Catalog No.S8077 Synonyms: RAD51 inhibitor 1
Molecular Weight(MW): 361.61
RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM.
1 Customer Review
Inhibition of Rad51 sensitizes PTEN-WT BT549 cells to olaparib. A. Immunofluorescence showed the foci of γH2AX in PTEN-WT BT549 cells treated with 5 μM olaparib (OLA), 5 μM RI-1, and their combination. B. The quantification of immunofluorescenct results. *p ≤ 0.05, ** p ≤ 0.01, ***p ≤ 0.001. C. MTT analysis of PTEN-WT BT549 treated with olaparib or olaparib in combining with RI-1. *p ≤ 0.05, **p ≤ 0.01, ***p ≤ 0.001. D. MTT analysis of PTEN-WT BT549 treated with IR-1 for 48 h.
Biomed Pharmacother, 2017, 94:165-168. RI-1 purchased from Selleck.
Purity & Quality Control
|Description||RI-1 is a RAD51 inhibitor with IC50 ranging from 5 to 30 μM.|
|Features||A selective recombinant RAD51 protein inhibitor discovered in 2012. Valuable tool for mechanistic studies of DNA repair and potential for use in many cancers.|
RI-1 sensitizes cells to DNA damage by directly and specifically disrupting HsRAD51 and inhibiting the ability of RAD51 to form filaments on ssDNA. In addition, RI-1 alone generates single-agent toxicity in all three cancer cell lines (HeLa, MCF-7 and U2OS) with LD50 values in the 20–40 µM range.  RI-1 decreases the rejoining of γ-H2AX foci in G2 phase cells and results in a higher level of unrepaired DSBs 6 hours after irradiation. 
DNA binding assays:All reactions are performed in black non-binding polystyrene 384-well plates with reaction volumes of 30–100 μL. Purified DNA strand exchange proteins and chemical compounds are pre-incubated at room temperature for 5 minutes; they are then further incubated at 37°C for 30 min with 100 nM of ssDNA substrate, consisting of a 45-mer poly-dT tagged with Alexa 488 at the 5’ terminus (synthesized and purified by Integrated DNA Technologies). Reactions are performed in 20 mM HEPES pH 7.5, 10 mM MgCl2, 0.25 μM BSA, 2% glycerol, 30 mM NaCl, 4% DMSO and 2 mM ATP. Some conditions included DTT or TCEP (tris(2-carboxyethyl)phosphine) as indicated. DNA binding is measured as a function of fluorescence polarization (FP) with a Safire2 plate reader, using the following settings: excitation 470±5nm, emission 530±5nm, 10 reads/well, Z height and G factor auto-calibrated from control wells. Displayed error bars represent standard deviation. For experiments involving a titration of protein concentrations, data are fit to an equation that accounts for the cooperative nature by which recombinase proteins bind DNA. For experiments involving a titration of RI-1, protein concentrations are selected to give an ∼80% saturation of the FP signal in the absence of RI-1.
|In vitro||DMSO||50 mg/mL (138.27 mM)|
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||RAD51 inhibitor 1|
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