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Catalog No. Product Name Information Product Use Citations Product Validations
S2228 Belnacasan (VX-765) Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2.
Sci Transl Med, 2021, 13(604)eabb1069
Cell Rep, 2021, 34(10):108756
Elife, 2021, 10e70938
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.
Arch Insect Biochem Physiol, 2021, e21824
PLoS Genet, 2021, 17(2):e1009352
PLoS Biol, 2019, 17(10):e3000145
S3267 Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-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.
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.
Cell Commun Signal, 2021, 19(1):115
S4513New 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.
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.
S5967New 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 Pharmacol, 2021, 12:632201
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.
J Cell Sci, 2022, 135(5)jcs259220
Nat Immunol, 2021, 22(9):1107-1117
Nat Cell Biol, 2021, 23(7):796-807
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.
Science, 2021, 371(6535)eabc5386
Sci Transl Med, 2021, 13(604)eabb1069
Dev Cell, 2021, 56(15):2207-2222.e7
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.
Sci Transl Med, 2021, 13(604)eabb1069
J Inflamm Res, 2021, 14:3969-3983
Int J Biol Sci, 2021, 17(2):589-602
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.
Sci Adv, 2021, 7(25)eabf8577
Acta Pharm Sin B, 2021, 11(6):1513-1525
Int J Biol Sci, 2021, 17(2):589-602
S7314 Z-IETD-FMK Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK) is a specific Caspase-8 inhibitor.
Sci Transl Med, 2021, 13(604)eabb1069
Adv Sci (Weinh), 2021, e2102666
Nat Commun, 2021, 12(1):476
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.
Sci Transl Med, 2021, 13(604)eabb1069
Mol Cell, 2021, S1097-2765(21)00458-5
Nat Commun, 2021, 12(1):3526
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.
Sci Transl Med, 2021, 13(604)eabb1069
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
Adv Healthc Mater, 2021, e2101926
S8102 Z-VAD(OH)-FMK (Caspase Inhibitor VI) Z-VAD(OH)-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor.
EMBO Rep, 2021, 22(2):e51162
Int J Biol Sci, 2021, 17(2):589-602
Cell Death Dis, 2021, 12(2):140
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 Oncol, 2021, 14(1):100982
Biomed Pharmacother, 2020, 127:110151
Biol Pharm Bull, 2020, 43(10):1481-1489
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.
Exp Eye Res, 2021, 211:108750
Int Immunopharmacol, 2019, 73:17-22
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.
S9817New 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.
A5013 Caspase-3 Rabbit Recombinant mAb Caspase-3 Rabbit Recombinant mAb detects endogenous levels of total Caspase-3
Int J Pharm, 2021, 608:121066
A5074 cleaved Caspase-9 Rabbit Recombinant mAb cleaved Caspase-9 Rabbit Recombinant mAb detects endogenous level of cleaved Caspase-9.
Arch Biochem Biophys, 2021, 700:108774
Andrology, 2021, 10.1111/andr.13119
A5079 Caspase-2 Rabbit Recombinant mAb Caspase-2 Rabbit Recombinant mAb detects endogenous level of caspase-2.
A5186 Caspase-8 Rabbit Recombinant mAb Caspase-8 Rabbit Recombinant mAb detects endogenous level of total Caspase-8.
A5259 APAF1 Rabbit Recombinant mAb APAF1 Rabbit Recombinant mAb detects endogenous level of total APAF1.
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.
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.
S1029 Lenalidomide (CC-5013) Lenalidomide (CC-5013) 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.
Adv Sci (Weinh), 2021, e2004846
Sci Adv, 2021, 7(6)eabd6263
Sci Adv, 2021, 7(23)eabg2697
S2271 Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) 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 Pharmacol, 2021, 12:632201
Molecules, 2021, 26(5)1210
Biology (Basel), 2021, 10(3)250
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-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.
Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0775
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.
Nature, 2021, 10.1038/s41586-021-03785-9
J Hazard Mater, 2020, 18;396:122605
Cell Death Dis, 2020, 11(6):482
S2768 Dinaciclib (SCH727965) Dinaciclib (SCH727965, PS-095760) 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, 2021, 184(25):6119-6137.e26
Gut, 2021, 70(5):890-899
Sci Adv, 2021, 7(7)eabd2645
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.
Biosci Biotechnol Biochem, 2021, 85(3):675-686
Cancer Res, 2020, canres.1992.2020
Mol Neurobiol, 2020, 10.1007/s12035-020-02156-1
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.
Aging (Albany NY), 2021, 13(5):7096-7119
J Agric Food Chem, 2021, 69(13):3942-3951
Antioxidants (Basel), 2021, 10(2)184
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.
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
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.
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).
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.
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.
S6990 Phytohemagglutinin

Phytohemagglutinin (PHA, Phaseolus vulgaris agglutinin) 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.

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
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.
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.
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
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.

