| Identification | Back Directory | [Name]
[1,2,4]Triazolo[1,5-a]pyrimidine, 7-(4-ethyl-1-piperazinyl)-5-methyl-2-[(2-methyl-1-piperidinyl)methyl]- | [CAS]
1359415-02-3 | [Synonyms]
UBE2T/FANCL-IN-1
[1,2,4]Triazolo[1,5-a]pyrimidine, 7-(4-ethyl-1-piperazinyl)-5-methyl-2-[(2-methyl-1-piperidinyl)methyl]- | [Molecular Formula]
C19H31N7 | [MOL File]
1359415-02-3.mol | [Molecular Weight]
357.5 |
| Hazard Information | Back Directory | [Biological Activity]
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]. | [References]
[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. |
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