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-152758
    Caspase-3/7 activator 3
    		Activator
    Caspase-3/7 activator 3 is an effective activator of Caspase-3/7. Caspase-3/7 activator 3 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability.
    Caspase-3/7 activator 3
  • HY-B0347S1
    Lacidipine-13C8
    Lacidipine-13C8 is the deuterium labeled Lacidipine. Lacidipine is an orally active and highly selective L-type calcium channel blocker that acts on smooth muscle calcium channels, primarily dilates peripheral arteries, reduces peripheral resistance, and has long-lasting anti-hypertensive activity. Lacidipine protects HKCs from apoptosis induced by ATP depletion and recovery by modulating the caspase-3 pathway. Lacidipine can be used in studies of hypertension, atherosclerosis and acute kidney injury (AKI).
    Lacidipine-<sup>13</sup>C<sub>8</sub>
  • HY-B0835R
    Fenobucarb (Standard)
    		Activator
    Fenobucarb (Standard) is the analytical standard of Fenobucarb. This product is intended for research and analytical applications. Fenobucarb is a carbamate insecticide. Fenobucarb induces zebrafish developmental neurotoxicity through pathways involved in inflammation, oxidative stress, degeneration and apoptosis. Fenobucarb is a possible risk factor to cardiovascular and cerebrovascular systems in animals.
    Fenobucarb (Standard)
  • HY-P10454
    (Z-IETD)2-Rh 110
    (Z-IETD)2-Rh 110 is a fluorescent substrate of caspase-8 (λex= 488 nm, λem= 523 nm), which can be used to detect the activity of caspase-8 and the process of apoptosis.
    (Z-IETD)2-Rh 110
  • HY-164452
    A-1155905
    A-1155905 is a MCL-1 inhibitor (IC50=33.5 nM; Ki=0.58 nM) with anticancer activity. A-1155905 selectively binds to MCL-1 with sufficient affinity to disrupt the MCL-1-bim complex in living cells. A-1155905-induced death of MCL-1-dependent cell lines is caspase-dependent and occurs via apoptosis.
    A-1155905
  • HY-N0576R
    Solanesol (Standard)
    		Inhibitor
    Solanesol (Standard) is the analytical standard of Solanesol (HY-N0576). This product is intended for research and analytical applications. Solanesol is an orally active aliphatic terpene alcohol. Solanesol is mainly found in tobacco and other Solanaceae plants. Solanesol induces HO-1 and Hsp70 expression, activates p38 and Akt signaling pathways, and inhibits Apoptosis (reduces caspase-3 and PARP cleavage). Solanesol has antioxidant, anti-inflammatory, and neuroprotective activities. Solanesol can be used in the research of Huntington's disease, alcoholic liver disease, chronic inflammatory pain, anxiety, Alzheimer's disease, and bipolar disorder.
    Solanesol (Standard)
  • HY-P0110
    (Iso)-Z-VAD(OMe)-FMK
    		Control
    (Iso)-Z-VAD(OMe)-FMK ((Iso)-Z-Val-Ala-Asp(OMe)-FMK) is an isomer of the caspase and UCHL1 inhibitor Z-VAD(OMe)-FMK (HY-16658).
    (Iso)-Z-VAD(OMe)-FMK
  • HY-179052
    Apoptosis inducer 50
    		Activator
    Apoptosis inducer 50 (Compound 5e) is an apoptosis inducer as well as an autophagy inducer agent. Apoptosis inducer 50 exhibits potent and selective anti-cancer activity against triple-negative breast cancer cells and metastatic colon cancer cells. Apoptosis inducer 50 upregulates the expression of pro-apoptotic proteins (Bax, Bim, cleaved Caspase-9) and downregulates the expression of the anti-apoptotic protein (BCL-XL). Apoptosis inducer 50 upregulates key autophagy markers such as Beclin-1 and ATG5, and enhances the conversion of LC3-I to LC3-II., Apoptosis inducer 50 arrests cancer cells in the G1/S phase by upregulating the expression of p21 and p27 while downregulating Cyclin D1. Apoptosis inducer 50 increases the level of ROS.
    Apoptosis inducer 50
  • HY-178104
    HDAC-IN-93
    		Agonist
    HDAC-IN-93 is a HDAC inhibitor with promising total pan-HDAC inhibitory activity. HDAC-IN-93 demonstrates significant broad-spectrum antiproliferative activity across various cancer cell lines. HDAC-IN-93 induces cell apoptosis along with necrosis. HDAC-IN-93 can be used for the studies of prostate cancer and breast cancer.
