MI-3

• CAT Number: I001085
• CAS Number: 1271738-59-0
• Molecular Formula: C₁₈H₂₅N₅S₂
• Molecular Weight: 375.55
• Purity: ≥95%
• Synonyms: 4-(4-(5,5-dimethyl-4,5-dihydrothiazol-2-yl)piperazin-1-yl)-6-isopropylthieno[2,3-d]pyrimidine
• Target: Menin-MLL
• Solubility: in DMSO > 10 mM
• Storage: Store at -20°C
• IC50: 648 ± 25 nM [1]
• InChI: InChI=1S/C18H25N5S2/c1-12(2)14-20-15(13-5-10-24-16(13)21-14)22-6-8-23(9-7-22)17-19-11-18(3,4)25-17/h5,10,12H,6-9,11H2,1-4H3
• InChIKey: BYEYBIAXHABAEB-UHFFFAOYSA-N
• SMILES: CC(C)C1=NC(=C2C=CSC2=N1)N3CCN(CC3)C4=NCC(S4)(C)C

MI-3 is a Menin-MLL interaction inhibitor with IC50 value of 648 ± 25 nM.IC50 value: 648 ± 25 nM [1]Target: Menin-MLLin vitro: The menin-MLL inhibitors very effectively blocked proliferation of MLL-AF9 and MLL-ENL transduced BMC, with GI50 values of about 5 μM for MI-2 and MI-3. MI-2 and MI-3 showed only a small effect on the cell growth of E2A-HLF transduced BMC (GI50 > 50 μM). MI-2 and MI-3 substantially and specifically reduce the immortalization potential of cells transformed with MLL fusion oncoproteins [1].in vivo: MLL-AF9 transformed BMC that remained viable after 7 days of treatment with MI-2 and MI-3 showed substantial changes in morphology, indicative of monocytic differentiation, as evidenced by increased cell size, lower nuclear to cytoplasmic ratio and highly vacuolated cytoplasm. Consistent with the change in cell morphology, the expression of CD11b was substantially increased on MLL-AF9 transformed BMC after 7 days of treatment with MI-2 and MI-3 [1].

Reference

1:Fine mapping of the nematode resistance gene Mi-3 in Solanum peruvianum and construction of a S. lycopersicum DNA contig spanning the locus. Yaghoobi J, Yates JL, Williamson VM.Mol Genet Genomics. 2005 Aug;274(1):60-9. Epub 2005 Jul 14. PMID: 16021467 2:Behavior of the [mi-3] mutation and conversion of polymorphic mtDNA markers in heterokaryons of Neurospora crassa. Hawse A, Collins RA, Nargang FE.Genetics. 1990 Sep;126(1):63-72. PMID: 1977658 Free PMC Article3:A missense mutation in the oxi-3 gene of the [mi-3] extranuclear mutant of Neurospora crassa. Lemire EG, Nargang FE.J Biol Chem. 1986 Apr 25;261(12):5610-5. PMID: 3007516 Free Article4:Conversion of a mitochondrial precursor polypeptide into subunit 1 of cytochrome oxidase in the mi-3 mutant of Neurospora crassa. Werner S, Bertrand H.Eur J Biochem. 1979 Sep;99(3):463-70. PMID: 227683 Free Article5:Deficiency of subunit two of cytochrome oxidase in the mi-3 cytoplasmic mutant of Neurospora crassa. Bertrand H, Werner S.Eur J Biochem. 1977 Oct 3;79(2):599-606. No abstract available. PMID: 72665 Free Article6:Comparison of the respiratory chain of Neurospora crassa wild type and the mi-mutants mi-1 and mi-3. von Jagow G, Weiss H, Klingenberg M.Eur J Biochem. 1973 Feb 15;33(1):140-57. No abstract available. PMID: 4144164 Free Article