CID-5721353

CID-5721353 is an inhibitor of the transcriptional repressor B cell lymphoma 6 (Bcl-6, Ki = 147 µM). It is selective for Bcl-6 over Kaiso, hypermethylated in cancer 1 (HIC1), and promyelocytic leukemia zinc finger (PLZF) at 50 µM. CID-5721353 is cytotoxic against Bcl-6-dependent SU-DLH-6, SU-DLH-4, Farage, OCI-LY7, OCI-LY1, and OCI-LY10 diffuse large B cell lymphoma (DLBCL) cells (GI50s = 0.024-0.936 mM) but not Bcl-6-independent Toledo or OCI-LY4 DLBCL cells (GI50 = >15 mM for both). It increases expression of the Bcl-6 target genes ATR, TP53, CD69, p21, and CD44 in SU-DLH-6 and SU-DHL-4 cells when used at a concentration of 50 µM. CID-5721353 (50 mg/kg) reduces tumor growth in OCI-LY7 and SU-DHL-6 mouse xenograft models.Formal Name: 2-[5-(5-bromo-1,2-dihydro-2-oxo-3H-indol-3-ylidene)-4-oxo-2-thioxo-3-thiazolidinyl]-butanedioic acid. CAS Number: 301356-95-6. Molecular Formula: C15H9BrN2O6S2. Formula Weight: 457.3. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Soluble, DMSO: Soluble. SMILES: BrC1=CC=C2C(/C(C(N2)=O)=C3C(N(C(C(O)=O)CC(O)=O)C(S\3)=S)=O)=C1. InChi Code: InChI=1S/C15H9BrN2O6S2/c16-5-1-2-7-6(3-5)10(12(21)17-7)11-13(22)18(15(25)26-11)8(14(23)24)4-9(19)20/h1-3,8H,4H2,(H,17,21)(H,19,20)(H,23,24)/b11-10-. InChi Key: QGNRETMYLHRUBB-KHPPLWFESA-N.