Phospholipase Inhibitor
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D-myo-Inositol 1,4,5-trisphosphate sodium salt
0 ImagesD-myo-inositol 1,4,5-trisphosphate sodium salt is a widely distributed intracellular second messenger. D-myo-inositol 1,4,5-trisphosphate sodium salt acts as a potent agonist of the Ins (1,4,5) P3 receptor with an EC50 of 0.12 μM and inhibits bovine PLC-δ1, with an IC50 of 5.4 μM for binding and an IC50 of 12.4 μM for hydrolysis. D-myo-inositol 1,4,5-trisphosphate sodium saltis metabolized into Ins (1,4) P2 and Ins (1,3,4,5) P4. D-myo-inositol 1,4,5-trisphosphate sodium salt mediates various cellular processes, including growth, development, fertilization, secretion, contraction and neuromodulation. D-myo-inositol 1,4,5-trisphosphate sodium salt inhibits PIP2 hydrolysis and Ca2+-ATPase activity. D-myo-inositol 1,4,5-trisphosphate sodium salt is used for cardiac preconditioning, exerts cardioprotective effects and mimics ischemic preconditioning. D-myo-inositol 1,4,5-trisphosphate sodium salt is applied in studies related to intracellular calcium and phosphoinositol signaling pathways.
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Parameritannin A-1
0 ImagesCat. No.: HY-N16481CAS No.: 347406-26-2Parameritannin A-1 is a tetrameric proanthocyanidin (PAC) that can be isolated from the bark of Parameria laevigata Moldenke (Apocynaceae). Parameritannin A-1 is a COX-2 inhibitor. Parameritannin A-1 also inhibits the activity of phospholipase A2 (PLA2).
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Lp-PLA2-IN-17
0 ImagesCat. No.: HY-160637CAS No.: 1818842-74-8Lp-PLA2-IN-17 (Compound 39) is an inhibitor of Lp-PLA2. Lp-PLA2-IN-17 can be used to study disorders involving the hydrolysis of oxidized lipids into two inflammatory substances with the participation of Lp-PLA2.
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M119
0 ImagesCat. No.: HY-177218CAS No.: 500533-94-8Synonyms: NSC 119910M119 (NSC 119910) is a Gβγ subunit and PLCβ3 inhibitor with selective activity toward μ-opioid receptor-related pathways. M119 selectively inhibits Gβγ-dependent PLCβ3 activation, reduces inositol phosphate production, and enhances μ-opioid receptor-mediated antinociception. M119 attenuates acute μ-opioid receptor agonist-induced antinociceptive tolerance and physical dependence in mice. M119 can be used for pain-related research.
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AX048
0 ImagesCat. No.: HY-112738CAS No.: 873079-69-7AX048 is an inhibitor for calcium-dependent phospholipase A2 cPLA2 with a XI(50) of 0.022 mole fraction and reveals an antihyperalgesic efficacy.
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BMS-229724
0 ImagesCat. No.: HY-120621CAS No.: 221914-85-8BMS-229724 is an orally active and tight-binding cytosolic phospholipase A2 (cPLA2) inhibitor with an IC50 of 2.8 μM. BMS-229724 can inhibit the production of arachidonic acid and eicosanoids in U937 cells, neutrophils, platelets, and other cells. BMS-229724 has anti-inflammatory activity and can be used in the research of diseases such as skin inflammation.
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WAY-196025
0 ImagesCat. No.: HY-119094CAS No.: 540523-42-0WAY-196025 is a selective and orally active indole cytosolic phospholipase A2 alpha (cPLA2α) inhibitor with an IC50 of 0.01μM and a Kd of 0.013 μM. WAY-196025 can inhibit the production of prostaglandins (such as PGE2) and leukotrienes (such as LTB4), and reduce the release of inflammatory mediators. WAY-196025 can be used for the researches of inflammation and immunology, such as asthma.
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Plipastatin B1
0 ImagesCat. No.: HY-113560CAS No.: 103955-73-3Plipastatin B1 is a lipopeptide antibiotic, an inhibitor of phospholipase A2 (PLA2), which has antifungal activity.
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Cacospongionolide B
0 ImagesCat. No.: HY-N21818CAS No.: 172854-76-1Cacospongionolide B is an orally active sesterterpene compound that can be isolated from Fasciospongia cavernosa. Cacospongionolide B is a secreted phospholipase A2 (sPLA2) inhibitor with an IC50 of 4.3 μM. Cacospongionolide B exhibits antibacterial activity. Cacospongionolide B downregulates the expression of iNOS, COX-2 and TNF-α by inhibiting NF-κB nuclear translocation and its DNA binding, and simultaneously selectively and irreversibly inhibits sPLA2 enzymatic activity. Cacospongionolide B can be used in studies related to bacterial infection and adjuvant arthritis.
