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-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-179695
    Microtubule destabilizing agent-3
    Microtubule destabilizing agent-3, a B32B3 (HY-12240) analog, is a microtubule destabilizing agent. Microtubule destabilizing agent-3 exerts its antimyeloma phenotypes by destabilizing microtubules and promoting mitotic arrest, leading to cell death. Microtubule destabilizing agent-3 induces G2/M phase arrest and caspase-dependent apoptosis. Microtubule destabilizing agent-3 can be used for the research of multiple myeloma.
    Microtubule destabilizing agent-3
  • 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
  • HY-W020050S
    Cystamine-d8 dihydrochloride
    Cystamine-d8 (dihydrochloride） is the deuterium labeled Cystamine (dihydrochloride）. 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).
    Cystamine-d<sub>8</sub> dihydrochloride
  • HY-182051
    HDAC3 degrader-2
    		Inhibitor
    HDAC3 degrader-2 is a selective HDAC3 degrader. HDAC3 degrader-2 inhibits the activation of the NLRP3 inflammasome by degrading HDAC3, thereby reducing the maturation of IL-1β and caspase-1. HDAC3 degrader-2 exhibits anti-inflammatory activity. HDAC3 degrader-2 can be used in research related to endotoxin shock, colitis and gouty arthritis.
    HDAC3 degrader-2
  • 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-181272
    MMP-9-IN-14
    		Agonist
    MMP-9-IN-14 is a MMP-9 inhibitor (IC50 = 34.46 μM). MMP-9-IN-14 induces G1-phase cell cycle arrest and caspase-dependent apoptosis in cancer cells. MMP-9-IN-14 promotes the accumulation of phosphorylated γH2AX. MMP-9-IN-14 inhibits the migration and invasion of cancer cells, and downregulates the expressions of MMP-2, MMP-9 and hTERT in cancer cells. MMP-9-IN-14 inhibits tumor growth and angiogenic spread in animal models. MMP-9-IN-14 can be used for the research of cancers such as lung adenocarcinoma, cervical cancer and colorectal cancer.
    MMP-9-IN-14
  • HY-175548
    Nrf2 activator-21
    		Inhibitor
    Nrf2 activator-21 is a Nrf2 activator with dual antioxidant and neuroprotective properties. Nrf2 activator-21 binds to Keap1 Kelch domain and disrupts Keap1-Nrf2 interactions and activate antioxidant defense mechanisms. Nrf2 activator-21 reduces apoptosis and decreases caspase-3 activity in the hippocampal neurons. Nrf2 activator-21 targets cerebral ischemia/reperfusion injury (CIRI) via Nrf2 pathway activation. Nrf2 activator-21 improves neurological function, alleviates anxiety-like behavior, enhances memory in rats with 2-vessel occlusion (2VO)-induced CIRI. Nrf2 activator-21 can be used for the study of cerebral ischemia/reperfusion injury.
    Nrf2 activator-21
  • 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-176718
    VEGFR-2-IN-69
    		Activator
    VEGFR-2-IN-69 (Compound 5A) is a dual inhibitor of VEGFR-2 and Telomerase, which upregulates the expression of caspase 3, caspase 8 and caspase 9, while downregulating CDK-2, CDK-4 and CDK-6. VEGFR-2-IN-69 exhibits an IC50 of 15.46 µM against HCT116 cells.
    VEGFR-2-IN-69
  • HY-181815
    SBP-5147
    		Activator
    SBP-5147 is an orally active ULK1/ULK2 inhibitor, with an IC50 of 2 nM against ULK1 and an IC50 of 53 nM against ULK2. SBP-5147 inhibits the phosphorylation of Beclin-1 and Vps34, reduces autophagy flux, downregulates the expression of ATG13 and ATG101, upregulates the expression of MHC-I, induces caspase-dependent apoptosis, and decreases the viability of non-small cell lung cancer cells. SBP-5147 is applicable to research related to non-small cell lung cancer[1].
    SBP-5147
  • HY-N1970R
    5,7-Dihydroxychromone (Standard)
    		Activator
    5,7-Dihydroxychromone (Standard) is the analytical standard of 5,7-Dihydroxychromone (HY-N1970). This product is intended for research and analytical applications. 5,7-Dihydroxychromone is a flavonoid compound with antioxidant properties. 5,7-Dihydroxychromone induces Nrf2 nuclear translocation, increases Nrf2/ARE binding activity, and up-regulates Nrf2-dependent antioxidant genes HO-1, NQO1, GCLc. 5,7-Dihydroxychromone attenuates excessive ROS generation, inhibits activated caspase-3, caspase-9, cleaved PARP expression, and prevents neuronal apoptosis and cell death. 5,7-Dihydroxychromone increases LXRα and PPARγ mRNA expression, induces preadipocyte differentiation, and regulates blood glucose levels. 5,7-Dihydroxychromone inhibits radial growth of soil pathogenic fungi, radicle elongation of select seedlings, and transiently inhibits Bradyrhizobium sp. growth in high mannitol medium. 5,7-Dihydroxychromone can be used for the research of Parkinson’s disease, type 2 diabetes mellitus and pathogenic fungal infection.
