TC-E 5003

TC-E 5003 is an inhibitor of protein arginine methyltransferase 1 (PRMT1, IC50 = 1.5 µM for human PRMT1 in a methylation assay). It is selective for PRMT1 over PRMT4/CARM1 and SET7/9 methyltransferases, with less than 5% inhibition at a concentration of 50 µM for SET7/9. TC-E 5003 inhibits growth of MCF-7a breast cancer and LNCaP prostate cancer cells (GI50s = 1.97 and 4.49 µM, respectively) and decreases androgen-dependent gene transcription in vitro. TC-E 5003 (80 mg/kg) also has antimalarial properties and eradicates P. berghei in mice.Formal Name: N,N'-(sulfonyldi-4,1-phenylene)bis[2-chloro]-acetamide. CAS Number: 17328-16-4. Synonyms: NSC 30176. Molecular Formula: C16H14Cl2N2O4S. Formula Weight: 401.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml. lambdamax: 257, 283 nm. SMILES: ClCC(NC1=CC=C(S(C2=CC=C(NC(CCl)=O)C=C2)(=O)=O)C=C1)=O. InChi Code: InChI=1S/C16H14Cl2N2O4S/c17-9-15(21)19-11-1-5-13(6-2-11)25(23,24)14-7-3-12(4-8-14)20-16(22)10-18/h1-8H,9-10H2,(H,19,21)(H,20,22). InChi Key: SHRCVZJKZJGIHQ-UHFFFAOYSA-N.