1875036-74-0
Chemical Structure
BI8622
- CAS No.: 1875036-74-0
- Formula:C25H26N6O
- Molecular Weight:426.51
IUPAC Name: N-(4-(aminomethyl)phenyl)-6-(4-cyano-4-phenylpiperidin-1-yl)-5-methylpyrimidine-4-carboxamide
InChIKey: IJHAXMJRQQTBPL-UHFFFAOYSA-N
SMILES: O=C(C1=NC=NC(N2CCC(C3=CC=CC=C3)(C#N)CC2)=C1C)NC4=CC=C(CN)C=C4
Biological Activity: BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM. BI8622 can decrease the protein expression levels of c-myc and glycolytic markers as well as immune modulatory markers after HUWE1 inhibition in triple-negative breast cancer (TNBC) cell lines. BI8622 significantly protects against cisplatin (HY-17394)-induced acute kidney injury (AKI). BI8622 significantly reduces the growth of multiple myeloma (MM) cell lines and induces cell cycle arrest. BI8622 can prevent HUWE1-dependent TTBK2 ubiquitination. BI8622 can be studied in research for various diseases including medulloblastoma, acute kidney injury, breast cancer and MM[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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BI8622 | 98.16% | BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM. BI8622 can decrease the protein expression levels of c-myc and glycolytic markers as well as immune modulatory markers after HUWE1 inhibition in triple-negative breast cancer (TNBC) cell lines. BI8622 significantly protects against cisplatin (HY-17394)-induced acute kidney injury (AKI). BI8622 significantly reduces the growth of multiple myeloma (MM) cell lines and induces cell cycle arrest. BI8622 can prevent HUWE1-dependent TTBK2 ubiquitination. BI8622 can be studied in research for various diseases including medulloblastoma, acute kidney injury, breast cancer and MM. | ||||||||||||||||||||
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- [1]. Peter S, et al. Tumor cell-specific inhibition of MYC function using small molecule inhibitors of the HUWE1 ubiquitin ligase. EMBO Mol Med. 2014 Dec;6(12):1525-41. [Content Brief]
- [2]. S. Kahol and S. Mathur (2023) 29P HUWE1 inhibition has tumor suppressive effect in triple-negative breast cancer cell lines by modulating glycolytic and immune modulatory markers. Annals of oncology, Volume 34, Supplement 4S1484.
- [3]. Crawford, L. J., et al., (2020). The E3 ligase HUWE1 inhibition as a therapeutic strategy to target MYC in multiple myeloma. Oncogene, 39(27), 5001–5014. [Content Brief]
- [4]. Yang, Y., et al., (2025). HUWE1-Mediated Degradation of MUTYH Facilitates DNA Damage and Mitochondrial Dysfunction to Promote Acute Kidney Injury. Advanced science (Weinheim, Baden-Wurttemberg, Germany), 12(13), e2412250 [Content Brief]
- [5]. Lin, I. H., et al., (2024). Regulation of primary cilia disassembly through HUWE1-mediated TTBK2 degradation plays a crucial role in cerebellar development and medulloblastoma growth. Cell death and differentiation, 31(10), 1349–1361. [Content Brief]
Keywords