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ML256
0 ImagesCat. No.: HY-128762CAS No.: 2415152-07-5ML256 is a covalent lipoprotein-associated phospholipase A2 (Lp-PLA2 inhibitor. ML256 can be used for the study of neoplasms harboring a constitutively active variant of one or both of KRAS or HRAS.
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AGN-190383
0 ImagesCat. No.: HY-165327CAS No.: 120755-15-9AGN-190383 is a bee venom phospholipase A2 inhibitor. AGN 190383 inhibits both hormone-operated and depolarization-dependent calcium mobilization as well as fMLP stimulated increases in free cytosolic calcium. AGN-190383 has anti-inflammatory activity.
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Ro 23-9358
0 ImagesCat. No.: HY-108132CAS No.: 153125-17-8Ro 23-9358 is a potent secretory phospholipase A2 inhibitor with anti-inflammatory activity.
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ASM-IN-2
0 ImagesCat. No.: HY-162613CAS No.: 2305789-66-4ASM-IN-2 (Compound 46) is a potent ASM inhibitor with an IC50 value of 0.87 μM, displaying good drug-like properties. ASM-IN-2 involves in multiple antidepressant mechanisms of actionin, which are associated with a decline of ceramide. It demostrates remarkable antidepressant effects in the CUMS-induced mouse, which is promising for research in the field of antidepressant drugs.
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ML114
0 ImagesCat. No.: HY-128020CAS No.: 866149-26-0ML114 is a specific inhibitor of RBBP9 serine hydrolase, with an IC50 of 0.63 μM against recombinant RBBP9. ML114 can inhibit the proliferation of human pluripotent stem cells (hPSCs) by regulating the expression of NFYA and other factors, but does not induce differentiation. ML114 can be used in the research of diseases such as retinoblastoma.
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Difluprednate-d3-1
0 ImagesCat. No.: HY-17569S2Difluprednate-d3-1 is the deuterium labeled Difluprednate (HY-17569). Difluprednate is a glucocorticoid receptor (GC receptor) agonist with a Ki of 0.78 nM. Difluprednate's active metabolite 21-deacetylated difluprednate (DFB) is a competitive agonist of GC receptors with a Ki of 0.061 nM. Difluprednate binds to GC receptors through metabolism to DFB, regulating the transcription of inflammatory mediator genes, thereby exerting anti-inflammatory activity. Difluprednate can be used for research related to ocular inflammation, such as postoperative inflammation, anterior uveitis, etc.
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Thioetheramide-PC
0 ImagesSynonyms: 1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholineThioetheramide-PC (1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine) is a structurally modified phospholipid that acts as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). Thioetheramide-PC has an IC50 value of 2 μM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, Thioetheramide-PC also binds to the activation site of the enzyme. Thioetheramide-PC binds more tightly to the activation site than to the catalytic site. As a result of this dual interaction, at low concentrations, Thioetheramide-PC may activate phospholipase activity rather than inhibit it.
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NDs-IN-1
0 ImagesCat. No.: HY-158334CAS No.: 3033806-97-9(Neurodegenerative diseases) NDs-IN-1 (Compound 3g) inhibits the activities of key enzymes such as hBACE-1, hAChE and hMAO-B. NDs-IN-1 is a novel non-covalent multi-target inhibitor. NDs-IN-1 is mainly used in the study of neurodegenerative diseases.
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sPLA2-IIA Inhibitor
0 ImagesCat. No.: HY-P10053CAS No.: 236394-37-9sPLA2-IIA Inhibitor is a cyclic pentapeptide analog of FLSYK (cyclic 2-Nal-Leu-Ser-2-Nal-Arg (c2)), that binds to hGIIA (human IIA phospholipase A2) and inhibits its hydrolytic ability. sPLA2 is a member of the esterase superfamily that catalyzes the hydrolysis of the ester bond at the sn-2 position of glycerophospholipids, releasing free fatty acids such as arachidonic acid and lysophospholipids.
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Lp-PLA2-IN-6
0 ImagesCat. No.: HY-142774CAS No.: 2637485-13-1Lp-PLA2-IN-6 (compound 18), a tetracyclic pyrimidinone compound, is a potent Lp-PLA2 inhibitor with a pIC50 of 10.0 for rhLp-PLA2. Lp-PLA2-IN-6 has the potential for neurodegenerative related diseases research.
