Human Antigen R (HuR)

CMLD-2 is an inhibitor of the HuR-ARE interaction that competitively binds to the HuR protein, disrupting its binding to adenine-uridine rich elements (ARE) within mRNAs (Ki=350 nM). This compound induces apoptosis and exhibits notable antitumor activity across various cancer cell lines, including colon, pancreatic, thyroid, and lung cancers. HuR (Hu antigen R) is a critical RNA-binding protein involved in the regulation of mRNA stability and translation, making CMLD-2 a valuable tool for studying post-transcriptional regulation in cancer research.

KH-3 is an effective inhibitor of the RNA-binding protein Hu antigen R (HuR), exhibiting an IC50 value of 0.35 μM. This compound demonstrates notable anti-proliferative activity and is capable of suppressing breast cancer cell invasion. Additionally, KH-3 delays the initiation of lung colonies by disrupting the interaction between HuR and FOXQ1 mRNA, making it a valuable tool for research in cancer biology.

HuR degrader 2 is a molecular glue that specifically targets the RNA-binding protein Hu antigen R (HuR), leading to a significant degradation of approximately 30% of HuR at a concentration of 0.1 μM. This compound effectively inhibits the proliferation of the Colo-205 cancer cell line, demonstrating an IC50 of ≤200 nM. Additionally, HuR degrader 2 shows a high affinity for cereblon, with an HTRF ratio of less than 0.02, making it a valuable tool for studying HuR's role in cancer biology.

MG-HuR2 is a molecular glue degrader that specifically targets the oncogenic RNA-binding protein HuR, exhibiting an IC50 of 0.5 μM. This compound is particularly relevant for research involving HuR-overexpressing malignancies, such as breast cancer, providing a valuable tool for investigating therapeutic strategies aimed at modulating HuR activity in cancerous tissues.

SRI-43265 is a selective inhibitor of human antigen R (HuR) dimerization, a crucial process impacting HuR's role in post-transcriptional regulation of target mRNAs. By disrupting HuR multimers, SRI-43265 demonstrates potential in studying cancer and inflammatory processes, where HuR's activity contributes to pathogenesis. This reagent is valuable for investigating the molecular mechanisms underlying these diseases and for exploring therapeutic strategies targeting HuR functions.

ZM-32 is a potent inhibitor of human antigen R (HuR), a critical regulator of mRNA stability. By downregulating the expression of vascular endothelial growth factor A (VEGF-A) and matrix metalloproteinase 9 (MMP9), ZM-32 effectively inhibits angiogenesis in breast cancer. Demonstrating broad-spectrum anti-proliferative effects across various cancer cell lines, ZM-32 also shows significant antitumor efficacy in mouse models of the MDA-MB-231 breast cancer cell line.

Azaphilone-9 (AZA-9) is a potent inhibitor of the HuR-ARE RNA interaction, demonstrating an IC50 value of 1.2 μM. By binding to the RNA-binding protein Hu antigen R (HuR), Azaphilone-9 disrupts the stabilization of various oncogenic mRNAs in tumor cells. This mechanism suggests that Azaphilone-9 may serve as a valuable tool for investigating cancer cell growth and progression in research applications targeting RNA-protein interactions.

Okicenone is an inhibitor of Hu protein R (HuR), a key regulator of messenger RNA stability and translation. By disrupting HuR oligomerization and its RNA binding capabilities, Okicenone modulates HuR trafficking, influencing cytokine expression and T-cell activation. This compound is valuable in research focused on immune response modulation and the role of mRNA-binding proteins in cellular processes.