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-178940
    Apoptosis inducer 49
    		Activator
    Apoptosis inducer 49 is a selective apoptosis inducer with high specificity against CCRF-CEM leukemia cells (IC50 = 2.68 μM). Apoptosis inducer 49 enhances RNA synthesis and replication stress, activates the Chk1-p21 axis, leading to S-phase arrest. Apoptosis inducer 49 can inhibit Bcl-2 and activate caspase-3. Apoptosis inducer 49 can be used for the study of Leukemia.
    Apoptosis inducer 49
  • HY-W009141S
    1-Monopalmitin-d31
    1-Monopalmitin-d31 (Glyceryl palmitate-d31) is the deuterium labeled 1-Monopalmitin (HY-W009141). 1-Monopalmitin (Glyceryl palmitate) is an activator of the PI3K/Akt pathway and an inhibitor of P-glycoprotein (P-gp). 1-Monopalmitin can induce G2/M arrest and caspase-dependent apoptosis in cancer cells, while inhibiting IAPs protein expression. 1-Monopalmitin can increase drug accumulation by inhibiting P-gp activity in intestinal Caco-2 cells. 1-Monopalmitin has the ability to induce protective autophagy and apoptosis of lung cancer cells (IC50=50-58 μg/mL), with low toxicity to normal cells.
    1-Monopalmitin-d<sub>31</sub>
  • HY-168067
    CDK-IN-14
    CDK-IN-14 (B34) is a CDK2 inhibitor (IC50=0.097 μM) with anti-hepatocellular carcinoma activity. CDK-IN-14 blocks the cell cycle of HepG-2 cancer cells through a caspase-mediated mechanism and induces apoptosis.
    CDK-IN-14
  • HY-N12461
    Cucurbitacin F
    		Activator
    Cucurbitacin F is a tetracyclic protostane-type triterpenoid with low toxicity, antibacterial and anti-inflammatory activities, and is also a related compound of Cucurbitacin B (HY-N0416). Cucurbitacin F widely exists in plants such as Cucurbitaceae plants, Quisqualis indica and Sorbaria sorbifolia. Cucurbitacin F acts as an actin aggregator and reduces cell viability in a dose-dependent manner. Cucurbitacin F induces apoptosis by triggering G2/M phase cell cycle arrest and activating the caspase-3-dependent apoptosis.
    Cucurbitacin F
  • HY-147514
    Anticancer agent 64
    		Activator
    Anticancer agent 64 (compound 5m) shows cytotoxic activity in CCRF-CEM cells, with IC50 of 2.4 μM. Anticancer agent 64 shows good anticancer activity through apoptosis induction. Anticancer agent 64 induces caspase 3 and 7 activation and PARP cleavage. Anticancer agent 64 induces significant effect of mitochondria depolarization.
    Anticancer agent 64
  • HY-N15380
    4,4′-Secalonic acid D
    		Activator
    4,4′-Secalonic acid D (Compound 12) is a PARP1 inhibitor. 4,4′-Secalonic acid D induces the accumulation of ROS and DNA damage, activates the caspase-3/GSDME pathway, and triggers apoptosis and pyroptosis of tumor cells by inhibiting PARP1. 4,4′-Secalonic acid D has anti-tumor activity.
    4,4′-Secalonic acid D
  • HY-178942
    EGFR/VEGFR2-IN-9
    		Activator
    EGFR/VEGFR2-IN-9 (Compound 9b) is an inhibitor of VEGFR-2 (IC50 = 1.325 μM) and EGFR (IC50 = 1.891 μM). EGFR/VEGFR2-IN-9 significantly inhibits the proliferation of multiple cancer cell lines, particularly leukemia cells. EGFR/VEGFR2-IN-9 upregulates the expression levels of Bax, caspase-3, and p53, while downregulating the expression of Bcl-2. EGFR/VEGFR2-IN-9 induces apoptosis and arrests the cell cycle in the G1 phase. EGFR/VEGFR2-IN-9 can be used to investigate anti-tumor angiogenesis and multi-drug resistant cancers.
    EGFR/VEGFR2-IN-9
  • HY-P5936
    Ac-AAVALLPAVLLALLAP-DEVD-CHO
    		Inhibitor
    Ac-AAVALLPAVLLALLAP-DEVD-CHO (DEVD-CHO-CPP 32) is a potent and reversible caspase-3 inhibitor.
    Ac-AAVALLPAVLLALLAP-DEVD-CHO
  • HY-175176
    HDAC1/6-IN-3
    		Agonist
    HDAC1/6-IN-3 is a potent HDAC inhibitor. HDAC1/6-IN-3 shows excellent inhibitory activities against HDAC1 (IC50 = 1.1 nM) and HDAC6 (IC50 = 2.7 nM). HDAC1/6-IN-3 significantly arrests HepG2 cells at the G0/G1 phase and induces apoptosis and pyroptosis. HDAC1/6-IN-3 exhibits significant antitumor activity in the HepG2 xenograft mode. HDAC1/6-IN-3 can be used for the study of cancers such as liver cancer, lung cancer, colon cancer and breast cancer.
    HDAC1/6-IN-3
  • HY-101374
    AGN 192403
    		Inhibitor
    AGN 192403 (BRD4780) is a potent and selective imidazoline-1 receptor antagonist with a Ki value of 42 nM. AGN 192403 is also a TMED9 inhibitor. AGN 192403 shows protective effects on oxidative cytotoxicity and mitochondrial inhibitor-induced cytotoxicity in astrocytes. AGN 192403 mitigates the proliferation and migration of differentiated glioma tumor cells. AGN 192403 can be used for glioma tumor and neurological diseases research.
