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Caspase

Isoform-selective Products

Caspase-1 Caspase-3 Caspase-8 Caspase-9 Caspase-4 Capase-7 Caspase-2 Caspase-5 Caspase-6 Caspase-10 Caspase-7

Signaling Pathway

Caspase Products

All (52)
Caspase Inhibitors (22)
Caspase Activators (24)
Caspase Agonist (1)
Caspase Modulators (3)
New Caspase Products

Catalog No.	Product Name	Information	Product Use Citations
S7023	Z-VAD-FMK	Z-VAD-FMK (Z-VAD(OMe)-FMK) is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.	Nature, 2024, 626(7998):411-418. Nature, 2024, 626(7998):411-418. Cell, 2024, 187(15):4061-4077.e17
S1029	Lenalidomide	Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.	Nat Commun, 2024, 15(1):9559 Nat Commun, 2024, 15(1):7388 J Immunother Cancer, 2024, 12(11)e009805
S2768	Dinaciclib	Dinaciclib is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.	Cell Death Dis, 2024, 15(4):285 Cell Death Dis, 2024, 15(5):345 Cell Death Dis, 2024, 15(4):285
S2228	Belnacasan (VX-765)	Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with K_i of 0.8 nM in a cell-free assay. Phase 2.	Journal of Environmental Sciences, 2025, Volume 148 Mol Cancer, 2024, 23(1):240 Nat Commun, 2024, 15(1):8266
S7312	Z-DEVD-FMK	Z-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.	Cell Rep Med, 2024, 5(3):101476 J Immunother Cancer, 2024, 12(10)e009032 Cancer Lett, 2024, 588:216797
S7311	Q-VD-Oph	Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection.	Nat Commun, 2024, 15(1):830 Cell Death Dis, 2024, 15(5):363 Cell Death Discov, 2024, 10(1):125
S7314	Z-IETD-FMK	Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK) is a specific Caspase-8 inhibitor. Z-IETD-FMK is also an inhibitor of granzyme B.	Nat Commun, 2024, 15(1):1282 J Immunother Cancer, 2024, 12(10)e009032 Mol Metab, 2024, 87:101988
S7775	Emricasan (IDN-6556)	Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.	Immunity, 2024, S1074-7613(24)00221-8 Acta Neuropathol, 2024, 147(1):56 Cell Death Differ, 2024, 31(7):938-953
S7901	Ac-DEVD-CHO	Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2.	Environ Pollut, 2024, 345:123467 Int J Mol Sci, 2024, 25(1)627 Cell, 2023, 186(14):3033-3048.e20
S7313	Z-LEHD-FMK TFA	Z-LEHD-FMK TFA (Caspase-9 Inhibitor) is a cell-permeable, competitive and irreversible inhibitor of enzyme caspase-9, which helps in cell survival.	Front Immunol, 2024, 15:1384606 Ecotoxicol Environ Saf, 2024, 284:116944 PLoS Pathog, 2024, 20(4):e1012146
S8102	Z-VAD(OH)-FMK (Caspase Inhibitor VI)	Z-VAD(OH)-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor.	Cell, 2024, 187(15):4043-4060.e30 Nat Commun, 2024, 15(1):9464 J Ethnopharmacol, 2024, 328:118057
S2891	GW441756	GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.	Cells, 2023, 12(3)373 Cells, 2023, 12(3):373 J Cell Mol Med, 2023, 10.1111/jcmm.17906
S2738	PAC-1	PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.	Nat Commun, 2023, 14(1):5773 Nat Commun, 2023, 14(1):5773 Microb Cell, 2023, 10(8):157-169
S8507	Z-YVAD-FMK	Z-YVAD-FMK is a cell-permeable and irreversible caspase-1 specific inhibitor with anti-inflammatory and anti-tumor activities.	Transl Psychiatry, 2024, 14(1):166 EMBO J, 2023, e113118. J Nanobiotechnology, 2023, 21(1):426
S2927	Apoptosis Activator 2	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.	BMC Mol Cell Biol, 2023, 24(1):14 BMC Mol Cell Biol, 2023, 24(1):14 Antioxidants (Basel), 2021, 10(2)184
S2417	20-Hydroxyecdysone	20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone, Crustecdysone) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods.20-Hydroxyecdysone (Ecdysterone, 20E) inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP.	bioRxiv, 2024, 10.1101/2024.01.04.574133 Appl Sci, 2023, 13(2), 860 Biomed Environ Sci, 2022, 35(6):504-517
S2448	Gambogic Acid	Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, 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.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Cancers (Basel), 2022, 14(22)5505
S9042	Wedelolactone	Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11.	Int J Ophthalmol, 2024, 17(4):616-624 PeerJ, 2022, 10:e13766 Exp Eye Res, 2021, 211:108750
