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-146253
    CDK1/2/4-IN-1
    		Inhibitor
    CDK1/2/4-IN-1 (compound 3a) is a potent CDK inhibitor with IC50 values of 1.47, 0.78 and 0.87 μM for CDK1, CDK2 and CDK4, respectively. CDK1/2/4-IN-1 arrests cell cycle at G2/M phase and induces apoptosis. CDK1/2/4-IN-1 elevates Bax, caspase-3, P53 levels and decreases Bcl-2 level. CDK1/2/4-IN-1 can be used for cancer research.
    CDK1/2/4-IN-1
  • HY-175021
    HDAC-IN-91
    		Agonist
    HDAC-IN-91 is a multiple inhibitor of HDAC (IC50 = 134.22 nM for HDAC1, 66.29 nM for HDAC2), carbonic anhydrase (CA) (Ki = 72.03 nM for CA IX, 50.76 nM for XII), and tubulin polymerization ( IC50 = 2.56 μM). HDAC-IN-91 inhibits PARP1 and increases the Bax/Bcl-2 ratio. HDAC-IN-91 blocks the cell cycle at the G2/M phase and induces apoptosis through a mitochondrial apoptosis activation mechanism. HDAC-IN-91 can exert potent cytotoxic activity through tubulin polymerization inhibition. HDAC-IN-91 can be used in breast, colorectal, cervical and lung cancer research.
    HDAC-IN-91
  • HY-178953
    NLRP3-IN-84
    		Inhibitor
    NLRP3-IN-84 (Compound 32) is a NLRP3 inflammasome inhibitor. NLRP3-IN-84 can interfere with the oligomerization process of NLRP3 by inhibiting the activity of NLRP3 ATPase (IC50 = 158.4 nM). NLRP3-IN-84 inhibits Caspase-1 (IC50 = 27.7 nM), IL-1β release (PBMC: IC50 = 19.5 nM; mPBMC: IC50 = 24.2 nM), and ASC plaque formation (IC50 = 131 nM). NLRP3-IN-84 has no inhibitory activity on NLRC4 and AIM2 inflammasomes. NLRP3-IN-84 exhibits significant in vivo anti-inflammatory effects in a mouse acute peritonitis model. NLRP3-IN-84 can be used for the study of NLRP3-related inflammatory diseases.
    NLRP3-IN-84
  • HY-P10146
    Ac-LETD-CHO
    		Inhibitor
    Ac-LETD-CHO is a caspases 8 inhibitor. Ac-LETD-CHO has specific inhibition to casp-8 with an IC50 value of 6.71 nM. Ac-LETD-CHO can be used for the research of anticancer.
    Ac-LETD-CHO
  • HY-N2135R
    Puerarin 6''-O-Xyloside (Standard)
    Puerarin 6''-O-Xyloside (Standard) is the analytical standard of Puerarin 6''-O-Xyloside (HY-N2135). This product is intended for research and analytical applications. Puerarin 6''-O-Xyloside is one of the major iso-flavones found in P. lobata. Puerarin 6''-O-Xyloside inhibits cancer cells proliferation, induces apoptosis by upregulating cleaved caspase-3, 7, 9, Bax and downregulating Bcl-2 levles and inhibits tumor growth in mice. Puerarin 6''-O-Xyloside has anti-osteoporotic activity in ovariectomized mice. Puerarin 6''-O-Xyloside inhibits mushroom tyrosinase with an IC50 of 513.8 μM. Puerarin 6''-O-Xyloside can be used for the research of human lung carcinoma, osteoporosis, melanosis and melanomar.
    Puerarin 6''-O-Xyloside (Standard)
  • HY-181752
    FGFR3-IN-12
    FGFR3-IN-12 is a selective fibroblast growth factor receptor 3 (FGFR3) inhibitor with an IC50 of 6.8 nM. FGFR3-IN-12 shows an IC50 of 19.2 nM against FGFR3V555M and an IC50 of 16.9 nM against TNK1 (Thirty-eight Negative Kinase 1). FGFR3-IN-12 inhibits cancer cells proliferation and induces caspase-mediated apoptosis. FGFR3-IN-12 exhibits antitumor activity in bladder cancer xenografts mice models. FGFR3-IN-12 can be used for the research of cancer, such as bladder cancer.
