Z-VAD-FMK (Caspase Inhibitor VI) is a broad-spectrum inhibitor of caspases.Z-VAD-FMK binds to activated caspases and inhibits apoptosis.Z-VAD-FMK does not inhibit UCHL1 activity, even at concentrations up to 440 μM.

Birinapant (TL32711) is a synthetic small molecule that is both a peptidomimetic of second mitochondrial-derived activator of caspases (SMAC) and inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins, with potential antineoplastic activity.

Calycosin (Cyclosin) acts as a selective estrogen receptor modulator. Calycosin induces apoptosis in human ovarian cancer SKOV3 cells by activating caspases and Bcl-2 family proteins. Calycosin suppresses breast cancer cell growth via ERβ-dependent regulation of IGF-1R, p38 MAPK and PI3K/Akt pathways. Calycosin has antineoplastic effects against osteosarcoma through inducing apoptosis showing in vitro and in vivo investigations. Calycosin was shown to induce angiogenesis in human umbilical vein endothelial cell cultures (HUVEC) in vitro. Calycosin may be an effective skin-lightening agent that regulates the expression of melanogenic enzymes. Calycosin exhibited tyrosinase inhibitory activity with an IC(50) value of 38.4 microM.

Dehydrocavidine (Dehydrocorydaline) has antitumor activity, it inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

(R)-CR8 ((R)-Isomer) is a potent and selective CDK inhibitor.

Ac-AAVALLPAVLLALLAP-LEHD-CHO is a caspase inhibitor targeting caspases 4, 5, and 9, demonstrating protective effects in MCF-7 cells treated with Neocarzinostatin [1].

CAY10406 is a trifluoromethyl analog of an isatin sulfonamide compound that selectively inhibits caspases 3 and 7. The non-trifluoromethyl compound exhibits Ki values of 1.2 nM and 6 nM for caspases 3 and 7, respectively. For all of the other caspases tested, it is 100 to 1,000 times less potent. Caspases 3 and 7 are 'effector caspases' that are downstream from the initiating steps of apoptosis, and are implicated in the main proteolytic processing of the apoptotic signal. No data is currently available for caspase inhibition by CAY10406.

Asukamycin is polyketide isolated from the S. nodosus subspecies asukaensis that demonstrates a broad range of antibiotic functions. It has been shown to inhibit growth of various tumor cell lines by activating caspases 8 and 3.

VRT-043198, the drug metabolite of VX-765 (Belnacasan), is a potent, selective, and blood-brain barrier permeable inhibitor of the interleukin-converting enzyme/caspase-1 subfamily caspases, displaying Ki values of 0.8 nM for ICE/caspase-1 and 0.6 nM for caspase-4, respectively.

Kea1-97 is a selective disruptor of interaction between thioredoxin and caspase-3 (IC50 = 10 μ M). Kea1-97 destroys the interaction between thioredoxin and caspase 3 and activates caspases without affecting the activity of thioredoxin.

Z-AEVD-FMK is an irreversible inhibitor of caspase-10 and related caspases.[1] At 10 µM, it can prevent the initiation of Fas signaling by caspase-10 in Jurkat T lymphoma cells, preventing Bid cleavage into its active form, caspase cascade activation, and apoptosis.[2]

GRI977143 is a selective and non-lipid agonist of LPA2 (EC50 = 3.3 μM). GRI977143 inhibits the activation of caspases 3, 7, 8, and 9 and and reduces DNA fragmentation.

Anticancer agent 137 (8q), a potent PI3k inhibitor, exhibits broad-spectrum anticancer activity by inducing G2/M cell cycle arrest and apoptosis. It increases levels of cleaved PARP, and caspases 3 and 7, making it useful in cancer research [1].

Clerosterol exerts its cytotoxic effect in A2058 human melanoma cells by caspases-dependent apoptosis.

Gambogic Acid (Guttic Acid) ( EC50=0.78-1.64 uM) activates caspases. Gambogic Acid competitively suppresses Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1. The IC50s of Gambogic Acid for Bcl-XL, Bcl-2, Bcl-W, Bcl-B, Bfl-1 and Mcl-1 are 1.47, 1.21, 2.02, 0.66, 1.06 and 0.79 uM, respectively.

Uncarinic acid E has anti-cancer activity, it induces apoptosis in HepG2 cells via accumulation of p53, alters the Bax/Bcl-2 ratio, and activates caspases, resulting in cytochrome c release from the mitochondria. A mixture of uncarinic acid E and 27-O-p-(

SW IV-52 is an XIAP-inhibitor that acts as a second mitochondria-derived activator of caspases (SMAC) mimetic.

