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-P10276
    Ac-VAD-AFC
    Ac-VAD-AFC is a fluorescent substrate for caspases and can be used to test the activity of caspases.
    Ac-VAD-AFC
  • HY-N3584R
    Paris saponin VII (Standard)
    		Inhibitor
    Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia.
    Paris saponin VII (Standard)
  • HY-13610
    N1,N11-Diethylnorspermine
    		Activator
    N1,N11-Diethylnorspermine is a synthetic analog of the naturally occurring polyamine spermine, can induce polyamine depletion and inhibit tumor cell growth. N1,N11-Diethylnorspermine activates polyamine catabolism and downregulates mTOR protein. N1,N11-Diethylnorspermine induces the release of cytochrome c from mitochondria, resulting in activation of caspase 3. N1,N11-Diethylnorspermine tetrahydrochloride kills glioblastoma multiforme (GBM) through induction of SSAT (spermidine/spermine N1-acetyltransferase) coupled with H2O2 production.
    N1,N11-Diethylnorspermine
  • HY-175037
    DNH28
    		Agonist
    DNH28 is a potent NF-κB and MAPK inhibitor with an IC50 of 0.93 μM against HepG2 cells. DNH28 promotes apoptosis by down-regulating the expression of Bcl-2, up-regulating the expression of BAX and Cleaved-caspase-3. DNH28 blocks the cell cycle and inhibits migration. DNH28 can be used for the study of hepatocellular carcinoma (HCC).
    DNH28
  • HY-RS01949
    CASP2 Human Pre-designed siRNA Set A
    		Inhibitor

    CASP2 Human Pre-designed siRNA Set A contains three designed siRNAs for CASP2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    CASP2 Human Pre-designed siRNA Set A
  • HY-10396A
    (2R,3S)-Emricasan
    		Inhibitor
    (2R,3S)-Emricasan ((2R,3S)-PF 03491390) is an isomer of Emricasan (HY-10396). Emricasan is an orally active and irreversible pan-caspase inhibitor. Emricasan inhibits Zika virus (ZIKV)-induced increases in caspase-3 activity and protected human cortical neural progenitors.
    (2R,3S)-Emricasan
  • HY-RS01953
    Casp3 Mouse Pre-designed siRNA Set A
    		Inhibitor

    Casp3 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Casp3 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
    Casp3 Mouse Pre-designed siRNA Set A
  • HY-P991235
    FS102
    		Activator
    FS102 is a selective Fc fragment with antigen binding (Fcab) that targets HER2 with a KD value of 0.8 nM. FS102 induces the degradation of HER2, activates Caspase 3/7 and disrupts the integrity of the cell membrane, triggering apoptosis of tumor cells. FS102 is promising for research of cancers such as breast cancer, gastric cancer, and colorectal cancer.
    FS102
  • HY-P10939
    Ac-DMLD-CMK
    		Inhibitor
    Ac-DMLD-CMK is a polypeptide targeting the mouse caspase 3-Gsdme signaling pathway. Ac-DMLD-CMK can specifically inhibit the activation of caspase 3 and Gsdme. Ac-DMLD-CMK blocks the cleavage of Gsdme by caspase 3, inhibits the occurrence of pyroptosis, thereby reducing renal tubular epithelial cell injury and the secretion of inflammatory cytokines. Ac-DMLD-CMK reduces the levels of serum creatinine and blood urea nitrogen in mice induced by Cisplatin (HY-17394) and alleviates the deterioration of kidney function. Ac-DMLD-CMK is promising for research of chemotherapy drug-induced nephrotoxicity.
    Ac-DMLD-CMK
  • HY-152748
    Caspase-3/7 activator 1
    		Activator
    Caspase-3/7 activator 1 is an effective activator of Caspase-3/7. Caspase-3/7 activator 1 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability.
    Caspase-3/7 activator 1
  • HY-179044
    MKK7-JNK activator 1
    		Activator
    MKK7-JNK activator 1 (Compound 10) is a MKK7-JNK pathway activator. MKK7-JNK activator 1 effectively inhibits the proliferation and migration of MDA-MB-468 cells, induces G2/M phase arrest and caspase -dependent apoptosis (independent of ROS production). MKK7-JNK activator 1 significantly increases the levels of p-MKK7 and p-JNK, but does not affect p-ERK or p-p38. MKK7-JNK activator 1 can be used for the study of triple-negative breast cancer (TNBC).