    FGFR3-IN-12
  • HY-N0716AR
    Berberine hemisulfate (Standard)
    		Inhibitor
    Berberine (hemisulfate) (Standard) is the analytical standard of Berberine (hemisulfate). This product is intended for research and analytical applications. Berberine hemisulfate is the hemisulfate form of Berberine (HY-N0716). Berberine hemisulfate is an alkaloid isolated from the Chinese herbal medicine Huanglian. Berberine hemisulfate exhibits anti-inflammatory, antibiobic, antitumor, cardiovascular protective and neuroprotective activity.
    Berberine hemisulfate (Standard)
  • HY-120736
    MEB55
    		Activator
    MEB55 is an antitumor agent. MEB55 shows anti-proliferative activity. MEB55 has the potential for the research of prostate cancer.
    MEB55
  • HY-134563
    Z-Asp(OMe)-Gln-Met-Asp(OMe)-FMK
    		Inhibitor
    Z-Asp(OMe)-Gln-Met-Asp(OMe)-FMK is an inhibitor for caspase-3, and inhibits Dihydroartemisinin (HY-N0176) and Dictamnine (HY-N0849) co-induced apoptosis.
    Z-Asp(OMe)-Gln-Met-Asp(OMe)-FMK
  • HY-177740
    BTX306
    		Inhibitor
    BTX306 is a cereblon-targeting molecular glue degrader. BTX306 reduces myeloma cell viability and induces apoptosis. BTX306 overcomes myeloma cell resistance to Lenalidomide (HY-A0003) or Bortezomib (HY-10227). BTX306 is active against primary myeloma cells, and shows efficacy in vivo. BTX306 can be used for myeloma research.
    BTX306
  • HY-19345
    Vacquinol-1
    		Modulator 99.33%
    Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates the MAPK pathway. Vacquinol-1 inhibits the growth, migration and colony formation, and induces apoptosis of cancer cells. Vacquinol-1 is applicable to research related to cancers such as hepatocellular carcinoma.
    Vacquinol-1
  • HY-157546
    VEGFR-2-IN-40
    VEGFR-2-IN-40 is a VEGFR-2 inhibitor. VEGFR-2-IN-40 boosts early and late apoptosis. VEGFR-2-IN-40 decreases the levels immunomodulatory proteins TNF-α and IL-6 while showing a four-fold rise in an apoptotic marker caspase-3.
    VEGFR-2-IN-40
  • HY-180948
    PZ-11
    PZ-11 is a derivative of thiazolidinedione with anti-tumor activity. PZ-11 can induce cancer cells apoptosis by downregulating anti-apoptotic gene AIFM1, BAG3 and BIRC3 and regulating pro-apoptotic gene BAD, HRK, CASP10 and CASP10. PZ-11 can be used for research of breast cancer.
    PZ-11
  • HY-181587
    PDGFRA/CAIX/XII-IN-1
    		Activator 98.10%
    PDGFRA/CAIX/XII-IN-1 is an inhibitor of PDGFRA, CA IX and CA XII, with an IC50 of 20 nM against PDGFRA, a Ki of 93.3 nM against CA IX, and a Ki of 80.0 nM against CA XII. PDGFRA/CAIX/XII-IN-1 binds to the ATP-binding pocket of PDGFRA and blocks the downstream STAT3, AKT and ERK1/2 signaling pathways. PDGFRA/CAIX/XII-IN-1 induces G0/G1 cell cycle arrest and endogenous apoptosis (Apoptosis), including cleavage of PARP-1, caspase-9 and caspase-3, activation of caspase 3/7, and down-regulation of Mcl-1. PDGFRA/CAIX/XII-IN-1 exhibits antiproliferative activity in eosinophilic leukemia cells. PDGFRA/CAIX/XII-IN-1 can be used for the research of leukemia.
