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Isoforms Recommended: Caspase 1
Results for "

caspase-1

" in MedChemExpress (MCE) Product Catalog:

153

Inhibitors & Agonists

2

Screening Libraries

4

Fluorescent Dye

1

Biochemical Assay Reagents

36

Peptides

1

MCE Kits

1

Inhibitory Antibodies

31

Natural
Products

3

Recombinant Proteins

3

Isotope-Labeled Compounds

4

Antibodies

1

Click Chemistry

3

Oligonucleotides

1

GMP Molecules

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13205
    Belnacasan
    165+ Cited Publications

    VX-765

    		 Caspase Inflammation/Immunology
    Belnacasan (VX-765) is an orally bioactive proagent of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM [1] .
    Belnacasan
  • HY-16990
    Ac-YVAD-cmk
    30+ Cited Publications

    caspase-1 Inhibitor II

    		 Caspase Inflammation/Immunology
    Ac-YVAD-cmk (Caspase-1 Inhibitor II) is a selective caspase-1 (IL-1beta converting enzyme, ICE)) inhibitor with neuroprotective and anti-inflammatory effects. Ac-YVAD-cmk effectively suppresses the expression of IL-1β and IL-18. Ac-YVAD-cmk inhibits pyroptosis in many diseases [1] .
    Ac-YVAD-cmk
  • HY-100573
    Necrosulfonamide
    135+ Cited Publications

    		 Mixed Lineage Kinase Necroptosis Pyroptosis Caspase NOD-like Receptor (NLR) Keap1-Nrf2 TNF Receptor Interleukin Related NO Synthase Heme Oxygenase (HO) Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Endocrinology
    Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways [1] .
    Necrosulfonamide
  • HY-101092
    QS-21-Api
    5+ Cited Publications

    Stimulon

    		 NOD-like Receptor (NLR) Inflammation/Immunology Cancer
    QS-21-Api, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21-Api stimulates Th2 humoral and Th1 cell-mediated immune responses through action on antigen presenting cells (APCs) and T cells. QS-21-Api can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18 [1] .
    QS-21-Api
  • HY-132591
    Inclisiran
    5+ Cited Publications

    ALN-PCSsc

    		 PCSK9 Small Interfering RNA (siRNA) Pyroptosis PPAR NOD-like Receptor (NLR) Caspase Interleukin Related Cardiovascular Disease Metabolic Disease
    Inclisiran is a double-stranded small interfering RNA (siRNA) molecule. Inclisiran inhibits the transcription of PCSK9. Inclisiran inhibits Pyroptosis, activates PPARγ, and reduces NLRP3, cleaved caspase-1, IL-1β, and IL-18. Inclisiran has anti-inflammatory, lipid-regulating and anti-atherosclerotic activities. Inclisiran can be used in researches of hyperlipidemia and cardiovascular disease (CVD) [1] .
    Inclisiran
  • HY-132591A
    Inclisiran sodium
    5+ Cited Publications

    ALN-PCSsc sodium

    		 PCSK9 Small Interfering RNA (siRNA) Pyroptosis PPAR NOD-like Receptor (NLR) Caspase Interleukin Related Cardiovascular Disease Metabolic Disease
    Inclisiran sodium is a double-stranded small interfering RNA (siRNA) molecule. Inclisiran sodium inhibits the transcription of PCSK9. Inclisiran sodium inhibits Pyroptosis, activates PPARγ, and reduces NLRP3, cleaved caspase-1, IL-1β, and IL-18. Inclisiran sodium has anti-inflammatory, lipid-regulating and anti-atherosclerotic activities. Inclisiran sodium can be used in researches of hyperlipidemia and cardiovascular disease (CVD) [1] .
    Inclisiran sodium
  • HY-N0619
    Mulberroside A
    4 Publications Verification

    		 TNF Receptor Interleukin Related Tyrosinase Inflammation/Immunology
    Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.) [1]. Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects . Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM .
    Mulberroside A
  • HY-130413
    Protectin D1