S3275	Senkyunolide I	Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.	iScience, 2024, 27(7):110367 World J Emerg Med, 2024, 15(3):206-213 SSRN , 2024, 10.2139/ssrn.4696834
S5967	Berberine chloride hydrate	Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Biosci (Landmark Ed), 2022, 27(8):242 Front Pharmacol, 2021, 12:632201
S3865	Taurochenodeoxycholic acid	Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic.	Nat Commun, 2021, 12(1):6479 Microbiome, 2019, 7(1):145
S7326	Tasisulam	Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.	Skin Pharmacol Physiol, 2016, 29(6):281-290
S3238	Resibufogenin	Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.	Research Square, 2024, 10.21203/rs.3.rs-3790060/v1 Phytomedicine, 2022, 102:154182
S0563	10-Deacetyl-7-xylosyl paclitaxel	10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol, 7-xylosyl-10-deacetylpaclitaxel), a derivative of paclitaxel and naturally occurring xyloside isolated from Taxus chinensis, causes significant mitotic arrest in PC-3 cells followed by up-regulating expression of pro-apoptotic Bax and Bad protein, as well as down-regulating expression of anti-apoptotic Bcl-2 and Bcl-XL , which leads to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9.	Cell Death Dis, 2022, 13-9:799
S8487	AP20187	AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.	Front Immunol, 2022, 13:1110322
S9817	Ac-FLTD-CMK	Ac-FLTD-CMK is a specific inhibitor for inflammatory caspases. Ac-FLTD-CMK inhibits gasdermin D (GSDMD) cleavage by caspases-1, -4, -5, and -11 in vitro. Ac-FLTD-CMK is effective against caspases-1, caspases-4 and caspases-5 with IC50 of 46.7 nM, 1.49 μM and 329 nM, respectively.	Cell Death Discov, 2024, 10(1):416 Biomolecules, 2022, 12(11)1660
S9634	Phenoxodiol (Haginin E)	Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.	Anticancer Res, 2018, 38(10):5709-5716
E3037	Solanum lyratum Extract	Solanum lyratum Extract (300 μg/ml) increases Bax levels and decreases Bcl-2 levels, which cause the loss of mitochondrial membrane potential (Δæm) followed by cytochrome C release and caspase-9 and -3 activation, finally leading to apoptosis. Solanum lyratum Extract (300 μg/ml) also promotes p53 and p27, but decreases the levels of cyclin B1 thus causing S-phase arrest.
S6899	Licochalcone D	Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S0913	4',5,7-Trimethoxyflavone	4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.
S6501	NVP 231	NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.
S3224	Cinobufagin	Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
E3053	Mentha Arvensis Leaf Extract	Mentha Arvensis Leaf Extract is extracted from the leaf of Mentha Arvensis, which might be considered as a promising anticancer agent in breast cancer therapy in combination with synthesised GSNPs because they are less toxic and nonmutagenic and mediate caspase 9-dependent apoptosis.
E3835	Cordyceps Militaris Extract	Cordyceps Militaris Extract is extracted from Cordyceps militaris, which induces apoptosis and pyroptosis via caspase-3 and can be used as an anticancer agent.
S3267	Nicotiflorin (Kaempferol-3-O-rutinoside)	Nicotiflorin (Kaempferol-3-O-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
E2354	Valepotriate	Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABA_A, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.
S9276	Alisol B	Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
S2271	Berberine chloride	Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Adv Healthc Mater, 2023, e2300591. Transl Oncol, 2023, 35:101712 J Biomol Struct Dyn, 2022, 1-11
S0354	Alsterpaullone	Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
E3281	Eleutherine Plicata Extract	Eleutherine Plicata Extract is extracted from Eleutherine plicata, which is a promising medicinal plant, and its activity is associated with cytotoxicity by binding to caspase-8.
E3638	Lysinotus pauciflorus Extract	Lysinotus Pauciflorus Extract is extracted from Lysinotus Pauciflorus, which induces apoptosis of hepatocellular carcinoma cells via caspase-3 mediated mitochondrial pathway.
