UBE2T/FANCL-IN-1

• CAT Number: I044340
• CAS Number: 1359415-02-3
• Molecular Formula: C19H31N7
• Molecular Weight: 357.50
• Purity: ≥95%
• Synonyms: 7-(4-ethylpiperazin-1-yl)-5-methyl-2-[(2-methylpiperidin-1-yl)methyl]-[1,2,4]triazolo[1,5-a]pyrimidine
• InChI: InChI=1S/C19H31N7/c1-4-23-9-11-24(12-10-23)18-13-15(2)20-19-21-17(22-26(18)19)14-25-8-6-5-7-16(25)3/h13,16H,4-12,14H2,1-3H3
• InChIKey: FJHJBABGFHVIDS-UHFFFAOYSA-N
• SMILES: CCN1CCN(CC1)C2=CC(=NC3=NC(=NN23)CN4CCCCC4C)C

UBE2T/FANCL-IN-1 is a potent inhibitor of UBE2T/FANCL-mediated FANCD2 monoubiquitylation that sensitizes cells to the DNA cross-linking agent, Carboplatin[1].
UBE2T/FANCL-IN-1 (CU2) completely inhibits the ubiquitylation of GST-FANCLRING at 100 μM. UBE2T/FANCL-IN-1 (500 μM) reduced the level of mUb-FANCD2 in response to HU treatment. UBE2T/FANCL-IN-1 (500 μM) also reducesthe level of mUb-FANCD2 generated in response to Cisplatin (10 μM) treatment for 6, 12, and 24 hours. The combination of 250 μM UBE2T/FANCL-IN-1 with 15 μM carboplatin led to an even more pronounced decrease in cell proliferation/growth, with the cells being <50% confluent after 8 days[1].

Reference

[1]. Cornwell MJ, et al. Small-Molecule Inhibition of UBE2T/FANCL-Mediated Ubiquitylation in the Fanconi Anemia Pathway. ACS Chem Biol. 2019;14(10):2148-2154.
 [Content Brief]