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
MDL number:
UNSPSC Code:
12352107
NACRES:
NA.77
Quality Level
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
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).
WGK
WGK 3
Regulatory Information
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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
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
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
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
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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