IUPAC/Chemical Name
3-chloro-1-(3,4-dichlorophenyl)-4-(4-morpholinyl)-1H-pyrrole-2,5-dione
InChi Key
MWSUIZKGNWELRF-UHFFFAOYSA-N
InChi Code
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
SMILES Code
O=C(C(Cl)=C1N2CCOCC2)N(C3=CC=C(Cl)C(Cl)=C3)C1=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Biological target:
RI-1 is an irreversible inhibitor of RAD51 (IC50s = 5-30 µM). RI-1 specifically reduces gene conversion in human cells while stimulating single strand annealing. RI-1 binds covalently to the surface of RAD51 protein at cysteine 319 that likely destabilizes an interface used by RAD51 monomers to oligomerize into filaments on DNA. RI-1 holds promise as an oncologic drug.
In vitro activity:
RI-1 potentiates the lethal effects of a DNA cross-linking drug in human cells. RI-1 represents a unique tool to dissect the network of reaction pathways that contribute to DNA repair in cells.
Reference: Nucleic Acids Res. 2012 Aug;40(15):7347-57. https://pubmed.ncbi.nlm.nih.gov/22573178/
In vivo activity:
To be determined
|
Solvent |
mg/mL |
mM |
| Solubility |
| DMF |
13.0 |
35.95 |
| DMSO |
2.0 |
5.53 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
361.60
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Budke B, Logan HL, Kalin JH, Zelivianskaia AS, Cameron McGuire W, Miller LL, Stark JM, Kozikowski AP, Bishop DK, Connell PP. RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells. Nucleic Acids Res. 2012 Aug;40(15):7347-57. doi: 10.1093/nar/gks353. Epub 2012 May 9. PMID: 22573178; PMCID: PMC3424541.
In vitro protocol:
1. Budke B, Logan HL, Kalin JH, Zelivianskaia AS, Cameron McGuire W, Miller LL, Stark JM, Kozikowski AP, Bishop DK, Connell PP. RI-1: a chemical inhibitor of RAD51 that disrupts homologous recombination in human cells. Nucleic Acids Res. 2012 Aug;40(15):7347-57. doi: 10.1093/nar/gks353. Epub 2012 May 9. PMID: 22573178; PMCID: PMC3424541.
In vivo protocol:
To be determined
1: Budke B, Logan HL, Kalin JH, Zelivianskaia AS, Cameron McGuire W, Miller LL,
Stark JM, Kozikowski AP, Bishop DK, Connell PP. RI-1: a chemical inhibitor of
RAD51 that disrupts homologous recombination in human cells. Nucleic Acids Res.
2012 Aug;40(15):7347-57. doi: 10.1093/nar/gks353. Epub 2012 May 9. PubMed PMID:
22573178; PubMed Central PMCID: PMC3424541.
2: Golec P, Wiczk A, Majchrzyk A, Łoś JM, Węgrzyn G, Łoś M. A role for accessory
genes rI.-1 and rI.1 in the regulation of lysis inhibition by bacteriophage T4.
Virus Genes. 2010 Dec;41(3):459-68. doi: 10.1007/s11262-010-0532-1. Epub 2010 Oct
14. PubMed PMID: 20945083; PubMed Central PMCID: PMC2962797.
3: Bartmann P, Bamberger U, Pohlandt F, Gortner L. Immunogenicity and
immunomodulatory activity of bovine surfactant (SF-RI 1). Acta Paediatr. 1992
May;81(5):383-8. PubMed PMID: 1498502.
