2. Signaling Pathways
  3. Apoptosis
  4. Caspase

Caspase

Caspase

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Caspase is a family of cysteine proteases that play essential roles in apoptosis (programmed cell death), necrosis, and inflammation. There are two types of apoptotic caspases: initiator (apical) caspases and effector (executioner) caspases. Initiator caspases (e.g., CASP2, CASP8, CASP9, and CASP10) cleave inactive pro-forms of effector caspases, thereby activating them. Effector caspases (e.g., CASP3, CASP6, CASP7) in turn cleave other protein substrates within the cell, to trigger the apoptotic process. The initiation of this cascade reaction is regulated by caspase inhibitors. CASP4 and CASP5, which are overexpressed in some cases of vitiligo and associated autoimmune diseases caused by NALP1 variants, are not currently classified as initiator or effector in MeSH, because they are inflammatory enzymes that, in concert with CASP1, are involved in T-cell maturation.

Caspase Isoform Specific Products:

Caspase Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-108312
    Ac-VEID-CHO
    		Inhibitor
    Ac-VEID-CHO is a peptide-derived caspase inhibitor and has potency of inhibition for Caspase-6, Caspase-3 and Caspase-7 with IC50 values of 16.2 nM, 13.6 nM and 162.1 nM, respectively. Ac-VEID-CHO also inhibits VEIDase activity an IC50 value of 0.49 µM. Ac-VEID-CHO can be used for the research of neurodegenerative conditions including Alzheimer’s and Huntington’s disease.
    Ac-VEID-CHO
  • HY-N0265R
    Asperosaponin VI (Standard)
    		Inhibitor
    Asperosaponin VI (Standard) is the analytical standard of Asperosaponin VI. This product is intended for research and analytical applications. Asperosaponin VI is a saponin component from Dipsacus asper. Asperosaponin VI induces osteoblast differentiation through the BMP-2/p38 and ERK1/2 signaling pathways. Asperosaponin VI protects against hypoxia-induced cardiomyocyte apoptosis by activating the PI3K/Akt and CREB pathways. Additionally, Asperosaponin VI also has antidepressant and wound-healing-promoting activities.
    Asperosaponin VI (Standard)
  • HY-117047
    ALC67
    		Activator
    ALC67 is a cytotoxic thiazolidine compound with an IC50 of approximately 5 μM against liver, breast cancer, colon cancer, and endometrial cancer cell lines. ALC67 induces apoptosis in cancer cells by activating caspase-9 and causing cell cycle arrest at the SubG1/G1 phase, via a pathway that is independent of death receptors. ALC67 can be used in cancer research.
    ALC67
  • HY-171031
    TFGF-18
    		Activator
    TFGF-18 is a GSK-3β inhibitor (IC50: 0.59 μM). TFGF-18 inhibits LPS-induced microglia activation and proinflammatory mediators release via inhibiting GSK-3β and downstream p65/NF-κB signaling. TFGF-18 inhibits neuronal apoptosis and oxidative stress, inhibits expressions of Bax, caspase3 and cleaved-caspase3 and increases the expression of Bcl-2. TFGF-18 has neuroprotection effect, inhibit neuroinflammation and attenuates cognitive impairment.
    TFGF-18
  • HY-171447
    LPT99
    		Inhibitor
    LPT-99 is an antagonist of apoptotic protease activating factor 1 (APAF-1). LPT-99 suppresses the activation of procaspase-9. LPT99 suppresses Cisplatin (HY-17394)-induced apoptosis. LPT99 can effectively mitigate cisplatin-induced hearing loss in rats.
    LPT99
  • HY-14584A
    PQ-1 succinate
    		Inhibitor
    PQ-1 succinate is an inhibitor for gap junction, which suppresses the gap junction dye transfer activity in retinal neurosensory R28 cells, and inhibits the CoCl2-induced ischemic apoptosis in retinal cell.
    PQ-1 succinate
  • HY-16658C
    Z-VA-DL-D-FMK
    		Inhibitor
    Z-VA-DL-D-FMK (Z-VA-DL-D(OH)-FMK) is an inhibitor for caspase. Z-VA-DL-D-FMK binds irreversibly to caspases, increases the sensitivity of TNF-α, and activates HIV replication in infected T cell ACH-2.
    Z-VA-DL-D-FMK
  • HY-N12503
    Patuletin
    		Activator
    Patuletin is a flavonol, that can be isolated from the flowers of Tagetes patula. Patuletin shows anti-proliferative activity against cancer cells. Patuletin causes significant nuclear fragmentation and has a great capacity to induce caspase-3 activation.
    Patuletin
  • HY-B1138R
    Fenbufen (Standard)
    		Inhibitor
    Fenbufen (Standard) is the analytical standard of Fenbufen. This product is intended for research and analytical applications. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor.
    Fenbufen (Standard)
  • HY-N1431A
    Tabersonine hydrochloride
    		Activator
    Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.
    Tabersonine hydrochloride
  • HY-W033813
    Caspase-3/7 Inhibitor I
    		Inhibitor
    Caspase-3/7 inhibitor I is a potent and reversible inhibitor of caspase-3 and caspase-7, with Kis of 60 and 170 nM, respectively. Caspase-3/7 inhibitor I can inhibit apoptosis in Camptothecin (HY-16560)-treated Jurkat cells and in chondrocytes.
    Caspase-3/7 Inhibitor I
  • HY-162059
    Pim-1 kinase inhibitor 10
    		Activator
    Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7 activation.
    Pim-1 kinase inhibitor 10
  • HY-B0347R
    Lacidipine (Standard)
    		Modulator
    Lacidipine (Standard) is the analytical standard of Lacidipine. This product is intended for research and analytical applications. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).
    Lacidipine (Standard)
  • HY-W011683S7
    2'-Deoxyadenosine monohydrate-15N5
    		Activator
    2'-Deoxyadenosine monohydrate-15N5 is the 15N labeled 2'-Deoxyadenosine monohydrate (HY-W011683). 2′-Deoxyadenosine monohydrate is an adenine nucleoside that inhibits glucose-stimulated insulin release. 2′-Deoxyadenosine monohydrate inhibits glucose-stimulated increases seen in islet cyclic AMP (cAMP) accumulation. 2'-Deoxyadenosine monohydrate activates caspase-3 and promotes apoptosis. 2'-Deoxyadenosine monohydrate inhibits the activity of S-adenosyl-L-homocysteine hydrolase (SAHH). 2'-Deoxyadenosine monohydrate inhibits the growth of various cells. 2'-Deoxyadenosine monohydrate has an anticancer effect on colon cancer.
    2'-Deoxyadenosine monohydrate-<sup>15</sup>N<sub>5</sub>
  • HY-17548
    VMY-1-103
    		Activator
    VMY-1-103 is an inhibitor for cyclin/Cdk complex, that arrests the cell cycle at G1 phase. VMY-1-103 reduces mitochondrial membrane potential, induces p53 phosphorylation and and PARP cleavage, activates caspase-3, and thus induces apoptosis in prostate cancer cell LNCaP.
    VMY-1-103
  • HY-B1357R
    Digitoxin (Standard)
    Digitoxin (Standard) is the analytical standard of Digitoxin. This product is intended for research and analytical applications. Digitoxin is an anti-cancer agent. Digitoxin induces apoptosis, inhibits influenza cytokine storm, causes DNA double-stranded breaks (DSBs) and blocks the cell cycle at the G2/M phase. Digitoxin induces calcium uptake into cells by forming transmembrane calcium channels and can be used for research of heart failure .
    Digitoxin (Standard)
  • HY-137225
    HTS07944
    		Agonist
    HTS07944 (HTS07944SC, C3) is a potent modulator of laminin receptor (37 LR). HTS07944 (HTS07944SC, C3) possesses anti-cancer activity in PC-3 cells and activates Caspase 3/7.
    HTS07944
  • HY-127149
    Mofarotene
    		Activator
    Mofarotene (Ro 40-8757), an arotinoid, is anticancer compound. Mofarotene induces apoptosis, associated with mitochondrial membrane depolarization, activation of caspase-3 and -9, and enhanced production of reactive oxygen species. Mofarotene inhibits hematopoiesis in vitro by inhibiting maturation from primitive progenitor cells.
    Mofarotene
  • HY-169922
    HDAC-IN-82
    		Activator
    HDAC-IN-82 (Compound 18b) is a histone deacetylase (HDAC) inhibitor with selective antiplasmodial and anticancer activity. HDAC-IN-82 shows potent antiproliferative activity and caspase 3/7 activation in cancer cells. HDAC-IN-82 causes hyperacetylation of histone H3 and α-tubulin.
    HDAC-IN-82
  • HY-116664
    DPQZ
    DPQZ is an anti-tubulin agent that inhibits cell separation and induces cell cycle arrest at the G2/M phase. In addition, DPQZ induces caspase-dependent apoptosis of HSC-3 cells by inhibiting Ras/Raf and activating MAP kinase. DPQZ can be used in the study of oral cancer.
    DPQZ
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
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Download Caspase Signaling Pathway Map.

