MI-3

MI-3 is an inhibitor of the interaction between menin and mixed lineage leukemia (MLL) fusion proteins (IC50 = 648 nM). MI-3 binds to menin (Kd = 201 nM) and inhibits the menin interaction with the MLL fusion protein MLL-AF9 in HEK293 cells without affecting protein levels of menin or MLL-AF9. It inhibits growth of mouse bone marrow cells (BMCs) expressing the Hoxa9 transformation-dependent MLL fusion proteins MLL-AF9 or MLL-ENL (IC50 = 5 µM for both), as well as reduces colony formation and induces differentiation of MLL-AF9-transformed BMCs. MI-3 inhibits growth of human leukemia cell lines containing MLL translocations and decreases the expression of the transcription factors HOXA9, HOXA10, and MEIS1 in THP-1 cells.Formal Name: 4-[4-(4,5-dihydro-5,5-dimethyl-2-thiazolyl)-1-piperazinyl]-6-(1-methylethyl)-thieno[2,3-d]pyrimidine. CAS Number: 1271738-59-0. Molecular Formula: C18H25N5S2. Formula Weight: 375.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: slightly soluble, Ethanol: slightly soluble. lambdamax: 224, 288 nm. SMILES: CC(C)C1=CC2=C(N3CCN(C4=NCC(C)(C)S4)CC3)N=CN=C2S1. InChi Code: InChI=1S/C18H25N5S2/c1-12(2)14-9-13-15(20-11-21-16(13)24-14)22-5-7-23(8-6-22)17-19-10-18(3,4)25-17/h9,11-12H,5-8,10H2,1-4H3. InChi Key: FUGQNAUKABUDQI-UHFFFAOYSA-N.