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-W750678
    9-cis-Canthaxanthin
    		Inhibitor
    9-cis-Canthaxanthin is a carotenoid with pro-apoptotic activity in THP-1 macrophage cells. 9-cis-Canthaxanthin induces cell apoptosis by increasing caspase-3 and caspase-8 activity.
    9-cis-Canthaxanthin
  • HY-157992
    LM-021
    		Inhibitor 98.27%
    LM-021 is a coumarin-chalcone derivative with anti-aggregatory, antioxidant, neuroprotective and anti-inflammatory properties which suppresses nitric oxide (NO), IL-1β, IL-6, TNF-α production, CD68 antigen (CD68) and histocompatibility-2 (MHCII) expression. LM-021 also attenuates the increase of caspase 1 activity, lactate dehydrogenase release and ROS level. LM-021 can be used for neurological research.
    LM-021
  • HY-N6777R
    Penicillic acid (Standard)
    		Inhibitor
    Tetracaine (hydrochloride) (Standard) is the analytical standard of Tetracaine (hydrochloride). This product is intended for research and analytical applications. Tetracaine hydrochloride (Amethocaine hydrochloride) is a calcium channel protein inhibitor and blocks voltage-sensitive release of Ca2+ from sarcoplasmic reticulum. Tetracaine hydrochloride is mainly used topically in ophthalmology and as an antipruritic.
    Penicillic acid (Standard)
  • HY-P10450
    (Asp)2-Rhodamine 110
    (Asp)2-Rhodamine 110 (D2R) is a fluorescent caspase substrate.
    (Asp)2-Rhodamine 110
  • HY-158328A
    CA IX/VEGFR-2-IN-2
    		Activator
    CA IX/VEGFR-2-IN-2 (compound 5e) is a dual-targeted inhibitor. CA IX/VEGFR-2-IN-2 shows strong inhibitory effects on both CA IX (Ki=3.1 μM) and VEGFR-2 (IC50=32.1 nM). CA IX/VEGFR-2-IN-2 can be used for the study of pancreatic (PANC1), breast cancer (MCF7) and prostate cancer (PC3) .
    CA IX/VEGFR-2-IN-2
  • HY-N7015R
    Zerumbone (Standard)
    Zerumbone (Standard) is the analytical standard of Zerumbone. This product is intended for research and analytical applications. Zerumbone is an orally active natural cyclic sesquiterpene and can be isolated from Zingiber zerumbet. Zerumbone has anti-proliferative, anti-inflammation, anti-cancer, anti-bacterial and anti-mutagenic activity.
    Zerumbone (Standard)
  • HY-174312
    NLRP3-IN-81
    		Inhibitor
    NLRP3-IN-81 (N102) is a BBB-penetrable inhibitor against NLRP3 inflammasome-dependent pyroptosis with an EC50 of 0.029 μM against cell pyroptosis induced by Nigericin (HY-127019). NLRP3-IN-81 potently inhibits NLRP3-dependent activation of caspase-1 and the release of IL-1β. NLRP3-IN-81 disturbs the interaction of NLRP3 with the adaptor protein ASC and inhibits ASC oligomerization. NLRP3-IN-81 can be used for pyroptosis-related diseases research, such as inflammatory bowel diseases and type 2 diabetes.
    NLRP3-IN-81
  • HY-W710827
    N,N'-Methylenebisacrylamide-d6
    N,N'-Methylenebisacrylamide-d6 is the deuterium labeled N,N'-Methylenebisacrylamide (HY-D0848). N,N'-Methylenebisacrylamide (Bisacrylamide) is an orally active acrylamide dimer and crosslinker. N,N'-Methylenebisacrylamide increases CYP2E1, P53, cleaved caspase-3. N,N'-Methylenebisacrylamide promotes hepatic cancer. N,N'-Methylenebisacrylamide changes sperm abnormality rate and sperm count. N,N'-Methylenebisacrylamide decreases the number of various cells in the blood as well as induces liver and testicular damage. N,N'-Methylenebisacrylamide is used to prepare polyacrylamide gel.
    N,N'-Methylenebisacrylamide-d<sub>6</sub>
  • HY-W011683S2
    2'-Deoxyadenosine monohydrate-3′-13C
    		Activator
    2'-Deoxyadenosine monohydrate-3′-13C is the 13C labeled 2'-Deoxyadenosine monohydrate (HY-W011683)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-3′-<sup>13</sup>C
  • HY-N8423R
    α-Amyrin (Standard)
    		Inducer
    α-Amyrin (Standard) is a pentacyclic triterpenoid compound with oral activity. α-Amyrin (Standard) activates the ERK and GSK-3β signaling pathways. α-Amyrin (Standard) can inhibit cancer cells proliferation and induce apoptosis. α-Amyrin (Standard) shows anti-bacterial and anti-inflammation activity. α-Amyrin (Standard) can reduce blood glucose level. α-Amyrin (Standard) can be used for the researches of cancer, infection, inflammation, metabolic disease and neurological disease, such as breast cancer, Streptococcus oralis infection, skin inflammation and diabetes.
