Apoptosis

Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.

ABT-737 is a pan-Bcl-2 inhibitor. IC50 values ranged from 192 nM (the pre-B cell line Hal-01) to <10 μM (Nalm-6, K562 and HL-60).

Bcl-2 homology domain-3 (BH3) mimetic,antagonize all antiapoptotic Bcl-2 family proteins (average IC50, 3 umol/L), including Mcl-1 (IC50, 2.9 umol/L) and Bfl-1 (IC50, 5 umol/L).

Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2

Pomalidomide is a derivative of thalidomide and acts as an immunomodulator.

Thalidomide can directly inhibit angiogenesis induced by bFGF or VEGF in vivo.

TW-37, a small-molecule inhibitor of Bcl-2, inhibits cell growth and induces apoptosis in pancreatic cancer mediated through a novel pathway involving inactivation of Notch-1 and Jagged-1.

VX-765 is a novel Caspase-1 inhibitor,which is an enzyme that controls the generation of two cytokines, IL-1b and IL-18.

YM155 is a novel small molecule survivin suppressant with an IC50 of 0.54 nM for the inhibition of survivin promoter activity.

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.

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 3a is a potent inhibitor of MDM2 (mouse double minute 2) binding to p53 that induces the expression of p53 regulated genes, and shows potent antiproliferative activity in cells expressing functional p53.

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.

Necrostatin-1 is an ATP-competitive, allosteric inhibitor of receptor-interacting protein kinase 1 (RIPK1) (EC50 = 182 nM).

GW4869 is a cell permeable, selective inhibitor of N-SMase (neutral sphingomyelinase).

Gambogic acid is a natural product isolated from the Garcinia hanburyi tree. Gambogic Acid activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 with IC50 of 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 μM, respectively.

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

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

C87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.

Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor. Inhibits caspase processing and apoptosis induction in tumor cells in vitro (IC50 = 0.0015 - 5.8 mM). Active in vivo.

CID 2011756 is a protein kinase D (PKD) inhibitor (IC50 values are 0.6, 0.7 and 3.2 μM for PKD2, PKD3 and PKD1 respectively).

kb NB 142-70 is a selective protein kinase D (PKD) inhibitor (IC50 values are 28.3, 58.7 and 53.2 nM for PKD1, 2 and 3 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.

RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 nM.

ABT-199 is a so-called BH3-mimetic drug, which is designed to block the function of the protein Bcl 2.

Z-VEID-FMK is the specific recognition sequence for caspase-6/Mch2. Z-VEID-FMK is a synthetic peptide that irreversibly inhibits activity of VEID-dependent caspases (e.g., caspase-6). The inhibitor is designed as a methyl ester to facilitate cell permeability.

GSK481 is a novel benzoxazepinone (BOAz) series of RIP1 inhibitors. Receptor Interacting Protein Kinase 1 (RIP1) has been implicated as a key contributor to inflammation through the regulation of programmed necrosis. Inhibition of this kinase has been shown to hinder cell necrotic death, thereby establishing RIP1 as a viable target for the potential treatment of multiple inflammatory diseases.

Z-VDVAD-FMK is a cell-permeable, irreversible inhibitor of caspase-2. Caspase inhibitors play an important role in investigating biological processes.

Salubrinal is a cell-permeable, selective inhibitor of cellular phosphatase complexes that dephosphorylate eukaryotic translation initiation factor 2 subunit α (eIF2α). Protects cells from endoplasmic reticulum stress-induced apoptosis (EC50 ~ 15 μM).

Z-DQMD-FMK is a synthetic peptide that irreversibly inhibits the activity of Caspase-3.

QNZ inhibits the activation of the transcription factor NF-κB and has been used to investigate NF-κB signaling.

GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM.

NQDI 1 is a selective inhibitor of apoptosis signal-regulating kinase 1 (ASK1, MAP3K5) (IC50 = 3 μM, Ki = 500 nM).

CASIN is a novel and potent Cdc42 inhibitor.

Embelin is a cell-permeable benzoquinone compound that exhibits antitumor properties.

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.

Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is a competitive heme oxygenase-1 (HO-1) inhibitor, markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2.

Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor.

GSK2656157 is an ATP-competitive inhibitor of PERK enzyme activity with an IC(50) of 0.9 nmol/L. It is highly selective for PERK with IC(50) values >100 nmol/L against a panel of 300 kinases.

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

AVN-944 (also known as VX-944) serves as an effective oral inhibitor, specifically targeting and inhibiting IMPDH (inosine monophosphate dehydrogenase). This enzyme plays a crucial role as a rate-limiting factor in the synthesis of guanine nucleotides from scratch. Additionally, AVN-944 acts against the synthesis of RNA in arenaviruses, effectively preventing arenavirus infections. Demonstrating a wide spectrum of anti-cancer properties, AVN-944 is utilized in research related to multiple myeloma (MM) and acute myeloid leukemia (AML).

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).