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-B0263
    Thiabendazole
    		99.94%
    Thiabendazole is an orally available benzimidazole fungicide with repellent and anticancer activities. Thiabendazole can result in developmental malformations. Thiabendazole can be used for modeling.
    Thiabendazole
  • HY-101374A
    AGN 192403 hydrochloride
    		Inhibitor 99.96%
    AGN 192403 (BRD4780) hydrochloride is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 hydrochloride is also a TMED9 inhibitor. AGN 192403 hydrochloride shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 hydrochloride mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 hydrochloride can be used for glioma tumor and neurological diseases research.
    AGN 192403 hydrochloride
  • HY-W012499
    N-Acetyl-L-methionine
    		Activator 99.93%
    N-Acetyl-L-methionine is a dietary supplementation. N-Acetyl-L-methionine increases caspase-3 activity and inhibits mitochondrial activity. N-Acetyl-L-methionine promotes lactation and improves meat quality.
    N-Acetyl-L-methionine
  • HY-Y0319G
    Magnesium acetate tetrahydrate
    		Activator 99.47%
    Magnesium acetate tetrahydrate is a carboxylic acid and short-chain fatty acid (SCFAs). Magnesium acetate tetrahydrate activates AMPK, increases ROS, cleaved caspase 9, PPARα, downregulates SREBP-1c, ChREBP expression. Magnesium acetate tetrahydrate exhibits antifungal activity against Saccharomyces cerevisiae W303-1A. Magnesium acetate tetrahydrate regulates energy metabolism. Magnesium acetate tetrahydrate has anticancer activity against gastric cancer. Magnesium acetate tetrahydrate induces writhing reaction and ulcerative colitis. Magnesium acetate tetrahydrate can be used in the researches for gastric cancer, ulcerative colitis, hepatic steatosis, and pain.
    Magnesium acetate tetrahydrate
  • HY-Y0396
    N-Hydroxyphthalimide
    		Activator 99.89%
    N-Hydroxyphthalimide is a blocking agent and catalyst. N-Hydroxyphthalimide promotes oxidation reactions by generating PINO free radicals and activating hydrogen atom transfer processes. N-Hydroxyphthalimide reduces the expression of anti-apoptotic proteins Survivin and Bcl-xL and activates caspase 9 and caspase 3. N-Hydroxyphthalimide induces Apoptosis. N-Hydroxyphthalimide inhibits the phosphorylation of mTOR (Ser2448, Ser2481) and Akt (Ser473). N-Hydroxyphthalimide has anticancer effects against breast and colon cancer.
    N-Hydroxyphthalimide
  • HY-N0876
    Arenobufagin
    		99.82%
    Arenobufagin is a natural bufadienolide that can be extracted from toad venom. Arenobufagin can induce apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Arenobufagin has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. Arenobufagin can inhibit VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway.
    Arenobufagin
  • HY-W011978
    N-Acetyl-L-tryptophan
    		Inhibitor 99.82%
    N-Acetyl-L-tryptophan is an antagonist of the neurokinin-1 receptor (NK-1R), disrupting the binding of substance P (SP) to NK-1R. This action provides neuroprotective effects, improving memory deficits and motor impairments. N-Acetyl-L-tryptophan is also an inhibitor of cytochrome c (Cytochrome c), and it exerts antioxidant and anti-inflammatory effects by inhibiting the expression of IL-1β and the activation of caspase-1. N-Acetyl-L-tryptophan holds promise for research in neurodegenerative and inflammatory diseases.
    N-Acetyl-L-tryptophan
  • HY-119272
    EF24
    		Activator 99.34%
    EF24, a curcumin analogue, is an NF-kB inhibitor with great anti-tumor efficacy and oral bioavailability via deactivation of the MAPK/ERK signaling pathway in oral squamous cell carcinoma (OSCC). EF24 is active against melanoma and breast cancer cell lines with GI50 values of 0.7 μM and 0.8 μM, respectively. EF24 induces cell cycle arrest and apoptosis in MDA-MB-231 human breast cancer cells and DU-145 human prostate cancer cells. EF24 increases the levels of activated caspase 3 and 9, and decreases the phosphorylated forms of MEK1 and ERK.
    EF24
  • HY-B0621
    Triclabendazole
    		99.36%
    Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica.
    Triclabendazole
  • HY-N0826
    Corynoline
    		Modulator 98.84%
    Corynoline is an orally active acetylcholinesterase (AChE) inhibitor with an IC50 of 30.6 μM. Corynoline exhibits multiple activities including anti-inflammatory, antinociceptive, antitumor and analgesic effects. Corynoline can be used in the research of diseases such as tumors and inflammatory pain.
    Corynoline
  • HY-12294A
    PEAQX tetrasodium hydrate
    		Activator 99.72%
    PEAQX tetrasodium hydrate (NVP-AAM077 tetrasodium hydrate) is a tetrasodium hydrate of PEAQX (HY-12294). PEAQX tetrasodium hydrate is an orally active and selective NMDA antagonist, with IC50 values of 270 nM and 29.6 μM for hNMDAR 1A/2A and hNMDAR 1A/2B, respectively. PEAQX tetrasodium hydrate can promote the activation of caspase-3 and induce cell apoptosis in cortical striatal slice cultures.