CMLD-2 is an inhibitor of HuR-ARE interaction (Ki: 350 nM) that competitively binds HuR protein and disrupts its interaction with adenine element-rich (ARE) mRNA targets.CMLD-2 induces apoptosis and exhibits antitumor effects through MAD2 downregulation. CMLD-2 (1-75 μM ; 24-72 h) had an inhibitory effect on the viability of thyroid cancer cells.CMLD-2 (20-30 μM ; 24-48 h) activated caspases and induced apoptosis in H1299 and A549 cells.CMLD-2 (30 μM ; 24-48 h) induced G1 cell cycle arrest in H1299 and A549 cells and mitochondrial perturbation. CMLD-2 (30 μM ; 24-48 h) reduced the expression of HuR and HuR-regulated mRNAs and proteins in H1299 cells.CMLD-2 (35 μM ; 72 h) decreased the directional migration ability of SW1736, 8505C, BCPAP and K1 cells.CMLD-2 induced the migration of SW1736, 8505C, BCPAP and K1 cells with a strong decrease in MAD2 mRNA levels.

Boc-Glu-OBzl is an amino acid building block.1,2It has been used in the synthesis of peptide-based inhibitors of human caspases and human rhinovirus (HRV) 3C protease that have enzyme inhibitory activityin vitro. 1.Garcia-Calvo, M., Peterson, E.P., Leiting, B., et al.Inhibition of human caspases by peptide-based and macromolecular inhibitorsJ. Biol. Chem.273(49)32608-32613(1998) 2.Dragovich, P.S., Webber, S.E., Babine, R.E., et al.Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 2. peptide structure-activity studiesJ. Med. Chem.41(15)2819-2934(1998)

Fenbufen (Lederfen) is a non-steroidal anti-inflammatory drug used primarily to treat inflammation in osteoarthritis, ankylosing spondylitis, and tendinitis. It can also be used to relieve backaches, sprains, and fractures. Fenbufen is available as a capsule or tablet sold with the brand names Cepal, Cinopal, Cybufen, Lederfen, and Reugast. Fenbufen acts by preventing cyclooxygenase from producing prostaglandins which can cause inflammation.

Alpinetin ((-)-alpinetin) has antibacterial activity.Alpinetin has anti-inflammatory activity.Alpinetin can enhance the sensitivity of HepG2 hepatoma cells to the chemotherapeutic agent CDDP. Alpinetin has strong anti-hepatoma and pancreatic cancer cells effects, by inhibiting proliferation , regulating of the Bcl-2 family and XIAP expression, releasing of cytochrome c and activating caspases.

Ac-FLTD-CMK is an inhibitor derived from abscisicin D (GSDMDD) with specific inhibitory effects on inflammatory caspases. ac-FLTD-CMK showed inhibitory effects on caspases-1, caspases-4 and caspases-11 with IC50s of 46.7 nM, 1.49 μM and 329 nM, respectively. Ac-FLTD-CMK showed potency against caspases-1, caspases-4 and caspases-11, but not against apoptosis-associated caspase-3.

Anticancer agent 56 (compound 4d) is a powerful anti-cancer compound with favorable drug-like properties. It shows significant anticancer activity against multiple cancer cell lines, with an IC50 value of less than 3 μM. Anticancer agent 56 exerts its effects by causing cell cycle arrest at the G2/M phase and activating the mitochondrial apoptosis pathway. Mechanistically, it induces the accumulation of reactive oxygen species (ROS), upregulates BAX, downregulates Bcl-2, and triggers the activation of caspases 3, 7, and 9 [1].

Ivachtin (Caspase-3 Inhibitor VII) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor(IC50 = 23 nM) and is a modest inhibitor of the remaining caspases.

Guggulsterone (Guggulsterone E&Z) E&Z is a 3-hydroxy steroid. It has a role as an androgen.

Biotin-VAD-FMK is a cell-permeable, irreversible biotin-labeled inhibitor of caspase. It is used to identify active caspases in cell lysates.

