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RI-2

Catalog No.GC12752

Optimized reversible RAD51 inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

RI-2 Chemical Structure

Cas No.: 1417162-36-7

Size Price Stock Qty
10mM (in 1mL DMSO)
$200.00
In stock
10mg
$278.00
In stock
50mg
$879.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

HEK293 cells are plated into 96-well tissue culture plates at a density of 300 cells per well in the presence or absence of 50 nM mitomycin C (MMC) for 24 hours at 37°C, 5% CO2. Media is subsequently replaced with fresh media containing 0.5% DMSO plus RI-2 for an additional 24 hours. RI-2 is then removed, and cultures are allowed to grow to a 50-70% confluence. Average survival from at least three replicates is measured using CellGlo reagentor. RI-2 is deemed successful in sensitizing cells to MMC if they generate significantly greater toxicity in the presence of MMC relative to the absence of MMC. Specifically, sensitization is scored as a “+” when non-overlapping standard errors are observed for at least two pairs of compound doses[1].

References:

[1]. Budke B, et al. An optimized RAD51 inhibitor that disrupts homologous recombination without requiring Michael acceptor reactivity. J Med Chem. 2013 Jan 10;56(1):254-63.

Background

Description:

IC50: 44.17 μM

Homologous recombination (HR) is an essential process in cells that provides repair of DNA double-strand breaks and lesions that block DNA replication. RAD51 is an evolutionarily conserved protein that is central to HR. Overexpression of RAD51 protein is common in cancer cells and represents a potential therapeutic target in oncology. RI-2 is an optimized reversible RAD51 inhibitor.

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].

Clinical trial: Up to now, RI-2 is still in the preclinical development stage.

Reference:
[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.

Chemical Properties

Cas No. 1417162-36-7 SDF
Chemical Name 1-(3,4-dichlorophenyl)-3-(4-methoxyphenyl)-4-morpholino-1H-pyrrole-2,5-dione
Canonical SMILES COC1=CC=C(C(C(N2C3=CC(Cl)=C(Cl)C=C3)=O)=C(N4CCOCC4)C2=O)C=C1
Formula C21H18Cl2N2O4 M.Wt 433.28
Solubility ≥ 21.65mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.308 mL 11.5399 mL 23.0798 mL
5 mM 0.4616 mL 2.308 mL 4.616 mL
10 mM 0.2308 mL 1.154 mL 2.308 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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