BI8622

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].

Product Specifications

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.