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-178373
    Topoisomerase I-IN-18
    		Activator
    Topoisomerase I-IN-18, a derivative of Thiosemicarbazide (HY-Y0032), is a Topoisomerase I inhibitor. Topoisomerase I-IN-18 can disrupt DNA synthesis and transcription. Topoisomerase I-IN-18 inhibits tumor cell proliferation by inducing S-phase cell cycle arrest. Topoisomerase I-IN-18 can enhance mitochondria-mediated apoptosis, suppress cell migration, and increase intracellular Reactive Oxygen Species (ROS) levels. Topoisomerase I-IN-18 can increase p53 protein expression, γH2AX phosphorylation, upregulate Bax expression, downregulate Bcl-2 expression, and activate the caspase cascade. Topoisomerase I-IN-18 can be used for the study of lung cancer.
    Topoisomerase I-IN-18
  • HY-117614
    WF-210
    		Activator
    WF-210 is a potent procaspase-3 activator with an EC50 value of 0.95 μM. WF-210 induces Apoptosis. WF-210 has anti-tumor activity.
    WF-210
  • HY-159891
    Microtubule destabilizing agent-2
    		Activator
    Microtubule destabilizing agent-2 (Compound 21) is an orally active and selective antitumor compound targeting microtubule protein. Microtubule destabilizing agent-2 destabilizes microtubule proteins and inhibits microtubule polymers. Microtubule destabilizing agent-2 arrests the G0/G1 phase in human tumor cells. Microtubule destabilizing agent-2 induces Apoptosis by activating the cascade pathway of caspases. Microtubule destabilizing agent-2 has anti-inflammatory activity, as inhibiting TNF-α and IL-6 in vitro. Microtubule destabilizing agent-2 reduces tumors growth in xenograft mice.
    Microtubule destabilizing agent-2
  • HY-176222
    IRF1 antagonist 1
    		Inhibitor
    IRF1 antagonist 1 (8003-3282) is a potent IRF1 (interferon regulatory factor) antagonist with anti-inflammatory activity. IRF1 antagonist 1 can maintain blood-brain barrier integrity and reduce brain edema. IRF1 antagonist 1 can improve neurological outcomes in an acute traumatic brain injury (TBI) mouse model.
    IRF1 antagonist 1
  • HY-13610B
    N1,N11-Diethylnorspermine hydrobromide
    		Activator
    N1,N11-Diethylnorspermine hydrobromide is a potent anticancer agent. N1,N11-Diethylnorspermine hydrobromide is a spermine analog that activates polyamine catabolism. N1,N11-Diethylnorspermine hydrobromide induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine hydrobromide kills glioblastoma multiforme (GBM) cells through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H2O2 production.
    N1,N11-Diethylnorspermine hydrobromide
  • HY-175640
    Troponin-IN-1
    		Inhibitor
    Troponin-IN-1 is a troponin inhibitor. Troponin-IN-1 protects OGD/R-injured H9c2 cardiomyocytes by reducing LDH leakage, pyroptosis and ROS accumulation. Troponin-IN-1 inhibits NO production and IL-1β/TNF-α/IL-18 release in LPS (HY-D1056)-induced RAW264.7 cells. Troponin-IN-1 acts via caspase-1/GSDMD/IL-18 pathway. Troponin-IN-1 reduces myocardial infarct size in LAD-induced myocardial ischemia/reperfusion (MI/R) male rats. Troponin-IN-1 can be used for the study of myocardial ischemia/reperfusion (MI/R) injury.
    Troponin-IN-1
  • HY-172393
    TCF4/β-catenin-IN-1
    		Inducer
    TCF4/β-catenin-IN-1 (Compound 8b) is an inhibitor of TCF4/β-catenin, and induces apoptosis. TCF4/β-catenin-IN-1 up-regulates p53, caspase-3, caspase-8, caspase-9 levels and Bax protein expression as well as down-regulates Bcl-2 protein expression. TCF4/β-catenin-IN-1 can inhibit CYP3A4, CYP1A2, CYP2C19, and shows promising cytotoxic activity in cancer cells.
    TCF4/β-catenin-IN-1
  • HY-N0551R
    Wedelolactone (Standard)
    		Inhibitor
    Wedelolactone (Standard) is the analytical standard of Wedelolactone. This product is intended for research and analytical applications. Wedelolactone suppresses LPS-induced caspase-11 expression by directly inhibits the IKK Complex. Wedelolactone also inhibits 5-lipoxygenase (5-Lox) with an IC50 of 2.5 μM. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Wedelolactone can extract from Eclipta alba, and it can be used for the research of cancer.
    Wedelolactone (Standard)
  • HY-P10992
    YVPGP
    		Activator
    YVPGP is an oligopeptide exacted from Anthopleura anjunae. YVPGP has a significant antitumor activity by mediating PI3K/AKT/mTOR signaling pathway. YVPGP arrests DU-145 cells in the S phase and induces apoptosis via mitochondrial and death receptor pathways (caspase3, 7, 8, 9). YVPGP effectively inhibits tumor growth in DU-145 xenografts mice model, promising for prostate cancer research.
    YVPGP
  • HY-P2012
    TRP-601
    		Inhibitor
    TRP-601 is a caspase inhibitor. TRP-601 reversed the increased expression of active caspase-2, the activation of endogenous apoptotic pathway and the up-regulation of key protein triggered by hyperoxia.
