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| | [1,2,4]Triazolo[1,5-a]pyrimidine, 7-(4-ethyl-1-piperazinyl)-5-methyl-2-[(2-methyl-1-piperidinyl)methyl]- Basic information |
| | [1,2,4]Triazolo[1,5-a]pyrimidine, 7-(4-ethyl-1-piperazinyl)-5-methyl-2-[(2-methyl-1-piperidinyl)methyl]- Chemical Properties |
| density | 1.28±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | pka | 7.53±0.10(Predicted) | | form | Solid | | color | Off-white to yellow |
| | [1,2,4]Triazolo[1,5-a]pyrimidine, 7-(4-ethyl-1-piperazinyl)-5-methyl-2-[(2-methyl-1-piperidinyl)methyl]- Usage And Synthesis |
| Uses | 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]. | | 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. |
| | [1,2,4]Triazolo[1,5-a]pyrimidine, 7-(4-ethyl-1-piperazinyl)-5-methyl-2-[(2-methyl-1-piperidinyl)methyl]- Preparation Products And Raw materials |
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