Sirtuins

Tenovin-6 is a analog of tenovin-1. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 in vitro with IC50 values of 21, 10, and 67 uM, respectively.

JNJ-26854165 is one of p53-activating agents and synergizes with AraC or doxorubicin to induce p53-mediated apoptosis and may provide a novel therapeutic approach for the treatment of acute leukemias.

RITA, also referred to as NSC 652287, is a trycyclic thiophene derivative that binds to MDM2, disrupting the MDM2-p53 complex and subsequently activating p53 and inducing apoptosis.

Tenovin-1 is a small molecule activator of p53 transcriptional activity that protects against MDM2-mediated p53 degradation.

NSC 319726 is a potent and selective activator of mutant p53R175

NSC59984 induces mutant p53 protein degradation via MDM2 and the ubiquitin-proteasome pathway. The EC50 of NSC59984 in most cancer cells is significantly lower than those of normal cells, with EC50 of 8.38 uM for p53-null HCT116 cells.

PRIMA-1 is a small molecule identified for its p53 reactivating effect.

Tenovin-3 is a sirtuin inhibitor.

NSC 146109 hydrochloride is a cell-permeable, genotype-selective antitumor agent that activates p53-dependent transcription.

RETRA hydrochloride is an antitumor agent which inhibits tumor cell growth in a mutant p53- and p73-dependent manner in vitro and iin vivo.

WR 1065, a dephosphorylated metabolite of amifostine (Ethyol), can protect against the immediate and delayed effects of radiation exposure.

PK11007 is an anti-p53 drug that stabilizes wild type and mutant p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. It exerts antitumor functions not only via reactivating p53 but also via other cellular mechanisms, such as increase of cellular ROS to toxic levels and activation of the UPR.

CBL0137(CBL-0137) activates p53 and inhibits NF-kB with EC50s of 0.37 μM and 0.47 μM in the cell-based p53 and NF-kB reporter assays, respectively. It also inhibits histone chaperone FACT (facilitates chromatin transcription complex).