    Neuroprotectin D1; NPD1

    		 Endogenous Metabolite PI3K Akt HIF/HIF Prolyl-Hydroxylase Reactive Oxygen Species (ROS) Caspase Interleukin Related MicroRNA Cardiovascular Disease Neurological Disease Inflammation/Immunology
    Protectin D1, a neuroprotectin D1 produced by neuronal cells, is a member of a newly discovered family of bioactive products derived from docosahexaenoic acid. Protectin D1 also serves as a specialized pro-resolving mediator, exhibiting effective in vivo pro-resolving activity in various human disease models. Additionally, Protectin D1 is an inhibitor of NALP3 inflammasomes and regulates the PI3K/AKT and HIF-1α signaling pathways. Protectin D1 exerts anti-inflammatory effects by reducing ROS levels, inhibiting the expression of NALP3, ASC, and Caspase-1, and consequently decreasing the release of pro-inflammatory cytokines IL-1β and IL-18. Furthermore, Protectin D1 enhances miRNA-210 expression, activates the PI3K/AKT signaling pathway, and exerts cardioprotective effects. Protectin D1 holds promise for research in cardiovascular diseases and inflammatory disorders [1] .
    Protectin D1
  • HY-B2176R
    ATP (Standard)

    Adenosine 5'-triphosphate (Standard)

    		 Reference Standards Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    ATP (Standard) is the analytical standard of ATP. This product is intended for research and analytical applications. ATP (Adenosine 5'-triphosphate) is a central component of energy storage and metabolism in vivo. ATP provides the metabolic energy to drive metabolic pumps and serves as a coenzyme in cells. ATP is an important endogenous signaling molecule in immunity and inflammation [1] . In Vitro: ATP (5 mM; 1 hour) co-treatment with LPS (1 μg/mL) has a synergistic effect on the activation of the NLRP3 inflammasome in HGFs .
    ATP (2 mM; 0.5-24 hours) induces secretion of IL-1β, KC and MIP-2 from BMDMs in a caspase-1 activation-dependent manner .
    ATP promotes neutrophil chemotaxis in vitro .
    In Vivo: ATP (50 mg/kg; i.p.) protects mice against bacterial infection in vivo .
    ATP induces the secretion of IL-1β, KC and MIP-2 and neutrophils recruitment in vivo .
    ATP (Standard)
  • HY-159520
    Ofirnoflastum

    Ofirnoflast; HT-6184

    		 NEKs NOD-like Receptor (NLR) Caspase Apoptosis Pyroptosis NF-κB Cardiovascular Disease Inflammation/Immunology Cancer
    Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia [1] .
    Ofirnoflastum
  • HY-W075517
    ZIF-8

    2-Methylimidazole zinc salt

    		 MOFs Caspase Pyroptosis Cancer
    ZIF-8 (2-Methylimidazole zinc salt) is a pyroptosis inducer that activates the caspase-1/gasdermin D-dependent pyroptosis pathway. ZIF-8 induces pyroptotic cell death accompanied by necrosis and immunogenic cell death. ZIF-8 initiates in situ immunity, activates anti-tumor immunity, and reprograms the immunosuppressive tumor microenvironment to inhibit tumor growth. ZIF-8 acts as a pH-responsive and stimulus-responsive drug release inducer. ZIF-8 is applicable to cancer-related research [1] .
    ZIF-8
  • HY-101019
    Ossirene
    2 Publications Verification

    AS101

    		 Interleukin Related Caspase Inflammation/Immunology Cancer
    Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor [1]. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies .
    Ossirene
  • HY-N0260
    Epmedin C
    5+ Cited Publications

