RITA | p53 Activator

RITA (reactivation of p53 and induction of tumor cell apoptosis, 213261-59-7) binds to p53 (Kd = 1.5 nM), changing its conformation, preventing it from binding to HDM2 and preventing its proteasomal degradation.1 It also weakly (computed Kd = 22 µM) binds HDM2 in the cleft that contacts the p53 transactivation domain.2 Its restoration of mutant p53 function depends on eIF2α phosphorylation, and it induces apoptosis via p53-dependent and -independent (JNK/SAPK/p38; protein translation) pathways.3-5 Induces senescence in head and neck cancer cells.6

References:

  1. Issaeva et al. (2004), Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors; Med., 10 1321
  2. Espinoza-Fonseca et al. (2005), Targeting MDM2 by the small molecule RITA: towards the development of new multi-target drugs against cancer; Biol. Med. Model, 2 38
  3. Ristau et al. (2019), RITA requires eIF2α-dependent modulation of mRNA translation for its anti-cancer activity; Cell Death Dis., 10 845
  4. Zhao et al. (2010), Rescue of the apoptotic-inducing function of mutant p53 by small molecule RITA; Cell Cycle, 9 1847
  5. Weilbacher et al. (2014), RITA can induce cell death in p53-defective cells independently of p53 function via activation of JNK/SAPK and p38; Cell Death Dis., 5 e1318
  6. Chuang et al. (2014), The p53-reactivating small molecule RITA induces senescence in head and neck cancer cells.; PLoS One, 9(8) e104821
Weight 0.1 mg
Dimensions 0.1 × 0.1 × 0.1 cm
Size:

5 mg, 25 mg

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CAS:
213261-59-7
Catalog Number:
10-3385
Activity:
P53 Activator
Chemical Names:
5,5′-(2,5-Furandiyl)bis-2-thiophenemethanol;
NSC 652287
Molecular Weight:
292.37
Molecular Formula:
C14H12O3S2
Solubility:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

RITA | p53 Activator

$70.00$300.00

CAS:
213261-59-7
Catalog Number:
10-3385
Activity:
P53 Activator
Chemical Names:
5,5′-(2,5-Furandiyl)bis-2-thiophenemethanol;
NSC 652287
Molecular Weight:
292.37
Molecular Formula:
C14H12O3S2
Solubility:
Soluble in DMSO (up to 20 mg/ml)
Physical Properties:
Yellow solid
Purity:
98% TLC
NMR (Conforms)
Storage Temperature:
RT
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT
  • 5 mg
  • 25 mg
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