    α-Amyrin (Standard)
  • HY-175885
    PROTAC FTO degrader 1
    		Inducer
    PROTAC FTO degrader 1 is a Fat Mass and Obesity-associated Protein (FTO) PROTAC degrader. PROTAC FTO degrader 1 selectively degrades FTO depending on VHL E3 ligase and ubiquitin-proteasome system. PROTAC FTO degrader 1 can increase m6A modifications on mRNAs associated with ribosome biogenesis and promote their YTHDF2-mediated decay. PROTAC FTO degrader 1 can inhibit cancer cells proliferation and induce apoptosis. PROTAC FTO degrader 1 can be used for the research of cancer, such as acute myeloid leukemia (AML). (Structure Note: Pink: FTO ligand (HY-175886); Blue: VHL ligand (HY-112078); Black: linker (HY-W002042); VHL ligand-Linker: (HY-139218))
    PROTAC FTO degrader 1
  • HY-W713878
    Ac-VDVAD-pNA
    Ac-VDVAD-pNA is a caspase-2 substrate. Ac-VDVAD-pNA can be used to test the activity of caspase-2.
    Ac-VDVAD-pNA
  • HY-16658BG
    Z-VAD-FMK (GMP)
    		Inhibitor
    Z-VAD-FMK (GMP) is Z-VAD-FMK (HY-16658B) in GMP grade. GMP-grade small molecules can be used as auxiliary reagents in cell therapy. Z-VAD-FMK (Z-VAD(OH)-FMK) is a well-know pan caspase inhibitor, which does not inhibit ubiquitin carboxy-terminal hydrolase L1 (UCHL1) activity even at concentrations as high as 440 μM.
    Z-VAD-FMK (GMP)
  • HY-155822
    TZ3O
    		Inhibitor 98.17%
    TZ3O is an anticholinergic agent with neuroprotective effects. TZ3O inhibits acetylcholinesterase (AChE) activity in human plasma with an IC50 of 304.5 μM. TZ3O can improve memory impairment and cognitive decline in rats in the Scopolamine (HY-N0296)-induced Alzheimer-type model. TZ3O could be used in Alzheimer’s research.
    TZ3O
  • HY-174377
    PeS-9
    		Activator

    PeS-9 is an Androgen Receptor (AR) degrader that induces androgen receptor degradation PeS-9 induces mitochondrial and ER stress by promoting cytotoxic ROS production, leading to the release of mitochondrial cytochrome C and AIF. PeS-9 subsequently activates caspases-9 and -3, causing DNA fragmentation and apoptotic cell death. PeS-9 has anticancer activity against prostate cancer and exerts in vivo antitumor and antimetastatic activity with minor side effects. PeS-9 can be used for the study of targeting monotherapy against GLUT-1-overexpressing tumors.
    PeS-9
  • HY-178022
    HDAC6-IN-63
    		Activator
    HDAC6-IN-63 (Compound 7) is an orally active HDAC6 inhibitor with an IC50 of 145  nM. HDAC6-IN-63 inhibits the expression of Sp1 and RAD51, thereby inducing Caspase-dependent apoptosis. HDAC6-IN-63 has antitumor activity and sensitizes Etoposide (HY-13629) and Gemcitabine (HY-17026), promoting synergistic death of NSCLC cells through the inhibition of homologous recombination and non-homologous end joining (NHEJ) pathways involved in DNA DSB repair. HDAC6-IN-63 can be used for chemotherapy of cancers like NSCLC research.
    HDAC6-IN-63
  • HY-168623
    EGFR-IN-134
    		Activator
    EGFR-IN-134 (compound 3f), a triazolo[3,4-a]isoquinoline derivative, is a potent EGFR inhibitor with an IC50 of 0.023 µM. EGFR-IN-134 induces apoptosis and necrosis. EGFR-IN-134 initiates cell cycle arrest at the G2/M and pre-G1 phases, downregulates anti-apoptotic protein Bcl2 and upregulates pro-apoptotic proteins: p53, Bax, and caspases 3, 8, and 9. EGFR-IN-134 shows antiproliferative and anticancer activity.
    EGFR-IN-134
  • HY-176269
    VS1150
    VS1150 (Compound 11) is a BCR-ABL-targeting phosphorylation-inducing chimeric small molecule (PHICS). VS1150 significantly inhibits oncogenic kinase BCR-ABL signaling by inducing inhibitory phosphorylation at its Y253 (EC50: 69 nM), subsequently triggering cell apoptosis. VS1150 also inhibits other oncogenic ABL fusions and drug-resistant mutants like T315I. VS1150 can be used for chronic myeloid leukemia (CML) and other ABL fusion-driven cancers research.
    VS1150
  • HY-146461
    Anticancer agent 58
    		Activator
    Anticancer agent 58 (compound 16) has inhibitory activity against kinds of cancer cell lines, especially in A549 and T24 with IC50s of 0.6 μM and 0.7 μM, respectively. Anticancer agent 58 induces apoptosis by activating caspase 3/8/9 activity, and induces an increase of Ca2+ and ROS in cancer cells. Anticancer agent 58 significantly decreases mitochondrial membrane potential. Anticancer agent 58 can suppress tumor growth in T24 mouse xenograft model.
    Anticancer agent 58
  • HY-145087A
    NP3-146 sodium
    		Inhibitor 99.26%
    NP3-146 sodium is a NLRP3 inflammasome inhibitor through locking the NACHT domain of NLRP3. NP3-146 sodium shows potent inhibitory activity against IL-1β release with an IC50 value of 0.171 μM in LPS (HY-D1056)/Nigericin (HY-127019)-stimulated BMDM cells. NP3-146 sodium regulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants. NP3-146 sodium can be used for the research of inflammatory diseases.
    NP3-146 sodium
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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