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-W013579
    (S)-(+)-Carvone
    		Activator 99.26%
    (S)-(+)-Carvone is an orally active natural product. (S)-(+)-Carvone increases the activity of antioxidant enzymes (SOD, CAT) and ROS, reduces the levels of oxidative stress markers (MDA, AChE), reduces the secretion of proinflammatory cytokines (IL-1β, IL-4, IL-6, IL-10), and downregulates NLRP3. (S)-(+)-Carvone increases the activities of caspase-8, -9 and -3. (S)-(+)-Carvone induces apoptotic death. (S)-(+)-Carvone has antimanic-like effect, liver protection and anticancer activity against skin cancer. (S)-(+)-Carvone improves memory and arthritis.
    (S)-(+)-Carvone
  • 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-120019
    Ac-YVAD-CHO
    		Inhibitor 98.23%
    Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO is also a caspase-1 inhibitor. Ac-YVAD-CHO can suppress the production of mature IL-lβ.
    Ac-YVAD-CHO
  • HY-129478
    TC11
    		Activator 99.55%
    TC11 is a MCL1 degrader and Caspase-9 and CDK1 activator. TC11 functions as a phenylacetylamide derivative and is structurally related to immunomodulatory active molecules. TC11 induces degradation of MCL1 leading to apoptotic death during prolonged mitotic arrest.
    TC11
  • 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-N7015
    Zerumbone
    		99.74%
    Zerumbone is an orally active natural cyclic sesquiterpene and can be isolated from Zingiber zerumbet. Zerumbone has anti-proliferative, anti-inflammation, anti-cancer, anti-bacterial and anti-mutagenic activity.
    Zerumbone
  • HY-10397A
    MX1013
    		Inhibitor ≥99.0%
    MX1013 is a potent, irreversible dipeptide caspase inhibitor vith antiapoptotic activity. MX1013 inhibits recombinant human caspase 3 with an IC50 of 30 nM.
    MX1013
  • HY-Y0152
    Cinchonine
    		Activator 99.71%
    Cinchonine is a natural compound present in Cinchona bark with antimalarial, antitumor, anti-inflammatory, anti platelet-aggregation and anti-obesity properties. Cinchonine inhibits cells proliferation and autophagy and induces apoptosis through activation of Caspase-3. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
    Cinchonine
  • 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-N0674A
    Dehydrocorydaline chloride
    		Activator 99.75%
    Dehydrocorydaline chloride (13-Methylpalmatine chloride) is an alkaloid that regulates protein expression of Bax, Bcl-2; activates caspase-7, caspase-8, and inactivates PARP. Dehydrocorydaline chloride elevates p38 MAPK activation. Anti-inflammatory and anti-cancer activities. Dehydrocorydaline chloride shows strong anti-malarial effects (IC50?=38 nM), and low cytotoxicity (cell viability?>?90%) using P. falciparum 3D7 strain.
    Dehydrocorydaline chloride
  • HY-138832
    BM-1244
    		99.85%
    BM-1244 (APG-1252-M1) is a Bcl-xL/Bcl-2 inhibitor with Kis of 134 nM and 450 nM. BM-1244 has anti-tumor effects by inducing apoptosis and suppressing tumor growth. BM-1244 can induce cytochrome C and Smac release from mitochondria with caspase-3 and PARP cleavage. BM-1244 exhibits synergy with chemotherapy in vivo. BM-1244 can be studied in research for colorectal cancer, acute myeloid leukemia and gastric cancer.
    BM-1244
  • HY-P10149
    Ac-IEPD-CHO
    		Inhibitor 99.61%
    Ac-IEPD-CHO is a reversible granzyme B inhibitor with a Ki of 80 nM. Ac-IEPD-CHO is also a caspase-8 inhibitor.
    Ac-IEPD-CHO
  • HY-Y0148
    10-Hydroxydecanoic acid
    		Inhibitor 99.77%
    10-Hydroxydecanoic acid (10-HDAA) is a saturated fatty acid derived from 10-hydroxy-trans-2-decenoic acid, which can be isolated from royal jelly. 10-Hydroxydecanoic acid exhibits various biological activities, including anti-inflammatory, insecticidal, anti-malarial, and anti-Leishmania properties, as well as enhancing antigen-specific immune responses. The anti-inflammatory effects of 10-Hydroxydecanoic acid are primarily mediated by inhibiting the activation of NF-κB and the translation of interferon regulatory factor 1 (IRF-1), which reduces the production of interleukin 6 (IL-6) and nitric oxide (NO) in inflammatory cells. Additionally, 10-Hydroxydecanoic acid alleviates neuroinflammatory responses through the p53-autophagy pathway and the p53-NLRP3 pathway. Finally, 10-Hydroxydecanoic acid enhances antigen-specific immune responses by promoting the effective uptake of antigens by microfold cells.
    10-Hydroxydecanoic acid
  • HY-105930
    Lobaplatin
    		Inducer 98.0%
    Lobaplatin (D-19466) is a diastereometric mixture of platinum(II) complexe. Lobaplatin arrests cell cycle at G1 and G2/M phase. Lobaplatin induces apoptosis by increasing expressions of caspase and Bax, decreasing expression of Bcl-2. Lobaplatin can be used for research of cancer.
    Lobaplatin
  • HY-B0723
    Ospemifene
    		Inhibitor 99.84%
    Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer.
    Ospemifene
  • HY-Y1881A
    Copper sulfate pentahydrate, 99.9%
    		Activator 99.90%
    Copper sulfate pentahydrate, 99% is a biochemical reagent. Copper sulfate pentahydrate, 99% reduces the production of ROS and the expression levels of MyD88 as well as c-Rel genes. Copper sulfate pentahydrate, 99% decreases the activities of T-SOD, CAT, and GSH, increases the activities of caspase-3, caspase-8, and caspase-9. Copper sulfate pentahydrate, 99% is cytotoxic to various cells. Copper sulfate pentahydrate, 99% has antioxidant activity. Copper sulfate pentahydrate, 99% can be used in the research of diabetes, Parkinson's disease and DMBA (HY-W011845)-induced tumors.
    Copper sulfate pentahydrate, 99.9%
  • HY-156413
    NLRP3 agonist 1
    		Activator 99.47%
    NLRP3 agonist 1 (Compound 23) is an orally active NLRP3 agonist. NLRP3 agonist 1 can activate the enzyme Caspase-1 to cleave pro-IL-1β and pro-IL-18 proinflammatory cytokines into their mature forms.
    NLRP3 agonist 1
  • HY-N6018
    Beta-Eudesmol
    		Activator 99.49%
    Beta-Eudesmol has anticancer and anti-inflammatory activities. Beta-Eudesmol can induce apoptosis. Beta-Eudesmol is a neostigmine antagonist. Beta-Eudesmol can antagonize neostigmine-induced neuromuscular failure. Beta-Eudesmol can be used in the study of sepsis diseases. Beta-Eudesmol is a sesquiterpene-like compound that can be extracted from the rhizome of Atractylodes lancea.
    Beta-Eudesmol
  • 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-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
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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