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:
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
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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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
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
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML3148-5MG | 04065266087765 |
| SML3148-25MG | 04065266087758 |