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-179078
    CT-179
    		Activator 99.61%
    CT-179 is a brain-penetrant and orally active OLIG2 inhibitor with a human IC50 of 1250 nM. CT-179 disrupts OLIG2 dimerization, phosphorylation, and DNA binding, blocking OLIG2-driven transcription. CT-179 induces G2/M phase arrest and increases G0 population. CT-179 induces apoptosis by reducing anti-apoptotic proteins and increasing cleaved caspase-3 and cleaved PARP. CT-179 can be used for the research of subgroup medulloblastoma.
    CT-179
  • HY-N2132
    Flavokawain B
    		Activator 99.99%
    Flavokawain B (Flavokavain B) is an orally active chalcone. Flavokawain B results in activation of caspase-9, -3 and -8, cleavage of PARP. Flavokawain B down-regulates Bcl-2 with concomitant increase in Bax level. Flavokawain B inhibits NF-κB, PI3K/Akt and MAPK signaling pathway. Flavokawain B exhibits Apoptotic effects. Flavokawain B inhibits MMP-9 and promotes ROS generation. Flavokawain B inhibits multiple tumors and inflammation.
    Flavokawain B
  • HY-156135
    NSC194598
    		98.90%
    NSC194598 is a p53 DNA-binding inhibitor with an IC50 value of 180 nM. NSC194598 inhibits p53 DNA binding and induction of target genesn when p53 is stabilized and activated by irradiation or chemotherapy. NSC194598 can interfere with transcriptional activation of mutated rearranged during transfection (RET) gene, induce apoptosis and G0/G1 phase arrest. NSC194598 can be used for the researches of acute radiation toxicity and medullary thyroid carcinoma.
    NSC194598
  • HY-P1169
    Ac-IETD-AFC
    		99.28%
    Ac-IETD-AFC is a fluorogenic substrate of caspase-8, caspase-3, caspase-10, and granzyme B.
    Ac-IETD-AFC
  • HY-N4183
    Licoflavone C
    		Activator 99.83%
    Licoflavone C is a broad-spectrum antiviral inhibitor with estrogen-like properties. Licoflavone C binds to viral endonuclease (CEN) and inhibits the replication of various bunyaviruses including severe fever with thrombocytopenia syndrome virus (SFTSV) and lymphocytic choriomeningitis virus in a non-substrate competitive manner. The IC50 values of Licoflavone C against SFTSV CEN and SFTSV CEN are 35.5 μM and 135.8 μM, respectively, and its Kd value against SFTSV CEN is 9.53 μM. After viral entry into cells, Licoflavone C reduces viral loads in mouse tissues in a dose-dependent manner, and exhibits extremely low cytotoxicity and genotoxicity. Licoflavone C induces apoptosis by increasing caspase 3/7 activity, blocks the cell cycle, and alleviates chemotherapy-induced chromosomal damage. Licoflavone C is applicable to the research on severe fever with thrombocytopenia syndrome and related viral infection mechanisms.
    Licoflavone C
  • HY-P1823
    C-Reactive Protein (CRP) (174-185)
    		Inhibitor 99.88%
    C-Reactive Protein (CRP) is an anti-pneumococcal plasma protein that can serve as an inflammatory marker. C-Reactive protein can protect mice from pneumococcal infection by activating complement. C-Reactive protein can inhibit the activation of caspase-3/9 through the CD64/AKT/mTOR pathway, thereby promoting chemotherapy resistance in mice with tongue squamous cell carcinoma.
    C-Reactive Protein (CRP) (174-185)
  • HY-W046353
    2-Methoxycinnamaldehyde
    		Activator 98.95%
    2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound that can be isolated from Cinnamomum cassia. 2-Methoxycinnamaldehyde inhibits topoisomerase-I/II and NF-κB signaling pathway, causes mitochondrial dysfunction, induces lysosomal vesiculation, thereby leading to DNA damage and cell apoptosis. 2-Methoxycinnamaldehyde exhibits antitumor effects.
    2-Methoxycinnamaldehyde
  • HY-120838
    Heptelidic acid
    		Inhibitor
    Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM.
    Heptelidic acid
  • HY-N0726
    Dracorhodin perchlorate
    		Activator 99.02%
    Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product that can be obtained from the natural active molecule Dragon's blood. Dracorhodin perchlorate inhibits PI3K/Akt and NF-κB activation, upregulates p53 expression, activates caspase, produces ROS, and promotes Apoptosis. Dracorhodin perchlorate regulates the TLR4. Dracorhodin perchlorate promotes wound healing, improves diabetes. Dracorhodin perchlorate has anti-tumor activity against prostate cancer, breast cancer, cervical cancer and other cancers.
    Dracorhodin perchlorate
  • HY-B0960
    Sulfabenzamide
    		99.68%
    Sulfabenzamide (N-Sulfanilylbenzamide) is a sulfonamide antibacterial agent. Sulfabenzamide exhibit antibacterial activity against Staphylococcus aureus (ATCC 25923) and Escherichia coli (ATCC 8739). Sulfabenzamide can promote autophagic cell autophagy in breast cancer cells through p53/ DRAM pathway. Sulfabenzamide increases caspase-3 activity, deactivates PARP1 and DNA-PK, downregulates AKT1 and AKT2. Sulfabenzamide can be used for the researches of breast cancer and bacterial infections.
