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-W042191R
    Oxychlororaphine (Standard)
    		Activator
    Oxychlororaphine (Standard) is the analytical standard of Oxychlororaphine. This product is intended for research and analytical applications. Oxychloroaphine could be isolated from the bacterium Pantoea agglomerans naturally present in soil. Oxychloroaphine has broad-spectrum antifungal activity. Oxychloroaphine has cytotoxicity in a dose-dependent manner and induces apoptosis. Oxychloroaphine can be used in research of cancer[1][2].
    Oxychlororaphine (Standard)
  • HY-178861
    dCDK9-202
    		Activator
    dCDK9-202 a potent CDK9 PROTAC degrader with an DC50 value of 3.5 nM. dCDK9-202 exhibits broad-spectrum anti-tumor activity and extensively disrupts the oncogenic transcriptome. dCDK9-202 can activate Caspase-3/7, increase the level of cleaved PARP, and directly induce apoptosis of tumor cells. dCDK9-202 effectively inhibits TC-71 tumor growth without any signs of toxicity in mice. dCDK9-202 can be used for the study of EGFR-driven cancers such as sarcoma (Pink: CDK9 ligand (HY-178862); Blue: CRBN ligand (HY-W248665); Black: Linker (HY-N8015)).
    dCDK9-202
  • HY-175815
    Apoptosis inducer 44
    		Agonist
    Apoptosis inducer 44 is an apoptosis inducer. Apoptosis inducer 44 triggers apoptosis in MDA-MB-231 cells by increasing the levels of Bax and Cyt C, reducing Bcl-2, and initiating caspase-3 cleavage. Apoptosis inducer 44 suppresses the invasion and migration of MDA-MB-231 cells by down-regulating MMP-2 and MMP-9 expression and up-regulating E-cadherin protein levels. Apoptosis inducer 44 can be used for the study of breast cancer.
    Apoptosis inducer 44
  • HY-161874
    RPS6-IN-1
    		Activator
    RPS6-IN-1 (Compound 22o) inhibits cell metastasis, induces cell apoptosis (increases the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). RPS6-IN-1 decreases mitochondrial membrane potential. RPS6-IN-1 activates autophagy through the PI3K-Akt-mTOR signaling pathway, damages intracellular mitochondria and lysosomes, and cause ER stress. RPS6-IN-1 inhibits RPS6 phosphorylation. RPS6-IN-1 is an anticancer agent with low systemic toxicity.
    RPS6-IN-1
  • HY-17495
    Carteolol
    		Activator
    Carteolol is a non-selective β-adrenoceptor antagonist. Carteolol induces apoptosis via a caspase activated and mitochondrial-dependent pathway. Carteolol can be used for glaucoma research.
    Carteolol
  • HY-P10669
    NDI-Lyso
    NDI-Lyso is a lysosome-targeted anticancer agent that induces the formation of rigid long fibers in cancer cell lysosomes through an enzyme-instructed self-assembly (EISA) mechanism catalyzed by cathepsin B. This process triggers lysosomal swelling, membrane permeabilization (LMP), and membrane disruption, ultimately leading to cancer cell apoptosis via a non-classical caspase-independent pathway. NDI-Lyso exhibits significant selective anticancer activity in various cancer cell lines and drug-resistant cancer cells (IC50 ~10 μM) while showing low toxicity to normal cells (IC50 > 60 μM).
    NDI-Lyso
  • HY-178448
    EGFR-IN-178
    		Activator
    EGFR-IN-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC).
    EGFR-IN-178
  • HY-P11114
    Periplanetasin-4
    		Inhibitor
    Periplanetasin-4 is an antimicrobial peptide that can be derived from the American cockroach (Periplaneta americana). Periplanetasin-4 reduces cell rounding and apoptosis. Periplanetasin-4 blocks Clostridium difficile toxin A-induced ROS production and the activation of downstream p38 MAPK and p21. Periplanetasin-4 significantly increases mitochondrial calcium level, reduces DPH fluorescence intensity and vacuolar dysfunction in Candida albicans ATCC 90028 cells. Periplanetasin-4 significantly ameliorates toxin A-induced mucosal damage in the mouse gut. Periplanetasin-4 can be used for the study of colitis.
    Periplanetasin-4
  • HY-P11198
    AC-P19M
    		Inhibitor
    AC-P19M is an anticancer peptide. AC-P19M induces apoptosis by disrupting the cell membrane of cancer cells. AC-P19M reverses epithelial-mesenchymal transition (EMT). AC-P19M shows anti-angiogenic activity through the inhibition of VEGF-VEGFR2/ERK/Akt signaling. AC-P19M can be used for lung cancer research.
