1. Signaling Pathways
  2. Apoptosis
  3. Caspase

Caspase

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-175381
    DeFer-2
    Agonist 98.25%
    DeFer-2 is a ferritin PROTAC degrader (Kd = 17.1 μM). DeFer-2 induces ferritin degradation, triggering caspase 3-GSDME-mediated pyroptosis in cancer cells through free iron accumulation and elevated ROS. DeFer-2 significantly inhibits tumor growth and prolongs survival in mice bearing B16F10 subcutaneous tumors. DeFer-2 can be used to study melanoma. (Pink: Oleic acid: HY-N1446, Blue: (S,R,S)-AHPC: HY-125845, Black: γ-Aminobutyric acid: HY-N0067, Blue + Black: (S,R,S)-AHPC-C3-NH2: HY-130711).
    DeFer-2
  • HY-157343B
    GD3 Ganglioside ammonium
    Activator ≥98.0%
    GD3 Ganglioside ammonium is an Apoptosis inducer and biomarker for mouse neural stem cells. GD3 Ganglioside ammonium expresses in neural stem cells and the subventricular zone of the adult mouse brain. GD3 Ganglioside ammonium targets the mitochondrial permeability transition pore complex, induces pore opening, dissipates mitochondrial transmembrane potential, triggers Mitochondrial swelling, releases pro-apoptotic factors, and activates Caspase-9. GD3 Ganglioside ammonium is applicable to research related to glioblastoma.
    GD3 Ganglioside ammonium
  • HY-P4890A
    Relaxin H3 (human) TFA
    Inhibitor
    Relaxin H3 (human) TFA is a relaxin peptide with anti-inflammatory, anti-apoptotic, anti-pyroptotic, anti-migratory, protective and anti-fibrotic activities. Relaxin H3 (human) TFA acts on RXFP1 to generate cAMP and reduce the levels of ATP and ROS. Relaxin H3 (human) TFA inhibits renal inflammatory pyroptosis (pyroptosis), NLRP3 inflammasome activation, caspase-1 activation, IL-1β/IL-18 secretion, collagen synthesis, TGF-β1 signaling pathway, Smad2 phosphorylation, myofibroblast differentiation, TIMP expression, and HRMEC migration. Relaxin H3 (human) TFA activates AMPK, upregulates MFN2 expression, improves mitochondrial quality control and membrane potential, inhibits apoptosis (apoptosis) and pyroptosis, restores retinal ultrastructure, and reverses excessive left ventricular collagen expression. Relaxin H3 (human) TFA can be used in studies related to kidney stones, nephrocalcinosis, diabetic cardiomyopathy, fibrotic cardiomyopathy, and diabetic retinopathy.
    Relaxin H3 (human) TFA
  • HY-170935
    SRSF1-IN-1
    Activator
    SRSF1-IN-1 is a SRSF1 inhibitor. SRSF1-IN-1 inhibits SRSF1 expression, thereby modulating the splicing of Bcl-x pre-mRNA. SRSF1-IN-1 inhibits the proliferation of various cancer cells. SRSF1-IN-1 induces apoptosis in gastric cancer cells, reduces Bcl-xl expression, and upregulates cleaved PARP and caspase 3. SRSF1-IN-1 induces autophagy and promotes cell death. SRSF1-IN-1 exhibits anti-tumor activity in a mouse gastric cancer xenograft model. SRSF1-IN-1 can be used for the research of various cancers including liver cancer, gastric cancer, breast cancer, colon cancer, glioma, and melanoma.
    SRSF1-IN-1
  • HY-P4449
    Ac-VRPR-AMC
    Ac-VRPR-AMC is a fluorogenic metacaspase substrate. Ac-VRPR-AMC can be used to tests metacaspase activity.
    Ac-VRPR-AMC
  • HY-N6651
    Isocryptotanshinone
    ≥98.0%
    Isocryptotanshinone is a dual STAT3 and PTP1B (IC50 = 56.1 μM) inhibitor. Isocryptotanshinone inhibits STAT3 by binding to the STAT3 SH2 domain to block phosphorylation and nuclear translocation[1][2]. Isocryptotanshinone exerts its anti-proliferative effect via the induction of cell cycle arrest, apoptosis, and pro-death autophagy, through the regulation of STAT3, AKT/mTOR and MAPK signaling pathways. Isocryptotanshinone suppresses the xenograft gastric cancer (GC) tumor growth in BALB/c nude mice. Isocryptotanshinone can be used for cancer research, such as lung cancer, breast cancer and GC.
    Isocryptotanshinone
  • 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)
  • HY-P10145
    Ac-LEVD-pNA
    99.17%
    Ac-LEVD-pNA is a chromogenic substrate for caspase-4 and can be used to detect caspase-4 activity.
    Ac-LEVD-pNA
  • HY-147889
    BBR-BODIPY
    Activator 98.15%
    BBR-BODIPY is a fluorescent probe that allows screening its interaction with the targeted cells. BBR-BODIPY induces apoptosis and changes the expression of apoptosis-related proteins.
    BBR-BODIPY
  • HY-N5033
    17-Hydroxy sprengerinin C
    Inhibitor 99.68%
    17-Hydroxy sprengerinin C (compound 10) is a glycoside compound isolated from rhizomes of Polygonatum sibiricum. 17-Hydroxy sprengerinin C possesses stronger anticancer activities. 17-Hydroxy sprengerinin C reduces the expression of Blc-2 and pro-caspase3 and increases the production of Bax.