S6882	HI-TOPK-032	HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
S4513	RGD peptide (GRGDNP)	RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3.
S9075	Mulberroside A	Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
S3088	(±)-Methyl Jasmonate	(±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate), a phytohormone that acts as a vital cell regulator in plants, is a new candidate for the treatment of Inflammatory bowel diseases (IBDs), modulating the expression of the major classes of caspase-type protease families.
S9097	Alisol B Acetate	Alisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
S5550	Ethyl gallate	Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. Ethyl gallat activates the death receptor-dependent pathway of apoptosis by enhancing the expression of caspases-8, -9, and -3 and the Bcl-2 interacting domain (Bid).
S5579	Chelidonic acid	Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.
S6990	Phytohemagglutinin (PHA)	Phytohemagglutinin (PHA) is expressed in Pichia pastoris using native signal peptides, or the Saccharomyces alpha-factor preprosequence, to direct proteins into the secretory pathway. Phytohemagglutinin induces apoptosis in human HEp-2 carcinoma cells via increasing proapoptotic protein Bax and activating caspases-3.	Molecules, 2023, 28(6)2426
S4353	Terfenadine	Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
S5584	Citronellol	Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.
S6846	Gly-Phe β-naphthylamide	Gly-Phe β-naphthylamide (Gly-Phe beta-naphthylamide) is a substrate of cathepsin C that accumulates within the lysosome. Gly-Phe-β-naphthylamide can inhibit the cathepsin-dependent activation of caspase-8.	Anticancer Res, 2024, 44(9):3793-3798
S7023	Z-VAD-FMK	Z-VAD-FMK (Z-VAD(OMe)-FMK) is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.	Nature, 2024, 626(7998):411-418. Nature, 2024, 626(7998):411-418. Cell, 2024, 187(15):4061-4077.e17
S2228	Belnacasan (VX-765)	Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with K_i of 0.8 nM in a cell-free assay. Phase 2.	Journal of Environmental Sciences, 2025, Volume 148 Mol Cancer, 2024, 23(1):240 Nat Commun, 2024, 15(1):8266
S7312	Z-DEVD-FMK	Z-DEVD-FMK (Caspase-3 Inhibitor) is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.	Cell Rep Med, 2024, 5(3):101476 J Immunother Cancer, 2024, 12(10)e009032 Cancer Lett, 2024, 588:216797
S7311	Q-VD-Oph	Q-VD-Oph (Quinoline-Val-Asp-Difluorophenoxymethylketone) is a potent pan-caspase inhibitor with IC50 ranged from 25 to 400 nM for caspases 1,3,8, and 9. Q-VD-OPh can inhibits HIV infection.	Nat Commun, 2024, 15(1):830 Cell Death Dis, 2024, 15(5):363 Cell Death Discov, 2024, 10(1):125
S7314	Z-IETD-FMK	Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK) is a specific Caspase-8 inhibitor. Z-IETD-FMK is also an inhibitor of granzyme B.	Nat Commun, 2024, 15(1):1282 J Immunother Cancer, 2024, 12(10)e009032 Mol Metab, 2024, 87:101988
S7775	Emricasan (IDN-6556)	Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.	Immunity, 2024, S1074-7613(24)00221-8 Acta Neuropathol, 2024, 147(1):56 Cell Death Differ, 2024, 31(7):938-953
S7901	Ac-DEVD-CHO	Ac-DEVD-CHO (Caspase-3 Inhibitor I, N-Ac-Asp-Glu-Val-Asp-CHO) is a potent aldehyde inhibitor of Group II caspases with Ki values of 0.2 nM and 0.3 nM for for caspase-3 and caspase-7, respectively. Weak inhibition for caspase-2.	Environ Pollut, 2024, 345:123467 Int J Mol Sci, 2024, 25(1)627 Cell, 2023, 186(14):3033-3048.e20
S7313	Z-LEHD-FMK TFA	Z-LEHD-FMK TFA (Caspase-9 Inhibitor) is a cell-permeable, competitive and irreversible inhibitor of enzyme caspase-9, which helps in cell survival.	Front Immunol, 2024, 15:1384606 Ecotoxicol Environ Saf, 2024, 284:116944 PLoS Pathog, 2024, 20(4):e1012146
