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Active Caspase-1 Inhibitors

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27

Inhibitors & Agonists

10

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1

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0535
    (+)-Magnoflorine chloride
    1 Publications Verification

    Magnoflorine chloride; α-Magnoflorine chloride; Thalictrine chloride

    		 Fungal Autophagy Apoptosis PINK1/Parkin NOD-like Receptor (NLR) Caspase JNK NF-κB Sirtuin AMPK Reactive Oxygen Species (ROS) Infection Metabolic Disease
    (+)-Magnoflorine (α-Magnoflorine) chloride is an orally active aporphine alkaloid with multiple biological activities. (+)-Magnoflorine chloride promotes Parkin/PINK1-mediated mitochondrial autophagy, inhibits the activation of NLRP3/Caspase-1 pathway, regulates the intestinal microbiota, and exhibits significant anti-inflammatory and immunomodulatory activities. (+)-Magnoflorine chloride inhibits JNK and TLR4/NF-κB signaling pathways, activates Sirt1/AMPK pathway, alleviates neuronal oxidative stress and apoptosis. Magnoflorine chloride upregulates miR-410-3p, inhibits HMGB1/NF-κB pathway, and has anti-tumor activity. (+)-Magnoflorine chloride also has significant antifungal activity .
    (+)-Magnoflorine chloride
  • 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 .
    Ofirnoflastum
  • 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 .
    Fenbufen
  • HY-N0260
    Epmedin C
    Maximum Cited Publications
    6 Publications Verification

    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 .
    Epmedin C
  • HY-N2414
    Periplogenin
    1 Publications Verification

    		 Reactive Oxygen Species (ROS) Necroptosis Pyroptosis Interleukin Related Caspase NOD-like Receptor (NLR) Neurological Disease Inflammation/Immunology Cancer
    Periplogenin is an orally active cardiac glycoside found in Cortex periplocae. Periplogenin can induce ROS production and necroptosis and cause G0/G1 phase arrest. Periplogenin can inhibit pyroptosis by regulating the NLRP3/Caspase-1/GSDMD signaling. Periplogenin suppresses growth of prostate carcinoma cells by docking to an ATP1A1 protein pocket and forming a hydrogen bond with T804. Periplogenin can be used for the researches of cancer, inflammation and immunology, such as prostate carcinoma, rheumatoid arthritis and psoriasis .
    Periplogenin
  • HY-N0334
    (+)-Magnoflorine

    Magnoflorine; α-Magnoflorine; Thalictrine

    		 Fungal Autophagy Apoptosis PINK1/Parkin NOD-like Receptor (NLR) Caspase JNK NF-κB Sirtuin AMPK Reactive Oxygen Species (ROS) Cardiovascular Disease Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    (+)-Magnoflorine (α-Magnoflorine) is an orally active aporphine alkaloid with multiple biological activities. (+)-Magnoflorine promotes Parkin/PINK1 -mediated mitochondrial autophagy, inhibits the activation of NLRP3/Caspase-1 pathway, regulates the intestinal microbiota, and exhibits significant anti-inflammatory and immunomodulatory activities. (+)-Magnoflorine inhibits JNK and TLR4/NF-κB signaling pathways, activates Sirt1/AMPK pathway, alleviates neuronal oxidative stress and apoptosis. Magnoflorine upregulates miR-410-3p, inhibits HMGB1/NF-κB pathway, and has anti-tumor activity. (+)-Magnoflorine also has significant antifungal activity .
    (+)-Magnoflorine
  • 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-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 .
    Tabersonine
  • HY-19676
    Pralnacasan
    1 Publications Verification

    VX-740; HMR 3480

    		 Caspase Inflammation/Immunology
    Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment .
    Pralnacasan
  • HY-N0334A
    (+)-Magnoflorine iodide
    1 Publications Verification

