RI-1 |
Catalog No.GC18140
One-Click Copy Product Info
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RI-1 is a RAD51 protein inhibitor, with IC50 values ranging from 5 to 30μM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 415713-60-9
Sample solution is provided at 25 µL, 10mM.
RI-1 is a RAD51 protein inhibitor, with IC50 values ranging from 5 to 30μM[1]. RI-1 contains a chloromaleimide group that functions chemically as a Michael acceptor, thereby inhibiting RAD51 by covalently binding to the Cys319 residue, and RI-1 disrupts RAD51-ssDNA binding by preventing oligomerization of RAD51 into filaments on DNA[2]. RI-1 has been widely used to increase the sensitivity of glioblastoma stem cell-like cells to ionizing radiation and to interfere with the DNA repair process[3].
In vitro, RI-1 treatment (20µM) in combination with etoposide (1µM) for 48 hours significantly inhibited the viability of FLO-1 cells and induced cell apoptosis[4]. Treatment with 20µM RI-1 for 48 hours markedly reduced the camptothecin-induced genomic instability of MCF7, HCT116, and OE19 cells[5]. Treatment with 1.5µM RI-1 for 3 weeks following 2Gy irradiation (2h) significantly reduced the survival of glioblastoma cells and decreased the expression level of SOX2 mRNA[6].
In vivo, RI-1 treatment via intraperitoneal injection at a dose of 5mg/kg every other day for 36 days significantly inhibited the growth of HeLa xenograft tumors in mice[7]. Intraperitoneal injection of RI-1 at a dose of 50mg/kg every 3 days for 30 days significantly reduced tumor growth in the MDA-MB-157 xenograft mouse model without affecting body weight[8].
References:
[1] Budke B, Logan H L, Kalin J H, et al. RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells[J]. Nucleic acids research, 2012, 40(15): 7347-7357.
[2] Budke, Brian, et al. "Recent developments using small molecules to target RAD51: how to best modulate RAD51 for anticancer therapy?." ChemMedChem 11.22 (2016): 2468-2473.
[3] Balbous, Anaïs, et al. "A radiosensitizing effect of RAD51 inhibition in glioblastoma stem-like cells." BMC cancer 16.1 (2016): 604.
[4] Liao C, Zhao J, Kumar S, et al. RAD51 inhibitor reverses etoposide-induced genomic toxicity and instability in esophageal adenocarcinoma cells[J]. Archives of clinical toxicology, 2020, 2(1): 3.
[5] Liao C, Talluri S, Zhao J, et al. RAD51 is implicated in DNA damage, chemoresistance and immune dysregulation in solid tumors[J]. Cancers, 2022, 14(22): 5697.
[6] King H O, Brend T, Payne H L, et al. RAD51 is a selective DNA repair target to radiosensitize glioma stem cells[J]. Stem cell reports, 2017, 8(1): 125-139.
[7] Chen Q, Cai D, Li M, et al. The homologous recombination protein RAD51 is a promising therapeutic target for cervical carcinoma[J]. Oncology reports, 2017, 38(2): 767-774.
[8] Shi Y, Jin J, Wang X, et al. DAXX, as a tumor suppressor, impacts DNA damage repair and sensitizes BRCA-proficient TNBC cells to PARP inhibitors[J]. Neoplasia, 2019, 21(6): 533-544.
| Cell experiment [1]: | |
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Cell lines |
FLO-1 cells |
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Preparation Method |
FLO-1 cells were cultured in DMEM medium supplemented with 10% fetal bovine serum (FBS), 2mM glutamine, and 1% penicillin-streptomycin at 37°C in 5% CO2/atmosphere. FLO-1 cells were seeded onto 96-well microplates (1×104 cells/well) and cultured for 24h. The cells were treated with PBS or RI-1 at different concentrations (0, 1, 10, and 20µM) in the presence of 1µM etoposide. After 48h incubation, cell viability was assessed. |
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Reaction Conditions |
0, 1, 10, and 20µM; 48h |
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Applications |
RI-1 treatment reduced the cell viability of FLO-1 cells in a dose-dependent manner in the presence of etoposide. |
| Animal experiment [2]: | |
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Animal models |
Female BALB/c-nude mice |
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Preparation Method |
Female BALB/c-nude mice (6-weeks old) were housed under controlled temperature (21-23°C), humidity (30-35%) and light cycle (7:00 AM to 7:00 PM) and maintained on a standard rodent diet. HeLa Cells (1×107) in the exponential growth phase were collected and suspended in 200µl phosphate-buffered saline and then injected subcutaneously into the posterior side of mice. RI-1 (5mg/kg in 200µl phosphate-buffered saline) was injected intraperitoneally every other day for 36 days into mice when the tumor volume reached 120mm3. Analyze the tumor volume of the mice every 3 days. |
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Dosage form |
5mg/kg; every other day; 36 days; i.p. |
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Applications |
RI-1 treatment significantly inhibited tumor growth in mice with HeLa xenografts. |
References: [1] Liao C, Zhao J, Kumar S, et al. RAD51 inhibitor reverses etoposide-induced genomic toxicity and instability in esophageal adenocarcinoma cells[J]. Archives of clinical toxicology, 2020, 2(1): 3. [2] Chen Q, Cai D, Li M, et al. The homologous recombination protein RAD51 is a promising therapeutic target for cervical carcinoma[J]. Oncology reports, 2017, 38(2): 767-774. | |
| Cas No. | 415713-60-9 | SDF | |
| Chemical Name | 3-chloro-1-(3,4-dichlorophenyl)-4-morpholin-4-ylpyrrole-2,5-dione | ||
| Canonical SMILES | C1COCCN1C2=C(C(=O)N(C2=O)C3=CC(=C(C=C3)Cl)Cl)Cl | ||
| Formula | C14H11Cl3N2O3 | M.Wt | 361.61 |
| Solubility | ≥ 18.1 mg/mL in DMSO, ≥ 8.89 mg/mL in EtOH with gentle warming | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.7654 mL | 13.8271 mL | 27.6541 mL |
| 5 mM | 553.1 μL | 2.7654 mL | 5.5308 mL |
| 10 mM | 276.5 μL | 1.3827 mL | 2.7654 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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)