    Epimedin-C; Baohuoside-VI

    		 Keap1-Nrf2 CDK Caspase Infection Metabolic Disease Inflammation/Immunology Cancer
    Epmedin C (Epimedin-C; Baohuoside-VI) is an orally active anti-inflammatory agent and immunomodulator that binds to multiple key proteins including UCP1, Caspase-1, CDK2 and Keap1. Epmedin C inhibits epithelial cell proliferation by disrupting the complex function of CDK2/Cyclin E. Epmedin C also upregulates Nrf2 expression, reduces ROS levels and inhibits pro-inflammatory cytokine secretion, thereby effectively restoring antibody production and alleviating tissue damage. Epmedin C has good safety with no hepatotoxicity or skin sensitization, and it has been used in studies on diseases such as obesity, Deoxynivalenol (HY-N6684)-induced immunotoxicity and mammary hyperplasia [1] .
    Epmedin C
  • HY-B1138
    Fenbufen
    1 Publications Verification

    CL-82204

    		 COX Caspase Infection Neurological Disease Inflammation/Immunology Cancer
    Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor [1] .
    Fenbufen
  • HY-143221
    AS-Inclisiran sodium

    		Drug Intermediate Cardiovascular Disease
    AS-Inclisiran sodium is the antisense of Inclisiran (HY-132591). Inclisiran is a double-stranded small interfering RNA (siRNA) molecule. Inclisiran inhibits the transcription of PCSK9. Inclisiran inhibits Pyroptosis, activates PPARγ, and reduces NLRP3, cleaved caspase-1, IL-1β, and IL-18. Inclisiran has anti-inflammatory, lipid-regulating and anti-atherosclerotic activities. Inclisiran can be used in researches of hyperlipidemia and cardiovascular disease (CVD) [1] .
    AS-Inclisiran sodium
  • HY-176860
    NEK7 degrader-1

    		Molecular Glues NEKs NOD-like Receptor (NLR) Caspase Interleukin Related Cardiovascular Disease Neurological Disease Inflammation/Immunology
    NEK7 degrader-1 is a NEK7 molecular glue degrader with a DC50 of 9  nM. NEK7 degrader-1 dose-dependently inhibits caspase-1 activity and IL-Ιβ release in macrophages in response to NLRP3 inflammasome activation. NEK7 degrader-1 can be used for autoinflammatory and autoimmune disorders like multiple sclerosis, neurodegeneraive diseases like Alzheimer's disease and cardiovascular and melabolic disorders like pericarditis and Type 2 diabetes research [1].
    NEK7 degrader-1
  • HY-148258
    GDC-2394

    		NOD-like Receptor (NLR) Interleukin Related Caspase Neurological Disease Inflammation/Immunology
    GDC-2394 is an orally active and selective NLRP3 inhibitor, and also inhibits IL-1β with IC50s of 0.4 μM (human IL-1β) and 0.1 μM (mouse IL-1β). GDC-2394 inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation. GDC-2394 could be used to study gouty arthritis.
    GDC-2394
  • HY-W011978
    N-Acetyl-L-tryptophan

    		Endogenous Metabolite Mitochondrial Metabolism Neurokinin Receptor Caspase Interleukin Related Neurological Disease Inflammation/Immunology
    N-Acetyl-L-tryptophan is an antagonist of the neurokinin-1 receptor (NK-1R), disrupting the binding of substance P (SP) to NK-1R. This action provides neuroprotective effects, improving memory deficits and motor impairments. N-Acetyl-L-tryptophan is also an inhibitor of cytochrome c (Cytochrome c), and it exerts antioxidant and anti-inflammatory effects by inhibiting the expression of IL-1β and the activation of caspase-1. N-Acetyl-L-tryptophan holds promise for research in neurodegenerative and inflammatory diseases [1] .
    N-Acetyl-L-tryptophan
  • HY-N1431
    Tabersonine
    3 Publications Verification

    		 NOD-like Receptor (NLR) Apoptosis Cytochrome P450 NF-κB PI3K Akt CDK Caspase Interleukin Related p38 MAPK Inflammation/Immunology Cancer
    Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer [1] .
    Tabersonine
  • HY-W923189
    Neral