    PDGFRA/CAIX/XII-IN-1
  • HY-171992
    COX-2-IN-55
    		Activator 99.20%
    COX-2-IN-55 (compound 1) is an orally active, Celecoxib (HY-14398)-based analog with broad-spectrum anticancer activity and weak COX-2 inhibition. COX-2-IN-55 specifically inhibits SERCA2, increases caspase-3 cleavage and DR5 levels, thereby activating GRP78 and inhibiting the development of triple-negative breast cancer (TNBC). COX-2-IN-55 can also downregulate the levels of angiogenic markers VEGF-α and IL-8, inhibiting the formation of microvessels.
    COX-2-IN-55
  • HY-179613
    D-Leucine amide-CDDO-Me-HMP
    D-Leucine amide-CDDO-Me-HMP is a prodrug composed of CDDO-Me (HY-13324) and ligustrazine (HY-N0264). D-Leucine amide-CDDO-Me-HMP can protect against CCl4-induced liver injury. D-Leucine amide-CDDO-Me-HMP can inhibit ROS production, alleviates mitochondrial damage and inhibits cell apoptosis. D-Leucine amide-CDDO-Me-HMP can be used for the research of liver injury.
    D-Leucine amide-CDDO-Me-HMP
  • HY-170434
    Bfl-1-IN-6
    		Activator
    Bfl-1-IN-6 (Compound 20) is an orally active inhibitor for Bcl-2 related protein A1 (BFL1) with an IC50 of 19 nM. Bfl-1-IN-6 stabilizes BFL1 protein, activates cleaved caspase 3, and exhibits antitumor efficacy in mouse models.
    Bfl-1-IN-6
  • HY-N17617
    S-Petasin
    		Activator
    S-Petasin is a phosphodiesterase (PDE) inhibitor with IC50 values of 25.5 μM and 17.5 μM for PDE3 and PDE4, respectively. S-Petasin inhibits cholesterol side-chain cleavage enzyme, 11β-hydroxylase, PPAR-γ, and iNOS induction at RNA and protein levels. S-Petasin induces apoptosis, activates caspases, cleaves PARP, modulates mitochondrial membrane permeability, and regulates BCL2/BAX, p53, Bcl-XL, MMP-2, MMP-9, p21, CDK4, and cyclin D1 expression. S-Petasin reduces inflammatory cell accumulation, cytokine and IgE levels, and enhances serum IgG2a levels. S-Petasin relaxes isolated sensitized guinea pig trachealis and exhibits gastrointestinal anti-spasmodic activity. S-Petasin reduces tonsillitis severity and asthmatic attack frequency. S-Petasin can be used for the research of prostate cancer, obesity, melanoma, allergic asthma, asthma, and peritonitis.
    S-Petasin
  • HY-W750678
    9-cis-Canthaxanthin
    		Inhibitor
    9-cis-Canthaxanthin is a carotenoid with pro-apoptotic activity in THP-1 macrophage cells. 9-cis-Canthaxanthin induces cell apoptosis by increasing caspase-3 and caspase-8 activity.
    9-cis-Canthaxanthin
  • HY-180154
    EGFR/BRAFV600E-IN-6
    		Activator
    EGFR/BRAFV600E-IN-6 (Compound 7c) is a dual EGFR/BRAFV600E inhibitor with IC50 values of 0.12 and 0.05 μM. EGFR/BRAFV600E-IN-6 can activate caspase-3/8/9, unregulate Bax expression and downregulate Bcl-2 levels. EGFR/BRAFV600E-IN-6 can induce apoptosis and shows antioxidant activity. EGFR/BRAFV600E-IN-6 can be used for the research of cancer, such as colon cancer.
    EGFR/BRAFV600E-IN-6
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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