1. Signaling Pathways
  2. Apoptosis
  3. Caspase

Caspase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P992200
    Anti-CD146 Antibody (AA98)
    Activator
    Anti-CD146 Antibody (AA98) is an antibody targeting CD146 and an angiogenesis inhibitor. Anti-CD146 Antibody (AA98) blocks the dimerization of CD146 as well as its downstream PI3K/AKT, p38 MAPK and NF-κB signaling pathways; it inhibits the expression of MMP9 and ICAM1, epithelial-mesenchymal transition (EMT), and the proliferation, migration and tube formation of endothelial cells. Anti-CD146 Antibody (AA98) enhances radiation-induced cancer cell apoptosis and survival inhibition, reduces tumor microvessel density, and suppresses tumor growth, invasion and vasculogenic mimicry. Anti-CD146 Antibody (AA98) can be used in research related to cervical cancer, liver cancer, malignant phyllodes tumor of the breast, uveal melanoma, leiomyosarcoma, pancreatic cancer, other tumors and angiogenesis.
    Anti-CD146 Antibody (AA98)
  • 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-181955
    MS1129
    Activator
    MS1129 is a DNMT degrader that induces proteasomal degradation of DNMT1, DNMT3A and DNMT3B proteins. MS1129 upregulates TRAIL, DR4 and DR5 proteins, downregulates the decoy receptor DcR2, and activates TRAIL-dependent apoptosis via the HIF-1/2 and Caspase-10 pathways. MS1129 is applicable to the research of VHL-deficient clear cell renal cell carcinoma.
    MS1129
  • 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-125857B
    Cytochrome C (Saccharomyces cerevisiae)
    Cytochrome C (Saccharomyces cerevisiae) is a type C cytochrome located in the intermembrane space of the mitochondria. As an electron carrier, Cytochrome C (Saccharomyces cerevisiae) transfers electrons between complex III (cytochrome c reductase) and complex IV (cytochrome c oxidase, CIV) of the respiratory chain. Cytochrome C (Saccharomyces cerevisiae) can play a crucial role in triggering apoptosis by being released from the mitochondria into the cytosol.
    Cytochrome C (Saccharomyces cerevisiae)
  • 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-159007
    BD-AcAc2
    Inhibitor
    BD-AcAc2 (R,S-1,3-Butanediol acetoacetate diester) is an orally active, CNS-penetrant antiepileptic agent. BD-AcAc2 inhibits NF-κB, NLRP3 inflammasome, caspase-1/3, pyroptosis, apoptosis, and enhances autophagy. BD-AcAc2 exhibits antioxidant activity by modulating ROS, MDA, SOD, and GSH levels, and alleviates oxidative stress. BD-AcAc2 mitigates chronic colitis, counteracts Dextran Sodium Sulfate (DSS)-induced pathology, protects against central nervous system oxygen toxicity and acute lung injury, and exhibits anti-seizure efficacy. BD-AcAc2 can be used for the research of colitis, sarcopenia, acute lung injury, seizure, and obesity.
    BD-AcAc2
  • 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-181746
    Bcl-2/Mcl-1-IN-5
    Activator
    Bcl-2/Mcl-1-IN-5 (Compound S6) is a Bcl-2 and Mcl-1 inhibitor. Bcl-2/Mcl-1-IN-5 promotes Apoptosis, downregulates anti-apoptotic proteins Bcl-2 and Mcl-1, induces mitochondrial membrane potential depolarization, and activates the Caspase-dependent apoptotic cascade, as evidenced by Caspase-3 activation and PARP1 cleavage. Bcl-2/Mcl-1-IN-5 has anti-hepatocellular carcinoma activity.
    Bcl-2/Mcl-1-IN-5
  • HY-183779
    Antiangiogenic agent 10
    Activator
    Antiangiogenic agent 10 is a potent orally active antiangiogenic agent with antiproliferative activity against breast cancer cells. Antiangiogenic agent 10 induces apoptosis via caspase-3 activation. Antiangiogenic agent 10 can be used for the research of breast cancer.
    Antiangiogenic agent 10
  • 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-156898
    NPT100-18A
    Activator
    NPT100-18A is an αSyn oligomerization inhibitor. NPT10018A rescues cleaved caspase-3 levels to control levels. NPT10018A attenuates mitochondrial oxidative stress probe levels in a compartment-specific manner and, at higher concentrations, increases ATP signals. NPT100-18A can be used for the study of Parkinson’s disease (PD).
    NPT100-18A
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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.

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