    MKK7-JNK activator 1
  • HY-178951
    STING-IN-17
    		Inhibitor
    STING-IN-17 is an orally active STING (human STING IC50 = 29 nM, mouse STING IC50 = 15 nM) inhibitor. STING-IN-17 can inhibit the phosphorylation of STING, TBK1 and IRF3. STING-IN-17 dose dependently inhibits the mRNA expression of IP10, IFNB1 and ISG56. STING-IN-17 can reduce ROS and inhibit the expression of cleaved-PARP/caspase-3. STING-IN-17 can improve kidney function. STING-IN-17 can be used for research on inflammatory conditions such as acute kidney injury.
    STING-IN-17
  • HY-131203
    PROTAC BRD4 Degrader-6
    		Activator
    PROTAC BRD4 Degrader-6 (compound 32a) is a potent small-molecule BRD4PROTAC degrader with IC50 value of 2.7 nM for BRD4 BD1. PROTAC BRD4 Degrader-6 potently degrades BRD4 protein and inhibits the expression of c-Myc. PROTAC BRD4 Degrader-6 inhibits the proliferation of pancreatic cancer cell line BxPC3 and induces apoptosis. PROTAC BRD4 Degrader-6 can be used for human pancreatic cancer research (Pink: Mivebresib (HY-100015); Black: linker, Azido-PEG1-CH2CO2H (HY-108369); Blue: Lenalidomide (HY-A0003)).
    PROTAC BRD4 Degrader-6
  • HY-149331
    TNF-α-IN-11
    		Inhibitor
    TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor with a KD value of 12.06 μM. TNF-α-IN-11 binds to TNF-α and blocks the activation of TNF-α-trigged caspase and NF-κB signaling pathway. TNF-α-IN-11 inhibits the phosphorylation of IκBα, as well as the nuclear translocation of NF κB p65. TNF-α-IN-11 can be used for research of TNF-α-mediated autoimmune diseases.
    TNF-α-IN-11
  • HY-W745905
    2'-Deoxyadenosine-15N1
    2'-Deoxyadenosine-15N1 is the 15N-labeled 2'-Deoxyadenosine (HY-W040329). 2′-Deoxyadenosine is an adenine nucleoside that inhibits glucose-stimulated insulin release. 2′-Deoxyadenosine inhibits glucose-stimulated increases seen in islet cyclic AMP (cAMP) accumulation. 2'-Deoxyadenosine activates caspase-3 and promotes apoptosis. 2'-Deoxyadenosine inhibits the activity of S-adenosyl-L-homocysteine hydrolase (SAHH). 2'-Deoxyadenosine inhibits the growth of various cells. 2'-Deoxyadenosine has an anticancer effect on colon cancer.
    2'-Deoxyadenosine-<sup>15</sup>N<sub>1</sub>
  • HY-150696
    Antitumor agent-72
    		Activator
    Antitumor agent-72 (compound 6w) is a potent anticancer agent. Antitumor agent-72 has anticancer activity and induces apoptosis through activation of caspase-3 and cleavage of PARP. Antitumor agent-72 can be used for cancer research.
    Antitumor agent-72
  • HY-155406
    Estrogen receptor modulator 10
    		Activator
    Estrogen receptor modulator 10 (compound G-5b) is an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 is developed based on the Fulvestrant (HY-13636) molecule and can rapidly degrade ER receptors through the proteasome pathway. Estrogen receptor modulator 10 can induce cell apoptosis and block cells in the G1/G0 phase and can be used in cancer research.
    Estrogen receptor modulator 10
  • HY-172873
    HDSI-18
    		Activator
    HDSI-18 is an orally active HDAC6 selective inhibitor (IC50: 1.6 nM). HDSI-18 is cytotoxic to K562, MV4-11, MOLM-13, THP-1, and Jurkat cells (IC50: 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively). HDSI-18 activates Caspase-3, induces mitochondrial depolarization and apoptosis, and has antitumor activity.
    HDSI-18
  • HY-170999
    Antitumor agent-196
    Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer activity, showing an IC50 of 90 nM against MCF-7 breast cancer cells. Antitumor agent-196 promotes Apoptosis by regulating the Bax-caspase 3 signaling pathway, and induces Ferroptosis through the modulation of key signaling molecules, including GPX4. Antitumor agent-196 holds promising potential for further research in the field of cancer therapy.
    Antitumor agent-196
  • HY-N2302R
    Fucoxanthin (Standard)
    Fucoxanthin (Standard) is the analytical standard of Fucoxanthin. This product is intended for research and analytical applications. Fucoxanthin (all-trans-Fucoxanthin) is a marine carotenoid and shows anti-obesity, anti-diabetic, anti-oxidant, anti-inflammatory and anticancer activities.
    Fucoxanthin (Standard)
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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