UMI-77

Myeloid cell leukemia-1 (Mcl-1) is a potent anti-apoptotic protein and a member of the pro-survival Bcl-2 family. UMI-77 is a selective Mcl-1 inhibitor with a Ki value of 490 nM and exhibits selectivity over other members of the Bcl-2 family (Kis = 5.3, 23.8, 33.0, and 8.2 µM) for A1/Bfl-1, Bcl-2, Bcl-xL, and Bcl-W, respectively). It has been shown to disrupt the heterodimerization of Mcl-1/Bax and Mcl-1/Bak, thus antagonizing Mcl-1 function. UMI-77 inhibits the growth of various pancreatic cancer cell lines with IC50s values ranging from 3.4-16.1 µM, inducing apoptosis through activation of the intrinsic apoptotic pathway and/or Bax conformational change. In a BxPC-3 xenograft mouse model, 60 mg/kg UMI-77 demonstrated antitumor activity without damaging normal tissues.Formal Name: 2-[[4-[[(4-bromophenyl)sulfonyl]amino]-1-hydroxy-2-naphthalenyl]thio]-acetic acid. CAS Number: 518303-20-3. Molecular Formula: C18H14BrNO5S2. Formula Weight: 468.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 2 mg/mL, DMSO: 0.5 mg/mL, Ethanol: 5 mg/mL, Ethanol:PBS (pH 7.2) (1:8): 0.11 mg/mL. lambdamax: 223, 237, 307 nm. SMILES: OC1=C(SCC(O)=O)C=C(NS(C2=CC=C(Br)C=C2)(=O)=O)C3=CC=CC=C31. InChi Code: InChI=1S/C18H14BrNO5S2/c19-11-5-7-12(8-6-11)27(24,25)20-15-9-16(26-10-17(21)22)18(23)14-4-2-1-3-13(14)15/h1-9,20,23H,10H2,(H,21,22). InChi Key: WUGANDSUVKXMEC-UHFFFAOYSA-N.