RA-9

RA-9 is an inhibitor of deubiquitinating enzymes It inhibits ubiquitin C-terminal hydrolase L1 (UCH-L1), UCH-L3, and ubiquitin-specific protease 8 (USP8) in a cell-free assay when used at a concentration of 10 µM, as well as USP5 in a reporter assay at the same concentration. RA-9 (10 µM) also inhibits the 26S proteasome, but not the 20S proteasome, in a reporter assay using HeLa cervical cancer cells. It increases the levels of polyubiquitinated proteins in HeLa and TOV-21G ovarian cancer cells when used at a concentration of 5 µM. RA-9 (10 µM) induces cell cycle arrest at the S and G2/M phases in HeLa cells. It decreases the viability of nine cancer cell lines with IC50 values ranging from 1.64 to 12.49 µM. In vivo, RA-9 (5 mg/kg every other day) increases survival and decreases tumor and ascitic fluid mass in an ES-2 ovarian cancer mouse xenograft model.Formal Name: 3E,5E-bis[(4-nitrophenyl)methylene]-4-piperidinone. CAS Number: 919091-63-7. Molecular Formula: C19H15N3O5. Formula Weight: 365.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Sparingly Soluble: 1-10 mg/ml. SMILES: O=C(/C(CNC/1)=C/C2=CC=C(C=C2)[N+]([O-])=O)C1=C\C3=CC=C(C=C3)[N+]([O-])=O. InChi Code: InChI=1S/C19H15N3O5/c23-19-15(9-13-1-5-17(6-2-13)21(24)25)11-20-12-16(19)10-14-3-7-18(8-4-14)22(26)27/h1-10,20H,11-12H2/b15-9+,16-10+. InChi Key: YUYPWAMLWZVHAE-KAVGSWPWSA-N.