CCG-203971

Signaling through small G proteins of the RhoA subfamily, including RhoC, induces actin-regulated cytosolic-to-nuclear translocation of the oncogene product megakaryoblastic leukemia 1 (MKL1), which binds to serum response factor (SRF). The MKL1/SRF complex, in turn, activates the transcription of serum response element (SRE) regulated genes, stimulating cell migration, a process that is central to metastasis. CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 µM), with 87% inhibition of SRE activation achieved at 100 µM. This compound also inhibits PC-3 cell migration (IC50 = 4.2 µM), as determined by a scratch wound assay. CCG-203971 causes no cytotoxicity when evaluated by WST-1 assay. It is well tolerated in normal mice up to doses of 100 mg/kg given intraperitoneally over five days.Formal Name: N-(4-chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide. CAS Number: 1443437-74-8. Molecular Formula: C23H21ClN2O3. Formula Weight: 408.9. Purity: >90%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 25 mg/ml, Ethanol: 50 mg/ml. lambdamax: 252, 281 nm. SMILES: O=C(N1CCCC(C(NC2=CC=C(Cl)C=C2)=O)C1)C3=CC(C4=CC=CO4)=CC=C3. InChi Code: InChI=1S/C23H21ClN2O3/c24-19-8-10-20(11-9-19)25-22(27)18-6-2-12-26(15-18)23(28)17-5-1-4-16(14-17)21-7-3-13-29-21/h1,3-5,7-11,13-14,18H,2,6,12,15H2,(H,25,27). InChi Key: HERLZBNILRVHQN-UHFFFAOYSA-N.