Caspase

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

Caspase Products

Catalog No. 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.

S4353New

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.

S2417

20-Hydroxyecdysone

20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone) 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.

S7023

Z-VAD-FMK

Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.

S7314

Z-IETD-FMK

Z-IETD-FMK is a specific Caspase-8 inhibitor.

S7313

Z-LEHD-FMK

Z-LEHD-FMK (Caspase-9 Inhibitor) is a cell-permeable, competitive and irreversible inhibitor of enzyme caspase-9, which helps in cell survival.

S7312

Z-DEVD-FMK

Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.

S7311

Q-VD-Oph

Q-VD-Oph 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.

S8102

Z-VAD(OH)-FMK (Caspase Inhibitor VI)

Z-VAD-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor.

S7775

Emricasan

Emricasan is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.

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.

S7901

Ac-DEVD-CHO

Ac-DEVD-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.

S5579

Chelidonic acid

Chelidonic 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, 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.

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.

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.

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.

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.

S9634New

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.

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.

S7326

Tasisulam

Tasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.

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.

S2448

Gambogic Acid

Gambogic Acid (Guttatic, Guttic) 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.

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, 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).

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.

Catalog No. 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.

S4353New

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.

S2417

20-Hydroxyecdysone

20-Hydroxyecdysone (Ecdysterone, 20E, B-ecdysone, Commisterone) 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.

S7023

Z-VAD-FMK

Z-VAD-FMK is a cell-permeable, irreversible pan-caspase inhibitor, blocks all features of apoptosis in THP.1 and Jurkat T-cells.

S7314

Z-IETD-FMK

Z-IETD-FMK is a specific Caspase-8 inhibitor.

S7313

Z-LEHD-FMK

Z-LEHD-FMK (Caspase-9 Inhibitor) is a cell-permeable, competitive and irreversible inhibitor of enzyme caspase-9, which helps in cell survival.

S7312

Z-DEVD-FMK

Z-DEVD-FMK is a specific, irreversible Caspase-3 inhibitor, and also shows potent inhibition on caspase-6, caspase-7, caspase-8, and caspase-10.

S7311

Q-VD-Oph

Q-VD-Oph 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.

S8102

Z-VAD(OH)-FMK (Caspase Inhibitor VI)

Z-VAD-FMK (Caspase Inhibitor VI) is an irreversible pan-caspase inhibitor.

S7775

Emricasan

Emricasan is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.

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.

S7901

Ac-DEVD-CHO

Ac-DEVD-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.

S5579

Chelidonic acid

Chelidonic 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, 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.

Catalog No. Information Product Use Citations Product Validations
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.

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.

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.

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.

S9634New

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.

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.

S7326

Tasisulam

Tasisulam is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.

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.

S2448

Gambogic Acid

Gambogic Acid (Guttatic, Guttic) 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.

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, 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).

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.

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