    17-Hydroxy sprengerinin C
  • HY-N1423S1
    Glycocholic acid-d5
    Activator 99.9%
    Glycocholic acid-d5 is the deuterium labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-d<sub>5</sub>
  • HY-B0762R
    Acetyl-L-carnitine hydrochloride (Standard)
    Inhibitor
    Acetyl-L-carnitine hydrochloride (Standard) is the analytical standard of Acetyl-L-carnitine hydrochloride. This product is intended for research and analytical applications. Acetyl-L-carnitine (O-Acetyl-L-carnitine; ALCAR) hydrochloride is an orally active mitochondrial energy metabolism regulator and neuroprotectant that can penetrate the blood-brain barrier. Acetyl-L-carnitine hydrochloride selectively enters cells and the brain through the organic cation transporter OCTN2. Acetyl-L-carnitine hydrochloride can participate in fatty acid β-oxidation, promote acetylcholine synthesis, regulate mitochondrial function and inhibit oxidative stress as an acetyl donor. Acetyl-L-carnitine hydrochloride exerts its activity by enhancing energy metabolism, protecting neurons and improving synaptic plasticity. Acetyl-L-carnitine hydrochloride is mainly used in the study of neurodegenerative diseases and metabolic disorder-related diseases such as neonatal hypoxic-ischemic brain damage, Alzheimer's disease, and depression.
    Acetyl-L-carnitine hydrochloride (Standard)
  • HY-N2199
    Sotetsuflavone
    Modulator
    Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits phosphorylation of PI3K, Akt, mTOR, JNK, and p38 MAPK; modulates expression of Cyclin D1, CDK4, Bcl-2, Bax, cleaved caspases 3/9, MMP-9, TGF-β, STAT3, and β-catenin. Sotetsuflavone induces G0/G1 cell cycle arrest, apoptosis, autophagy, and intracellular ROS elevation, inhibits cancer cell proliferation. Sotetsuflavone inhibits tumor growth in mouse tumor xenograft models. Sotetsuflavone can be used for the research of non-small cell lung cancer and Crohn’s disease.
    Sotetsuflavone
  • HY-P5890A
    YVAD-CHO TFA
    Inhibitor 98.48%
    YVAD-CHO TFA is an interleukin-1β converting enzyme (ICE, caspase 1) inhibitor (Ki: 0.76 nM). YVAD-CHO TFA inhibits mature IL-1β production. YVAD-CHO TFA partially delays motoneurone death in lesioned facial nerve mice.
    YVAD-CHO TFA
  • HY-14942A
    Berubicin hydrochloride
    Agonist
    Berubicin (RTA 744) hydrochloride is a Doxorubicin (HY-15142A) analog that can cross the blood-brain barrier. Berubicin hydrochloride inhibits P-gp and MRP1-mediated efflux and suppresses glioblastoma multiforme (GBM). Berubicin hydrochloride exerts toxic effects on leukemia cells by activating nuclear factor κB (NF-κB) and induces apoptosis in neuroblastoma cells. Berubicin hydrochloride can be used in the study of tumors related to the nervous system.
    Berubicin hydrochloride
  • HY-P3761
    Ac-Tyr-Val-Lys-Asp-aldehyde
    Inhibitor 99.89%
    Ac-Tyr-Val-Lys-Asp-aldehyde is a reversible caspase-1 inhibitor. Ac-Tyr-Val-Lys-Asp-aldehyde increases GATA1 levels by inhibiting caspase-1 and promotes erythroid differentiation. can be used for disease research including anemia-associated to chronic diseases, chemotherapy-induced anemia and Diamond-Blackfan anemia.
    Ac-Tyr-Val-Lys-Asp-aldehyde
  • HY-161470
    WS-384
    Agonist 98.23%
    WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC).
    WS-384
  • HY-10531
    ARRY-380 analog
    Activator 99.19%
    ARRY-380 analog (Compound PCM-0095494) is an ARRY-380 (HY-16069) analog. ARRY-380 analog activates caspases 3 and caspases 8. ARRY-380 analog inhibits Salmonella replication in cells.
    ARRY-380 analog
  • HY-N2490
    Dehydrotrametenolic acid
    Activator 99.95%
    Dehydrotrametenolic acid is a sterol isolated from the sclerotium of Poria cocos. Dehydrotrametenolic acid induces apoptosis through caspase-3 pathway. Dehydrotrametenolic acid has anti-tumor activity, anti-inflammatory, anti-diabetic effects.
    Dehydrotrametenolic acid
  • HY-154860
    PTD10
    PTD10 is a selective and potent BTK PROTAC degrader (DC50 = 0.5 nM, KD = 2.28 nM). PTD10 can recruit cereblon (CRBN) E3 ligase and form a ternary complex with BTK, thereby mediating the ubiquitination and proteasome-dependent degradation of BTK. PTD10 inhibits cancer cells proliferation, and induces cell apoptosis via activation of the caspase-dependent pathway and mitochondrial pathway. PTD10 potently inhibits the BCR, AKT and NF-κB signaling pathway. PTD10 can be used for researches of B-cell malignancies and autoimmune disease.
    PTD10
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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.

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.