HuR

CMLD-2 is an inhibitor of HuR-ARE interaction (Ki: 350 nM) that competitively binds HuR protein and disrupts its interaction with adenine element-rich (ARE) mRNA targets.CMLD-2 induces apoptosis and exhibits antitumor effects through MAD2 downregulation. CMLD-2 (1-75 μM ; 24-72 h) had an inhibitory effect on the viability of thyroid cancer cells.CMLD-2 (20-30 μM ; 24-48 h) activated caspases and induced apoptosis in H1299 and A549 cells.CMLD-2 (30 μM ; 24-48 h) induced G1 cell cycle arrest in H1299 and A549 cells and mitochondrial perturbation. CMLD-2 (30 μM ; 24-48 h) reduced the expression of HuR and HuR-regulated mRNAs and proteins in H1299 cells.CMLD-2 (35 μM ; 72 h) decreased the directional migration ability of SW1736, 8505C, BCPAP and K1 cells.CMLD-2 induced the migration of SW1736, 8505C, BCPAP and K1 cells with a strong decrease in MAD2 mRNA levels.

SRI-42127 is a novel small molecule inhibitor of the RNA regulatory factor HuR, which inhibits tumor growth, attenuates glial activation in a lipopolysaccharide-induced neuroinflammation model, and reduces neuropathic pain after nerve injury by inhibiting the neuroinflammatory response.

NSC243928 mesylate binds to human lymphocyte antigen 6 (LY6), a cell growth inhibitor with anticancer activity, and induces cell death in triple-negative breast cancer cells in a LY6K-dependent manner.

Azaphilone-9 (AZA-9) functions as an inhibitor of the HuR-ARE RNA interaction, with an inhibition constant (IC50) of 1.2 μM, by targeting the RNA-binding protein Hu antigen R (HuR). As HuR-RNA interactions play a critical role in stabilizing oncogenic mRNAs within tumors, Azaphilone-9 exhibits potential in inhibiting cancer cell growth and progression.

SRI-43265 (compound 40) inhibits the dimerization of human antigen R protein (HuR), which is involved in cancer and inflammation pathogenesis [1].

KH-3 is a potent inhibitor (IC50: 0.35 μM) of the RNA-binding protein Hu antigen R (HuR) and exhibits anti-proliferative effects. KH-3 interferes with HuR-FOXQ1 Mrna interactions, inhibits breast cancer cell invasion, and delays lung colony formation.

TM11, a tanshinone analog, serves as an effective inhibitor of HuR, preventing the formation of HuR-RNA complexes. It also reduces LPS-induced inflammatory responses in murine macrophages.

Okicenone is an antibiotic, interferring with HuR RNA binding, HuR trafficking, T-cell activation and cytokine expression.

HuRdegrader 2 (Compound 3) is a molecular glue that targets and degrades the RNA-binding protein Hu antigen R (HuR), achieving 30% degradation at 0.1 μM. It inhibits the proliferation of Colo-205 cancer cells with an IC50 of ≤200 nM. HuRdegrader 2 also shows high affinity for cereblon with an HTRF ratio < 0.02.