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-P3363
    Z-DEVD-AMC
    		99.55%
    Z-DEVD-AMC is a selective caspase-3 substrate that can be measured by fluorescence spectrometry. AMC can be used as a fluorescence reference standard for AMC-based enzyme substrates including AMC-based caspase substrates.
    Z-DEVD-AMC
  • HY-131688
    2-Chlorohexadecanoic acid
    		Inhibitor 99.88%
    2-Chlorohexadecanoic acid, an inflammatory lipid mediator, interferes with protein palmitoylation,induces ER-stress markers, reduced the ER ATP content, and activates transcription and secretion of IL-6 as well as IL-8.2-Chlorohexadecanoic acid disrupts the mitochondrial membrane potential and induces procaspase-3 and PARP cleavage.2-Chlorohexadecanoic acid can across blood-brain barrier (BBB) and compromises ER- and mitochondrial functions in the human brain endothelial cell line hCMEC/D3.
    2-Chlorohexadecanoic acid
  • HY-10131
    Procaspase-3/6 activator 1
    		Activator 98.97%
    Procaspase-3/6 activator 1 (compound 1541) is a highly specific and robust activator of executioner procaspases-3 and -6, with EC50 values of 2.4 ± 0.2 and 2.8 ± 0.3 μM, respectively. Procaspase-3/6 activator 1 does not activate procaspases-1 or -7.
    Procaspase-3/6 activator 1
  • HY-N0905
    Ginsenoside Rh4
    		Activator 99.28%
    Ginsenoside Rh4 is a rare saponin obtained from Panax notoginseng. Ginsenoside Rh4 activates Bax, caspase 3, caspase 8, and caspase 9. Ginsenoside Rh4 also induces autophagy.
    Ginsenoside Rh4
  • HY-153161
    CASP8-IN-1
    		Inhibitor 98.97%
    CASP8-IN-1 (Compound 63-R) is a selective inhibitor for caspase 8 (CASP8), with an IC50 of 0.7 μM. CASP8-IN-1 inhibits FasL-induced apoptosis in cell Jurkat.
    CASP8-IN-1
  • HY-131204
    CZL80
    		Inhibitor 98.31%
    CZL80, a brain-penetrable caspase-1 inhibitor with an IC50 of 0.01 μM, could be used in the study of febrile seizures and later enhanced epileptogenic susceptibility.
    CZL80
  • HY-156168
    M190S
    		Inhibitor 99.84%
    M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability.
    M190S
  • HY-N4238
    Dehydrocorydaline nitrate
    		Activator 99.90%
    Dehydrocorydaline nitrate (13-Methylpalmatine nitrate) is an alkaloid. Dehydrocorydaline regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline nitrate elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities.. Dehydrocorydaline nitrate shows strong anti-malarial effects (IC50 =38 nM), and low cytotoxicity (cell viability > 90%) using P. falciparum 3D7 strain.
    Dehydrocorydaline nitrate
  • HY-D1652
    Ac-LEHD-AMC
    		Chemical 98.96%
    Ac-LEHD-AMC is a fluorogenic substrate for caspase-9 (Excitation: 341 nm; Emission: 441 nm). Caspase-9 can induce hydrolysis of Ac-LEHD-AMC, resulting in the release of AMC fluorophore and its fluorescence can be used to quantify caspase-9 activity.
    Ac-LEHD-AMC
  • HY-P1095
    Ivachtin
    		Inhibitor 99.71%
    Ivachtin (Caspase-3 Inhibitor VII; compound 7a) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor with an IC50 of 23 nM. Ivachtin has modest selectivity for the remaining caspases.
    Ivachtin
  • 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-N7045
    Isosilybin B
    		Activator 99.32%
    Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.
    Isosilybin B
  • HY-N6690
    Destruxin B
    		Activator 99.86%
    Destruxin B, isolated from entomopathogenic fungus Metarhizium anisopliae, is one of the cyclodepsipeptides with insecticidal and anticancer activities. Destruxin B induces apoptosis via a Bcl-2 Family-dependent mitochondrial pathway in human nonsmall cell lung cancer cells. Destruxin B significantly activates caspase-3 and reduces tumor cell proliferation through caspase-mediated apoptosis, not only in vitro but also in vivo.
    Destruxin B
  • HY-N1157
    Thevetiaflavone
    		Inhibitor ≥98.0%
    Thevetiaflavone could upregulate the expression of Bcl-2 and downregulate that of Bax and caspase-3.
    Thevetiaflavone
  • HY-162858
    BRD-810
    		Inducer 98.00%
    BRD-810 is a highly selective MCL1 inhibitor. BRD-810 can bind to the BH3 groove of MCL1 and block the sequestration of pro-apoptotic proteins, quickly inducing caspase activation in MCL1-dependent cell lines. BRD-810 shows anti-tumor activity in models of blood cancers and solid tumors.
    BRD-810
  • HY-129119
    Akt1/Akt2-IN-2
    		Activator 98.57%
    Akt1/Akt2-IN-2 (compound 7) is an allosteric dual Akt1 and Akt2 inhibitor (IC50=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells.
    Akt1/Akt2-IN-2
  • HY-130326
    RAPTA-C
    		Activator 99.30%
    RAPTA-C (Ru(η6-p-cymene)Cl2(pta)) acts as an anti-cancer and anti-angiogenic agent. RAPTA-C exhibits anti-metastatic, anti-angiogenic, and anti-tumoral activities through protein and histone-deoxyribonucleic acid alterations. RAPTA-C exhibits cell growth inhibition by triggering G(2)/M phase arrest in cancer cells. RAPTA-C also enhances the levels of p53 and triggers the mitochondrial Apoptotic pathway, resulting in cytochrome C release and caspase-9 activation. RAPTA-C reduces the growth of tumors with the inhibition of angiogenesis in a ovarian carcinoma model.
    RAPTA-C
  • HY-129115
    S1QEL1.1
    		Inhibitor ≥99.0%
    S1QEL1.1 is a small molecule inhibitor that specifically inhibits the generation of superoxide and hydrogen peroxide at the IQ site during reverse electron transfer in mitochondrial respiratory chain complex I (Complex I), with an IC50 of 0.07 μM. S1QEL1.1 can significantly reduce the activation of cysteine-aspartic protease (caspase) triggered by endoplasmic reticulum stress. S1QEL1.1 helps to decrease excessive proliferation of stem cells by inhibiting the Reactive Oxygen Species signaling pathway initiated by endoplasmic reticulum stress.
    S1QEL1.1
  • HY-14521B
    Lometrexol hydrate
    		Inducer 99.20%
    Lometrexol (DDATHF) hydrate, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
    Lometrexol hydrate
  • HY-157800
    Trilexium
    		Activator 99.70%
    Trilexium (TRX-E-009-1) is a third-generation of benzopyran structurally related to TRX-E-002-1 (HY-114250). Trilexium increases p21 protein expression and induces apoptosis. Trilexium depolymerizes microtubules. Trilexium shows broad anti-cancer activity.
    Trilexium
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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