    		Interleukin Related COX TNF Receptor NOD-like Receptor (NLR) NO Synthase PERK p38 MAPK Reactive Oxygen Species (ROS) Caspase Autophagy Herbicide Inflammation/Immunology Cancer
    Neral is a plant-derived anti-inflammatory, antioxidant and anticancer agent. Neral inhibits the phosphorylation of ERK1/2, p38 MAPK and IκB in macrophages induced by LPS (HY-D1056), suppresses the secretion of TNF-α and IL-6, as well as the expression of pro-IL-1β, iNOS and COX-2 in cells, and reduces the production of ROS in cells. Neral inhibits the activation of the NLRP3 inflammasome, and decreases the activation of caspase-1 and the secretion of IL-1β in mouse macrophages. Neral induces autophagy, and exhibits antiproliferative activity both in in vitro breast cancer cell models and mouse xenograft models. Neral regulates brassinosteroid, jasmonic acid and ethylene signaling pathways, and induces the expression of AP2/ERF-ERF and bHLH family genes in rice roots. Neral acts as a herbicide safener, alleviates the damage induced by Fenoxaprop-P-ethyl (HY-B2013), and promotes the elongation of rice roots. Neral can be used in research related to breast cancer, inflammatory and immune system diseases, and herbicide safeners [1] .
    Neral
  • HY-153068
    CZL55

    		Caspase Neurological Disease
    CZL55 is a caspase-1 inhibitor. CZL55 can be used for the research of febrile seizures (FS) [1].
    CZL55
  • HY-152670
    JC2-11
    1 Publications Verification

    		 NOD-like Receptor (NLR) AIM2 Inflammation/Immunology
    JC2-11 is an inhibitor of inflammatory corpuscles. JC2-11 inhibits domain-containing protein NLRC 4, absent in melanoma 2 (AIM 2) and non-canonical (NC) inflammatory corpuscles. JC2-11 reduces the secretion of caspase-1 (p20), the cleavage of gasdermin D (GSDMD), and the releases of IL-1β and lactate dehydrogenases (LDH) in inflammatory bodies. JC2-11 inhibits the activation of inflammatory bodies by destroying the production of reactive oxygen species and the activity of caspase-1 [1].
    JC2-11
  • HY-10081
    GS-6201
    1 Publications Verification

    CVT-6883

    		 Adenosine Receptor Inflammation/Immunology
    GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM) [1]. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse . GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice .
    GS-6201
  • HY-W041489
    Chelidonic acid
    1 Publications Verification

    		 NF-κB Caspase Inflammation/Immunology Cancer
    Chelidonic acid is a component of Chelidonium majus L., used as an antimicrobial. Chelidonic acid also shows anti-inflammatory activity. Chelidonic acid has potential to inhibit IL-6 production by blocking NF-κB and caspase-1 [1]. Chelidonic acid is a glutamate decarboxylase inhibitor, with a Ki of 1.2 μM .
    Chelidonic acid
  • HY-107541
    O-1602
    1 Publications Verification

    		 GPR55 Neurological Disease
    O-1602 is an agonist of GPR55 (G protein-coupled receptor 55). O-1602 reduces the number and activation of hippocampal microglia induced by METH (methamphetamine). O-1602 decreases the expression levels of NLRP3 inflammasome proteins, including NLRP3, ASC and Caspase-1 [1].
    O-1602
  • HY-120019
    Ac-YVAD-CHO

    L-709049

    		 Interleukin Related Apoptosis Caspase Inflammation/Immunology
    Ac-YVAD-CHO (L-709049) 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 is also a caspase-1 inhibitor. Ac-YVAD-CHO can suppress the production of mature IL-lβ [1] .
    Ac-YVAD-CHO
  • HY-P0111
    Z-WEHD-FMK
    4 Publications Verification

