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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
203 Results for "
Slow Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (203)
203 Results for "Slow Inhibitors" in MCE Product Catalog:
29
29 Publications Verification
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PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
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29 Publications Verification
Cat. No.: HY-18731
CAS No.: 214358-33-5
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1400W dihydrochloride is the dihydrochloride form of 1400W (HY-18730). 1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation .
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29 Publications Verification
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Research Areas:
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
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1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation .
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28 Cited Publications
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SKF-96365 hydrochloride is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .
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28 Cited Publications
Cat. No.: HY-125942
CAS No.: 162849-90-3
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SKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .
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23 Cited Publications
Cat. No.: HY-16706A
CAS No.: 1622921-15-6
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Remodelin hydrobromide is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin hydrobromide inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin hydrobromide inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin hydrobromide enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
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23 Cited Publications
Cat. No.: HY-16706
CAS No.: 949912-58-7
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Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells. Remodelin inhibits the growth of prostate cancer and hepatocellular carcinoma in xenograft model. Remodelin enhances the healthspan in hutchinson-gilford progeria syndrome (HGPS) mouse model .
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Azeliragon (TTP488) is an orally bioavailable inhibitor of the receptor for advanced glycation end products (RAGE) in development as a potential treatment to slow disease progression with mild Alzheimer’s disease (AD) . Azeliragon also can cross the blood-brain barrier (BBB) .
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Ralimetinib is an ATP-competitive p38α and p38β MAPK inhibitor with an IC50 of 5.3 nmol/L against human p38α and an IC50 of 3.2 nmol/L against human p38β. Ralimetinib slows tumor growth in preclinical in vivo cancer models, exhibits oral bioavailability in mice, and achieves sustained target inhibition for 4 to 8 h. Ralimetinib is applicable for research on melanoma, non-small cell lung cancer, ovarian cancer, glioma, multiple myeloma, breast cancer, renal cancer, and head and neck squamous cell carcinoma .
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Diltiazem hydrochloride is a Ca 2+ influx inhibitor (slow channel blocker or calcium antagonist).
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Skp2 Inhibitor C1 (SKPin C1) is an S-phase kinase-related protein 2 (Skp2) inhibitor with an inhibitory effect on metastatic melanoma cells. Skp2 Inhibitor C1 slows the cell cycle, inhibits cell proliferation, and triggers apoptosis .
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Category:
Rumex crispus Linn. Quinones Polygonaceae Anthraquinones Plants Disease Research Fields Inflammation/Immunology
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6 Cited Publications
Synonyms: Arachidonyl trifluoromethyl ketone
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AACOCF3 (Arachidonyl trifluoromethyl ketone) is a cell-permeant trifluoromethyl ketone analog of arachidonic acid. AACOCF3 is a potent and selective slow binding inhibitor of the 85-kDa cytosolic phospholipase A2 (cPLA2). AACOCF3 blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. AACOCF3 inhibits glucose-induced insulin secretion from isolated rat islets. AACOCF3 has the potential for the research of cardiovascular disease .
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5 Cited Publications
Cat. No.: HY-19348
CAS No.: 937039-45-7
Synonyms: RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII
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Pimelic Diphenylamide 106 (TC-H 106) is a slow, tight binding class I HDAC inhibitor (inhibits HDAC1, 2, and 3 with IC50 values of 150 nM, 760 nM, and 370 nM, respectively), with no activity against class II HDACs. Pimelic Diphenylamide 106 modulates dopamine concentration and protects dopamine cells by inducing VMAT2 expression. Pimelic Diphenylamide 106 can be used in the study of neuropsychiatric diseases such as attention deficit hyperactivity disorder (ADHD) .
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3 Cited Publications
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BOS-318 is a potent, slowly dissociating, highly selective, and cell-permeable furin inhibitor with IC50 value of 1.9 nM. BOS-318 protects ENaC from subsequent activation by neutrophil elastase. BOS-318 can be used for the rsearch for CF lung disease .
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3 Cited Publications
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CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase. It binds to E. coli LpxC with a Ki of 4.0 nM. CHIR-090 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
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2 Cited Publications
Synonyms: UL-FS-49; UL-FS-49CL
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Zatebradine (UL-FS-49 (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 values 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
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2 Cited Publications
Synonyms: UL-FS-49 free base; UL-FS-49CL free base
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Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) is a potent inhibitor of hyperpolarization-activated cyclic nucleotide-gated (HCN) channels with an IC50 value of 1.96 µM. Zatebradine blocks the slow inward current through human HCN1, HCN2, HCN3 and HCN4 channels, with IC50 values of 1.83 µM, 2.21 µM, 1.90 µM and 1.88 µM, respectively .
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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