    TRP-601
  • HY-177268
    CHNQD-01426
    CHNQD-01426 (Compound 4a) is an anticancer agent. CHNQD-01426 has cytotoxic activities against cancer cells. CHNQD-01426 significantly inhibits hepatocellular carcinoma cells proliferation via arresting S and G2/M phase cell cycle and induces apoptosis by inducing ROS production and elevating apoptosis-related proteins expression. CHNQD-01426 potently inhibits tumor growth in HepG2 xenograft mice model.
    CHNQD-01426
  • HY-N2802
    Euptox A
    		Inducer
    Euptox A (9-Oxo-10, 11-dehydroageraphorone), a cadenine sesquiterpene, is the main toxin that can be isolated from Eupatorium adenophorum. Euptox A induces apoptosis by improving the gene expression level of apoptotic proteases such as caspase-10 in HeLa cells.
    Euptox A
  • HY-P5830A
    Biotin-DEVD-CHO TFA
    		Inhibitor
    Biotin-DEVD-CHO (TFA) is a biotin-conjugated form of the caspase-3 and -7 inhibitor – Ac-DEVD-CHO. Biotin-DEVD-CHO (TFA) can be used for affinity purification of the active caspase-3, -6, -7, and -8. Biotin-DEVD-CHO (TFA) can detect the active caspase-3 in vitro.
    Biotin-DEVD-CHO TFA
  • HY-116204
    SKLB70326
    		Activator
    SKLB70326 is a small molecule inhibitor of cell cycle progression that induces cell cycle arrest and apoptosis in human hepatocellular carcinoma cells. SKLB70326 is involved in downregulating cyclin-dependent kinase (CDK) 2, CDK4, and CDK6, while also activating PARP, caspase-3, caspase-9, and Bax, and downregulating Bcl-2.
    SKLB70326
  • HY-152756
    Caspase-3/7 activator 2
    		Activator
    Caspase-3/7 activator 2 is an effective activator of Caspase-3/7. Caspase-3/7 activator 2 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability.
    Caspase-3/7 activator 2
  • HY-N12235
    Sarglaroids F
    		Inhibitor
    Sarglaroids F (compound 6) is an anti-inflammatory agent isolated from the roots of Grass Coral. Sarglaroids F inhibits LPS/ATP-induced IL-1β release by affecting K+ efflux and reducing Caspase-1(P20) levels. Sarglaroids F is not cytotoxic to RAW264.7 cells.
    Sarglaroids F
  • HY-143235
    BRD4 Inhibitor-15
    		Activator
    BRD4 Inhibitor-15 (compound 13) is a potent BRD4 inhibitor, with an IC50 of 18 nM. BRD4 Inhibitor-15 induces apoptosis of 22RV1 cells by regulating Bcl-2/Bax proteins and activating caspase-3 signaling pathway. BRD4 Inhibitor-15 down-regulates the c-Myc level in 22RV1 cells. BRD4 Inhibitor-15 can be used for prostate cancer research.
    BRD4 Inhibitor-15
  • HY-W041489R
    Chelidonic acid (Standard)
    		Inhibitor
    Chelidonic acid (Standard) is the analytical standard of Chelidonic acid. This product is intended for research and analytical applications. Chelidonic acid is a component of Chelidonium majus L., used as an antimicrobial. Chelidonic acid also shows anti-inflammatory activity. Chelidonic acid has potential to inhibit IL-6 production by blocking NF-κB and caspase-1. Chelidonic acid is a glutamate decarboxylase inhibitor, with a Ki of 1.2 μM.
    Chelidonic acid (Standard)
  • HY-N7368R
    Hibifolin (Standard)
    Hibifolin (Standard) is the analytical standard of Hibifolin. This product is intended for research and analytical applications. Hibifolin is a flavonol glycoside that can be isolated from Helicteres isora. Hibifolin is an inhibitor of adenosine deaminase (ADA) (Ki = 49.92 μM). Hibifolin protects neurons against β-amyloid-induced neurotoxicity. Hibifolin possesses a potent protective activity against cell death induced by aggregated Aβ. Hibifolin can abolish Aβ-induced caspase-3 and caspase-7 activation. Hibifolin induces Akt phosphorylation in cortical neurons. Hibifolin is also a natural sortase A (SrtA) inhibitor (IC50 = 31.2 μM) through direct binding to SrtA protein. Hibifolin attenuates the pathogenic behavior of Staphylococcus aureus including adhesion, invasion, and biofilm formation. Hibifolin improves the survival of pneumonia induced by Staphylococcus aureus in mouse model and alleviates pathological damage. Hibifolin shows a synergistic antibacterial effect with Cefotaxime (HY-A0088A).
    Hibifolin (Standard)
  • HY-149517
    EGFR/BRAFV600E-IN-2
    		Activator
    EGFR/BRAFV600E-IN-2 (compound 3g) is a potential multi-target inhibitor of EGFR, BRAFV600E, and EGFRT790M, and an inducer of apoptosis. EGFR/BRAFV600E-IN-2 can activate caspase-3, 8, and Bax, and downregulate the anti-apoptotic protein Bcl2, inducing apoptosis. EGFR/BRAF V600E-IN-2 also has antioxidant activity and DPPH free radical scavenging potency.
    EGFR/BRAFV600E-IN-2
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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