    Z-WE(OMe)HD(OMe)-FMK

    		 Caspase Cathepsin Cancer
    Z-WEHD-FMK is a potent, cell-permeable and irreversible caspase-1/5 inhibitor. Z-WEHD-FMK also exhibits a robust inhibitory effect on cathepsin B activity (IC50=6 μM). Z-WEHD-FMK can be used to investigate cells for evidence of apoptosis [1] .
    Z-WEHD-FMK
  • HY-P4547
    Ac-Trp-Glu-His-Asp-AMC

    AC-WEHD-AMC

    		 Caspase Others
    Ac-Trp-Glu-His-Asp-AMC (AC-WEHD-AMC) is a potent fluorogenic substrate of caspase-1 [1].
    Ac-Trp-Glu-His-Asp-AMC
  • HY-P2377
    Ac-YVAD-AFC
    4 Publications Verification

    		 Fluorescent Dye Others
    Ac-YVAD-AFC is the the fluorometric peptide substrate of caspase-1, with λ excitation of 400 nm and λ emission of 505 nm [1] .
    Ac-YVAD-AFC
  • HY-150270A
    NP-1815-PX sodium

    		P2X Receptor Prostaglandin Receptor NOD-like Receptor (NLR) Caspase Interleukin Related Inflammation/Immunology
    NP-1815-PX sodium is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX sodium specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX sodium selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX sodium not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX sodium exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX sodium is used in studies related to asthma and inflammatory bowel disease (colitis) [1] .
    NP-1815-PX sodium
  • HY-100573A
    (E/Z)-Necrosulfonamide
    1 Publications Verification

    		 Mixed Lineage Kinase Necroptosis Pyroptosis Caspase NOD-like Receptor (NLR) Keap1-Nrf2 TNF Receptor Interleukin Related NO Synthase Heme Oxygenase (HO) Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Endocrinology
    (E/Z)-Necrosulfonamide is a racemic compound of Necrosulfonamide (HY-100573). Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
    (E/Z)-Necrosulfonamide
  • HY-P2617A
    Ac-WEHD-AFC TFA

    		Caspase Inflammation/Immunology Cancer
    Ac-WEHD-AFC TFA is a fluorogenic caspase-1 substrate. Ac-WEHD-AFC TFA can measure caspase-1 fluorogenic activity and can be used for the research of tumor and inflammation [1].
    Ac-WEHD-AFC TFA
  • HY-156413
    NLRP3 agonist 1
    3 Publications Verification

    		 NOD-like Receptor (NLR) Caspase Inflammation/Immunology
    NLRP3 agonist 1 (Compound 23) is an orally active NLRP3 agonist. NLRP3 agonist 1 can activate the enzyme Caspase-1 to cleave pro-IL-1β and pro-IL-18 proinflammatory cytokines into their mature forms [1].
    NLRP3 agonist 1
  • HY-P2091
    Ac-YVAD-pNA

    		Caspase Inflammation/Immunology
    Ac-YVAD-pNA is a specific Caspase-1 substrate. Ac-YVAD-pNA can be used to detect Caspase-1 activity. Caspase-1 is a key mediator of inflammatory processes [1] .
    Ac-YVAD-pNA
  • HY-124857
    7DG

    7-Desacetoxy-6,7-dehydrogedunin

    		 PERK Prokineticin Receptor P2X Receptor Caspase NOD-like Receptor (NLR) Pyroptosis Tyrosinase Neurological Disease Metabolic Disease Inflammation/Immunology
    7DG (7-Desacetoxy-6,7-dehydrogedunin) is a PKR inhibitor, P2X7 purinergic receptor inhibitor, and skin-lightening agent. 7DG binds outside the ATP-catalytic domain of PKR, blocks the kinase activity-independent protein-protein interactions of PKR, inhibits the phosphorylation and activity of PKR, disrupts ASC assembly and caspase-1 activation, and suppresses the activation of the NLRP1 inflammasome. 7DG inhibits pyroptosis, suppresses the ATP-P2X7 signaling pathway, and abolishes ATP-induced increases in the expression levels of MITF, tyrosinase, PMEL/gp100, and melanin content. 7DG exerts skin-lightening effects in cultured skin in vitro. 7DG can be used in research related to chronic obstructive pulmonary disease, gout, type 2 diabetes, Alzheimer's disease, and hyperpigmentary skin disorders [1] .
    7DG
  • HY-146765
    AMS-17

