RS-1 stimulates the binding of hRAD51 to ssDNA. Low-micromolar concentrations of this small molecule enhance DNA binding and result in longer protein–DNA complex lengths. In addition, RS-1 stabilizes the active form of hRAD51 filaments and this is reflected in an enhanced strand assimilation activity.
|Cell lines||PC3 cells|
|Preparation method||PC3 cells were treated with 60 μM RS-1 for the indicated times. Cells were collected and fixed in ice cold 70% ethanol for at least 4 hours. Cells were rinsed and stained with 50 μg/ml PI, 50 μg/ml RNAse A in PBS for 20 minutes. Cell cycle distributions were analyzed by flow cytometry using a LSR-II (BD biosciences) cytometer. The percentage of cells in G1, S, and G2/M phases of the cell cycle was determined using FlowJo software.|
|Incubation time||24 h|
|Animal models||Athymic nude mice|
|Formulation||30% DMSO, 35% PEG-400, 35% PBS|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||100 mg/mL in DMSO|
RS-1 enhances CRISPR/Cas9- and TALEN-mediated knock-in efficiency.
Song J, et al. Nat Commun. 2016 Jan 28;7:10548. PMID: 26817820.
The RAD51-stimulatory compound RS-1 can exploit the RAD51 overexpression that exists in cancer cells and tumors.
Mason JM, et al. Cancer Res. 2014 Jul 1;74(13):3546-55. PMID: 24753542.
Disufide crosslinks of cystines in proteins can be reduced to cysteine residues by TCEP (tris-(2-carboxyethyl)phosphine). Unlike DTT (dithiothreitol), TCEP does not contain thiols and therefore usually does not need to be removed prior to thiol modification.
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
6-Chloropurine is used in the preparation of 9-alkylpurines through alkylation with various substituted alkyl halides in dimethyl sulfoxide.
Lanolin is a wax secreted by the sebaceous glands of wool-bearing animals and used widely in the pharmaceutical and cosmetics industries.
Potassium acetate is the potassium salt of acetic acid, which is a synthetic carboxylic acid with antibacterial and antifungal properties.
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