BI 8626, BI-8626, N-(3-(Aminomethyl)benzyl)-8-(4-benzylpiperazin-1-yl)pyrimido[5,4-d]pyrimidin-4-amine, N1-[8-[4-(Phenylmethyl)-1-piperazinyl]pyrimido[5,4-d]pyrimidin-4-yl]-1,3-benzenedimethanamine
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BI8626 is a selective HUWE1 (HECTH9; MULE; ARF-BP1) inhibitor (IC50 = 0.9 µM by HUWE1 HECT-domain auto-ubiquitination assay; IC50 >50 µM against other HECT-domain Ub ligases tested). BI8626 inhibits the degradation of HUWE1 target proteiins, including MCL1, MIZ1, and TopBP1 (10-20 µM). BI8626 suppresses Ls174T colony formation (IC50 = 0.7 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.
Bee phonoreceptors are revealed by electrophysiological method. These are hair sensillae located between facet eyes and occipital commissure. The region of the highest sensitivity of receptors in within the range of the maximum energy of various sound signals used in
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
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
The MYC oncoprotein globally affects the function of RNA polymerase II (RNAPII). The ability of MYC to promote transcription elongation depends on its ubiquitylation. Here, we show that MYC and PAF1c (polymerase II-associated factor 1 complex) interact directly and mutually
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Unser Team von Wissenschaftlern verfügt über Erfahrung in allen Forschungsbereichen einschließlich Life Science, Materialwissenschaften, chemischer Synthese, Chromatographie, Analytik und vielen mehr..
