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-N0361S
    Dihydrocapsaicin-d3
    		Inhibitor
    Dihydrocapsaicin-d3 is the deuterium labeled Dihydrocapsaicin (HY-N0361). Dihydrocapsaicin, a capsaicin, is a potent and selective TRPV1 (transient receptor potential vanilloid channel 1) agonist. Dihydrocapsaicin reduces AIF, Bax, and Caspase-3 expressions, and increased Bcl-2, Bcl-xL and p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection following ischemic stroke via PI3K/Akt regulation in rat.
    Dihydrocapsaicin-d<sub>3</sub>
  • HY-P3476
    Mca-VDQVDGW-Lys(Dnp)-NH2
    		Substrate
    Mca-VDQVDGW-Lys(Dnp)-NH2 is a fluorogenic substrate of caspase-7. Mca-VDQVDGW-K(Dnp)-NH2 can be used to quantify caspase-7 activity.
    Mca-VDQVDGW-Lys(Dnp)-NH2
  • HY-RS01955
    CASP4 Human Pre-designed siRNA Set A
    		Inhibitor

    CASP4 Human Pre-designed siRNA Set A contains three designed siRNAs for CASP4 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CASP4 Human Pre-designed siRNA Set A
    CASP4 Human Pre-designed siRNA Set A
  • HY-P10452
    Ac-LEVDGWK(Dnp)-NH2
    Ac-LEVDGWK(Dnp)-NH2 is a substrate for Caspase-3, and can be used to detect Caspase-3 activity.
    Ac-LEVDGWK(Dnp)-NH2
  • HY-P4401A
    Z-VEID-AFC TFA
    Z-VEID-AFC (TFA) is the trifluoroacetate salt of Z-VEID-AFC (HY-P4401). Z-VEID-AFC (TFA) is a fluorescent substrate for caspase-6. When Z-VEID-AFC (TFA) is cleaved by caspase-6, 7-amino-4-trifluoromethylcoumarin (AFC) is released, and its fluorescence can be used to quantify caspase-6 activity (Ex/Em: 400/505 nm) .
    Z-VEID-AFC TFA
  • HY-P10832
    ATWLPPRAANLLMAAS
    		Activator
    ATWLPPRAANLLMAAS is a chimeric peptide with anti-angiogenic and potent anti-tumor effects. ATWLPPRAANLLMAAS can inhibit the proliferation, viability, migration, and invasion of human hepatocellular carcinoma cells, and induce apoptosis..
    ATWLPPRAANLLMAAS
  • HY-130476
    Satratoxin G
    		Activator
    Satratoxin G is a large cyclic mucor toxin. Satratoxin G induces apoptosis by activation of caspase .
    Satratoxin G
  • HY-P4392
    Z-VAD-AMC
    Z-VAD-AMC is a substrate of caspase-9.
    Z-VAD-AMC
  • HY-P10241
    Ac-LEHD-CHO
    		Inhibitor
    Ac-LEHD-CHO is an inhibitor for caspase 8/9. Ac-LEHD-CHO prevents GalN/TNF-α-induced hepatotoxicity and hepatocyte apoptosis.
    Ac-LEHD-CHO
  • HY-19696S2
    Tauroursodeoxycholate-d4-1
    		Inhibitor
    Tauroursodeoxycholate-d4-1 is the deuterium labeled Tauroursodeoxycholate. Tauroursodeoxycholate (Tauroursodeoxycholic acid) is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.
    Tauroursodeoxycholate-d<sub>4</sub>-1
  • HY-P1094
    AZ-10417808
    		Inhibitor
    AZ-10417808 is a selective caspase-3 inhibitor. AZ-10417808 blocks apoptosis signaling pathway by inhibiting caspase-3 activity. AZ-10417808 can be used to study the effect of nicotine on plasmacytoid dendritic cell migration.
    AZ-10417808
  • HY-P5938
    Ac-AAVALLPAVLLALLAP-YVAD-CHO
    		Inhibitor
    Ac-AAVALLPAVLLALLAP-YVAD-CHO is a cell-permeable caspase-1 inhibitor that has antitumor activity.
