Apoptosis

Apoptosis Inhibitor is a cell-permeable inhibitor of apoptosis induction.

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.

Trifloxystrobin (CGA 279202) is a fungicide, with EC50s of 23.0 μg/L and 1.7 μg/L for Daphnia magna neonate and embryos, respectively, after treatment for 48 h.

WEHI-539 hydrochloride is a small-molecule inhibitor of BCL-xL with IC50 value of 1.1 nM.

MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).

NSC207895 is a cell-permeable benzofuroxan compound that downregulates the p53 negative regulator MDMX protein level in MCF-7, LNCaP, and A549 cells (1 to 10 µM for 16 to 24 h) by suppressesing MDMX promoter transcription activity (IC50 = 2.5 µM in HT1080 cells), leading to enhanced p53 stabilization and activation.

TG101209, a novel JAK2 inhibitor, has significant in vitro activity in multiple myeloma and displays preferential cytotoxicity for CD45+ myeloma cells.

EP1013 is a broad-spectrum caspase selective inhibitor, used in the research of type 1 diabetes.

Lestaurtinib (CEP-701;KT-5555) is a multi-kinase inhibitor with potent activity against the Trk family of receptor tyrosine kinases. Lestaurtinib inhibits JAK2, FLT3 and TrkA with IC50s of 0.9, 3 and less than 25 nM, respectively.

Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor; inhibits apoptosis stimulated by TNF-α with an IC50 of 39 ?M.

Emricasan is a first-in-class caspase inhibitor in clinical trials for the treatment of liver diseases.

HA14-1 interacts with Bcl-2 and inhibits the antiapoptotic effect of Bcl-2.

Nutlin 3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 uM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite (-)-enantiomer Nutlin-3a.

RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2.

Regorafenib Hydrochloride is a multi-target inhibitor for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1 with IC50s of 13/4.2/46, 22, 7, 1.5 and 2.5 nM, respectively.

Geniposidic acid is an effective anticancer and radioprotection agent.

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

Apoptosis Activator 2 strongly induces caspase-3 activation, PARP cleavage, and DNA fragmentation which leads to the destruction of cells (Apaf-1 dependent) with IC50 of ~4 μM, inactive to HMEC, PREC, or MCF-10A cells

TPEN is a heavy metal chelator. Reacts with both Zn-proteome and Zn-metallothionein (MT) in LLC-PK1 cells; acts as an intracellular chelator of proteomic Zn2+.

Arctigenin is an antioxidant, anti-inflammatory, antiproliferative and antiviral agent. It inhibits LPS-induced iNOS expression via inhibition of IκBα phosphorylation and p65 nuclear translocation (IC50 = 10 nM)

Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor.

Jaceosidin is a pharmacologically active flavone derived from Artemisia argyi, inhibits phorbol-ester-induced upregulation of COX-2 and MMP-9 by blocking phosphorylation of ERK-1 and -2 in cultured human mammary epithelial cells.

SS28, a SRT501 analog with oral bioavailability, inhibits tubulin polymerization to cause cell cycle arrest at G2/M phase. SS28 results in apoptosis rather than necrosis tubulin.

KR-33493 is a potent inhibitor of Fas-mediated cell death (FAF1).

Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent.

Kinetin riboside is an activator of the Parkinson's Disease-associated PTEN-induced Putative Kinase 1 (PINK1), and acts independently from mitochondrial depolarization.

SID 3712249 (MiR-544 Inhibitor 1) is an inhibitor of the biogenesis of microRNA-544 (miR-544).

Ubiquitin Isopeptidase Inhibitor I, G5 (NSC 144303) is an apoptosome-independent caspase and apoptosis activator with IC50 values of 1.76 and 1.6 μM in E1A and E1A/C9DN cells, respectively.

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.

RIPGBM is a selective inducer of apoptosis in glioblastoma multiforme (GBM) cancer stem cells (CSCs) with an EC50 of ??500 nM.

MA242 is a dual inhibitor of murine double minute 2 (MDM2) and nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy.

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

AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM; does not inhibit BIR3 domain and BID

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

MDM2 Inhibitor is a cell-permeable boranyl-chalcone exhibiting strong binding to MDM2 and irreversibly disrupts the MDM2/p53 protein complex.

GSK2593074A (GSK??074) is a necroptosis inhibitor with dual targeting ability to both RIP1 and RIP3.

NVX-207 is a derivative of betulinic acid with anti-cancer activity.

MIF antagonist is an inhibitor of the dopachrome tautomerase activity of MIF in vitro (IC50 = 7 M) and in cells (IC50 = 25 M).

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

25-hydroxy Cholesterol is a side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of sterol regulatory element binding proteins (SREBPs) to suppress endogenous cholesterol synthesis in various cell types

Tenovin-3 is a sirtuin inhibitor.

TC-DAPK6 is a potent and selective, ATP-competitive inhibitor of death-associated protein kinase 1 (DAPK1) (IC50 values are 69 and 225 nM for DAPK1 and DAPK3 respectively, when assayed with 10 uM ATP).

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

CID755673 is a potent PKD inhibitor with IC50s of 182 nM, 280 nM and 227 nM for PKD1, PKD2 and PKD3, respectively.

CID797718 is a structural analog of CID755673 (Adooq Catalog No. A13804). It was a 10-time less potent PKD1 inhibitor with an IC50 value of 7.0 +/-0.8 uM.

ISRIB (mix-isomer) is a potent and selective small molecule inhibitor of PERK signaling (IC50 ~5 nM) that can potently reverse the effects of eIF2α phosphorylation.

RPI-1 is a competitive, potent ATP-dependent Ret kinase inhibitor.

Ecabet sodium is a widely employed mucoprotective agent for the treatment of gastric ulcers.

GDC-0152 is a second mitochondrial activator of caspases (Smac) mimetic inhibitor of IAPs (Inhibitor of Apoptosis Proteins) with potential antineoplastic activity.

Idasanutlin is a potent and selective p53-MDM2 inhibitor.