S8102	Z-VAD(OH)-FMK (Caspase Inhibitor VI)	Z-VAD(OH)-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor.	Cell, 2024, 187(15):4043-4060.e30 Nat Commun, 2024, 15(1):9464 J Ethnopharmacol, 2024, 328:118057
S8507	Z-YVAD-FMK	Z-YVAD-FMK is a cell-permeable and irreversible caspase-1 specific inhibitor with anti-inflammatory and anti-tumor activities.	Transl Psychiatry, 2024, 14(1):166 EMBO J, 2023, e113118. J Nanobiotechnology, 2023, 21(1):426
S2417	20-Hydroxyecdysone	20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone, Crustecdysone) is a naturally occurring ecdysteroid hormone which controls the ecdysis (moulting) and metamorphosis of arthropods.20-Hydroxyecdysone (Ecdysterone, 20E) inhibits caspase activity and induces autophagy via the 20E nuclear receptor complex, EcR-USP.	bioRxiv, 2024, 10.1101/2024.01.04.574133 Appl Sci, 2023, 13(2), 860 Biomed Environ Sci, 2022, 35(6):504-517
S9042	Wedelolactone	Wedelolactone, a medicinal plant-derived natural compound, is an inhibitor of IKK that is critical for activation of NF-κB by mediating phosphorylation and degradation of IκBα. Wedelolactone is also an inhibitor of caspase-11.	Int J Ophthalmol, 2024, 17(4):616-624 PeerJ, 2022, 10:e13766 Exp Eye Res, 2021, 211:108750
S3275	Senkyunolide I	Senkyunolide I (SEI, SENI) is an orally active compound isolated from Ligusticum chuanxiong with analgesic, anti-migraine, neuroprotective, anti-oxidation and anti-apoptosis activities. Senkyunolide I (SEI, SENI) up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. Senkyunolide I (SEI, SENI) promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.	iScience, 2024, 27(7):110367 World J Emerg Med, 2024, 15(3):206-213 SSRN , 2024, 10.2139/ssrn.4696834
S9817	Ac-FLTD-CMK	Ac-FLTD-CMK is a specific inhibitor for inflammatory caspases. Ac-FLTD-CMK inhibits gasdermin D (GSDMD) cleavage by caspases-1, -4, -5, and -11 in vitro. Ac-FLTD-CMK is effective against caspases-1, caspases-4 and caspases-5 with IC50 of 46.7 nM, 1.49 μM and 329 nM, respectively.	Cell Death Discov, 2024, 10(1):416 Biomolecules, 2022, 12(11)1660
E3053	Mentha Arvensis Leaf Extract	Mentha Arvensis Leaf Extract is extracted from the leaf of Mentha Arvensis, which might be considered as a promising anticancer agent in breast cancer therapy in combination with synthesised GSNPs because they are less toxic and nonmutagenic and mediate caspase 9-dependent apoptosis.
E3835	Cordyceps Militaris Extract	Cordyceps Militaris Extract is extracted from Cordyceps militaris, which induces apoptosis and pyroptosis via caspase-3 and can be used as an anticancer agent.
S3267	Nicotiflorin (Kaempferol-3-O-rutinoside)	Nicotiflorin (Kaempferol-3-O-rutinoside), a flavonoid extracted from Carthamus tinctorius, alters the shape and structure of injured neurons, decreases the number of apoptotic cells, down-regulates expression of p-JAK2, p-STAT3, caspase-3, and Bax and decreases Bax immunoredactivity, and increases Bcl-2 protein expression and immunoreactivity.
E2354	Valepotriate	Valepotriate, an unstable iridoid isolated from Valeriana jatamansi Jones, has anti-epileptic by significantly increasing the expression of GABA_A, glutamic acid decarboxylase 65, and Bcl-2 and reduce the expression of caspase-3.
S9075	Mulberroside A	Mulberroside A, isolated from the ethanol extract of Morus alba roots, is widely employed as an active ingredient in cosmetic products due to its anti-tyrosinase and anti-oxidant activities. Mulberroside A decreases the expressions of TNF-α, IL-1β and IL-6 and inhibits the activation of NALP3, caspase-1 and NF-κB and the phosphorylation of ERK, JNK and p38.
S5579	Chelidonic acid	Chelidonic acid (Jerva acid, Jervaic acid, γ-Pyrone-2,6-dicarboxylic acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. Chelidonic acid inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. Chelidonic acid is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.