Upon binding to their cognate ligand, death receptors such as Fas and TRAILR can activate initiator Caspases (Pro-caspase 8 and Pro-caspase 10) through dimerization mediated by adaptor proteins such as FADD and TRADD. Active Caspase 8 and Caspase 10 then cleave and activate the effector Caspase 3, 6 and 7, leading to apoptosis. ROS/DNA damage and ER stress trigger Caspase 2 activation. Active Caspase 2 cleaves and activates Caspase 3 and initiates apoptosis directly. Caspase 2, 8 and 10 can also cleave Bid, stimulate mitochondrial outer membrane permeabilization (MOMP) and initiate the intrinsic apoptotic pathway. Following MOMP, mitochondrial intermembrane space proteins such as Smac and Cytochrome C are released into the cytosol. Cytochrome C interacts with Apaf-1, triggering apoptosome assembly, which activates Caspase 9. Active Caspase 9, in turn, activates Caspase 3, 6 and 7, leading to apoptosis. Mitochondrial release of Smac facilitates apoptosis by blocking the inhibitor of apoptosis (IAP) proteins. 

 

Following the binding of TNF to TNFR1, TNFR1 binds to TRADD, which recruits RIPK1, TRAF2/5 and cIAP1/2 to form TNFR1 signaling complex I. Formation of the complex IIa and complex IIb is initiated either by RIPK1 deubiquitylation mediated by CYLD or by RIPK1 non-ubiquitylation due to depletion of cIAPs. The Pro-caspase 8 homodimer in complex IIa and complex IIb generates active Caspase 8. This active Caspase 8 in the cytosol then carries out cleavage reactions to activate downstream executioner caspases and thus induce classical apoptosis[1][2]. 

 

Reference:

[1]. Thomas C, et al. Caspases in retinal ganglion cell death and axon regeneration. Cell Death Discovery volume 3, Article number: 17032 (2017).
[2]. Brenner D, et al. Regulation of tumour necrosis factor signalling: live or let die. Nat Rev Immunol. 2015 Jun;15(6):362-74.

Caspase Isoform Comparison

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