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-14942A
    Berubicin hydrochloride
    		Agonist
    Berubicin (RTA 744) hydrochloride is a Doxorubicin (HY-15142A) analog that can cross the blood-brain barrier. Berubicin hydrochloride inhibits P-gp and MRP1-mediated efflux and suppresses glioblastoma multiforme (GBM). Berubicin hydrochloride exerts toxic effects on leukemia cells by activating nuclear factor κB (NF-κB) and induces apoptosis in neuroblastoma cells. Berubicin hydrochloride can be used in the study of tumors related to the nervous system.
    Berubicin hydrochloride
  • HY-N3126
    Orsellinic acid
    		Inhibitor 98.36%
    Orsellinic acid is a Benzoic acid (HY-N0216) derivative. Orsellinic acid can be isolated from Chaetomium globosum endophytic on Ephedra fasciculata (Mormon tea). Orsellinic acid blocks PAF-mediated Apoptosis, inhibits caspase-3/7 activation, and PARP cleavage. Orsellinic acid can be used in research of neurons and various tumors (non-small cell lung cancer, breast cancer, neuroblastoma, pancreatic cancer).
    Orsellinic acid
  • HY-N2993
    Polyporenic acid C
    		Activator 99.80%
    Polyporenic acid C is a lanostane-type triterpenoid. Polyporenic acid C can be isolated from Poria cocos. Polyporenic acid C causes the cleavage of caspase-8 and caspase-3, as well as the cleavage of PARP. Polyporenic acid C reduces the phosphorylation level of Akt (Ser473), increases the phosphorylation of PTEN and p53 (Ser15), and activates JNK. Polyporenic acid C induces Apoptosis. Polyporenic acid C shows anticancer activity against non-small cell lung cancer.
    Polyporenic acid C
  • HY-108312A
    Ac-VEID-CHO TFA
    		Inhibitor 98.7%
    Ac-VEID-CHO (TFA) is a peptide-derived caspase inhibitor and has potency of inhibition for Caspase-6, Caspase-3 and Caspase-7 with IC50 values of 16.2 nM, 13.6 nM and 162.1 nM, respectively. Ac-VEID-CHO (TFA) can be used for the research of neurodegenerative conditions including Alzheimer’s and Huntington’s disease.
    Ac-VEID-CHO TFA
  • HY-120838
    Heptelidic acid
    		Inhibitor
    Heptelidic acid (Koningic acid) is a sesquiterpene antibiotic. Heptelidic acid inhibits Etoposide-induced apoptosis via downregulation of caspases. Koningic acid (KA) is a specific GAPDH inhibitor with an IC50of 90 μM.
    Heptelidic acid
  • HY-N6037
    Gardenin B
    		Modulator 99.69%
    Gardenin B is a methoxyflavone compound and an inhibitor of USP7, ODC (IC50: 6.24 μg/mL), and Cathepsin D (IC50: 5.61 μg/mL). Gardenin B exhibits antioxidant and antitumor activities. Gardenin B shows IC50 values of 8.87 and 10.59 μg/mL for DPPH and NO scavenging, respectively, and also possesses ferric ion reducing ability. Additionally, Gardenin B can inhibit tumor cell proliferation, induce cell cycle arrest and apoptosis. Gardenin B can be used in cancer research.
    Gardenin B
  • HY-N1157
    Thevetiaflavone
    		Inhibitor 99.83%
    Thevetiaflavone could upregulate the expression of Bcl-2 and downregulate that of Bax and caspase-3.
    Thevetiaflavone
  • HY-121713
    Aniline mustard
    		Activator 99.36%
    Aniline mustard (N, n-BIS (2-chloroethyl) aniline) is an anticancer agent.
    Aniline mustard
  • HY-19696R
    Tauroursodeoxycholate (Standard)
    		Inhibitor
    Tauroursodeoxycholate (Standard) is the analytical standard of Tauroursodeoxycholate. This product is intended for research and analytical applications. 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 (Standard)
  • HY-12412
    ML132
    		Inhibitor 98.75%
    ML132 (NCGC-00183434) is a selective caspase 1 inhibitor with an IC50 of 34.9 nM. ML132 shows good stability that can be utilized as molecular probes of caspase 1. ML132 can be used for research in the field of anti-cancer and anti-inflammatory.