S5584	Citronellol	Citronellol (Dihydrogeraniol, (±)-β-Citronellol), a constituent of rose and geranium oils, is used in perfumes and insect repellents. Citronellol can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. Citronellol also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.
S6846	Gly-Phe β-naphthylamide	Gly-Phe β-naphthylamide (Gly-Phe beta-naphthylamide) is a substrate of cathepsin C that accumulates within the lysosome. Gly-Phe-β-naphthylamide can inhibit the cathepsin-dependent activation of caspase-8.	Anticancer Res, 2024, 44(9):3793-3798
S1029	Lenalidomide	Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.	Nat Commun, 2024, 15(1):9559 Nat Commun, 2024, 15(1):7388 J Immunother Cancer, 2024, 12(11)e009805
S2768	Dinaciclib	Dinaciclib is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM in cell-free assays, respectively. It also blocks thymidine (dThd) DNA incorporation. Dinaciclib induces apoptosis through the activation of caspases 8 and 9. Phase 3.	Cell Death Dis, 2024, 15(4):285 Cell Death Dis, 2024, 15(5):345 Cell Death Dis, 2024, 15(4):285
S2891	GW441756	GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. GW441756 produces a relevant increase of caspase-3 that leads to apoptosis.	Cells, 2023, 12(3)373 Cells, 2023, 12(3):373 J Cell Mol Med, 2023, 10.1111/jcmm.17906
S2738	PAC-1	PAC-1 is a potent procaspase-3 activator with EC50 of 0.22 μM and the first small molecule known to directly activate procaspase-3 to caspase-3.	Nat Commun, 2023, 14(1):5773 Nat Commun, 2023, 14(1):5773 Microb Cell, 2023, 10(8):157-169
S2927	Apoptosis Activator 2	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.	BMC Mol Cell Biol, 2023, 24(1):14 BMC Mol Cell Biol, 2023, 24(1):14 Antioxidants (Basel), 2021, 10(2)184
S2448	Gambogic Acid	Gambogic Acid (Guttatic Acid, Guttic Acid, Beta-Guttiferrin) activates caspases with EC50 of 0.78-1.64 μM and competitively inhibits Bcl-X_L, 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.	Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247 Cancers (Basel), 2022, 14(22)5505
S5967	Berberine chloride hydrate	Berberine (Natural Yellow 18) chloride hydrate is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Front Biosci (Landmark Ed), 2022, 27(8):242 Front Pharmacol, 2021, 12:632201
S3865	Taurochenodeoxycholic acid	Taurochenodeoxycholic acid (Taurochenodeoxycholate, TCDCA, Chenodeoxycholyltaurine), a bile acid formed in the liver of most species, is used as a cholagogue and choleretic.	Nat Commun, 2021, 12(1):6479 Microbiome, 2019, 7(1):145
S7326	Tasisulam	Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.	Skin Pharmacol Physiol, 2016, 29(6):281-290
S3238	Resibufogenin	Resibufogenin (Bufogenin, Recibufogenin), a component of huachansu with anticancer effect, triggers necroptosis through upregulating receptor-interacting protein kinase 3 (RIP3) and phosphorylating mixed lineage kinase domain-like protein at Ser358. Resibufogenin exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. Resibufogenin induces apoptosis and caspase-3 and caspase-8 activity. Resibufogenin increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.	Research Square, 2024, 10.21203/rs.3.rs-3790060/v1 Phytomedicine, 2022, 102:154182
S0563	10-Deacetyl-7-xylosyl paclitaxel	10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol, 7-xylosyl-10-deacetylpaclitaxel), a derivative of paclitaxel and naturally occurring xyloside isolated from Taxus chinensis, causes significant mitotic arrest in PC-3 cells followed by up-regulating expression of pro-apoptotic Bax and Bad protein, as well as down-regulating expression of anti-apoptotic Bcl-2 and Bcl-XL , which leads to a disturbance of the mitochondrial membrane permeability and to the activation of caspase-9.	Cell Death Dis, 2022, 13-9:799
S9634	Phenoxodiol (Haginin E)	Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity that activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. Phenoxodiol also inhibits DNA topoisomerase II.	Anticancer Res, 2018, 38(10):5709-5716
E3037	Solanum lyratum Extract	Solanum lyratum Extract (300 μg/ml) increases Bax levels and decreases Bcl-2 levels, which cause the loss of mitochondrial membrane potential (Δæm) followed by cytochrome C release and caspase-9 and -3 activation, finally leading to apoptosis. Solanum lyratum Extract (300 μg/ml) also promotes p53 and p27, but decreases the levels of cyclin B1 thus causing S-phase arrest.