Beta-Sitosterol (SKF 14463) has recently been shown to induce G2/M arrest, endoreduplication, and apoptosis through the Bcl-2 and PI3K/Akt signaling pathways. Beta-Sitosterol (SKF 14463) , a main dietary phytosterol found in plants, may have the potential for prevention and therapy for human cancer. Although the exact mechanism of action of Beta-Sitosterol (SKF 14463) is unknown, it may be related to cholesterol metabolism or anti-inflammatory effects (via interference with prostaglandin metabolism). Beta-Sitosterol (SKF 14463) induces apoptosis and activates key caspases in MDA-MB-231 human breast cancer cells.

AEG40826 (HGS1029) is the hydrochloride salt of a small-molecule inhibitor of IAP (Inhibitor of Apoptosis Protein) family proteins with potential antineoplastic activity. IAP inhibitor HGS1029 selectively inhibits the biological activity of IAP proteins, which may restore apoptotic signaling pathways; this agent may work synergistically with cytotoxic drugs to overcome tumor cell resistance to apoptosis. IAPs are overexpressed by many cancer cell types, suppressing apoptosis by binding and inhibiting active caspases-3, -7 and -9 via their BIR (baculoviral lAP repeat) domains.

15-Acetoxyscirpenol, a member of the acetoxyscirpenol moiety mycotoxins (ASMs), potently induces apoptosis and inhibits the growth of Jurkat T cells in a dose-dependent manner. This effect is mediated through the activation of caspases independent of caspase-3[1].

XK489 is a synthetic quinoxaline phenoxypropionic acid derivative with proapoptotic and antiproliferative activities. R(+)XK469 selectively inhibits topoisomerase II-beta, blocks activation of MEK/MAPK signaling kinases, stimulates caspases, and upregulates p53-dependent proteins, including cyclins A and B1, thereby arresting cancer cells in the G2/M phase of the cell cycle. Both R(+) and S(-) isomers of this agent are cytotoxic, although the R-isomer is more potent.

TP-110 is a new proteasome inhibitor, which shows potent growth inhibition in various tumor cell lines. Treatment with TP-110 for 24 h in vitro induced apoptosis in multiple myeloma cell line RPMI8226. TP-110 reduced the intrinsic inhibitor of apoptosis proteins (IAPs), cIAP-1 and XIAP, that suppress executioner caspases.

Polyphyllin II (Chonglou Saponin II) has hemostasis, expectorant, bacteriostasis, anticytotoxic, anti-pregnancy kill sperm effects.

UNBS-1450 is a sodium channel antagonist. UNBS-1450 is a hemi-synthetic cardenolide derived from 2″-oxovorusharin, it is effective against various cancer cell types with an excellent differential toxicity. At low nanomolar concentrations, UNBS-1450 induce

1. Dehydrocorydaline (13-Methylpalmatine) exerts anti-metastatic potential via suppression of MMPs and Bcl-2 signaling in NSC-LC cells. 2. Dehydrocorydaline stimulates p38 MAPK activation, which can enhance heterodimerization of MyoD and E proteins, thus resulting in MyoD activation and myoblast differentiation. 3. Dehydrocorydaline shows antiplatelet effects, it inhibits thrombin-induced platelet aggregation in a low dose ( IC50= 34.914 ug/mL). 4. Dehydrocorydaline has anti-inflammatory and antinociceptive effects. 5. Dehydrocorydaline inhibits MCF-7 cell proliferation by inducing apoptosis mediated by regulating Bax/Bcl-2, activating caspases as well as cleaving PARP.

AC-VEID-CHO (TFA) is a peptide-derived inhibitor targeting Caspases-6, -3, and -7, exhibiting IC50 values of 16.2 nM, 13.6 nM, and 162.1 nM, respectively. This compound demonstrates significant inhibitory potency and is applicable in the study of neurodegenerative diseases, such as Alzheimer’s and Huntington’s disease [1].

Verrucarin A (Muconomycin A) is a Type D macrocyclic mycotoxin. Verrucarin A (VA), a protein synthesis inhibitor, derived from the pathogen fungus Myrothecium verrucaria, inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53 [1] [2].

GW779439X is an inhibitor of CDK.

Z-FA-FMK can irreversibly inhibit cysteine protease and also inhibit effector caspases.

Phytohemagglutinin (PHA-M) is a lectin, isolated from the red kidney bean , induces apoptosis via increasing proapoptotic protein Bax and activating caspases-3. Anti-tumor activity

(S)-CR8 is an effective second-generation cyclin-dependent kinase inhibitor.

(R)-CR8 trihydrochloride (CR8, (R)-Isomer trihydrochloride) is a CDK1/2/5/7/9 inhibitor that acts as a molecular glue degrader with neuroprotective activity and induces apoptosis.