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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
31 Results for "
serine hydrolase inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (31)
31 Results for "serine hydrolase inhibitor" in MCE Product Catalog:
3
3 Cited Publications
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LY2183240 is a highly potent blocker of anandamide uptake (IC50= 270 pM; Ki=540 nM). LY2183240 is a potent, covalent inhibitor of the endocannabinoid-degrading enzyme fatty acid amide hydrolase (FAAH) with an IC50 of 12.4 nM. LY2183240 inactivates FAAH by carbamylation of the enzyme's serine nucleophile. LY2183240 also inhibits several other brain serine hydrolases with IC50s of 5.3, 0.09, 8.2 nM for MAG lipase, bh6 and KIAA1363, respectively .
3
3 Cited Publications
Cat. No.: HY-18977
CAS No.: 1380424-42-9
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KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH .
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2 Cited Publications
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PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a Ki of 0.23 μM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition .
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2 Cited Publications
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Lalistat 1 is a potent, selective, and competitive inhibitor of lysosomal acid lipase (LAL) and against purified human LAL (phLAL) with an IC50 of 68 nM. Lalistat 1 is a inhibitor of immunoglobulin A1 protease (IgA1P) proteases for H. influenzae, has less effects on other serine hydrolases (trypsin or β-lactamase, etc.). Lalistat 1 can be used for the research of niemann-pick type C (NPC) disease .
1
1 Cited Publications
Cat. No.: HY-124700
CAS No.: 1966129-74-7
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LYPLAL1-IN-1 (compound 11) is a selective, covalent, and irreversible inhibitor of the lysophospholipase-like enzyme LYPLAL1 (IC50 = 6 nM). LYPLAL1-IN-1 shows selectivity against other serine hydrolases such as carboxylesterase CES1 (IC50 > 50 μM for CES1). LYPLAL1-IN-1 inhibits the depalmitoylation function of LYPLAL1, blocking its depalmitoylation modification of cyclic GMP-AMP synthase (cGAS), thereby promoting cGAS dimerization and activation, and initiating the cGAS-STING pathway-mediated innate immune response. LYPLAL1-IN-1 can enhance DNA-induced type I interferon production, upregulate PD-L1 expression in tumor cells, and promote the accumulation of tumor-infiltrating CD8 + T cells, with the core function of strengthening the anti-tumor immune response. LYPLAL1-IN-1 is primarily used in tumor immunology research, especially in combination with PD-1/PD-L1 inhibitors .
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1 Cited Publications
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AMZ30 is selective protein phosphatase methylesterase-1(PME-1) inhibitor with IC50s of 600 nM and 3.5 µM in human cell lysates and in HEK 293T cells, respectively. AMZ30 shows >100-fold selectivity relative to other serine hydrolases. AMZ30 reduces the demethylated form of PP2A in living cells. AMZ30 attenuates muscle cell differentiation. AMZ30 increases the resistance of U87MG and U251MG glioblastoma cells to t-BHP-induced oxidative stress. AMZ30can be used for the study of glioblastoma .
Cat. No.: HY-18522
CAS No.: 1312782-34-5
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AA26-9 is a potent and broad spectrum serine hydrolase inhibitor. AA26-9 targets included serine peptidases, lipases, amidases, esterases, and thioesterases. AA26-9 shows inhibitory activity against approximately 1/3 of the 40+ serine hydrolases detected in immortalized T cell lines .
Synonyms: Benzothiazole analog 3
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FAAH inhibitor 1 (compound 3) is a selective reversible FAAH inhibitor. FAAH inhibitor 1 has no off-target activity with respect to other serine hydrolases. FAAH inhibitor 1 is exclusively specific against FAAH in rat brain with an IC50 value of 18 nM and had no missing protein bands in all the other tissues. FAAH inhibitor 1 can be used for neurological disorders research .
