An inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization

RITA – 1 mg

Brand:
Cayman
CAS:
213261-59-7
Storage:
-20
UN-No:
Non-Hazardous - /

HDM-2 (human double minute-2; MDM-2 in mouse) is a key negative regulator of p53 that binds to and targets p53 for proteasomal degradation. Overexpression of HDM-2 in some tumors leads to inactivation of p53 thereby allowing tumor cells to escape p53-induced apoptosis.{13684} RITA (reactivation of p53 and induction of tumor cell apoptosis) is a small molecule inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53.{12386} It binds to p53 with an apparent Kd of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation and activation.{12386} RITA potently inhibits the growth of a variety of cancer cell lines in the sub-micromolar range, inducing both DNA-protein and DNA-DNA cross links in human renal cancer cells.{13683} RITA reduced tumor size by 90% at a dose of 10 mg/kg in SCID mice bearing HCT116 tumors, and caused complete regression of A-498 tumor cell xenografts in nude mice at a dose of 45 mg/kg.{12386,13682}  

 

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SKU: 10006426 - 1 mg Category:

Description

An inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation

Formal name: 5,5′-(2,5-furandiyl)bis-2-thiophenemethanol

Synonyms:  2,5-bis(5-hydroxymethyl-2-thienyl) Furan|NSC 652287

Molecular weight: 292.4

CAS: 213261-59-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals||Research Area|Cancer|Cell Signaling|p53 Signaling||Research Area|Cancer|Transcription Factors|p53

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