    ML132
  • HY-N6576
    Hellebrigenin
    		Activator 99.69%
    Hellebrigenin is an inhibitor that selectively targets the MAPK signaling pathway (ERK, p38, JNK) and XIAP, and can inhibit Akt expression and phosphorylation. Hellebrigenin can activate endogenous apoptosis pathways (such as mitochondrial membrane potential disruption, Caspase family activation, PARP cleavage), downregulate anti-apoptotic proteins (Bcl-2, Bcl-xL) and upregulate pro-apoptotic proteins (Bax, Bak). Hellebrigenin can also induce DNA double-strand breaks to activate the ATM pathway. Hellebrigenin can inhibit tumor cell proliferation and clone formation, and is mainly used in the study of oral squamous cell carcinoma, liver cancer and other cancers.
    Hellebrigenin
  • HY-B1193R
    Terfenadine (Standard)
    		Activator
    Terfenadine (Standard) is the analytical standard of Terfenadine. This product is intended for research and analytical applications. Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
    Terfenadine (Standard)
  • 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-129119
    Akt1/Akt2-IN-2
    		Activator 98.57%
    Akt1/Akt2-IN-2 (compound 7) is an allosteric dual Akt1 and Akt2 inhibitor (IC50=138 nM and 212 nM, respectively). Akt1/Akt2-IN-2 increases activity of caspase-3, and inhibits viability of a number of tumor cells.
    Akt1/Akt2-IN-2
  • HY-P5983
    Ac-VEID-AFC
    		99.26%
    Ac-VEID-AFC is a caspase-6 fluorogenic substrate, and can be used in the caspase 6 activity assay.
    Ac-VEID-AFC
  • HY-130326
    RAPTA-C
    		Activator 99.30%
    RAPTA-C (Ru(η6-p-cymene)Cl2(pta)) acts as an anti-cancer and anti-angiogenic agent. RAPTA-C exhibits anti-metastatic, anti-angiogenic, and anti-tumoral activities through protein and histone-deoxyribonucleic acid alterations. RAPTA-C exhibits cell growth inhibition by triggering G(2)/M phase arrest in cancer cells. RAPTA-C also enhances the levels of p53 and triggers the mitochondrial Apoptotic pathway, resulting in cytochrome C release and caspase-9 activation. RAPTA-C reduces the growth of tumors with the inhibition of angiogenesis in a ovarian carcinoma model.
    RAPTA-C
  • HY-N0568R
    Madecassoside (Standard)
    		Inhibitor
    Madecassoside (Standard) is the analytical standard of Madecassoside. This product is intended for research and analytical applications. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica and has anti-inflammatory properties. Antioxidant and anti-aging effects. Madecassoside is a pentacyclic triterpene isolated from Centella asiatica. Madecassoside is orally active and has inhibitory properties against inflammation, oxidation, apoptosis and autophagy. Madecassosid inhibits activities of p38 MAPK and NF-kB, exhibits an anti-apopototic property, activates Nrf2 expression to reduce the neurotoxicity[10]. Madecassoside can be used in endocrine diseases, cardiovascular diseases, skin diseases and other diseases.
    Madecassoside (Standard)
  • HY-131204
    CZL80
    		Inhibitor 98.31%
    CZL80, a brain-penetrable caspase-1 inhibitor with an IC50 of 0.01 μM, could be used in the study of febrile seizures and later enhanced epileptogenic susceptibility.
    CZL80
  • HY-156168
    M190S
    		Inhibitor 99.84%
    M109S is a novel small molecule protecting cells from mitochondria-dependent apoptosis both in vitro and in vivo. M109S has the potential to become a research tool for studying cell death mechanisms and to develop therapeutics targeting mitochondria-dependent cell death pathway. M109S has orally bioactivity with excellent brain permeability.
    M190S
  • HY-B0835
    Fenobucarb
    		Activator 98.30%
    Fenobucarb is a carbamate insecticide. Fenobucarb induces zebrafish developmental neurotoxicity through pathways involved in inflammation, oxidative stress, degeneration and apoptosis. Fenobucarb is a possible risk factor to cardiovascular and cerebrovascular systems in animals.
    Fenobucarb
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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