    Sulfabenzamide
  • HY-W010155R
    Tryptophol (Standard)
    Tryptophol (Standard) (Indole-3-ethanol (Standard)) is an analytical standard of Tryptophol (HY-W010155). This product is intended for use in research and analytical applications.Tryptophol is an aromatic alcohol and secondary metabolite produced by microorganisms. Tryptophol induces Apoptosis and cleavage of caspase-8. Tryptophol inhibits Cunninghamella blakesleeana biofilm. Tryptophol has anti-phage infection, biofilm formation regulation, anti-inflammatory, hemolytic, sleep induction, temperature change, seizure susceptibility and immune regulation activities. Tryptophol is used in the research of African trypanosomiasis, sleep disorders, epilepsy.
    Tryptophol (Standard)
  • HY-100472
    ZYZ-488
    		Inhibitor 99.94%
    ZYZ-488 is a competitive apoptotic protease activating factor-1 (Apaf-1) inhibitor. ZYZ-488 inhibits the activation of binding protein procaspase-9 and procaspase-3.
    ZYZ-488
  • HY-103667
    2-HBA
    		Activator 99.46%
    2-HBA is a potent inducer of NAD(P)H:quinone acceptor oxidoreductase 1 (NQO1) which can also activate caspase-3 and caspase-10.
    2-HBA
  • HY-P1986
    Z-DEVD-AFC
    		98.08%
    Z-DEVD-AFC is a cell-permeant substrate for caspase-3, which causes a shift in fluorescence uponcleavage of the AFC fluorophore. Z-DEVD-AFC can be used to detect caspase-3-like enzymes activity.
    Z-DEVD-AFC
  • HY-N7719
    Oosporein
    		Activator 99.16%
    Oosporein is a microbial metabolite and a red crystalline toxin produced by various fungi. Oosporein can promote the reproduction of fungi in host bodies by inhibiting insect immunity, and possesses multiple activities such as antibacterial, antiviral (HSV), and insecticidal effects. Oosporein can inhibit plant growth. In addition, Oosporein can also induce apoptosis, cell membrane damage, oxidative stress, and mitochondrial damage. Oosporein has certain antitumor activity.
    Oosporein
  • HY-N6951
    Guaiazulene
    		Inducer 99.26%
    Guaiazulene is a bicyclic sesquiterpene. Guaiazulene exhibits various biological activities such as anti-inflammatory, antioxidant, hepatoprotective, antibacterial, and anti-tumor properties. Guaiazulene is also commonly used as a colorant in cosmetics. Guaiazulene shows in vitro cytotoxicity to rat neuronal cells and N2a neuroblastoma cells at high concentrations.
    Guaiazulene
  • HY-N2099
    Onjisaponin B
    		Inhibitor 99.31%
    Onjisaponin B is an orally active natural product derived from Polygala tenuifolia. Onjisaponin B inhibits NF-κB p65. Onjisaponin B enhances autophagy and accelerates the degradation of mutant α-synuclein and huntingtin. Onjisaponin B reduces β-amyloid (Aβ) production. Onjisaponin B reduces radiation-induced cell apoptosis. Onjisaponin B has anti-oxidant and anti-inflammatory activities. Onjisaponin B can be used for neurological disease and radiation injury study, and its metabolite tenuifolin (TF) can enter the brain through the BBB.
    Onjisaponin B
  • HY-P10285
    d-KLA Peptide
    		Activator 99.33%
    d-KLA Peptide (D-(KLAKLAK)2), KLA peptide (HY-P5345) isomer, is a pro-apoptosis peptide. d-KLA Peptide can specifically target mitochondria and induce apoptosis by destroying the mitochondrial membrane. d-KLA Peptide increases caspase 3/7 activity, exerts proapoptotic activity and enhances antitumor efficacy in mouse melanoma models.
    d-KLA Peptide
  • HY-P2617A
    Ac-WEHD-AFC TFA
    		98.84%
    Ac-WEHD-AFC TFA is a fluorogenic caspase-1 substrate. Ac-WEHD-AFC TFA can measure caspase-1 fluorogenic activity and can be used for the research of tumor and inflammation.
    Ac-WEHD-AFC TFA
  • HY-N0392
    Polygalasaponin F
    		Inhibitor 99.85%
    Polygalasaponin F is an orally active triterpenoid saponin monomer. Polygalasaponin F downregulates the expression of Bax, p53, caspase-3, NF-κB p65 and MEK1; restores and upregulates the expression of Bcl-2; activates the PI3K/Akt signaling pathway; inhibits the phosphorylation of p38 MAPK, nuclear translocation of NF-κB, TLR4-mediated signaling pathway, mitophagy (Mitophagy) and ROS production; enhances cell viability and suppresses apoptosis (Apoptosis). Polygalasaponin F maintains mitochondrial function, alleviates Ca2+ overload, upregulates pCREB and BDNF, preserves cell viability and inhibits the release of inflammatory cytokines. Polygalasaponin F alleviates lung injury induced by influenza A H1N1 and cerebral ischemia-reperfusion injury. Polygalasaponin F is applicable to researches related to Parkinson's disease, cerebral ischemia, pneumonia induced by influenza A H1N1, stroke and Alzheimer's disease.
    Polygalasaponin F
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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