| Identification | Back Directory | [Name]
RI-2 | [CAS]
1417162-36-7 | [Synonyms]
RI-2
CS-1675
RI2;RI 2
1-(3,4-Dichlorophenyl)-3-(4-methoxyphenyl)-4-(4-morpholinyl)-1H-pyrrole-2,5-dione
1H-Pyrrole-2,5-dione, 1-(3,4-dichlorophenyl)-3-(4-methoxyphenyl)-4-(4-morpholinyl)- | [Molecular Formula]
C21H18Cl2N2O4 | [MOL File]
1417162-36-7.mol | [Molecular Weight]
433.28 |
| Chemical Properties | Back Directory | [Boiling point ]
605.6±55.0 °C(Predicted) | [density ]
1.441±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≥21.65 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | [form ]
solid | [pka]
-0.77±0.20(Predicted) | [color ]
Yellow to orange |
| Hazard Information | Back Directory | [Description]
RI-2 is a reversible inhibitor of RAD51 (IC50 = 44.2 μM), a protein that is central to the homologous recombination process initiated upon DNA double-strand breaks and is often overexpressed in a wide range of human cancer cell types. At 150 μM, it has been shown to inhibit DNA repair and to sensitize cancer cells to cross-linking chemotherapy in vitro. | [Uses]
RI-2 is a reversible inhibitor of RAD51 (IC50 = 44.2 μM), a protein that is central to the homologous recombination process initiated upon DNA double-strand breaks and is often overexpressed in a wide range of human cancer cell types. At 150 μM, it has been shown to inhibit DNA repair and to sensitize cancer cells to cross-linking chemotherapy in vitro.[Cayman Chemical] | [in vitro]
although ri-2 did exhibit reduced activity relative to ri-1, it did retain enough activity to sensitize cells to mmc cell-based assays. ri-2 exhibited no reactivity toward glutathione after incubation for 24 hours. rad51 protein that had been treated with ri-2 prior to washing exhibited no measurable loss of dna binding activity, even though ri-2 is known to inhibit rad51 with an ic50 of 44.17 μm. this indicates that rad51 inhibition by ri-2 is fully reversible [1]. | [in vivo]
ri-1, the analogue of ri-2, facilitated mapping of the binding pocket within known crystal structures of rad51. however, this reactivity of ri-1 potentially may limit its development in pre-clinical animal models. ri-1 has been found to exhibit a relatively short half-life, due to reactivity in thiol-containing solutions [1]. | [IC 50]
44.17 μm | [storage]
Store at -20°C | [References]
[1] budke b, kalin jh, pawlowski m, zelivianskaia as, wu m, kozikowski ap, connell pp. an optimized rad51 inhibitor that disrupts homologous recombination without requiring michael acceptor reactivity. j med chem. 2013 jan 10;56(1):254-63. |
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