    Ac-AAVALLPAVLLALLAP-YVAD-CHO
  • HY-RS01962
    CASP7 Human Pre-designed siRNA Set A
    		Inhibitor

    CASP7 Human Pre-designed siRNA Set A contains three designed siRNAs for CASP7 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CASP7 Human Pre-designed siRNA Set A
    CASP7 Human Pre-designed siRNA Set A
  • HY-W020050S
    Cystamine-d8 dihydrochloride
    Cystamine-d8 (dihydrochloride） is the deuterium labeled Cystamine (dihydrochloride）[1]. Cystamine (dihydrochloride) is the disulfide form of the free thiol, cysteamine. Cystamine is an orally active transglutaminase (Tgase) inhibitor. Cystamine also has inhibition activity for caspase-3 with an IC50 value of 23.6 μM. Cystamine can be used for the research of severals diseases including Huntington's disease (HD)[2][3][4].
    Cystamine-d<sub>8</sub> dihydrochloride
  • HY-168589
    Apoptosis inducer 30
    		Activator
    Apoptosis inducer 30 (Compound 15a) is an anticancer agent. Apoptosis inducer 30 induces MCF-7 cells apoptosis through mitochondrial pathway. Apoptosis inducer 30 induces intracellular reactive oxygen species levels and decreases mitochondrial membrane potential, and blocks the cell cycle in the G0/G1 phase. Apoptosis inducer 30 inhibits cell growth, with an IC50 value of 0.32 μM against MCF-7 cells, and inhibits tumor growth in a mouse model of breast cancer.
    Apoptosis inducer 30
  • HY-N7045R
    Isosilybin B (Standard)
    		Activator
    Isosilybin B (Standard) is the analytical standard of Isosilybin B (HY-N7045). This product is intended for research and analytical applications. Isosilybin B is a flavonolignan. Isosilybin B can be isolated from Silybum marianum. Isosilybin B can regulate cell cycle-related proteins (e.g., reduce cyclins (D3, D1, A, E), Cdk4, Cdk2, Cdc25A), and activate Caspases (Caspase-9 and Caspase-3). Isosilybin B can promote Apoptosis, reduce androgen receptor (AR) and PSA. Isosilybin B has anticancer activity against prostate cancer.
    Isosilybin B (Standard)
  • HY-169431
    VEGFR-2/AKT-IN-2
    		Activator
    VEGFR-2/AKT-IN-2 (Compound 5) is a VEGFR-2/AKT inhibitor (IC50: 0.061 μM for VEGFRin HepG2 cell). VEGFR-2/AKT-IN-2 reduces total and phosphorylated AKT as well as up-regulates BAX and Caspase-3 and down-regulates Bcl-2 in cells, thereby promoting Apoptosis. VEGFR-2/AKT-IN-2 causes cell cycle arrest in S phase. VEGFR-2/AKT-IN-2 inhibits the growth of human liver tumor cells.
    VEGFR-2/AKT-IN-2
  • HY-N1970R
    5,7-Dihydroxychromone (Standard)
    		Activator
    5,7-Dihydroxychromone (Standard) is the analytical standard of 5,7-Dihydroxychromone. This product is intended for research and analytical applications. 5,7-Dihydroxychromone, the extract of Cudrania tricuspidata, activates Nrf2/ARE signal and exerts neuroprotective effects against 6-hydroxydopamine (6-OHDA)-induced oxidative stress and apoptosis. 5,7-Dihydroxychromone inhibits the expression of activated caspase-3 and caspase-9 and cleaved PARP in 6-OHDA-induced SH-SY5Y cells.
    5,7-Dihydroxychromone (Standard)
  • HY-158820
    Cosdosiran
    		98.48%
    Cosdosiran is a chemically modified siRNA designed to temporarily inhibit expression of the caspase 2 protein and can be used for the study of nonarteritic anterior ischemic optic neuropathy and other optic neuropathies such as glaucoma that result in the death of retinal ganglion cells.?
    Cosdosiran
  • HY-155402
    Antiproliferative agent-42
    		Inhibitor
    Antiproliferative agent-42 (compound 7m) is a dihydrodipyrrolo compound. Antiproliferative agent-42 showed antiproliferative activity against Panc-1 cell line with an IC50 value of 12.54 μM.
    Antiproliferative agent-42
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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