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.
S8487New AP20187 AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.
S2228 Belnacasan (VX-765) Belnacasan (VX-765) is a potent and selective inhibitor of caspase-1 with Ki of 0.8 nM in a cell-free assay. Phase 2.
Sci Transl Med, 2021, 13(604)eabb1069
Cell Rep, 2021, 34(10):108756
Elife, 2021, 10e70938
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.
Arch Insect Biochem Physiol, 2021, e21824
PLoS Genet, 2021, 17(2):e1009352
PLoS Biol, 2019, 17(10):e3000145
S3267 Kaempferol-3-O-rutinoside Kaempferol-3-O-rutinoside (Nicotiflorin, Nikotoflorin, Kaempferol 3-O-β-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.
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.
Cell Commun Signal, 2021, 19(1):115
S4513New 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.
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.
S5967New 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 Pharmacol, 2021, 12:632201
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.
J Cell Sci, 2022, 135(5)jcs259220
Nat Immunol, 2021, 22(9):1107-1117
Nat Cell Biol, 2021, 23(7):796-807
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.
Science, 2021, 371(6535)eabc5386
Sci Transl Med, 2021, 13(604)eabb1069
Dev Cell, 2021, 56(15):2207-2222.e7
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.
Sci Transl Med, 2021, 13(604)eabb1069
J Inflamm Res, 2021, 14:3969-3983
Int J Biol Sci, 2021, 17(2):589-602
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.
Sci Adv, 2021, 7(25)eabf8577
Acta Pharm Sin B, 2021, 11(6):1513-1525
Int J Biol Sci, 2021, 17(2):589-602
S7314 Z-IETD-FMK Z-IETD-FMK (Caspase-8 Inhibitor, Z-IE(OMe)TD(OMe)-FMK) is a specific Caspase-8 inhibitor.
Sci Transl Med, 2021, 13(604)eabb1069
Adv Sci (Weinh), 2021, e2102666
Nat Commun, 2021, 12(1):476
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.
Sci Transl Med, 2021, 13(604)eabb1069
Mol Cell, 2021, S1097-2765(21)00458-5
Nat Commun, 2021, 12(1):3526
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.
Sci Transl Med, 2021, 13(604)eabb1069
CHEM ENG J, 2021, 10.1016/j.cej.2021.130083
Adv Healthc Mater, 2021, e2101926
S8102 Z-VAD(OH)-FMK (Caspase Inhibitor VI) Z-VAD(OH)-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor.
EMBO Rep, 2021, 22(2):e51162
Int J Biol Sci, 2021, 17(2):589-602
Cell Death Dis, 2021, 12(2):140
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 Oncol, 2021, 14(1):100982
Biomed Pharmacother, 2020, 127:110151
Biol Pharm Bull, 2020, 43(10):1481-1489
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.
Exp Eye Res, 2021, 211:108750
Int Immunopharmacol, 2019, 73:17-22
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.
S9817New 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.
A5013 Caspase-3 Rabbit Recombinant mAb Caspase-3 Rabbit Recombinant mAb detects endogenous levels of total Caspase-3
Int J Pharm, 2021, 608:121066
A5074 cleaved Caspase-9 Rabbit Recombinant mAb cleaved Caspase-9 Rabbit Recombinant mAb detects endogenous level of cleaved Caspase-9.
Arch Biochem Biophys, 2021, 700:108774
Andrology, 2021, 10.1111/andr.13119
A5079 Caspase-2 Rabbit Recombinant mAb Caspase-2 Rabbit Recombinant mAb detects endogenous level of caspase-2.
A5186 Caspase-8 Rabbit Recombinant mAb Caspase-8 Rabbit Recombinant mAb detects endogenous level of total Caspase-8.
A5259 APAF1 Rabbit Recombinant mAb APAF1 Rabbit Recombinant mAb detects endogenous level of total APAF1.
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.
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.
S1029 Lenalidomide (CC-5013) Lenalidomide (CC-5013) 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.
Adv Sci (Weinh), 2021, e2004846
Sci Adv, 2021, 7(6)eabd6263
Sci Adv, 2021, 7(23)eabg2697
S2271 Berberine chloride (NSC 646666) Berberine chloride (NSC 646666, Natural Yellow 18) 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 Pharmacol, 2021, 12:632201
Molecules, 2021, 26(5)1210
Biology (Basel), 2021, 10(3)250
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-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.
Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-0775
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.
Nature, 2021, 10.1038/s41586-021-03785-9
J Hazard Mater, 2020, 18;396:122605
Cell Death Dis, 2020, 11(6):482
S2768 Dinaciclib (SCH727965) Dinaciclib (SCH727965, PS-095760) 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, 2021, 184(25):6119-6137.e26
Gut, 2021, 70(5):890-899
Sci Adv, 2021, 7(7)eabd2645
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.
Biosci Biotechnol Biochem, 2021, 85(3):675-686
Cancer Res, 2020, canres.1992.2020
Mol Neurobiol, 2020, 10.1007/s12035-020-02156-1
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.
Aging (Albany NY), 2021, 13(5):7096-7119
J Agric Food Chem, 2021, 69(13):3942-3951
Antioxidants (Basel), 2021, 10(2)184
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.
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
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.
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).
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.
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.
S6990 Phytohemagglutinin

Phytohemagglutinin (PHA, Phaseolus vulgaris agglutinin) 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.

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
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.
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.
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
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.

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.
S4513New 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.
S5967New 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 Pharmacol, 2021, 12:632201
S9817New 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.
S8487New AP20187 AP20187 (B/B Homodimerizer) is a chemical inducer of dimerization that activates FKBP-Casp8.
Tags: Caspases apoptosis | Caspase inhibition | Caspase activation | Caspase activity | Caspase pathway | Caspase phosphorylation | Caspase cleavage | Caspase activity assay | Procaspase activation | Caspase inhibitor in vivo | Caspase inhibitor clinical trial | Caspase-independent apoptosis | Caspase-dependent apoptosis | Caspase inhibitor review