    PEAQX tetrasodium hydrate
  • HY-D0848
    N,N'-Methylenebisacrylamide
    		Activator 99.98%
    N,N'-Methylenebisacrylamide (Bisacrylamide) is an orally active acrylamide dimer and crosslinker. N,N'-Methylenebisacrylamide increases CYP2E1, P53, cleaved caspase-3. N,N'-Methylenebisacrylamide promotes hepatic cancer. N,N'-Methylenebisacrylamide changes sperm abnormality rate and sperm count. N,N'-Methylenebisacrylamide decreases the number of various cells in the blood as well as induces liver and testicular damage. N,N'-Methylenebisacrylamide is used to prepare polyacrylamide gel.
    N,N'-Methylenebisacrylamide
  • HY-N0745
    Senkyunolide I
    		Inhibitor 99.37%
    Senkyunolide I is an orally active, blood-brain barrier-permeable metabolite of Z-ligustilide (HY-N0401A). Senkyunolide I is isolated from Ligusticum chuanxiong. Senkyunolide I upregulates p-Erk1/2 and Nrf2/HO-1, and inhibits Caspase 3. Senkyunolide I alleviates Apoptosis. Senkyunolide I increases the pain threshold in mice and reduces acetic acid-induced writhing responses in mice. Senkyunolide I improves neurological deficits, reduces infarct volume and alleviates cerebral edema in rats with focal cerebral ischemia-reperfusion injury. Senkyunolide I protects renal function and structural integrity in a mouse model of renal ischemia-reperfusion injury. Senkyunolide I is applicable to research related to focal cerebral ischemia-reperfusion injury, migraine, and renal ischemia-reperfusion injury.
    Senkyunolide I
  • HY-N0265
    Asperosaponin VI
    		Inhibitor 99.62%
    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
  • HY-130413
    Protectin D1
    		Inhibitor 99.10%
    Protectin D1, a neuroprotectin D1 produced by neuronal cells, is a member of a newly discovered family of bioactive products derived from docosahexaenoic acid. Protectin D1 also serves as a specialized pro-resolving mediator, exhibiting effective in vivo pro-resolving activity in various human disease models. Additionally, Protectin D1 is an inhibitor of NALP3 inflammasomes and regulates the PI3K/AKT and HIF-1α signaling pathways. Protectin D1 exerts anti-inflammatory effects by reducing ROS levels, inhibiting the expression of NALP3, ASC, and Caspase-1, and consequently decreasing the release of pro-inflammatory cytokines IL-1β and IL-18. Furthermore, Protectin D1 enhances miRNA-210 expression, activates the PI3K/AKT signaling pathway, and exerts cardioprotective effects. Protectin D1 holds promise for research in cardiovascular diseases and inflammatory disorders.
    Protectin D1
  • HY-101019
    Ossirene
    		Inhibitor 98.0%
    Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
    Ossirene
  • HY-NP0204
    Mouse Serum Albumin
    		Activator
    Mouse Serum Albumin is most abundant protein in plasma, which leaks into the brain parenchyma when the blood-brain barrier (BBB) is impaired. Mouse Serum Albumin induces astrocytes to A1 phenotype to remarkably increase levels of Elovl1. Mouse Serum Albumin promotes VLSFAs secretion and causes neuronal lippoapoptosis through endoplasmic reticulum stress response pathway. MSA-activated microglia triggeres remarkable tau phosphorylation at multiple sites (Ser202/Thr205) through NLRP3 inflammasome pathway. Mouse Serum Albumin decreases the spatial learning and memory abilities in mice. Mouse Serum Albumin can be used for the study of neurodegenerative diseases like Alzheimer’s disease (AD) and frontotemporal dementia (FTD).
    Mouse Serum Albumin
  • HY-N6018
    β-Eudesmol
    		Activator 99.49%
    β-Eudesmol has anticancer and anti-inflammatory activities. Beta-Eudesmol can induce apoptosis. β-Eudesmol is a neostigmine antagonist. β-Eudesmol can antagonize neostigmine-induced neuromuscular failure. β-Eudesmoll can be used in the study of sepsis diseases. β-Eudesmol is a sesquiterpene-like compound that can be extracted from the rhizome of Atractylodes lancea.
    β-Eudesmol
  • HY-19204
    Zinc phthalocyanine
    		Activator 98.0%
    Zinc phthalocyanine (ZnPc) is commonly applied in industry (catalysts, photoconductors) and biomedical (photodynamic therapy, PDT). Zinc phthalocyanine can be used to photooxidise cyclohexane and is promising for research of solar-cell applications.
    Zinc phthalocyanine
  • HY-W040129
    Chromomycin A3
    		Activator 99.66%
    Chromomycin A3 is an inhibitor that selectively binds to GC-rich DNA sequences. Chromomycin A3 targets the DNA minor groove after forming a dimer with Mg2+. Chromomycin A3 inhibits DNA replication and transcription, blocks the binding of Sp1 transcription factor to target gene promoters, downregulates the expression of anti-apoptotic proteins such as FLIP, Mcl-1, and XIAP, and induces S-phase cycle arrest and caspase-dependent apoptosis in tumor cells. Chromomycin A3 can antagonize oxidative stress induced by glutathione depletion and neuronal apoptosis induced by Camptothecin (HY-15660). Chromomycin A3 can be used in basic research on malignant tumors such as cholangiocarcinoma, and is a potential chemosensitizer and GC-rich region probe.
    Chromomycin A3
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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