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-120339
    STK899704
    		Activator
    STK899704 is a tubulin polymerization inhibitor. STK899704 exhibits broad-spectrum inhibitory activity against various cancer cell lines with IC50 values ​​ranging from 0.2 to 1.0 μM. STK899704 disrupts the mitotic spindle structure, inducing G2/M phase cell cycle arrest. STK899704 inhibits the migration ability of HT29 cells by downregulating the FAK-MEK-ERK signaling pathway, thereby suppressing the expression and activity of MMP-2 and MMP-9. STK899704 activates caspase-3/7/8/9, leading to PARP cleavage and inducing apoptosis. STK899704 induces cellular senescence through the p53 pathway. STK899704 can be used in research on skin cancer, lung cancer, colon cancer, and other cancers.
    STK899704
  • HY-N12669
    Curcumin monoglucoside
    		Inhibitor
    Curcumin monoglucoside is a flavonoid derivative possessing antioxidant, anti-apoptotic, neuroprotective effects, and antibacterial activity. Curcumin monoglucoside can be used in research on Parkinson's disease.
    Curcumin monoglucoside
  • HY-N7719R
    Oosporein (Standard)
    		Activator
    Oosporein (Standard) is the analytical standard of Oosporein (HY-N7719). This product is intended for research and analytical applications. Oosporein is a microbial metabolite and a red crystalline toxin produced by various fungi. Oosporein can promote the reproduction of fungi in host bodies by inhibiting insect immunity, and possesses multiple activities such as antibacterial, antiviral (HSV), and insecticidal effects. Oosporein can inhibit plant growth. In addition, Oosporein can also induce apoptosis, cell membrane damage, oxidative stress, and mitochondrial damage. Oosporein has certain antitumor activity.
    Oosporein (Standard)
  • HY-19696AR
    Tauroursodeoxycholate sodium (Standard)
    		Inhibitor
    Tauroursodeoxycholate (sodium) (Standard) is the analytical standard of Tauroursodeoxycholate (sodium). This product is intended for research and analytical applications. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TUDCA) sodium 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 sodium (Standard)
  • HY-175010
    STAT3-IN-44
    		Agonist
    STAT3-IN-44 is a potent STAT3 inhibitor with IC50s of 1.84 (C6 cells) and 4.81 μM (A549 cells). STAT3-IN-44 inhibits STAT3 phosphorylation, downregulates Bcl-2, and upregulates Caspase-3 to promote late-stage apoptosis. STAT3-IN-44 significantly suppresses tumor cell proliferation and migration. STAT3-IN-44 can be used for the study of cancers such as glioma and lung cancer.
    STAT3-IN-44
  • HY-P5955
    Ac-AAVALLPAVLLALLAP-LEVD-CHO
    		Inhibitor
    Ac-AAVALLPAVLLALLAP-LEVD-CHO is a cell-permeable caspase-4 inhibitor that has antitumor activity.
    Ac-AAVALLPAVLLALLAP-LEVD-CHO
  • HY-RS01970
    Casp9 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Casp9 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Casp9 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Casp9 Mouse Pre-designed siRNA Set A
  • HY-P10326
    Z-ATAD-FMK
    		Inhibitor
    Z-ATAD-FMK is an inhibitor of caspase-12. Z-ATAD-FMK is an inhibitor of caspase-12. Z-ATAD-FMK prevents endoplasmic reticulum stress-mediated apoptosis by inhibiting the activity of caspase-12 and reducing the activity of caspase-9.
    Z-ATAD-FMK
  • HY-144791
    Bcl-2-IN-6
    		Activator
    Bcl-2-IN-6 (compound 10) is a potent Bcl-2 (B-cell lymphoma-2) inhibitor. Bcl-2-IN-7 down-regulates the expression of Bcl-2, and increases the expression of p53, Bax, and caspase-7 mRNA. Bcl-2-IN-7 induces cell cycle arrest and apoptosis in breast cancer MCF-7 cells. Bcl-2-IN-7 shows good anticancer activity, with IC50 values of 20.91, 22.30, 42.29, and 48.00 μM against MCF-7, LoVo, HepG2, and A549 cell lines, respectively.
    Bcl-2-IN-6
  • HY-143265
    Topoisomerase I inhibitor 2
    		Inducer
    Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect.
