| Identification | Back Directory | [Name]
RI-1 | [CAS]
415713-60-9 | [Synonyms]
RI-1
CS-909
RI1;RI-1
RI-1, >=98%
RAD51 inhibitor
RI-1 >=98% (HPLC)
RAD51 inhibitor 1
RAD51 inhibitor RI-1
3-Chloro-1-(3,4-dichlorophenyl)-4-Morpholino-1H-pyrrole-2,5-dione
3-chloro-1-(3,4-dichlorophenyl)-4-morpholin-4-ylpyrrole-2,5-dione
3-Chloro-1-(3,4-dichlorophenyl)-4-(4-morpholinyl)-1H-pyrrole-2,5-dione
1H-Pyrrole-2,5-dione, 3-chloro-1-(3,4-dichlorophenyl)-4-(4-morpholinyl)-
3-chloro-1-(3,4-dichlorophenyl)-4-(morpholin-4-yl)-2,5-dihydro-1H-pyrrole-2,5-dione | [Molecular Formula]
C14H11Cl3N2O3 | [MDL Number]
MFCD00814248 | [MOL File]
415713-60-9.mol | [Molecular Weight]
361.61 |
| Chemical Properties | Back Directory | [Boiling point ]
483.0±45.0 °C(Predicted) | [density ]
1.61 | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble10mg/mL, clear | [form ]
powder | [pka]
-3.45±0.20(Predicted) | [color ]
yellow to orange | [biological source]
human blood | [Stability:]
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 2 months. | [InChI]
1S/C14H11Cl3N2O3/c15-9-2-1-8(7-10(9)16)19-13(20)11(17)12(14(19)21)18-3-5-22-6-4-18/h1-2,7H,3-6H2 | [InChIKey]
MWSUIZKGNWELRF-UHFFFAOYSA-N | [SMILES]
ClC1=C(Cl)C=CC(N2C(C(N3CCOCC3)=C(Cl)C2=O)=O)=C1 |
| Hazard Information | Back Directory | [Description]
RI-1 (415713-60-9) is a potent and selective inhibitor of RAD51 (IC50 = 5-30 μM), a highly conserved protein that catalyzes DNA repair via homologous recombination.1 It specifically reduces gene conversion in human cells and stimulates single strand annealing. It covalently binds to Cys319 on the surface of RAD51 and disrupts protein-protein interaction. It potentiates the effect of DNA-damaging agents on tumor cells and is a novel tool for studying DNA repair in cells.2 Potentiates the killing of glioblastoma cells by ionizing radiation3 and alkylating drugs4. | [Uses]
RI 1 is a chemical inhibitor of RAD51, which disrupts homologous recombination in human cells. | [Biochem/physiol Actions]
RI-1 is a cell-permeable RAD51 inhibitor that binds covalently to the protein surface at Cysteine 319. RI-1 disrupts homologous recombination in human cells. | [in vivo]
RI-1 (50 mg/kg; i.p. every 3 d for 30 d) significantly reduces triple negative breast cancer (TNBC) tumor growth in mice[2]. | Animal Model: | Female BALB/c nude mice (6 weeks) bearing TNBC tumor[2] | | Dosage: | 50 mg/kg | | Administration: | I.p. every 3 days for 30 days | | Result: | Resulted in significant inhibition of tumor growth.
Did not cause body weight loss significantly.
|
| [target]
RAD51 | [storage]
Store at -20°C | [References]
1) Anand et al. (2017), Rad51-mediated double-strand break repair and mismatch correction of divergent substrates; Nature, 544 377
2) Budke et al. (2012), RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells; Nucleic Acids Res., 40 7347
3) Balbous et al. (2016), A radiosensitizing effect of RAD51 inhibition in glioblastoma stem-like cells; BMC Cancer, 16 604
4) Berte et al. (2016), Targeting Homologous Recombination by Pharmacological Inhibitors Enhances the Killing response of Glioblastoma Cells Treated with Alkylating Drugs; Mol. Cancer Ther., 15 2665 |
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| Company Name: |
Sigma-Aldrich
|
| Telephone: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
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