HDAC

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.

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.

inhibits p53 binding to mitochondria by reducing its affinity for antiapoptotic proteins Bcl-2 and Bcl-XL.

Pifithrin-beta is a small molecule inhibitor of p53.

Pifithrin-a is a reversible inhibitor of p53-mediated apoptosis and p53-dependent gene transcription such as cyclin G, p21/waf1, and mdm2 expression.

NSC 319726 is a potent and selective activator of mutant p53R175

NSC348884 is a nucleolar phosphoprotein that displays several biological activities in ribosome biogenesis, cell proliferation, cytoplasmic/nuclear shuttle transportation, nucleic acid binding, ribonucleic cleavage, and centrosome duplication. NSC 348884 is a putative inhibitor of nucleophosmin (NPM). NSC 348884 inhibits NMP oligomer formation, up-regulates p53 and induces apoptosis.

CP 31398 2HCl has been shown to act as a stabilizing agent for p53, and to promotes activity of p53 in cancer cell lines.

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

APR-246 is a quinuclidinone derivative that targets the Wrap53 gene with potential antineoplastic activity.

Kevetrin (thioureidobutyronitrile), is a water-soluble, small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

Idasanutlin is a potent and selective p53-MDM2 inhibitor.

MIRA-1 restores wild-type conformation, function and DNA binding activity to mutant p53. Induces p53 transcriptional transactivation of p21, MDM2 and PUMA.

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.

COTI-2 is an orally available thiosemicarbazone that activates mutant forms of p53. It induces apoptosis in a wide variety of human tumor cells in culture, inhibits the proliferation of colorectal cancer cell lines, and is active against human glioblastoma cell lines at nanomolar concentrations.

Amifostine is a phosphorothioate proposed as a radiation-protective agent. It causes splenic vasodilation and may block autonomic ganglia.

Minocycline hydrochloride is a broad-spectrum tetracycline antibiotic, acting by binding to the bacterial 30S ribosomal subunit and inhibiting protein synthesis.

PhiKan 083 hydrochloride is a carbazole derivative, which binds to the surface cavity and stabilizes Y220C (a p53 mutant), with a Kd of 167 μM, and a relative binding affinity (Kd) of 150 μM in Ln229 cells.

Triglycidyl isocyanurate (TGIC; Teroxirone) is a triazene triepoxide with antiangiogenic and antineoplastic activities.