Caspase Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
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.	Nat Commun, 2025, 16(1):918 J Transl Med, 2025, 23(1):986 PLoS Pathog, 2025, 21(9):e1013491
S8102	Z-VAD(OH)-FMK	Z-VAD(OH)-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor.	Nat Commun, 2025, 16(1):480 Cell, 2024, 187(15):4043-4060.e30 Nat Commun, 2024, 15(1):9464
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.	PLoS Pathog, 2025, 21(8):e1013415 mSphere, 2025, e0011025. Nat Commun, 2023, 14(1):5773
S8507	Z-YVAD-FMK	Z-YVAD-FMK is a cell-permeable and irreversible caspase-1 specific inhibitor with anti-inflammatory and anti-tumor activities.	PLoS Pathog, 2025, 21(1):e1012915 Cancer Rep (Hoboken), 2025, 8(4):e70202 Transl Psychiatry, 2024, 14(1):166
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 Antioxidants (Basel), 2021, 10(2)184 J Agric Food Chem, 2021, 69(13):3942-3951
E5825	Z-VAD	Z-VAD is a competitive, irreversible pan-caspase inhibitor with broad specificity and weakly inhibits caspase-2. It induces autophagy and necrosis in irradiated breast and lung cancer models.	Cell Mol Immunol, 2025, 22(5):541-556 Cell Death Dis, 2025, 16(1):396 Sci Rep, 2025, 15(1):19413
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
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.	Acta Pharmacol Sin, 2025, 10.1038/s41401-025-01507-9 Anticancer Res, 2024, 44(9):3793-3798
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
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).	Front Pharmacol, 2024, 15:1403424
S9634	Phenoxodiol (Haginin E)	Phenoxodiol (Haginin E, Idronoxil, Dehydroequol, NV 06, PXD) is an isoflavone analog with antineoplastic activity. It activates the caspase system, inhibits XIAP (X-linked inhibitor of apoptosis), and disrupts FLICE inhibitory protein (FLIP) expression, resulting in tumor cell apoptosis. This compound also inhibits DNA topoisomerase II.	Anticancer Res, 2018, 38(10):5709-5716
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. This compound induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage.
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.
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.
E6477^New	Taurolithocholic acid	Taurolithocholic acid is a taurine-conjugated tertiary bile acid. It induces apoptosis in hepatoma cell lines via caspase-3/7 activation and serves as a model to study the endocrine and metabolic roles of bile acids in enterohepatic circulation and liver physiology.
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.
E7500	BOC-D-FMK	BOC-D-FMK is a broad-spectrum inhibitor of caspase. It inhibited TNFα-stimulated apoptosis in neutrophils with an IC50 values of 39 μM.
S2891	GW441756	GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. This compound produces a relevant increase of caspase-3 that leads to apoptosis.	Cell Res, 2025, 10.1038/s41422-025-01098-4 Neurochem Int, 2025, 191:106072 Cells, 2023, 12(3)373
S2271	Berberine chloride	Berberine chloride is a quaternary ammonium salt from the group of isoquinoline alkaloids. This compound activates caspase 3 and caspase 8, cleavage of poly ADP-ribose polymerase (PARP) and the release of cytochrome c. It decreases the expression of c-IAP1, Bcl-2 and Bcl-XL. This chemical induces apoptosis with sustained phosphorylation of JNK and p38 MAPK, as well as generation of the ROS. It is a dual topoisomerase I and II inhibitor. It is also a potential autophagy modulator.	J Cardiovasc Dev Dis, 2025, 12(7)278 Adv Healthc Mater, 2023, e2300591. Transl Oncol, 2023, 35:101712
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. This compound up-regulates the phosphorylation of Erk1/2 and induces Nrf2 nuclear translocation with enhanced HO-1 and NQO1 expressions. It also promotes the ratio of Bcl-2/Bax and inhibits the expressions of cleaved caspase 3 and caspase 9.	Blood Sci, 2025, 7(3):e00246 iScience, 2024, 27(7):110367 World J Emerg Med, 2024, 15(3):206-213
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.	Theranostics, 2025, 15(11):5420-5439 Cells, 2023, 12(18)2247 Cells, 2023, 10.3390/cells12182247
