2. Signaling Pathways
  3. Apoptosis
  4. Caspase

Caspase

Caspase

Related Products

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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-N6046
    Kamebakaurin
    		Activator 98.05%
    Kamebakaurin is an orally active diterpenoid compound that can be isolated from Isodon excia (Maxin.). Kamebakaurin can inhibit NF-κB activation by directly targeting the DNA-binding activity of p50. Kamebakaurin can induce apoptosis and cell cycle arrest in tumor cells. Kamebakaurin has anti-inflammatory and anti-tumor activities.
    Kamebakaurin
  • HY-136975
    Caspase-3-IN-1
    		Inhibitor
    Caspase-3-IN-1 (compound 11b) is a potent Caspase-3 inhibitor, with an IC50 of 14.5 nM.
    Caspase-3-IN-1
  • HY-N1970
    5,7-Dihydroxychromone
    		Activator 99.94%
    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
  • HY-N6777
    Penicillic acid
    		Inhibitor 99.83%
    Penicillic acid is a polyketide mycotoxin produced by several species of Aspergillus and Penicillium. Penicillic acid exhibits cytotoxicity in rat alveolar macrophages (AM) in vitro. Penicillic acid inhibits Fas ligand-induced apoptosis by blocking self-processing of caspase-8.
    Penicillic acid
  • 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-101287
    MPT0B392
    		Activator 99.63%
    MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.
    MPT0B392
  • HY-120149
    Inotodiol
    		Activator
    Inotodiol activates p53 signaling pathway, inhibits MMP-2/9, and exhibits antitumor activity in cancer cell HeLa. Inotodiol inhibits the generation of ROS and exhibits antioxidant and neuroprotective effects. Inotodiol inhibits the activation of MAPK and NF-κB signaling pathway, and exhibits anti-inflammatory activity. Inotodiol inhibits TLR-4 mediated TNF-α production (IC50s in BMMC and BMDM is 0.7 μM and 3.0 μM), inhibits the degranulation in mast cell, exhibits anti-allergic activity. Inotodiol is orally active.
    Inotodiol
  • HY-155612A
    (Rac)-M826
    		Inhibitor 99.75%
    (Rac)-M826 is the racemate of M826 (HY-155612). M826 is a selective and reversible inhibitor for caspase-3 with an IC50 of 0.005 μM. M826 inhibits apoptosis in cell NT2. M826 can be used for nervous system diseases research.
    (Rac)-M826
  • HY-131113
    N-Nitrosodibutylamine
    		99.96%
    N-Nitrosodibutylamine (N-Nitroso-di-n-butylamine) is a nitrosamine enriched in the drinking water. N-Nitrosodibutylamine regulates caspase pathway. N-Nitrosodibutylamine induces Apoptosis. N-Nitrosodibutylamine induces hepatocarcinoma and oxidative DNA damage.
    N-Nitrosodibutylamine
  • 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-B0862
    Pendimethalin
    		Activator 99.75%
    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-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-130413
    Protectin D1
    		Inhibitor 99.10%
    Protectin D1, a neuroprotectin D1 produced by neuronal cells, is a member of a newly discovered family of bioactive products derived from docosahexaenoic acid. Protectin D1 also serves as a specialized pro-resolving mediator, exhibiting effective in vivo pro-resolving activity in various human disease models. Additionally, Protectin D1 is an inhibitor of NALP3 inflammasomes and regulates the PI3K/AKT and HIF-1α signaling pathways. Protectin D1 exerts anti-inflammatory effects by reducing ROS levels, inhibiting the expression of NALP3, ASC, and Caspase-1, and consequently decreasing the release of pro-inflammatory cytokines IL-1β and IL-18. Furthermore, Protectin D1 enhances miRNA-210 expression, activates the PI3K/AKT signaling pathway, and exerts cardioprotective effects. Protectin D1 holds promise for research in cardiovascular diseases and inflammatory disorders.
    Protectin D1
  • HY-115630
    cRIPGBM chloride
    		Activator 99.73%
    cRIPGBM chloride, an orally active, proapoptotic derivative. cRIPGBM can be generated from glioblastoma multiforme (GBM) cancer stem cells (CSCs). cRIPGBM(chloride) targets to receptor-interacting protein kinase 2 (RIPK2) to induce caspase 1-dependent apoptosis. cRIPGBM(chloride) suppresses the formation of RIPK2/TAK1 (prosurvival complex), and increases the formation of RIPK2/caspase 1 (proapoptotic complex). cRIPGBM(chloride) exerts potent anti-tumor activity in vivo in animal models.
    cRIPGBM chloride
  • 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-137941
    Roxatidine
    		Inhibitor 98.25%
    Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is an orally active histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect. Roxatidine is promising for research of gastric and duodenal ulcers.
    Roxatidine
  • HY-155612
    M826
    		Inhibitor 99.75%
    M826 is a potent, selective and reversible non-peptide caspase-3 inhibitor with an IC50 value of 0.005 μM for enzymatic activity against caspase-3. M826 displays potent anti-apoptotic activity in animal models in vitro and in vivo. M826 can be used for nervous system diseases research.
    M826
  • HY-N1931
    Epifriedelanol
    		Inducer ≥98.0%
    Epifriedelanol is a triterpenoid found in the root bark of Ulmus davidiana. Epifriedelanol induces apoptosis in DU145 cells. Epifriedelanol has antitumor and anti-inflammatory activities. Epifriedelanol inhibits cellular senescence in human primary cells.
    Epifriedelanol
  • HY-14521A
    Lometrexol disodium
    		Inducer ≥98.0%
    Lometrexol (DDATHF) disodium, an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol disodium can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol disodium has anticancer activity. Lometrexol disodium also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
    Lometrexol disodium
  • HY-N2099
    Onjisaponin B
    		Inhibitor 99.10%
    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
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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