deregulated expression of MYC is a driver of colorectal carcinogenesis, necessitating novel strategies to inhibit MYC function. The ubiquitin ligase HUWE1 (HECTH9, ARF-BP1, MULE) associates with both MYC and the MYC-associated protein MIZ1. We show here that HUWE1 is required
Viktoria Kunz et al.
Scientific reports, 10(1), 18419-18419 (2020-10-30)
Experimental evidence suggests that ubiquitin-protein ligases regulate a number of cellular processes involved in tumorigenesis. We analysed the role of the E3 ubiquitin-protein ligase HUWE1 for pathobiology of multiple myeloma (MM), a still incurable blood cancer. mRNA expression analysis indicates
Hye In Cho et al.
Cell death and differentiation, 27(12), 3273-3288 (2020-06-20)
Brpf-histone acetyltransferase (HAT) complexes have important roles in embryonic development and regulating differentiation in ESCs. Among Brpf family, Brpf3 is a scaffold protein of Myst2 histone acetyltransferase complex that plays crucial roles in gene regulation, DNA replication, development as well
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