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. This compound exerts cytotoxic effect by inducing reactive oxygen species (ROS) accumulation. It induces apoptosis and caspase-3 and caspase-8 activity. This chemical increases Bax/Bcl-2 expression, and suppresses cyclin D1, cyclin E, PI3K, p-AKT, p-GSK3β and β-catenin protein expression.	bioRxiv, 2025, 2025.07.17.665404 Research Square, 2024, 10.21203/rs.3.rs-3790060/v1 Phytomedicine, 2022, 102:154182
S9817	Ac-FLTD-CMK	Ac-FLTD-CMK is a specific inhibitor for inflammatory caspases. This compound inhibits gasdermin D (GSDMD) cleavage by caspases-1, -4, -5, and -11 in vitro. It is effective against caspases-1, caspases-4 and caspases-5 with IC50 of 46.7 nM, 1.49 μM and 329 nM, respectively.	World J Gastroenterol, 2025, 31(36):111557 Cell Death Discov, 2024, 10(1):416 Biomolecules, 2022, 12(11)1660
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
S6990	Phytohemagglutinin (PHA)	A potent mitogen from red kidney beans (Phaseolus vulgaris), phytohemagglutinin (PHA) stimulates lymphocyte proliferation and transforms them into large blast cells. It can suppress humoral antibody responses and enhance the survival of homografts by inhibiting immune rejection. It also triggers T-cell activation and apoptosis by upregulating pro-apoptotic proteins like Bax, leading to the activation of caspase-3.	Transl Cancer Res, 2025, 14(1):78-92 Molecules, 2023, 28(6)2426
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. This compound 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. It induces apoptosis by activation of caspase-9. This chemical has antitumor activity and possesses potential for the treatment of neurodegenerative and proliferative disorders.	Cell Mol Life Sci, 2025, 82(1):311
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
S4513	RGD peptide (GRGDNP)	RGD peptide (GRGDNP) is an inhibitor of binding of integrins to the extracellular matrixs. This compound induces apoptosis presumably through direct activation of caspase-3.	Tradit Med Res, 2023, 8(9):50
S8487	AP20187 (B/B Homodimerizer)	AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.	Front Immunol, 2022, 13:1110322
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. This compound 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. This compound inhibits phosphorylation of NF-κB p65 in LPS signaling pathway. It inhibits JAK2, EGFR and Met (c-Met) activities and induces ROS-dependent apoptosis. This chemical 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. This compound 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.
S3224	Cinobufagin	Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. This compound increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. It inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, this chemical induces cell cycle arrest at the G2/M phase and apoptosis.
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.
S6882	HI-TOPK-032	HI-TOPK-032 is a potent and specific inhibitor of TOPK. This compound also reduces ERK-RSK phosphorylation, regulates of the abundance of p53, cleaved caspase-7, and cleaved PARP, and induces apoptosis in cancer cells.
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. This compound 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-dicarboxyl acid) is a secondary metabolite found in several plants with therapeutic potential in allergic disorders in experimental animals. This compound inhibits IL-6 production by blocking NF-κB and caspase-1 in HMC-1 cells. It is also an inhibitor of glutamate decarboxylase with Ki of 1.2 μM.
S4353	Terfenadine	Terfenadine is an antihistamine, generally completely metabolizes to the active form fexofenadine in the liver by the enzyme cytochrome P450 CYP3A4 isoform. This compound is a potent open-channel blocker of hERG with an IC50 of 204 nM. This chemical, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. It 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. This compound can cause necrotic apoptosis of NCI-H1299 cells by up-regulating TNF-α, RIP1 / RIP3 activities, and down-regulating caspase-3 / caspase-8 activities. It also results in a biphasic increase in ROS production at 1 h and at 12 h in NCI-H1299 cells.