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-W011683
    2'-Deoxyadenosine monohydrate
    		Activator 99.89%
    2′-Deoxyadenosine monohydrate is an adenine nucleoside that inhibits glucose-stimulated insulin release. 2′-Deoxyadenosine monohydrate inhibits glucose-stimulated increases seen in islet cyclic AMP (cAMP) accumulation. 2'-Deoxyadenosine monohydrate activates caspase-3 and promotes apoptosis. 2'-Deoxyadenosine monohydrate inhibits the activity of S-adenosyl-L-homocysteine hydrolase (SAHH). 2'-Deoxyadenosine monohydrate inhibits the growth of various cells. 2'-Deoxyadenosine monohydrate has an anticancer effect on colon cancer.
    2'-Deoxyadenosine monohydrate
  • HY-N4323
    14-Deoxyandrographolide
    		Inhibitor 99.47%
    14-Deoxyandrographolide is a diterpene with calcium channel blocking activity and acts as a uterine smooth muscle relaxant. 14-Deoxyandrographolide stimulates the release of nitric oxide (NO) in endothelial cells. 14-Deoxyandrographolide gradually desensitizes liver cells to TNF-α mediated apoptosis by inducing the release of TNFRSF1A.
    14-Deoxyandrographolide
  • HY-107150
    Reproxalap
    		Inhibitor 98.49%
    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
  • HY-100676
    GRI977143
    		Inhibitor 99.84%
    GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM .
    GRI977143
  • HY-P6440
    Met-12
    		Inhibitor 99.66%
    Met-12 is a small peptide inhibitor of the Fas receptor. Met-12 can inhibit Fas receptor-mediated photoreceptor cell apoptosis, reduce Caspase activation. Met-12 can be used in the research of photoreceptor.
    Met-12
  • HY-123230
    Trifloxystrobin
    		99.49%
    Trifloxystrobin (CGA 279202) is a type of fungicide. Trifloxystrobin has toxicity, antiparasitic activity and induce apoptosis, oxidative stress and DNA damage. Trifloxystrobin can be used for the reaesrch of fungal diseases.
    Trifloxystrobin
  • HY-103346
    MMPSI
    		Inhibitor 99.09%
    MMPSI is a potent and selective small molecule caspase 3 and caspase 7 inhibitor with an IC50 of 1.7 μM for human caspase-3. MMPSI can significantly reduce ischemia-reperfusion-induced infarct size in the isolated rabbit heart, and reduce apoptosis in both the ischemic myocardium and isolated cardiomyocytes. MMPSI can be used for researching cardioprotection.
    MMPSI
  • HY-N6951
    Guaiazulene
    		Inducer 99.26%
    Guaiazulene is a bicyclic sesquiterpene that can cross the blood-brain barrier. Guaiazulene exhibits various biological activities such as anti-inflammatory, antioxidant, hepatoprotective, antibacterial, and anti-tumor properties. Guaiazulene is also commonly used as a colorant in cosmetics. Guaiazulene shows in vitro cytotoxicity to rat neuronal cells and N2a neuroblastoma cells at high concentrations.
    Guaiazulene
  • HY-N2099
    Onjisaponin B
    		Inhibitor 99.06%
    Onjisaponin B is an orally active natural product derived from Polygala tenuifolia. Onjisaponin B inhibits NF-κB p65. Onjisaponin B enhances autophagy and accelerates the degradation of mutant α-synuclein and huntingtin. Onjisaponin B reduces β-amyloid (Aβ) production. Onjisaponin B reduces radiation-induced cell apoptosis. Onjisaponin B has anti-oxidant and anti-inflammatory activities. Onjisaponin B can be used for neurological disease and radiation injury study, and its metabolite tenuifolin (TF) can enter the brain through the BBB.
    Onjisaponin B
  • HY-W041489
    Chelidonic acid
    		Inhibitor 99.91%
    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
  • HY-B0862
    Pendimethalin
    		Activator 99.88%
    Pendimethalin is an orally active herbicide that controls annual grasses and certain broadleaf weeds. Pendimethalin induces Apoptotic cell death through activating ER stress-mediated mitochondrial dysfunction in human umbilical vein endothelial cells.
    Pendimethalin
  • HY-14569
    CDPPB
    		Inhibitor 98.01%
    CDPPB is a selective, orally active mGluR5 allosteric modulator. CDPPB increases AKT and ERK1/2 activation and augments the BDNF mRNA. CDPPB inhibits caspase-3 activation and mitochondrial dysfunction. CDPPB improves cognitive impairment, depression, and Huntington's disease.
