CMP8

CMP8 is a mutant estrogen receptor alpha (ERalpha) antagonist and ligand used for bump and hole, a technique to study single protein isoforms when familial homology would interfere with other isoform-selective approaches. It is selective for an ERalpha triple mutant containing a lysine-to-methionine substitution at position 384 (EralphaL384M), a methionine-to-glycine substitution at position 421 (EralphaM421G), and a glycine-to-arginine substitution at position 521 (EralphaG521R), over wild-type ERalpha and ERbeta (IC50s= 29, 1,085, and 2,232 nM, respectively). It reduces reporter gene expression in HeLa cells expressing the triple mutant ERalpha (EC50 = 41 nM).Formal Name: 9a-[(4-chlorophenyl)methyl]-1,2,9,9a-tetrahydro-7-hydroxy-4-[4-[2-(1-piperidinyl)ethoxy]phenyl]-3H-fluoren-3-one. CAS Number: 851107-28-3. Molecular Formula: C33H34ClNO3. Formula Weight: 528.1. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 346 nm. SMILES: O=C1C(C2=CC=C(OCCN3CCCCC3)C=C2)=C4C5=CC=C(C=C5CC4(CC1)CC6=CC=C(C=C6)Cl)O. InChi Code: InChI=1S/C33H34ClNO3/c34-26-8-4-23(5-9-26)21-33-15-14-30(37)31(32(33)29-13-10-27(36)20-25(29)22-33)24-6-11-28(12-7-24)38-19-18-35-16-2-1-3-17-35/h4-13,20,36H,1-3,14-19,21-22H2. InChi Key: YHOXIEXEPIIKMD-UHFFFAOYSA-N.