ARUK3001185 is a potent, selective, orally active and brain-penetrant inhibitor of Notum (IC50 = 6.7 nM). ARUK3001185 can restore Wnt signaling in the presence of Notum in vitro. ARUK3001185 is selective against serine hydrolases, kinases, and drug targets. ARUK3001185 can be used to research the role of Notum plays in diseases .
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WWL113 is a selective and orally active Ces3 and Ces1f inhibitor, with IC50 values of 120 nM and 100 nM for Ces3 and Ces1f, respectively. WWL113 appears to show excellent selectivity for the 60-kDa serine hydrolase (or hydrolases) .
Cat. No.: HY-18081
CAS No.: 959151-50-9
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PF 750 is a selective, covalent and brain-penetrant fatty acid amide hydrolase (FAAH) inhibitor. PF 750 covalently carbamylates FAAH's catalytic serine nucleophile to inactivate the enzyme .
Cat. No.: HY-164838
CAS No.: 1831135-57-9
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ABC47 is a potent inhibitor of serine hydrolases. ABC47 shows IC50s of 0.03 and 0.1 μM for ABHD4 and ABHD3, respectively. ABC47 plays an important role in infantile neuronal ceroid lipofuscinosis research .
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Serine Hydrolase inhibitor-21 (compound 8), a pyridine, is a serine hydrolase inhibitor with a Ki of 429 nM for BuChE. Serine Hydrolase inhibitor-21 has the potential for Alzheimer's disease research .
Cat. No.: HY-18544
CAS No.: 65815-76-1
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AA38-3 is a serine hydrolase (SH) inhibitor. AA38-3 can inhibit three SHs, ABHD6, ABHD11, and FAAH .
Cat. No.: HY-126031
CAS No.: 2055172-60-4
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(R)-KT109 is a peripherally restricted serine hydrolase inhibitor that cannot cross the blood-brain barrier. (R)-KT109 irreversibly inhibits ABHD6, DAGLα and DAGLβ via carbamoylation of the active-site serine. (R)-KT109 exerts selective inhibitory effects on serine hydrolases in mouse brains, with pIC50 values of 8.6, 9.1 and 8.2 against human ABHD6, DAGLα and DAGLβ, respectively. (R)-KT109 effectively reduces the levels of 2-arachidonoylglycerol, arachidonic acid, eicosanoids and TNF-α. (R)-KT109 is widely used in studies of metabolic syndrome-related diseases and neuroinflammation .
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ABC44 is a potent serine hydrolase inhibitor with IC50s of 0.1 μM and 6.5 μM for palmitoyl protein thioesterase 1 (PPT1) in situ and in vitro, respectively. ABC44 can be used for researching infantile neuronal ceroid lipofuscinosis .
Cat. No.: HY-103463
CAS No.: 1346169-63-8
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SA57 is a potent, selective FAAH inhibitor with IC50s of 3.2 nM and 1.9 nM for mouse and human FAAH. SA57 also inhibits the 2-arachidonoylglycerol hydrolases MAGL (IC50s of 410 nM and 1.4 μM for mouse and human MAGL) and mouse α/β-hydrolase domain-containing protein 6 (mABHD6; IC50 of 850 nM), but not other brain serine hydrolases .
Cat. No.: HY-12909
CAS No.: 1207745-58-1
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MK-4409 is an orally active and blood-brain barrier-penetrant fatty acid amide hydrolase (FAAH) inhibitor (human IC50 = 11 nM; rat IC50 = 11 nM) that reversibly and non-covalently inhibits this serine hydrolase, elevating endogenous fatty acid ethanolamides. MK-4409 alleviates inflammatory and neuropathic pain, with a long duration of action, and reduces edema. MK-4409 can be used for research on inflammatory and neuropathic pain .
Cat. No.: HY-128020
CAS No.: 866149-26-0
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ML114 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 .
Cat. No.: HY-32207S
CAS No.: 2089333-15-1
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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
