2. Signaling Pathways
  3. Apoptosis
  4. Caspase

Caspase

Caspase

Related Products

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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-N1710
    28-Deoxonimbolide
    		Modulator
    28-Deoxonimbolide is a Nimbin (HY-N3187) type limonoid, that can be isolated from Azadirachta indica seed extracts. 28-Deoxonimbolide shows anticancer activity. 28-Deoxonimbolide induces apoptotic cell death in HL60 cells via both the mitochondrial- and the death receptor-mediated pathways.
    28-Deoxonimbolide
  • HY-136893
    SP-6-27
    		Activator
    SP-6-27 is a tubulin depolymerizing agent that binds to the colchicine site of β-tubulin. SP-6-27 induces G2/M cell cycle arrest in ovarian cancer cells. SP-6-27 enhances intrinsic apoptosis in ovarian cancer cells through upregulation of Bax, Apaf-1, caspase-6, caspase-9, and caspase-3. SP-6-27 reduces ovarian cancer cell migration. SP-6-27 inhibits capillary tube formation by human umbilical vein endothelial cells. SP-6-27 shows minimum cytotoxicity to normal ovarian epithelia. SP-6-27 shows enhanced cytotoxicity in chemo-sensitive/resistant ovarian cancer cells when combined with Cisplatin (HY-17394). SP-6-27 can be used for the research of ovarian cancer.
    SP-6-27
  • HY-B0835S
    Fenobucarb-d3
    		Activator
    Fenobucarb-d3 is the deuterium labeled Fenobucarb. Fenobucarb is a carbamate insecticide. Fenobucarb induces zebrafish developmental neurotoxicity through pathways involved in inflammation, oxidative stress, degeneration and apoptosis. Fenobucarb is a possible risk factor to cardiovascular and cerebrovascular systems in animals.
    Fenobucarb-d<sub>3</sub>
  • HY-W743417
    (-)-Norgestrel-d6
    (-)-Norgestrel-d6 is the deuterium labeled Levonorgestrel (HY-B0257). Levonorgestrel is an orally active inhibitor of progesterone (HY-N0437). Levonorgestrel has anticancer activity and can induce Apoptosis. Levonorgestrel can be used as a contraceptive and in combination with other medications. Levonorgestrel can be used in the study of osteoporosis and uterine leiomyoma.
    (-)-Norgestrel-d<sub>6</sub>
  • HY-N11784
    Triptolidenol
    		Activator
    Triptolidenol, a traditional Chinese medicine, is an epoxy diterpene lactone that can be isolated from Tripterygium wilfordii. Triptolidenol has anti-inflammatory and anticancer activities. Triptolidenol significantly inhibits tumor cell proliferation and migration, arrests cell cycle arrest at S phase and induces apoptosis by activating the cytochrome c/caspase cascade signaling pathway. Triptolidenol disrupts NF-κB/COX-2 pathway by inhibiting IKKβ at ATP-binding sites. Triptolidenol can be used for chronic nephritis and kidney cancer like clear cell renal cell carcinoma (ccRCC) research.
    Triptolidenol
  • HY-181854
    ZX079
    		Inhibitor
    ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC50 value of 0.035 nM and a CBP DC50 value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia.
    ZX079
  • HY-N11846
    4′-O-Methylglabridin
    		Activator
    4′-O-Methylglabridin is an apoptosis inducer with antioxidant, cell cycle-disrupting and anticancer cytotoxic activities. 4′-O-Methylglabridin inhibits various cancer cell lines including liver cancer, breast cancer and colorectal cancer cell lines. By reducing the expression levels of phosphorylated Rb (Ser807/811) and p21 proteins, 4′-O-Methylglabridin promotes cell accumulation at the subG1 and G2/M phases, and triggers caspase-dependent apoptosis via cytochrome C release and caspase-9 activation. 4′-O-Methylglabridin also exerts antioxidant effects by inhibiting lipid peroxide levels and reducing β-carotene consumption, thereby blocking LDL oxidation. 4′-O-Methylglabridin can be used in the research of various cancers and atherosclerotic diseases.
    4′-O-Methylglabridin
  • HY-123605
    CAY10406
    		Inhibitor
    CAY10406 is an inhibitor for caspase 3/7. CAY10406 inhibits the expression of 28-kDa IL-1β fragment, without significant cytotoxicity (10 μM).
    CAY10406
  • HY-163983
    Tubulin polymerization-IN-68
    		Activator
    Tubulin polymerization-IN-68 (compound 32) is a tubulin inhibitor that can inhibit tubulin polymerization and destroy the cellular microtubule network. Tubulin polymerization-IN-68 can upregulate the expression of PARP-1 and caspase-3 and induce cell apoptosis, and has anticancer activity. Tubulin polymerization-IN-68 can effectively inhibit HepG2 (IC50=93 nM) and significantly inhibit the growth of HepG2 xenograft tumors in nude mice by oral administration.
    Tubulin polymerization-IN-68
  • HY-183739
    CQ31
    		Activator
    CQ31 is a PEPD and XPNPEP1 inhibitor, with an IC50 of 0.67 μM against PEPD and an IC50 of 122 μM against XPNPEP1. CQ31 inhibits the M24B aminopeptidase activity of PEPD and XPNPEP1. CQ31 induces the accumulation of Xaa-Pro-containing peptides, mildly inhibits DPP8/9, and triggers CASP1-dependent pyroptosis via activation of the CARD8 inflammasome and caspase-1. CQ31 can be used in research related to cancers such as acute myeloid leukemia.
    CQ31
  • HY-120923
    GUT-70
    		Activator
    GUT-70, a tricyclic coumarin, is a Hsp90 inhibitor. GUT-70 activates the caspase 2, 3, 8 and 9, and induces the apoptosis in leukemic cells. GUT-70 inhibits HIV-1 replication in chronically infected cells via suppression of the NF-κB pathway. GUT-70 can be used for the study of leukemic, mantle cell lymphoma (MCL) and HIV-1 infection.
    GUT-70
  • HY-168171
    ERK1/2 inhibitor 11
    		Activator
    ERK1/2 inhibitor 11 (compound L6) is a dual inhibitor of ERK1/2, lending to DSB accumulation and ERK1/2 expression degradation. ERK1/2 inhibitor 11 lowers the levels of BCL-2, and induces DNA damage by inhibiting PARP and ERK1/2. ERK1/2 inhibitor 11 activates caspase 3 to inducing apoptosis..
    ERK1/2 inhibitor 11
  • HY-120314A
    GEA 3162 hydrochloride
    		Activator
    GEA 3162 hydrochloride is an orally active compound that acts as a NO/ONOO⁻ donor. GEA 3162 hydrochloride significantly inhibits the activation of human polymorphonuclear leukocytes (PMNs) through the cGMP pathway, inhibits the release of inflammatory mediators, and exerts anti-inflammatory and protective effects. GEA 3162 hydrochloride induces apoptosis of neutrophils and bone marrow cells by activating caspase-2/3/8/9 through the ONOO⁻ pathway. GEA 3162 hydrochloride has a bidirectional effect in the rat gastric ulcer model: at low doses, it significantly reduces gastric mucosal damage, while at high doses, it aggravates the ulcer area. GEA 3162 hydrochloride can be used for research on inflammatory conditions such as gastric ulcers.
    GEA 3162 hydrochloride
  • HY-P5345A
    KLA peptide acetate
    		Activator 99.81%
    KLA peptide acetate is a naturally occurring Antibiotic peptide that is nontoxic outside of cells but is toxic when it enters into the interior of targeted cells. KLA peptide acetate can induce cell Apoptosis by disrupting mitochondrial membranes and activating Caspase. MG1-KLA acetate, formed by the coupling of KLA peptide acetate with MG1, can selectively induce apoptosis in pro-inflammatory microglia. KLA peptide acetate can be used for the research of liver fibrosis. KLA peptide acetate can be used for the research of neonatal hypoxic-ischemic encephalopathy.
    KLA peptide acetate
  • HY-RS01957
    Casp4 Rat Pre-designed siRNA Set A
    		Inhibitor