S6899	Licochalcone D	Licochalcone D (Lico D, LCD, LD), a flavonoid isolated from a Chinese medicinal plant Glycyrrhiza inflata, has antioxidant, anti-inflammatory and anti-cancer properties. Licochalcone D inhibit phosphorylation of NF-κB p65 in LPS signaling pathway. Licochalcone D inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. Licochalcone D also induces caspases activation and poly (ADP-ribose) polymerase (PARP) cleavage.
S0913	4',5,7-Trimethoxyflavone	4',5,7-Trimethoxyflavone (5,7,4'-Trimethoxyflavone, TMF) is a flavonoid isolated from Kaempferia parviflora (KP) that induces apoptosis. 4',5,7-Trimethoxyflavone increases sub-G1 phase, DNA fragmentation, annexin-V/PI staining and Bax/Bcl-xL ratio, activates caspase-3 and degrades poly (ADP-ribose) polymerase (PARP) protein.
S6501	NVP 231	NVP 231 is a novel CerK inhibitor that inhibits the catalytic activity of recombinant CerK in vitro with an IC50 of 12 nM. NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.
S9276	Alisol B	Alisol B, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
S2271	Berberine chloride	Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. Berberine activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. Berberine chloride decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. Berberine chloride induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. Berberine chloride is a dual topoisomerase I and II inhibitor. Berberine chloride is also a potential autophagy modulator.	Adv Healthc Mater, 2023, e2300591. Transl Oncol, 2023, 35:101712 J Biomol Struct Dyn, 2022, 1-11
S0354	Alsterpaullone	Alsterpaullone (Alp, 9-Nitropaullone, NSC 705701) is a potent inhibitor of CDK with IC50 of 35 nM, 15 nM, 200 nM and 40 nM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E and CDK5/p35, respectively. Alsterpaullone also acts as a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 of both 4 nM for GSK-3α and GSK-3β. Alsterpaullone induces apoptosis by activation of caspase-9. Alsterpaullone has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.
S4513	RGD peptide (GRGDNP)	RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. RGD peptide (GRGDNP) induces apoptosis presumably through direct activation of caspase-3.
S9097	Alisol B Acetate	Alisol B acetate, a triterpene from Alismatis rhizoma, induces Bax up-regulation and nuclear translocation, the activation of initiator caspase-8 and caspase-9, and executor caspase-3, suggesting the involvement of both extrinsic and intrinsic apoptosis pathways.
S5550	Ethyl gallate	Ethyl gallat (Phyllemblin, gallic acid ethyl ester), which could be found naturally in a variety of plant sources, is a food additive with antimicrobial activity. Ethyl gallat activates the death receptor-dependent pathway of apoptosis by enhancing the expression of caspases-8, -9, and -3 and the Bcl-2 interacting domain (Bid).
S6990	Phytohemagglutinin (PHA)	Phytohemagglutinin (PHA) is expressed in Pichia pastoris using native signal peptides, or the Saccharomyces alpha-factor preprosequence, to direct proteins into the secretory pathway. Phytohemagglutinin induces apoptosis in human HEp-2 carcinoma cells via increasing proapoptotic protein Bax and activating caspases-3.	Molecules, 2023, 28(6)2426
S4353	Terfenadine	Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
E3638	Lysinotus pauciflorus Extract	Lysinotus Pauciflorus Extract is extracted from Lysinotus Pauciflorus, which induces apoptosis of hepatocellular carcinoma cells via caspase-3 mediated mitochondrial pathway.
S3224	Cinobufagin	Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.
S6882	HI-TOPK-032	HI-TOPK-032 is a potent and specific inhibitor of TOPK. HI-TOPK-032 also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
S3088	(±)-Methyl Jasmonate	(±)-Methyl Jasmonate (MeJA, Methyl jasmonate, Methyl 2-(3-oxo-2-(pent-2-en-1-yl)cyclopentyl)acetate), a phytohormone that acts as a vital cell regulator in plants, is a new candidate for the treatment of Inflammatory bowel diseases (IBDs), modulating the expression of the major classes of caspase-type protease families.

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