    AC-P19M
  • HY-N6037R
    Gardenin B (Standard)
    		Modulator
    Gardenin B (Standard) is the analytical standard of Gardenin B (HY-N6037). This product is intended for research and analytical applications. Gardenin B is a flavonoid isolated from Gardenia jasminoides. 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 (Standard)
  • HY-P10104
    Smac-N7, Penetratin conjugated
    		Activator
    Smac-N7, Penetratin conjugated is a caspase activator derived from the second mitochondria-derived activator of caspases (SMAC).
    Smac-N7, Penetratin conjugated
  • HY-136727A
    Ac-LEVD-CHO TFA
    		Inhibitor
    Ac-LEVD-CHO (TFA) is an inhibitor of caspase-4. Ac-LEVD-CHO (TFA) can inhibit the expression and secretion of IL-1α expression as well as the activation of caspase-4 induced by the T. denticola periodontal pathogen surface protein Td92 in human gingival fibroblasts. Ac-LEVD-CHO (TFA) can also reduce the apoptosis due to the expression of the dominant negative adenoviral RNA-dependent protein kinase in A549 and PC3 cancer cell lines.
    Ac-LEVD-CHO TFA
  • HY-N15449
    Vicanicin
    		Activator
    Vicanicin is a depsidone compound found in lichens. Vicanicin inhibits the expression of Hsp70, regulates the redox-sensitive mechanisms within cells, promotes the increase of reactive oxygen species (ROS) in cancer cells, changes the Bax/Bcl-2 ratio, activates caspase-3, and triggers apoptosis. Vicanicin inhibits cell growth and induces apoptosis in androgen-sensitive (LNCaP) and androgen-insensitive (DU-145) human prostate cancer cells. Vicanicin is promising for research of prostate cancer.
    Vicanicin
  • HY-160962
    SM1044
    		Activator
    SM1044 is a dihydroartemisinin (DHA) dimer. SM1044 activates caspase, induces apooptosis in RL95-2 and KLE cells. SM1044 inhibits proliferations of cancer cells RL95-2, KLE, HEC-50, HEC-1-A, HEC-1-B, AN3CA, with IC50 < 3.6 μM . SM1044 inhbits tumor growth in RL95-2 xenograft mouse model.
    SM1044
  • HY-170929
    EMT inhibitor-3
    		Activator
    EMT inhibitor-3 (compound 11i) is a epithelial-mesenchymal transition (EMT) inhibitor. EMT inhibitor-3 inhibits neuroblastoma SK-N-SH cells with an IC50 of 2.5 μM. EMT inhibitor-3 inhibits SK-N-SH cell proliferation, migration, and invasion. EMT inhibitor-3 increases the Bax/Bcl-2 protein expression ratio, promotes Cytochrome C ( HY-125857) release from mitochondria, and activates caspases 9 and caspases 3, inducing mitochondria-mediated endogenous tumor cell Apoptosis. EMT inhibitor-3 is potential for cancer research.
    EMT inhibitor-3
  • HY-13523S
    PAC-1-d8
    PAC-1-d8 (Procaspase activating compound 1-d8) is the deuterium labeled PAC-1 (HY-13523). PAC-1 is a procaspase-3 activator that induces apoptosis in cancer cells with an EC50 of 2.08 μM.
    PAC-1-d<sub>8</sub>
  • HY-147928
    Apoptotic agent-2
    		Activator
    Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research.
    Apoptotic agent-2
  • HY-RS01945
    CASP12 Human Pre-designed siRNA Set A
    		Inhibitor

    CASP12 Human Pre-designed siRNA Set A contains three designed siRNAs for CASP12 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CASP12 Human Pre-designed siRNA Set A
  • HY-178367
    PFKFB4-IN-1
    		Activator
    PFKFB4-IN-1 is a potent and selective ATP-competitive PFKFB4 inhibitor (IC50 = 4.50 μM) that reduces intracellular PFKFB4 protein levels. PFKFB4-IN-1 exhibits >12-fold selectivity over PFKFB1/4 and PFKFB3/4. PFKFB4-IN-1 inhibits cancer cell proliferation, induces apoptosis, and inhibits cell migration. PFKFB4-IN-1 inhibits tumor growth in the MDA-MB-231 xenograft mouse model. PFKFB4-IN-1 can be used for breast, lung and liver cancer research.
    PFKFB4-IN-1
  • HY-175666
    ISAM-CG557
    		Inhibitor
    ISAM-CG557 is a selective CB2R agonist, with a Ki of 54.6 nM. ISAM-CG557 reduces intracellular ROS levels and caspase activity. ISAM-CG557 exhibits significant MAPK bias and moderate G-protein bias, with CB2R EC50s of 0.60 nM (cAMP), 60.9 nM (β-arrestin) and 0.03 nM (MAPK). ISAM-CG557 exerts potent anti-inflammatory effects by reducing pro-inflammatory cytokines and increasing anti-inflammatory cytokines in cells. ISAM-CG557 can be used for the study of neuroinflammatory and neurodegenerative disorders.
    ISAM-CG557
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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