    Magnoflorine iodide; α-Magnoflorine iodide; Thalictrine iodide

    		 Fungal Autophagy Apoptosis PINK1/Parkin NOD-like Receptor (NLR) Caspase JNK NF-κB Sirtuin AMPK Reactive Oxygen Species (ROS) Cardiovascular Disease Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    (+)-Magnoflorine (α-Magnoflorine) iodide is an orally active aporphine alkaloid with multiple biological activities. (+)-Magnoflorine iodide promotes Parkin/PINK1 -mediated mitochondrial autophagy, inhibits the activation of NLRP3/Caspase-1 pathway, regulates the intestinal microbiota, and exhibits significant anti-inflammatory and immunomodulatory activities. (+)-Magnoflorine iodide inhibits JNK and TLR4/NF-κB signaling pathways, activates Sirt1/AMPK pathway, alleviates neuronal oxidative stress and apoptosis. Magnoflorine upregulates miR-410-3p, inhibits HMGB1/NF-κB pathway, and has anti-tumor activity. (+)-Magnoflorine iodide also has significant antifungal activity .
    (+)-Magnoflorine iodide
  • 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) .
    NP-1815-PX sodium
  • 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 .
    Fc 11a-2
  • 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 .
    Tabersonine hydrochloride
  • 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 .
    Isoandrographolide
  • 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) .
    NP-1815-PX
  • HY-159007
    BD-AcAc2

    R,S-1,3-Butanediol acetoacetate diester

    		 Pyroptosis NF-κB NOD-like Receptor (NLR) Caspase Apoptosis Autophagy Reactive Oxygen Species (ROS) Oxidative Phosphorylation Interleukin Related Neurological Disease Metabolic Disease Inflammation/Immunology
    BD-AcAc2 (R,S-1,3-Butanediol acetoacetate diester) is an orally active, CNS-penetrant antiepileptic agent. BD-AcAc2 inhibits NF-κB, NLRP3 inflammasome, caspase-1/3, pyroptosis, apoptosis, and enhances autophagy. BD-AcAc2 exhibits antioxidant activity by modulating ROS, MDA, SOD, and GSH levels, and alleviates oxidative stress. BD-AcAc2 mitigates chronic colitis, counteracts Dextran Sodium Sulfate (DSS)-induced pathology, protects against central nervous system oxygen toxicity and acute lung injury, and exhibits anti-seizure efficacy. BD-AcAc2 can be used for the research of colitis, sarcopenia, acute lung injury, seizure, and obesity .
    BD-AcAc2
  • HY-141622
    SDZ 224-015

    		Interleukin Related Caspase SARS-CoV Infection Inflammation/Immunology
    SDZ 224-015 is an orally active inhibitor of the interleukin-1 beta (IL-1β) converting enzyme and caspase-1. SDZ 224-015 possesses anti-COVID-19 activity, targeting M pro (IC50 of 30 nM) .
    SDZ 224-015
  • HY-168503
    NLRP3-IN-54

    		NOD-like Receptor (NLR) Interleukin Related Inflammation/Immunology
    NLRP3-IN-54 (Compound C4) is an NLRP3 inhibitor. NLRP3-IN-54 can significantly reduce the levels of active Caspase-1 and active IL-1β (IC50 = 0.805 μM), can be used for inflammation research .
    NLRP3-IN-54
  • HY-B1138R
    Fenbufen (Standard)

    CL-82204 (Standard)

    		 Reference Standards COX Caspase Inflammation/Immunology
    Fenbufen (Standard) is the analytical standard of Fenbufen. This product is intended for research and analytical applications. 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 .
    Fenbufen (Standard)
  • HY-B1138S
    Fenbufen-d9

    		Isotope-Labeled Compounds COX Caspase Inflammation/Immunology
    Fenbufen-d9 (CL-82204-d9) is the deuterium labeled Fenbufen. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with 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 .
    Fenbufen-d9
  • HY-N0260R
    Epmedin C (Standard)

    Epimedin-C (Standard); Baohuoside-VI (Standard)

    		 Reference Standards Keap1-Nrf2 CDK Caspase Inflammation/Immunology
    Epmedin C (Standard) is the analytical standard of Epmedin C. This product is intended for research and analytical applications. 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 .
    Epmedin C (Standard)
  • HY-N2414R
    Periplogenin (Standard)