    5,7-Dihydroxychromone (Standard)
  • HY-N2420R
    Flavokawain A (Standard)
    		Activator
    Flavokawain A is a chalcone compound and an orally active inhibitor of PRMT5 and cytochrome P450. Flavokawain A has anti-inflammatory, anti-tumor, and immunomodulatory effects. Flavokawain A can inhibit the proliferation of tumor cells and induce apoptosis. Flavokawain A can be used in the research of diseases such as bladder cancer.
    Flavokawain A (Standard)
  • HY-N18905
    α-D-Glucosyl hesperidin
    		Inhibitor
    α-D-Glucosyl hesperidin is an orally effective structural modification derivative of Hesperidin (HY-15337) with anti-apoptotic (apoptosis) and antioxidant activities. α-D-Glucosyl hesperidin upregulates the expression of the Bcl-2 gene, while downregulating the expressions of the Bax and caspase-3 genes. α-D-Glucosyl hesperidin increases total antioxidant capacity, SOD and catalase levels, and decreases malondialdehyde and glutathione levels. α-D-Glucosyl hesperidin improves sperm motility, viability and plasma membrane function, while restoring reproductive organ weight and seminiferous tubule structure. α-D-Glucosyl hesperidin increases fertility index and exerts a synergistic protective effect with Proanthocyanidins (HY-N0794) in male rats with testicular ischemia-reperfusion injury. α-D-Glucosyl hesperidin can be used in the research of testicular ischemia-reperfusion injury.
    α-D-Glucosyl hesperidin
  • HY-100894R
    Biotin-VAD-FMK (Standard)
    		Inhibitor
    Biotin-VAD-FMK (Standard) is the analytical standard of Biotin-VAD-FMK (HY-100894). This product is intended for research and analytical applications. Biotin-VAD-FMK is a cell permeable, irreversible biotin-labeled caspase inhibitor, used to identify active caspases in cell lysates.
    Biotin-VAD-FMK (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-N12378A
    α-Patchoulene
    		Inhibitor
    α-Patchoulene is an orally active anti-inflammatory, antioxidant, and anti-apoptotic agent. α-Patchoulene inhibits the NF-κB, TLR4, and cAMP/PKA/CREB signaling pathways; activates the Sirt1/Nrf2 and AMPK signaling pathways; and targets Fas/FasL, Caspase-3, ERK1/2, ROCK1/MLC2 for inhibition. α-Patchoulene regulates cytokine secretion, inflammatory cell infiltration, lipid peroxidation, cell polarization, gut microbiota, and lipid metabolism, restores barrier function, mitochondrial function, and cell viability, and exhibits repellent activity against Spodoptera exigua larvae. α-Patchoulene can be used in research related to various inflammatory, ischemic, fibrosis-associated diseases, as well as hepatocellular carcinoma.
    α-Patchoulene
  • HY-13721R
    Phenoxodiol (Standard)
    		Activator
    Phenoxodiol (Standard) is the analytical standard of Phenoxodiol. This product is intended for research and analytical applications. Phenoxodiol (Idronoxil), a synthetic analog of Genestein, activates the mitochondrial caspase system, inhibits XIAP (an apoptosis inhibitor), and sensitizes the cancer cells to Fas-mediated apoptosis. Phenoxodiol also inhibits DNA topoisomerase II by stabilizing the cleavable complex. Phenoxodiol induces cell cycle arrest in the G1/S phase of the cell cycle and upregulates p21WAF1 via a p53 independent manner.
    Phenoxodiol (Standard)
  • HY-107150R
    Reproxalap (Standard)
    		Inhibitor
    Reproxalap (Standard) (ADX-102 (Standard)) is the analytical standard of Reproxalap (HY-107150). This product is intended for research and analytical applications. Reproxalap (ADX-102) is an active aldehyde sequestering agent. Reproxalap reduces the PKCα activity. Reproxalap blocks caspase 3/7 activation. Reproxalap protects cells from the cytotoxicity of C18:0-al. Reproxalap has anti-inflammatory and pain-relieving effects. Reproxalap is used in studies of dry eye, allergic conjunctivitis, and non-infectious anterior uveitis.
    Reproxalap (Standard)
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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