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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
87 Results for "
Reversible Inhibition
" in MedChemExpress (MCE) Product Catalog:
Products (87)
87 Results for "Reversible Inhibition" in MCE Product Catalog:
Cat. No.: HY-176542
CAS No.: 3030718-42-1
TD034 is a selective, reversible and noncovalent HDAC11 inhibitor with an IC50 of 5.1 nM and a Ki of 1.5 nM. TD034 does not inhibit other HDACs or sirtuins. TD034 inhibits the defatty acylation of SHMT2 (HDAC11 substrate). TD034 decreases the YAP1 level via HDAC11 inhibition. TD034 can be used for the study of lung cancer .
Cat. No.: HY-N3474
CAS No.: 94805-83-1
Category:
Flavonols other families Flavonoids Other Diseases Phenols Polyphenols Plants Disease Research Fields
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Synonyms: BIA 3-202
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Nebicapone (BIA 3-202), a reversible catechol-O-methyltransferase (COMT) inhibitor, is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of COMT, and it is potential for the treatment of Parkinson's disease .
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MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .
Cat. No.: HY-117853
CAS No.: 154355-76-7
Synonyms: ABT-761; VIA-2291
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Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation . Atreleuton is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
Synonyms: MK-678; L-363586
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Synonyms: SAR 444727; PRN473
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Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling .
Cat. No.: HY-129923
CAS No.: 161796-77-6
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(R)-Omeprazole sodium is a gastric acid resistant compound with activity to inhibit gastric acid secretion. (R)-Omeprazole sodium is metabolized in vivo, and its metabolism is primarily affected by cytochrome P450 enzymes. The interaction between (R)-Omeprazole sodium and mannitol may affect its bioavailability in formulations. (R)-Omeprazole sodium exhibits reversible direct and metabolism-dependent inhibition of CYP2C19 .
Cat. No.: HY-15427A
CAS No.: 1133432-46-8
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GDC-0834 Racemate is the racemic form of GDC-0834 (HY-15427). GDC-0834 is an orally active selective, potent, and reversible BTK inhibitor with an IC50 of 5.9 nM. GDC-0834 demonstrates pBTK-Tyr223 inhibition in mice and rats. GDC-0834 can be used for research of rheumatoid arthritis (RA) .
Cat. No.: HY-P5272
CAS No.: 112844-49-2
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Cat. No.: HY-110137A
CAS No.: 73819-26-8
Synonyms: DB75; NSC 305831
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Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .
Cat. No.: HY-12733
CAS No.: 1254318-44-9
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AZD5248 is an orally active, selective dipeptidyl peptidase 1 (cathepsin C) inhibitor, with IC50 values of 1 nM and 17 nM against human CatC, 44 nM against human DPP1, and 67 nM against rat DPP1. It exhibits low clearance and high bioavailability in animal models. AZD5248 forms an irreversible covalent bond with the catalytic Cys234 residue of CatC, exerts reversible inhibition via its nitrile moiety, blocks CatC-dependent amyloid formation, and reduces the activation levels of neutrophil serine proteases in bone marrow and blood. AZD5248 reacts with aortic elastin aldehydes to form stable 4-imidazolinones, induces ultrastructural changes in aortic tissue, and has an α-amino acid-based backbone. AZD5248 reduces the severity of acute pancreatitis in mouse models. AZD5248 can be used in research on chronic obstructive pulmonary disease, acute pancreatitis, neurodegenerative diseases, lysosomal storage disorders, acute lung injury, cystic fibrosis, and neutrophil-mediated inflammatory diseases .
Cat. No.: HY-162837
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AURKA against 1 is an inhibitor of AURKA (IC50 less than 0.5 nM), targeting endogenous lysine (K162) acetylation, and has anti-proliferation activity against tumor cells. AURKA against 1 induces K162 acetylation, and the kinase activity of AURKA is reversibly restored in HCT116 cells transfected with SIRT3 .
Cat. No.: HY-123129
CAS No.: 85073-83-2
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RS 2232 is an orally active, competitive 5-HT deamination inhibitor with a Ki of 0.054 μM. RS-2232 exhibits reversible and specific inhibition of type A monoamine oxidase. RS 2232 can be used in brain research .
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A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
Cat. No.: HY-165498
CAS No.: 220854-06-8
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AU-461 is an orally active and reversible inhibitor of the gastric H⁺/K⁺ ATPase with IC₅₀ values for rabbit-derived and pig-derived enzymes are 12.15 μM and 4.20 μM respectively. AU-461 competes with activated cationic K⁺ (Kᵢ = 1.64 μM). AU-461 reduces both histamine-stimulated gastric acid secretion and basal gastric acid secretion in rats. AU-461 inhibits ulcer formation caused by ethanol or sodium hydroxide, and restores the plasma gastrin level to normal. AU-461 can be used for the study of peptic ulcers .
Cat. No.: HY-13007A
CAS No.: 1279034-84-2
Synonyms: PF-03758309 hydrochloride
PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
Cat. No.: HY-13007B
Synonyms: PF-03758309 dihydrochloride
PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
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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
