Product Name :
RITA
Description:
RITA, also known as NSC 652287, is an inducer of both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks. RITA is also an inhibitor of MDM2-p53 interaction by targeting p53 and induces apoptosis in tumor cells.
CAS:
213261-59-7
Molecular Weight:
292.37
Formula:
C14H12O3S2
Chemical Name:
[5-[5-[5-(hydroxymethyl)thiophen-2-yl]furan-2-yl]thiophen-2-yl]methanol
Smiles :
OCC1=CC=C(S1)C1=CC=C(O1)C1=CC=C(CO)S1
InChiKey:
KZENBFUSKMWCJF-UHFFFAOYSA-N
InChi :
InChI=1S/C14H12O3S2/c15-7-9-1-5-13(18-9)11-3-4-12(17-11)14-6-2-10(8-16)19-14/h1-6,15-16H,7-8H2
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
RITA, also known as NSC 652287, is an inducer of both DNA-protein and DNA-DNA cross-links with no detectable DNA single-strand breaks. RITA is also an inhibitor of MDM2-p53 interaction by targeting p53 and induces apoptosis in tumor cells.|Product information|CAS Number: 213261-59-7|Molecular Weight: 292.37|Formula: C14H12O3S2|Synonym:|NSC 652287|NSC-652287|NSC652287|Chemical Name: [5-[5-[5-(hydroxymethyl)thiophen-2-yl]furan-2-yl]thiophen-2-yl]methanol|Smiles: OCC1=CC=C(S1)C1=CC=C(O1)C1=CC=C(CO)S1|InChiKey: KZENBFUSKMWCJF-UHFFFAOYSA-N|InChi: InChI=1S/C14H12O3S2/c15-7-9-1-5-13(18-9)11-3-4-12(17-11)14-6-2-10(8-16)19-14/h1-6,15-16H,7-8H2|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 100 mg/mL (342.{{Lonidamine} web|{Lonidamine} Hexokinase|{Lonidamine} Activator|{Lonidamine} Protocol|{Lonidamine} Data Sheet|{Lonidamine} manufacturer} 03 mM)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Bathophenanthroline} MedChemExpress|{Bathophenanthroline} {Fluorescent Dye}|{Bathophenanthroline} Technical Information|{Bathophenanthroline} In Vivo|{Bathophenanthroline} custom synthesis|{Bathophenanthroline} Epigenetics} |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|RITA inhibits p53-HDM-2 interaction, binding to p53dN, with a Kd of 1.5 nM. RITA (10 μM) blocks complex formation between p53 and HDM-2 in HCT116 cells and HDFs and in NHF-ERMyc cells irrespective of c-Myc expression.PMID:25027343 RITA (0.5 μM) reduces the viability of tumor cells in a wild-type p53-dependent manner. Moreover, RITA (0.1 μM) induces p53-dependent apoptosis. RITA induces p53 but does not via DNA damage-signaling pathway. RITA (NSC 652287) induces DNA-DNA cross-links. RITA induces G2-M cell cycle arrest at 10 nM and causes apoptosis at 100 nM. RITA (100 nM) also elevates p53 and causes dose-dependent effects on p21WAF1 protein levels. RITA inhibits the growth of HeLa and CaSki cells, with IC50s of 1 and 10 μM. In addition, RITA (1 μM) stabilizes p53 by inhibiting p53/E6AP interaction.|In Vivo:|RITA (0.1, 1 or 10 mg/kg, i.p.) shows potent antitumor activity in SCID mice bearing HCT116 and HCT116 TP53−/− xenografts. RITA (10 mg/kg, i.p.) also suppresses the growth of HeLa cells in SCID mice.|References:|Issaeva N, et al. Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors. Nat Med. 2004 Dec;10(12):1321-8. Epub 2004 Nov 21.Nieves-Neira W, et al. DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells. Mol Pharmacol. 1999 Sep;56(3):478-84.Zhao CY, et al. Rescue of p53 function by small-molecule RITA in cervical carcinoma by blocking E6-mediated degradation. Cancer Res. 2010 Apr 15;70(8):3372-81.Products are for research use only. Not for human use.|