    Casp4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Casp4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Casp4 Rat Pre-designed siRNA Set A
  • HY-W635511
    Caspase-6-IN-1
    		Inhibitor
    Caspase-6-IN-1 is a Caspase-6 inhibitor with an IC50 of 5.6 μM. Caspase-6-IN-1 can inhibit Caspase-6 activity and reduce lamin A hydrolysis. Caspase-6-IN-1 can be used for the research of neurodegenerative diseases such as Huntington's disease and Alzheimer's disease.
    Caspase-6-IN-1
  • HY-145087
    NP3-146
    		Inhibitor
    NP3-146 is a NLRP3 inflammasome inhibitor through locking the NACHT domain of NLRP3. NP3-146 shows potent inhibitory activity against IL-1β release with an IC50 value of 0.171 μM in LPS (HY-D1056)/Nigericin (HY-127019)-stimulated BMDM cells. NP3-146 regulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants. NP3-146 can be used for the research of inflammatory diseases.
    NP3-146
  • HY-RS01960
    Casp6 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Casp6 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Casp6 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Casp6 Mouse Pre-designed siRNA Set A
  • HY-N16409
    Berkeleyamide C
    		Inhibitor
    Berkeleyamide C is a selective matrix metalloproteinase-3 (MMP-3) and caspase-1 inhibitor. Berkeleyamide C blocks MMP-3-mediated tumor cell invasion and metastasis, as well as the abnormal activation of inflammation and apoptosis related to caspase-1. Berkeleyamide C is promising for research of cancers and inflammation-related diseases.
    Berkeleyamide C
  • HY-181174
    Antioxidant agent-22
    		Activator
    Antioxidant agent-22 is a paraben derivative tetracyclic spermine cyclotriphosphazene compound. Antioxidant agent-22 exhibits antioxidant, anti-Inflammatory, and apoptotic activities. Antioxidant agent-22 significantly upregulates CAT, SOD, caspase-3 and IL-6 expression, suppresses GSH, IL-1β, and reduces BCL-2 and BAX levels. Antioxidant agent-22 can be used for the research of cancer, such as lung cancer.
    Antioxidant agent-22
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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