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BI8622

CAT: 0804-HY-120929-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-120929-01Size:5 mg
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Description
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 -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].
CAS Number
1875036-74-0
UNSPSC
12352005
Target
C-Myc; E1/E2/E3 Enzyme
Type
Reference compound
Related Pathways
Apoptosis; Metabolic Enzyme/Protease
Applications
Cancer-programmed cell death
Field of Research
Cancer; Inflammation/Immunology
Assay Protocol
https://www.medchemexpress.com/bi8622.html
Purity
99.35
Solubility
DMSO : 125 mg/mL (ultrasonic)
Smiles
O=C(C1=NC=NC(N2CCC(C3=CC=CC=C3)(C#N)CC2)=C1C)NC4=CC=C(CN)C=C4
Molecular Formula
C25H26N6O
Molecular Weight
426.51
References & Citations
[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.|[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.|[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|[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
No Development Reported

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