1417162-36-7 Usage
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
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.
Check Digit Verification of cas no
The CAS Registry Mumber 1417162-36-7 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,4,1,7,1,6 and 2 respectively; the second part has 2 digits, 3 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 1417162-36:
(9*1)+(8*4)+(7*1)+(6*7)+(5*1)+(4*6)+(3*2)+(2*3)+(1*6)=137
137 % 10 = 7
So 1417162-36-7 is a valid CAS Registry Number.
1417162-36-7Relevant articles and documents
METHODS AND COMPOSITIONS INVOLVING RAD51 INHIBITORS
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, (2014/06/23)
The present invention concerns methods and compositions involving inhibitors and of RAD51, a protein involved in homologous recombination. In some embodiments, there are methods for sensitizing cells to the effects of DNA damaging agents, which can have p