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-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-N8210
    Homoeriodictyol
    		99.86%
    Homoeriodictyol is an orally active, bitter-tasting flavanone that can penetrate the blood-brain barrier. Homoeriodictyol enhances synaptic-related protein expression through NCOA4-mediated ferritin autophagy. Homoeriodictyol improves memory impairment in mice by inhibiting the NLRP3 inflammasome. Homoeriodictyol protects human endothelial cells from oxidative damage by activating Nrf2 and inhibiting mitochondrial dysfunction. Homoeriodictyol enhances ROS activity and induces apoptosis, exhibiting anticancer effects. Homoeriodictyol inhibits the survival and migration of androgen-resistant prostate cancer cells in vitro. Homoeriodictyol exerts antinociceptive activity in mice in vivo.
    Homoeriodictyol
  • HY-100676
    GRI977143
    		Inhibitor 99.29%
    GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM .
    GRI977143
  • 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-149265
    ROS-generating agent 1
    		Activator 99.11%
    ROS-generating agent 1 is a selective ROS-generating agent. ROS-generating agent 1 inhibits TrxR activity and expression in cancer cells. ROS-generating agent 1 induces ROS-dependent apoptosis and ferroptosis in cancer cells. ROS-generating agent 1 selectively kills lung cancer cells and inhibits the growth of cancer cell xenograft tumors in nude mice. ROS-generating agent 1 can be used for the research of non-small cell lung cancer.
    ROS-generating agent 1
  • HY-P10939A
    Ac-DMLD-CMK TFA
    		Inhibitor 98.44%
    Ac-DMLD-CMK TFA is a caspase 3 inhibitor and a GSDME inhibitor. Ac-DMLD-CMK TFA binds directly to the catalytic domain of caspase-3, blocks caspase-3-mediated cleavage of GSDME, inhibits the activation of caspase 3 and Gsdme in the caspase 3-Gsdme signaling pathway, and reduces the levels of pyroptosis and apoptosis as well as the expression of LDH, IL-6, IL-1β and IL-18. Ac-DMLD-CMK TFA alleviates renal function deterioration, renal tubular epithelial cell injury, inflammatory cytokine secretion, pulmonary structural damage, and chemotherapy-induced nephrotoxicity.
    Ac-DMLD-CMK TFA
  • HY-P991669
    IGN523
    		Agonist
    IGN523 is an anti-CD98 antibody (hCD98, KD = 0.55 nM). IGN523 induces antibody-dependent cell-mediated cytotoxicity (ADCC) activity, lysosomal membrane permeabilization, and inhibition of essential amino acid transport, ultimately leading to caspase-3 and caspase-7-mediated apoptosis of tumor cells. IGN523 inhibits tumor growth in multiple tumor xenograft models. IGN523 is useful in the research of non-small cell lung cancer (NSCLC), acute myeloid leukemia (AML), and other cancers..
    IGN523
  • HY-14942
    Berubicin
    		Agonist
    Berubicin (RTA 744 free base) is a Doxorubicin (HY-15142A) analog that can cross the blood-brain barrier. Berubicin inhibits P-gp and MRP1-mediated efflux and suppresses glioblastoma multiforme (GBM). Berubicin exerts toxic effects on leukemia cells by activating nuclear factor κB (NF-κB) and induces apoptosis in neuroblastoma cells. Berubicin can be used in the study of tumors related to the nervous system.
    Berubicin
  • HY-N0864
    Macranthoidin B
    		Modulator 98.35%
    Macranthoidin B (Macranthoiside I) is an orally active triterpene saponin. Macranthoidin B inhibits epithelial-mesenchymal transition in endometriosis via the COX‑2/PGE2 pathway, and also induces tumor cell apoptosis and inhibits their proliferation by regulating metabolism and increasing ROS levels. Macranthoidin B can be used in studies related to endometriosis, colorectal cancer and hepatocellular carcinoma.
    Macranthoidin B
  • HY-101310
    SYM 2081
    		98.0%
    SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain.
    SYM 2081
  • HY-14569
    CDPPB
    		Inhibitor 98.01%
    CDPPB is a selective, orally active and brain-penetrant 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-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-18712
    BG45
    		Inhibitor 99.95%
    BG45 is a potent HDAC3 inhibitor with IC50 values of 0.289, 2, 2.2 and ﹥20 μM for HDAC3, HDAC1, HDAC2 and HDAC6, respectively. BG45 selectively targets multiple myeloma (MM) cells and induces caspase-dependent apoptosis.
    BG45
  • HY-15472
    PRX-08066
    		Inhibitor
    PRX-08066 is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 inhibits pulmonary vascular remodeling. PRX-08066 can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).
    PRX-08066
  • HY-112749
    ME-344
    		Activator 99.80%
    ME-344 is an Isoflavone. ME-344 increases mitochondrial ROS generation. ME-344 inhibits tubulin polymerization. ME-344 inhibits HO-1 and impacts its mitochondrial translocation. ME-344 induces Apoptosis through Caspase 3 activation. ME-344 synergizes with Vinblastine in leukemia cells. ME-344 displays anti-tumor activity against leukemia and lung tumor. ME-344 can be used in the research of lung cancer, acute myeloid leukemia, and HER2-negative breast cancer.
    ME-344
  • HY-N1931
    Epifriedelanol
    		Inducer 99.69%
    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-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-B1138
    Fenbufen
    		Inhibitor 98.50%
    Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor.
    Fenbufen
  • HY-113953
    Z-Asp-CH2-DCB
    		Inhibitor 99.64%
    Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.
    Z-Asp-CH2-DCB
  • HY-D1652
    Ac-LEHD-AMC
    		Chemical 98.96%
    Ac-LEHD-AMC is a fluorogenic substrate for caspase-9 (Excitation: 341 nm; Emission: 441 nm). Caspase-9 can induce hydrolysis of Ac-LEHD-AMC, resulting in the release of AMC fluorophore and its fluorescence can be used to quantify caspase-9 activity.
    Ac-LEHD-AMC
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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