    AGN 192403
  • HY-N12999
    Stigmast-5-en-3-ol
    		Agonist
    Stigmast-5-en-3-ol induces cancer cell apoptosis and inhibits proliferation by increasing the production of Bax, Caspase-9, p53, and PARP cleavage and reducing Bcl-xl expression. Stigmast-5-en-3-ol exhibits potent inhibitory activity against glucoamylase and α-amylase and possesses high antioxidant activity. Stigmast-5-en-3-ol can be used in the research of diseases such as leukemia, breast cancer, type 2 diabetes, and obesity.
    Stigmast-5-en-3-ol
  • HY-182307
    OH14
    OH14 is a cellular FLICE-like inhibitory protein (cFLIP) inhibitor and TNF-related apoptosis-inducing ligand (TRAIL) sensitizer. OH14 selectively binds to the DED1 pocket of cFLIP, disrupting its recruitment to the TRAIL-death inducing signalling complex without affecting procaspase-8 recruitment to FADD, allowing procaspase-8 activation. OH14 promotes TRAIL-mediated apoptosis and impairs cell viability in breast cancer systems when combined with TRAIL. OH14 can be used for the research of breast cancer.
    OH14
  • HY-180324
    Candidone
    		Activator
    Candidone is a type of flavanone phenolic compound with anti-cancer and antibacterial activities. Candidone inhibits the proliferation of hepatoblastoma and cholangiocarcinoma cells and induces their apoptosis by up-regulating p21, Bax, and caspase 3/9, and down-regulating Bcl-2 and survivin. It reduces the metastatic ability of cancer cells by inhibiting the expression of phosphorylated p38 and matrix metalloproteinase MMP-9. Candidone has inhibitory effects on multidrug-resistant bacterial strains. Candidone binds to the base pairs of DNA in a groove-binding manner, thereby slightly altering the conformation of DNA.
    Candidone
  • HY-181019
    iMPZ-8
    iMPZ-8 is a β-tubulin polymerization inhibitor that inhibits β-tubulin protein expression, disrupts microtubule structure, impairs microtubule organization. iMPZ-8 inhibits proliferation and reduces cellular migration and colonization in cancer cells. iMPZ-8 induces G2/M phase arrestand induces apoptosis via the BAX-Caspase-3 intrinsic apoptotic signaling pathway. iMPZ-8 can be used for the research of cancer, suah as breast cancer, neuroblastoma and colon cancer.
    iMPZ-8
  • HY-180849
    Caspase-3 activator 5
    		Activator
    Caspase-3 activator 5 (Compound 11) is a caspase-3 activator. Caspase-3 activator 5 reduces MRP1 levels and induces Apoptosis through Caspase-3 activation. Caspase-3 activator 5 exhibits anticancer activity against leukemia, cervical cancer, and breast cancer. Caspase-3 activator 5 shows no antibacterial or antifungal effects.
    Caspase-3 activator 5
  • HY-179022
    CAIX/CDK-2-IN-1
    		Inducer
    CAIX/CDK-2-IN-1 is a dual-acting inhibitor of carbonic anhydrase IX (CA IX) and cyclin-dependent kinase-2 (CDK-2) with IC50 values of 0.29 μM and 0.32 μM. The zein nanoparticls of CAIX/CDK-2-IN-1 can induce cancer cells apoptosis. CAIX/CDK-2-IN-1 can be used for the research of cancer, such as lung cancer.
    CAIX/CDK-2-IN-1
  • HY-183140
    DH20931
    		Activator
    DH20931 is a ceramide synthase 2 (CerS2) activator. DH20931 inhibits growth of cancer cells by inducing lipotoxic endoplasmic reticulum (ER) stress. DH20931 shows synergistic anti-tumor efficacy with Doxorubicin (HY-15142A). DH20931 can be used for the research of breast cancer.
    DH20931
  • HY-P5890
    YVAD-CHO
    		Inhibitor
    YVAD-CHO is an interleukin-1β converting enzyme (ICE, caspase 1) inhibitor (Ki: 0.76 nM). YVAD-CHO inhibits mature IL-1β production. YVAD-CHO partially delays motoneurone death in lesioned facial nerve mice.
    YVAD-CHO
  • HY-161857
    Akt/mTOR-IN-1
    		Inhibitor
    Akt/mTOR-IN-1 (Compound 8r) is an AKT/mTOR signaling pathway inhibitor exhibiting an IC50 value of 0.8 µM with anticancer activity. Akt/mTOR-IN-1 can decrease the expression of Caspase 3 and increase the expression of the autophagic protein Cyclin B1, thereby inducing cell autophagy and apoptosis. Akt/mTOR-IN-1 can be used in research related to non-small cell lung cancer (NSCLC).
    Akt/mTOR-IN-1
  • HY-W011683S6
    2'-Deoxyadenosine monohydrate-13C10,15N5 hydrate
    		Activator 99.7%
    2'-Deoxyadenosine monohydrate-13C10,15N5 is the 13C and 15N labeled 2'-Deoxyadenosine monohydrate (HY-W011683). 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-<sup>13</sup>C<sub>10</sub>,<sup>15</sup>N<sub>5</sub> hydrate
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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