    Topoisomerase I inhibitor 2
  • HY-178099
    Apoptosis inducer 45
    		Agonist
    Apoptosis inducer 45 is an apoptosis inducer. Apoptosis inducer 45 is cytotoxically active against the MCF-7 cell line. Apoptosis inducer 45 elicits MCF-7 cell apoptosis via the mitochondrial pathway (increases the Bax/Bcl-2 ratio) by activating cleavage of caspase-9, thereby inducing the fragmentation of DNA repair protein PARP. Apoptosis inducer 45 also can induce caspase-8 cleavage, subsequently initiating cleavage of caspase-3 and its downstream protein PARP to culminate in the extrinsic apoptosis. Apoptosis inducer 45 can be used in the research of breast cancer.
    Apoptosis inducer 45
  • HY-P1333A
    Dynorphin A TFA
    		Activator
    Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease.
    Dynorphin A TFA
  • HY-118304A
    AKN-028 TFA
    		Activator
    AKN-028 TFA, a novel tyrosine kinase (TK) inhibitor, is a potent, orally active FMS-like receptor tyrosine kinase 3 (FLT3) inhibitor with an IC50 value of 6 nM. AKN-028 TFA inhibits FLT3 autophosphorylation. AKN-028 TFA induces dose-dependent cytotoxic response (mean IC50=1 μM). AKN-028 TFA induces apoptosisby activation of caspase 3. AKN-028 TFA can be used in research of acute myeloid leukemia (AML).
    AKN-028 TFA
  • HY-178142
    Multi-kinase-IN-7
    		Agonist
    Multi-kinase-IN-7 is a multikinase inhibitor with IC50s of 2.19, 2.95, 3.59 and 9.31 μM against EGFR, VEGFR2, TrKA and CDK2, respectively. Multi-kinase-IN-7 shows moderate and weaker activity against FAK, AKT1, GSK3β and CDK5 with IC50 values of 6.3, 9.2, 11.7 and 23.4 μM, respectively. Multi-kinase-IN-7 displays broad spectrum anti­proliferative potential against NCI cancer cell lines. Multi-kinase-IN-7 induces cell cycle arrest, apoptosis and necrosis. Multi-kinase-IN-7 Inhibitor can be used for the study of breast cancer.
    Multi-kinase-IN-7
  • HY-172623
    EGFR/HER2-IN-17
    		Activator
    EGFR/HER2-IN-17 (Compound 7h) is a dual inhibitor of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2). EGFR/HER2-IN-17 inhibits cancer cell proliferation. EGFR/HER2-IN-17 interacts with the binding pockets of EGFR and HER2, activating caspase-3 and caspase-8, and decreases the expression of Bcl-2, thereby inducing apoptosis. EGFR/HER2-IN-17 is promising for research of cancers.
    EGFR/HER2-IN-17
  • HY-RS01959
    CASP6 Human Pre-designed siRNA Set A
    		Inhibitor

    CASP6 Human Pre-designed siRNA Set A contains three designed siRNAs for CASP6 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CASP6 Human Pre-designed siRNA Set A
  • HY-B0739R
    Citicoline (Standard)
    		Inhibitor
    Citicoline (Cytidine diphosphate-choline) (Standard) is the analytical standard of Citicoline. This product is intended for research and analytical applications. Citicoline is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline inhibits reactive oxygen species (ROS) and apoptosis. Citicoline can be used for neurological disease and hearing loss study.
    Citicoline (Standard)
  • HY-123786
    NSC745887
    		Activator
    NSC745887 (compound 25) is an inhibitor that targets DNA topoisomerase cleavage, activates the caspase-8/9-caspase-3-poly (ADP-ribose) polymerase cascade, and induces apoptosis in cancer cells. NSC745887 enhances γH2AX expression and causes DNA fragmentation leading to DNA damage.
    NSC745887
  • HY-W650842
    Boc-Asp(OBzl)-CMK
    		Inhibitor
    Boc-Asp(OBzl)-CMK is an inhibitor for IL-1 converting enzyme (ICE, caspase1). Boc-Asp(OBzl)-CMK prevents death of CHP100 neuroblastoma cell, and IL-1β release elicited by the viral coat protein.
    Boc-Asp(OBzl)-CMK
  • HY-P1001A
    Ac-DEVD-CHO TFA
    		Inhibitor
    Ac-DEVD-CHO TFA is a peptide inhibitor of caspase-3 (Ki=230 pM) and caspase-7. Ac-DEVD-CHO TFA reduces caspase-3 activity and apoptosis induced by Prostaglandin E2 (HY-101952) in rat cortical neurons. Ac-DEVD-CHO TFA is promising for research of neurodegenerative diseases and cancers.
    Ac-DEVD-CHO TFA
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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