推荐产品
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
SMILES字符串
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
生化/生理作用
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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
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
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
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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