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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
25 Results for "
gasdermins
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "gasdermins" in MCE Product Catalog:
488
488 Publications Verification
Synonyms: BAY 11-7821
Target:
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BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells .
155
155 Cited Publications
Synonyms: Tetraethylthiuram disulfide; TETD
Research Areas:
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram, a copper ion carrier, with Cu 2+ increases intracellular ROS levels and induces cuproptosis .
144
144 Cited Publications
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 .
52
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Idasanutlin (RG7388) is an orally bioavailable MDM2 inhibitor with an IC50 of 6 nM. Idasanutlin disrupts MDM2-p53 binding, stabilizes and activates p53, triggering cell cycle arrest, apoptosis, and reduced cancer cell viability. Idasanutlin reduces EGFR protein expression and phosphorylation, suppresses downstream SHP2, MEK1/2, ERK1/2, AKT, mTOR, p70(S6K1), and S6 signaling. Idasanutlin induces mitochondrial ROS production, drives p38 MAPK phosphorylation, upregulates NOXA, and mediates caspase-3-dependent apoptosis and gasdermin E-mediated pyroptosis. Idasanutlin can be used for the research of TP53-mutant non-small cell lung cancer, T-cell acute lymphoblastic leukemia, colorectal carcinoma, melanoma, diffuse large B-cell lymphoma, mantle cell lymphoma, non-Hodgkin lymphoma, severe fever with thrombocytopenia syndrome, neuroblastoma, acute lymphoblastic leukemia, relapsed or refractory acute myeloid leukemia, osteosarcoma, solid tumors, and hematological tumors .
23
23 Cited Publications
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LDC7559 is a gasdermin D (GSDMD) inhibitor via blocking neutrophil extracellular trap (NET) in the late stages .
12
12 Cited Publications
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Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is effective against caspases-1 (IC50 of 46.7 nM), caspases-4 (IC50 of 1.49 μM), caspases-5 (IC50 of 329 nM), and caspases-11 , but not the apoptotic caspases such as caspase-3 .
6
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Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica .
1
1 Cited Publications
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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
1 Cited Publications
(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.
1
1 Cited Publications
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Research Areas:
NLRP3-IN-21 (compound L38) is a NLRP3 inflammasome inhibitor with inflammatory properties. NLRP3-IN-21 inhibits NLRP3 inflammasome activation and pyroptosis by suppressing gasdermin D cleavage, ASC oligomerization, and NLRP3 inflammasome assembly .
Cat. No.: HY-W075517
CAS No.: 59061-53-9
Synonyms: 2-Methylimidazole zinc salt
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ZIF-8 (2-Methylimidazole zinc salt) is a caspase-1/Gasdermin D activator and a pH- and stimulus-responsive inducer of drug release, which serves as a highly efficient drug delivery carrier. ZIF-8 is a metal-organic framework (MOF). ZIF-8 activates the caspase-1/Gasdermin D-dependent pyroptosis pathway, induces pyroptosis, necrosis and immunogenic cell death, initiates in situ anti-tumor immunity, reprograms the immunosuppressive tumor microenvironment and inhibits tumor proliferation. ZIF-8 is applicable to related research on multiple cancers including colorectal cancer and breast cancer .
Synonyms: EBC-46
Tigilanol tiglate (EBC-46) is a protein kinase C (PKC)/C1 domain activator. Tigilanol tiglate is associated with mitochondrial/endoplasmic reticulum (ER) dysfunction, leading to activation of the unfolded protein response (UPRmt/ER) and subsequent induction of ATP depletion, organelles expansion, Caspase activation, gasdermin E cleavage, and terminal necrosis. Tigilanol tiglate, as a small anti-tumor molecule with immunomodulatory effects, can be used in the study of head and neck squamous cell carcinoma and soft tissue sarcoma .
Cat. No.: HY-18711A
CAS No.: 1174161-86-4
Synonyms: Metatinib anhydrous; c-Met inhibitor 2
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SCR-1481B1 (Metatinib anhydrous; c-Met inhibitor 2) is an inhibitor of the N-terminal fragment of Gasdermin D (GSDMD), with an IC50 of 1.04 μM and a Ka of 0.42 μM in mice. SCR-1481B1 effectively blocks GSDMD-NT oligomerization and pore formation, inhibits GSDMD-mediated pyroptosis (Pyroptosis), preserves mitochondrial integrity, and reduces proinflammatory cytokine secretion. SCR-1481B1 also inhibits angiogenesis, exerts GSDMD-independent antitumor effects, and enhances the infiltration of antitumor immune cells. SCR-1481B1 is also an inhibitor targeting to c-MET and VEGFR2, can be used in studies related to melanoma and sepsis .
Cat. No.: HY-P99618
CAS No.: 2377419-89-9
Synonyms: IBI-315; BH2950
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Synonyms: Tetraethylthiuram disulfide (Standard); TETD (Standard)
Target:
Reference Standards Aldehyde Dehydrogenase (ALDH) Interleukin Related Pyroptosis Apoptosis Cuproptosis
Research Areas:
Disulfiram (Standard) is the analytical standard of Disulfiram. This product is intended for research and analytical applications. Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram + Cu 2+ increases intracellular ROS levels triggering apoptosis of ovarian cancer stem cells [1-6].
Cat. No.: HY-161727
CAS No.: 2728291-29-8
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P2Y14R antagonist 1 (compound I-17) is a selective P2Y14R antagonist with an IC50 of 0.6 nM. It exhibits potent P2Y14R antagonistic activity, both in vitro and in vivo efficacy, and favorable pharmacokinetic profiles. P2Y14R antagonist 1 reduces the release of inflammatory factors and cell pyroptosis through the NOD-like receptor family pyrin domain-containing 3 (NLRP3)/gasdermin D (GSDMD) signaling pathway. P2Y14R antagonist 1 holds promise for research in the field of acute gouty arthritis .
Cat. No.: HY-173234
CAS No.: 1008710-58-4
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GI-Y2 is an orally active, selective Gasdermin D (GSDMD) inhibitor (Kd = 36.0 μM) with anti-pyroptosis activity. GI-Y2 targets GSDMD, impairs membrane anchoring of GSDMD-NT, and blocks GSDMD‑dependent lipid binding and pore formation. GI-Y2 suppresses GSDMD‑dependent pyroptosis and inflammation, mitigates atherosclerosis and cardiac injury, boosts cell survival, and reduces IL‑1β/IL‑18 secretion. GI-Y2 can be used for the research of atherosclerosis and septic myocardial injury .
Cat. No.: HY-B0621R
CAS No.: 68786-66-3
Synonyms: CGA89317 (Standard)
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Triclabendazole (Standard) is the analytical standard of Triclabendazole. This product is intended for research and analytical applications. Triclabendazole is an orally active parasite inhibitor. Triclabendazole has anti-Leishmania activity and induces gasdermin E (GSDME)-dependent pyroptosis by caspase-3 activation. Triclabendazole can be used for the research of fasciola hepatica .
Cat. No.: HY-B0621S
CAS No.: 1353867-93-2
Synonyms: CGA89317-d3
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
