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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
23 Results for "
Ap2 Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (23)
23 Results for "Ap2 Inhibitors" in MCE Product Catalog:
29
29 Publications Verification
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BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
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29 Publications Verification
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BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
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2 Cited Publications
Cat. No.: HY-P2259
CAS No.: 1404188-93-7
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1 Cited Publications
SGC-AAK1-1, a chemical probe, is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor with an IC50 of 270 nM and a Ki of 9 nM. SGC-AAK1-1 also potently inhibits BMP2K. SGC-AAK1-1 is used to study Wnt pathway related to AAK1 .
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1 Cited Publications
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HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
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1 Cited Publications
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LEI110 is a pan-inhibitor of the HRASLS family and an inhibitor of AP-2α, with a Ki of 20 nM against PLA2G16. LEI110 exhibits inhibitory activity against PLA2G16, HRASLS2, RARRES3 and iNAT, with pIC50 values of 7.0, 6.8, 6.8 and 7.6, respectively. LEI110 binds to the active site of PLA2G16, reduces intracellular arachidonic acid levels, and attenuates oleic acid-induced lipolysis. LEI110 stabilizes AP-2α, impairs its DNA-binding ability, inhibits the transcription of DNA damage repair genes, induces the accumulation of oxidative DNA damage, suppresses cell proliferation and clonogenicity, and sensitizes HCC cells to DNA-damaging agents. LEI110 can be used in research related to obesity, fatty liver disease, the common cold and hepatocellular carcinoma .
Cat. No.: HY-W923189
CAS No.: 106-26-3
Target:
Interleukin Related COX TNF Receptor NOD-like Receptor (NLR) NO Synthase PERK p38 MAPK Reactive Oxygen Species (ROS) Caspase Autophagy Herbicide
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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 .
Cat. No.: HY-N10361
CAS No.: 53755-58-1
Category:
Cat. No.: HY-N4177
CAS No.: 24577-90-0
Synonyms: Rubrofusarin-6-β-gentiobioside
Category:
Seeds of Cassia tora Linn. other families Monophenols Leguminosae Metabolic Disease Phenols Plants Disease Research Fields
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Cat. No.: HY-147083
CAS No.: 2242913-80-8
SGC-AAK1-1N is a potent and selective AAK1 (AP2 associated kinase 1) inhibitor, with an IC50 of 1.8 μM .
Cat. No.: HY-159931
CAS No.: 2920698-73-1
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HW161023 (compound 5) is an orally active AP2-associated protein kinase 1 (AAK1) inhibitor with IC50 values of 5.4 nM and 11.9 μM aganist of AAK1and hERG, respectively. HW161023 inhibits the pain in chronic constriction injury of the sciatic nerve rat model .
Cat. No.: HY-N7661
CAS No.: 54334-04-2
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Cat. No.: HY-174214
CAS No.: 2969205-90-9
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AAK1-IN-8 (Compound 18) is a pan-NAK inhibitor. AAK1-IN-8 inhibits AAK1 and GAK (EC50 values are 50 and 190 nM, respectively). AAK1-IN-8 inhibits the phosphorylation of AP2-µ2 subunit at T156 .
Cat. No.: HY-174213
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AAK1-IN-7 (Compound 16) is a dual AAK1/GAK inhibitor (EC50 values are 40 and 80 nM, respectively). AAK1-IN-7 inhibits the phosphorylation of AP2-µ2 subunit at T156. AAK1-IN-7 has weak antiviral activity against RNA viruses .
Cat. No.: HY-101903AR
CAS No.: 2802523-05-1
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BMS-309403 (sodium) (Standard) is the analytical standard of BMS-309403 (sodium). This product is intended for research and analytical applications. BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor, with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
Cat. No.: HY-101903R
CAS No.: 300657-03-8
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Research Areas:
BMS-309403 (Standard) is the analytical standard of BMS-309403. This product is intended for research and analytical applications. BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (also known as FABP4, aP2) inhibitor with Kis of <2, 250, and 350 nM for FABP4, FABP3, and FABP5, respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells .
Cat. No.: HY-119875
CAS No.: 533889-36-0
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BMS-480404 is an inhibitor of keratinocyte fatty acid-binding protein (kFABP) and adipocyte lipid-binding protein (aP2). BMS-480404 has a Ki value of 33 nM for kFABP. BMS-480404 can be used in the research of metabolic disorders .
Cat. No.: HY-101503R
CAS No.: 682741-29-3
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HTS01037 (Standard) is the analytical standard of HTS01037 (HY-101503). This product is intended for research and analytical applications. HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
Cat. No.: HY-159879
CAS No.: 3061058-16-7
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AAK1-IN-6 (Compound 23) is an inhibitor of AP-2-associated protein kinase 1 (AAK1, IC50 = 12 nM) with antiviral activity against the dengue virus (DNEV2, EC50 = 0.24 μM) and Venezuelan equine encephalitis virus (VEEV, EC50 = 0.30 μM). AAK1-IN-6 can be utilized in antiviral research .
Cat. No.: HY-169405
AAK1/HDACs-IN-1 (Compound 12) is the dual inhibitor for AAK1 and HDAC, that inhibits AAK1, HDAC1, and HDAC6 with IC50s of 15.9, 148.6, and 5.2 nM, respectively. AAK1/HDACs-IN-1 inhibits SARS-CoV-2 infection, suppresses the endocytosis of ACE2-SARS-CoV-2 complex, as well as AP2M1-ACE2 interaction .
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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