    CDPPB
  • HY-B0420A
    Moroxydine hydrochloride
    		Inhibitor 99.45%
    Moroxydine (ABOB) hydrochloride is a broad-spectrum agent with multi-antiviral activities against DNA and RNA viruses, including influenza virus, herpes simplex, varicella zoster, measles, mumps disease, hepatitis C virus, etc. Moroxydine hydrochloride exhibits excellent antiviral activity and shows low cytotoxicity to cells infected by dsRNA viruses (grass carp reovirus, GCRV) and large DNA viruses (giant salamander iridovirus, GSIV). Moroxydine hydrochloride blocks the GCRV-induced cytopathic effects and eliminates nucleocapsids in ctenopharyngodon idella kidney (CIK) cells to keep the normal morphological structure. Moroxydine hydrochloride significantly inhibits the apoptosis, the caspase 3 activity, Bax expression and down-regulates Bcl-2 levels.
    Moroxydine hydrochloride
  • HY-W010155R
    Tryptophol (Standard)
    Tryptophol (Standard) (Indole-3-ethanol (Standard)) is an analytical standard of Tryptophol (HY-W010155). This product is intended for use in research and analytical applications.Tryptophol is an aromatic alcohol and secondary metabolite produced by microorganisms. Tryptophol induces Apoptosis and cleavage of caspase-8. Tryptophol inhibits Cunninghamella blakesleeana biofilm. Tryptophol has anti-phage infection, biofilm formation regulation, anti-inflammatory, hemolytic, sleep induction, temperature change, seizure susceptibility and immune regulation activities. Tryptophol is used in the research of African trypanosomiasis, sleep disorders, epilepsy.
    Tryptophol (Standard)
  • HY-12286
    PI-1840
    		Inducer 98.78%
    PI-1840 is a potent and selective chymotrypsin-like (CT-L) inhibitor for with an IC50 value of 27 nM. PI-1840 inhibits cell proliferation and arrest cell cycle at G2/M phase. PI-1840 induces apoptosis and induces autophagy. PI-1840 induces the accumulation of proteasome substrates p27, Bax, and IκB-α.
    PI-1840
  • HY-13326
    ASP3026
    		99.88%
    ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research.
    ASP3026
  • HY-B2046
    Simazine
    		99.44%
    Simazine is a triazine herbicide. Simazine is widely used in agriculture, potted plant and tree production. In addition, Simazine can induce the apoptosis of immune cells in the spleen of mice and inhibit the proliferation of B cells and T cells in mice.
    Simazine
  • HY-110077
    API-1
    		Inducer 99.62%
    API-1 is a potent selective Akt/PKB inhibitor that reduces the level of phosphorylated Akt (IC50 = 0.8 μM). API-1 binds to the PH domain and inhibits Akt membrane translocation. API-1 induces c-FLIP degradation. API-1 reduces cell proliferation and induces apoptosis. API-1 decreases tumor growth in mouse xenograft model.
    API-1
  • HY-N3138
    Ombuoside
    		Inhibitor 99.68%
    Ombuoside has antioxidant properties, inhibiting ROS production and apoptosis. Ombuoside exerts neuroprotective effects through the ERK-JNK-caspase-3 system. Ombuoside promotes Dopamine biosynthesis through TH and CREB activation. Ombuoside exhibits antimicrobial activity against several Gram-positive and Gram-negative bacteria, as well as Candida albicans
    Ombuoside
  • HY-N3001
    Isolinderalactone
    		Activator 98.79%
    Isolinderalactone is a sesquiterpene that exhibits anti-cancer, anti-inflammatory, and neuroprotective effects. Isolinderalactone inhibits VEGF expression and tyrosine phosphorylation of VEGFR2. Isolinderalactone decreases viability and induces apoptosis in U-87 glioblastoma (GBM) cells and colorectal cancer (CRC) cells. Isolinderalactone induces G2/M phase cell cycle arrest, ROS generation, pJNK/p38 MAPK activation, in colorectal cancer (CRC) cells. Isolinderalactone blocks LPS (HY-D1056)-induced NF-κB activation while activating Nrf2-HMOX1 signaling in RAW264.7 macrophages. Isolinderalactone improves cognitive dysfunction in APP/PS1 mice. Isolinderalactone can be used for the study of Glioblastoma multiforme (GBM), colorectal cancer, Alzheimer’s disease and acute lung injury.
    Isolinderalactone
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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