    		Reference Standards Reactive Oxygen Species (ROS) Necroptosis Pyroptosis Interleukin Related Caspase NOD-like Receptor (NLR) Inflammation/Immunology Cancer
    Periplogenin (Standard) is the analytical standard of Periplogenin (HY-N2414). Periplogenin is an orally active cardiac glycoside found in Cortex periplocae. Periplogenin can induce ROS production and necroptosis and cause G0/G1 phase arrest. Periplogenin can inhibit pyroptosis by regulating the NLRP3/Caspase-1/GSDMD signaling. Periplogenin suppresses growth of prostate carcinoma cells by docking to an ATP1A1 protein pocket and forming a hydrogen bond with T804. Periplogenin can be used for the researches of cancer, inflammation and immunology, such as prostate carcinoma, rheumatoid arthritis and psoriasis .
    Periplogenin (Standard)
  • HY-179494
    M464

    		NOD-like Receptor (NLR) Pyroptosis Caspase Interleukin Related Reactive Oxygen Species (ROS) Metabolic Disease
    M464, a non-steroidal anti-inflammatory compound, is a potent and orally active NLRP3 inflammasome inhibitor. M464 inhibits pyroptosis and hinders the activation of downstream Caspase-1 expression and the release of IL-1β by impeding ASC oligomerisation and curtailing ROS production. M464 exhibits protective effects against acute lung and liver injury in mice. M464 can be used for the research of NLRP3-related inflammatory diseases .
    M464
  • HY-148258A
    GDC-2394 sodium

    		NOD-like Receptor (NLR) Interleukin Related Caspase Metabolic Disease Inflammation/Immunology
    GDC-2394 (Compound 20) sodium 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 sodium inhibits NLRP3-induced caspase-1 activity without inhibiting NLRC4-dependent inflammasome activation. GDC-2394 sodium could be used to study gouty arthritis .
    GDC-2394 sodium
  • HY-181488
    NLRP3-IN-87

    		NOD-like Receptor (NLR) Caspase Interleukin Related Metabolic Disease Inflammation/Immunology
    NLRP3-IN-87 is a selective and orally active NLRP3 inhibitor with a Kd of 0.23 μM. NLRP3-IN-87 binds directly to the NLRP3 NACHT domain, disrupts NLRP3-NEK7 and NLRP3-ASC interactions, inhibits ASC oligomerization, and blocks inflammasome assembly. NLRP3-IN-87 suppresses caspase-1 activation and IL-1β secretion. NLRP3-IN-87 exhibits anti-inflammatory and analgesic activity, reducing joint swelling, inflammation, and pain in an MSU (HY-B2130A)-induced acute gout mouse model. NLRP3-IN-87 can be used for the research of gout .
    NLRP3-IN-87
  • HY-185311
    NEK7 degrader-3

    		Molecular Glues NEKs NOD-like Receptor (NLR) Caspase Interleukin Related Pyroptosis Neurological Disease Inflammation/Immunology
    NEK7 degrader-3 is an orally active and brain-penetrant NEK7 molecular glue degrader with a DC50 of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon, promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β, IL-1α, and IL-18, and pyroptosis-related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS (HY-D1056)-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation .
    NEK7 degrader-3
  • HY-W017087
    1,2,4-Trimethoxybenzene

    		NOD-like Receptor (NLR) Caspase Interleukin Related Infection Metabolic Disease
    1,2,4-Trimethoxybenzene is an orally active NLRP3 selective inhibitor. 1,2,4-Trimethoxybenzene can markedly suppress Nigericin (HY-127019) or ATP (HY-B2176)-induced NLRP3 inflammasome activation, thus decreasing caspase-1 activation and IL-1β secretion. 1,2,4-Trimethoxybenzene specifically inhibits the activation of NLRP3 inflammasome without affecting absent in melanoma 2 (AIM2) inflammasome activation. 1,2,4-Trimethoxybenzene inhibits oligomerization of the apoptosis-associated speck-like protein containing a CARD (ASC) and protein-protein interaction between NLRP3 and ASC, thus blocking NLRP3 inflammasome assembly. 1,2,4-Trimethoxybenzene can be used for the study of experimental autoimmune encephalomyelitis (EAE), multiple sclerosis, and type 2 diabetes .
    1,2,4-Trimethoxybenzene

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