    HDAC-IN-93
  • HY-120019A
    Ac-YVAD-CHO acetate
    		Inhibitor
    Ac-YVAD-CHO (L-709049) acetate is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO acetate is also a caspase-1 inhibitor. Ac-YVAD-CHO acetate can suppress the production of mature IL-lβ.
    Ac-YVAD-CHO acetate
  • HY-P5956
    Ac-AAVALLPAVLLALLAP-LEHD-CHO
    		Inhibitor
    Ac-AAVALLPAVLLALLAP-LEHD-CHO is an inhibitor of caspases 4, 5 and 9. Ac-AAVALLPAVLLALLAP-LEHD-CHO shows protective effects upon Neocarzinostatin (HY-111183)-treated MCF-7 cells.
    Ac-AAVALLPAVLLALLAP-LEHD-CHO
  • HY-P0034
    Ac-DEVD-CMK
    		Inhibitor
    Ac-DEVD-CMK (Caspase-3 Inhibitor III) is a selective and irreversible caspase-3 inhibitor. Ac-DEVD-CMK significantly inhibits apoptosis induced by high levels of glucose or Ingenol 3,20-dibenzoate?(HY-137295). Ac-DEVD-CMK can be used in a variety of experimental approaches to inhibit apoptosis.
    Ac-DEVD-CMK
  • HY-147504
    Anticancer agent 63
    		Modulator
    Anticancer agent 63 (compound 3h) shows active in reducing the viability of different cancer cell lines, including SW480, HeLa, A549 and MCF-7, with IC50 values at 24 h of 4.9, 11.5, 9.4, and 3.4 μM, respectively. Anticancer agent 63 induce apoptosis in MCF-7 cells via down-regulating the expression of Bcl-2 and up-regulating the expression of IL-2 and Caspase-3. Anticancer agent 63 also shows antioxidant activity.
    Anticancer agent 63
  • HY-161076
    KTt-45
    KTt-45 is a T-type calcium channel blocker. KTt-45 has anticancer effect by inducing apoptosis on HeLa cervical cancer cell line.
    KTt-45
  • HY-176283
    Tubulin/LSD1-IN-1
    		Inducer
    Tubulin/LSD1-IN-1 is an effective dual inhibitor of Tubulin polymerization and LSD1 (IC50 = 1.72 μM). Tubulin/LSD1-IN-1 has broad-spectrum antiproliferative activity against cancer cell lines. Tubulin/LSD1-IN-1 inhibits tubulin polymerization by targeting colchicine binding sites, thereby disrupting the microtubule network in gastric cancer cells. Tubulin/LSD1-IN-1 increases the methylation levels of H3K4me1/2 and H3K9me2/3, thereby achieving epigenetic regulation. Tubulin/LSD1-IN-1 induces G2/M arrest, promotes apoptosis, and effectively inhibits colony formation of gastric cancer cells.
    Tubulin/LSD1-IN-1
  • HY-P991570
    Zaptuzumab
    		Inhibitor
    Zaptuzumab (AD5-10) is a DR5-specific humanized monoclonal antibody that selectively binds to DR5 with high affinity. Zaptuzumab specifically induces cancer cell death by both caspase-apoptosis and autophagic cell death (ACD). Zaptuzumab activates both ADCC and CDC. Zaptuzumab induces ROS generation and GSH level reduction. Zaptuzumab shows a significant suppression of the tumor growth and good safety in various xenografts mice tumor models.
    Zaptuzumab
  • HY-N0281R
    Daphnetin (Standard)
    		Inducer
    Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research.
    Daphnetin (Standard)
  • HY-134567
    Ac-VDVAD-CHO
    		Inhibitor
    Ac-VDVAD-CHO is a caspase-2/3 inhibitor (IC50: 46 and 15 nM).
    Ac-VDVAD-CHO
  • HY-P4535
    Ac-Trp-Glu-His-Asp-Aldehyde
    		Inhibitor
    Ac-Trp-Glu-His-Asp-Aldehyde is a potent and selective caspase-1 inhibitor with a Ki value of 56 pM.
    Ac-Trp-Glu-His-Asp-Aldehyde
  • HY-RS01951
    Casp2 Rat Pre-designed siRNA Set A
    		Inhibitor

    Casp2 Rat Pre-designed siRNA Set A contains three designed siRNAs for Casp2 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Casp2 Rat Pre-designed siRNA Set A
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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