tcsc1403 RITA

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Product Description

RITA is an inhibitor of p53-HDM-2 interaction, binds to p53dN, with a Kd of 1.5 nM, and also induces DNA-DNA cross-links.

IC50 & Target: Kd: 1.5 nM (p53dN)[1]


DNA Crosslinker[2]

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. 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[1]. 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[2]. 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[3].

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[1]. RITA (10 mg/kg, i.p.) also suppresses the growth of HeLa cells in SCID mice[3].

Information

CAS No213261-59-7
FormulaC14H12O3S2
Clinical Informationclinicalinformation
PathwayCell Cycle/DNA Damage
Autophagy
Apoptosis
TargetDNA Alkylator/Crosslinker
Autophagy
MDM-2/p53

Specifications

Purity / Grade>98%
SolubilityDMSO 205.0 mg/mL (701.2 mM)
Water: Insoluble
Smilessmiles

Misc Information

Storage InstructionPowder-20°C for 3 years
In solvent -80°C for 12 months
Alternative NamesNSC 652287
Observed Molecular Weight292.37
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