    		NOD-like Receptor (NLR) Neurological Disease Inflammation/Immunology
    AMS-17 is a potent NLRP3 inhibitor, inhibiting microglia activation in vitro and in vivo. AMS-17 also inhibits cytokines such as caspase-1, TNF-α, IL-1β and inducible nitric oxide synthase (iNOS) in N9 cells. AMS-17 can be used for researching inflammation-associated neurological disorders, such as vascular dementia (VaD) [1] .
    AMS-17
  • HY-131204
    CZL80

    		Caspase Neurological Disease
    CZL80, a brain-penetrable caspase-1 inhibitor with an IC50 of 0.01 μM, could be used in the study of febrile seizures and later enhanced epileptogenic susceptibility [1].
    CZL80
  • HY-N16409
    Berkeleyamide C

    		MMP Caspase Inflammation/Immunology Cancer
    Berkeleyamide C is a selective matrix metalloproteinase-3 (MMP-3) and caspase-1 inhibitor. Berkeleyamide C blocks MMP-3-mediated tumor cell invasion and metastasis, as well as the abnormal activation of inflammation and apoptosis related to caspase-1. Berkeleyamide C is promising for research of cancers and inflammation-related diseases [1].
    Berkeleyamide C
  • HY-P2617
    Ac-WEHD-AFC

    		Caspase Inflammation/Immunology Cancer
    Ac-WEHD-AFC is a fluorogenic caspase-1 substrate. Ac-WEHD-AFC can measure caspase-1 fluorogenic activity and can be used for the research of tumor and inflammation [1].
    Ac-WEHD-AFC
  • HY-130480
    Fructose-arginine

    		AIM2 Inflammation/Immunology
    Fructose-arginine, an amino-sugar, is an AIM2 inflammasome activation inhibitor. Fructose-arginine attenuates the secretion of IL-1β, IL-18, and caspase-1, and Asc pyroptosome formation and Gsdmd cleavage resulting from AIM2 inflammasome activation [1].
    Fructose-arginine
  • HY-111662
    Fc 11a-2

    		NOD-like Receptor (NLR) Inflammation/Immunology
    Fc 11a-2, a benzimidazole compound, is an orally active and potent NLRP3 inflammasome inhibitor. Fc 11a-2 restrains the formation of NLRP3 inflammasome by inhibiting activation of caspase-1 and thus the activation of IL-1b/IL-18. Fc 11a-2 prevents the development of Dextran sulfate sodium (DSS; HY-116282C)-induced murine experimental colitis [1] .
    Fc 11a-2
  • HY-P2616A
    Mca-YVADAP-Lys(Dnp)-OH TFA

    		Cholinesterase (ChE) Caspase Others
    Mca-YVADAP-Lys(Dnp)-OH TFA is a fluorogenic substrate for caspase-1 and angiotensin-converting enzyme 2 (ACE2) [1].
    Mca-YVADAP-Lys(Dnp)-OH TFA
  • HY-100573S
    Necrosulfonamide-d4

    		Isotope-Labeled Compounds Mixed Lineage Kinase Necroptosis Pyroptosis Caspase NOD-like Receptor (NLR) Keap1-Nrf2 TNF Receptor Integrin NO Synthase Heme Oxygenase (HO) Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Endocrinology
    Necrosulfonamide-d4 is the deuterium labeled Necrosulfonamide (HY-100573). Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.
    Necrosulfonamide-d4
  • HY-N1431A
    Tabersonine hydrochloride
    3 Publications Verification

    		 NOD-like Receptor (NLR) Apoptosis Cytochrome P450 NF-κB PI3K Akt CDK Caspase Interleukin Related p38 MAPK Neurological Disease Inflammation/Immunology
    Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer [1] .
    Tabersonine hydrochloride
  • HY-16275
    Nivocasan

    GS 9450; LB-84451

    		 Caspase Interleukin Related Inflammation/Immunology
    Nivocasan (GS 9450; LB-84451) is a pan-caspase inhibitor that irreversibly arrests caspase-1 activity and inhibits that of caspase-8. Nivocasan inhibits IL-1β cleavage and blocks osteoclast differentiation. Nivocasan inhibits the protein expression of NFATc1 and CSTK [1].
    Nivocasan
  • HY-P2616
    Mca-YVADAP-Lys(Dnp)-OH

    		Caspase Angiotensin-converting Enzyme (ACE) Others
    Mca-YVADAP-Lys(Dnp)-OH is a fluorogenic substrate for caspase-1 and angiotensin-converting enzyme 2 (ACE2) [1].
    Mca-YVADAP-Lys(Dnp)-OH
  • HY-N10359
    Isoandrographolide

    		NOD-like Receptor (NLR) Caspase Akt GSK-3 β-catenin Metabolic Disease Inflammation/Immunology Cancer
    Isoandrographolide is an orally active NLRP3 inflammasome inhibitor and AKT/GSK-3β/β-catenin pathway inhibitor. Isoandrographolide inhibits the expression of NLRP3, ASC, and caspase-1, and reduces the levels of phosphorylated AKT, phosphorylated GSK-3β, and β-catenin. Isoandrographolide alleviates inflammatory responses, reduces collagen deposition, suppresses epithelial-mesenchymal transition (EMT), induces differentiation of leukemia cells, inhibits the growth of leukemia cells, protects lung and kidney tissues, regulates cytokine levels, and also exhibits hepatoprotective effects. Isoandrographolide can be used in studies related to silicosis, murine myeloid leukemia, renal tubulointerstitial fibrosis, and non-alcoholic fatty liver disease [1] .
    Isoandrographolide
  • HY-13205R
    Belnacasan (Standard)

    VX-765 (Standard)

    		 Caspase Reference Standards Inflammation/Immunology
    Belnacasan (Standard) is the analytical standard of Belnacasan. This product is intended for research and analytical applications. Belnacasan (VX-765) is an orally bioactive proagent of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM [1] .
    Belnacasan (Standard)
  • HY-145087
    NP3-146

    NLRP3-IN-5

    		 NOD-like Receptor (NLR) Interleukin Related Caspase Inflammation/Immunology
    NP3-146 is a NLRP3 inflammasome inhibitor through locking the NACHT domain of NLRP3. NP3-146 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 regulates the levels of cleaved Caspase-1 and cleaved IL-1β in cell supernatants. NP3-146 can be used for the research of inflammatory diseases [1] .
    NP3-146
  • HY-150270
    NP-1815-PX

    		Prostaglandin Receptor P2X Receptor NOD-like Receptor (NLR) Caspase Interleukin Related Neurological Disease Inflammation/Immunology
    NP-1815-PX is an orally active dual inhibitor of P2X4 and prostaglandin TP receptors, with an IC50 of 0.26 μM against human P2X4 receptors. NP-1815-PX specifically inhibits ATP-mediated prostaglandin production, TP receptor-induced calcium elevation, and the canonical/non-canonical NLRP3 inflammasome signaling pathway. NP-1815-PX selectively blocks smooth muscle contractions induced by ATP, U46619 (HY-108566) and prostaglandin F2α. NP-1815-PX not only produces anti-allodynic effects in vivo, but also significantly alleviates symptoms of DNBS (HY-W324435)-induced colitis (such as weight loss and tissue damage). NP-1815-PX exerts anti-inflammatory effects by downregulating IL-1β levels and Caspase-1 activity. NP-1815-PX is used in studies related to asthma and inflammatory bowel disease (colitis) [1] .
    NP-1815-PX

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