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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
19 Results for "
Kinetic Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "Kinetic Inhibitors" in MCE Product Catalog:
1
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WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
Cat. No.: HY-W583212
CAS No.: 14354-67-7
Synonyms: ZnMP
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Cat. No.: HY-130076
CAS No.: 869577-51-5
MMP-2 Inhibitor II (compound 2) is a selective MMP-2 inhibitor. The Kinetic parameters for MMP inhibition are 2.4 μM (MMP-2), 45 μM (MMP-1), and 379 μM (MMP-7), respectively .
Cat. No.: HY-P3123A
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Synonyms: U-99194A; PNU-99194A maleate; JPC-211 maleate
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U-99194 (PNU-99194) maleate is a selective, potent dopamine D3 receptor antagonist (Ki =160 nM). U-99194 maleate inhibits the activation of D3 receptor mediated by endogenously released dopamine or exogenous D3 agonists. U-99194 maleate abrogates the IPSC-suppressive effect of the D3 agonist PD 128907 in rat hippocampal slices. U-99194 maleate significantly suppresses Nicotine (HY-127019)-induced tremor in mice. U-99194 maleate can be used for the study of dopamine D3 receptor-mediated motor disorders, particularly kinetic tremors .
Cat. No.: HY-179227
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HDAC6 ligand-7 (Compound 16a) is a positron emission tomography (PET) tracer for the deacetylase 6 (HDAC6) enzyme with a Kd value of 1.66 nM. HDAC6 ligand-7 exhibits excellent HDAC6 inhibitory activity, with IC50 values of 2.7 and 3.7 nM for hHDAC6 and mHDAC6, respectively, and has high selectivity for HDAC1/4/7/8. HDAC6 ligand-7 after being radioactively labeled with fluorine-18, [¹⁸F]HDAC6 ligand-7 shows varying degrees of radioactive uptake in PET, which can reflect the specific binding to HDAC6. HDAC6 ligand-7 can be used for the study of HDAC6 imaging .
Cat. No.: HY-133668R
CAS No.: 2306-33-4
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Cat. No.: HY-174800
CAS No.: 2230854-98-3
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ARN21929 is a Topoisomerase II inhibitor with an IC50 of 4.5 μM. ARN21929 exhibits excellent kinetic and thermodynamic solubility as well as metabolic stability. However, ARN21929 shows poor antiproliferative activity against A549, DU145, MCF7, HeLa, and A375 cells. ARN21929 can be used in the study of cancer .
Cat. No.: HY-147711
CAS No.: 329783-03-1
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α-Amylase/α-Glucosidase-IN-1 (compound 33) is a potent α-amylase/α-glucosidase inhibitor with IC50s of 2.01, 2.09 µM for α-amylase and α-glucosidase, respectively. Kinetic studies predict that α-Amylase/α-Glucosidase-IN-1 has the potential of anti hyperglycemia .
Cat. No.: HY-159081
CAS No.: 3052008-10-0
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AChE/BChE-IN-20 (compound 3m) is an acetylcholinesterase (AChE, IC50=34.81 μM) and butylcholinesterase (BChE, IC50=20.66 μM) inhibitor, which has been demonstrated to have affinity for key enzyme pockets and favorable interaction profiles by molecular docking and kinetic simulations, and can be used in the study of Alzheimer's disease .
Cat. No.: HY-143743
CAS No.: 2303917-78-2
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Cap-dependent endonuclease-IN-2 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-2 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-2 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent WO2019052565A1, compound 28) .
Cat. No.: HY-143755
CAS No.: 2631005-84-8
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Cap-dependent endonuclease-IN-9 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-9 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-9 has strong inhibitory effect on RNA polymerase activity of A virus (extracted from patent CN112521386A, compound VI-1) .
Cat. No.: HY-P3123
CAS No.: 172666-82-9
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Cat. No.: HY-179216
CAS No.: 2397562-26-2
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KTT-1 is a kinetically selective and orally active HDAC2 inhibitor. KTT-1 exhibits high HDAC2-selectivity over HDAC1. KTT-1 inhibits osteoclast differentiation at an early stage by downregulating c-Fos expression. KTT-1 effectively suppresses arthritis symptoms in the collagen-induced arthritis (CIA) mouse model. KTT-1 can be used for the research of rheumatoid arthritis and neurodegenerative diseases .
Cat. No.: HY-12701
CAS No.: 82668-33-5
Synonyms: U-99194A free base; PNU-99194A; JPC-211
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U-99194 (PNU-99194) is a selective, potent dopamine D3 receptor antagonist. U-99194 inhibits the activation of D3 receptor mediated by endogenously released dopamine or exogenous D3 agonists. U-99194 abrogates the IPSC-suppressive effect of the D3 agonist PD 128907 in rat hippocampal slices. U-99194 significantly suppresses Nicotine (HY-127019)-induced tremor in mice. U-99194 can be used for the study of dopamine D3 receptor-mediated motor disorders, particularly kinetic tremors .
Cat. No.: HY-180919
CAS No.: 3047675-62-4
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ERG-IN-5 (Compound M1) is a metabolite of ERG-IN-4 (HY-180918), and it is a hERG potassium channel inhibitor with an IC50 of 1.5 μM. ERG-IN-5 is cytotoxic to MTAP del HCT116 and its CC50 is 28 nM. ERG-IN-5 can be used for the study of colon cancer .
Cat. No.: HY-187358
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Polθ-IN-12 is a DNA polymerase θ (PolQ) polymerase domain inhibitor with a human pIC50 of 8.3. Polθ-IN-12 binds to the allosteric pocket of the PolQ polymerase domain, forming salt bridge interactions with residues Arg-2347 and Arg-2419. Polθ-IN-12 displays improved human metabolic stability and high kinetic solubility at pH 7.4. Polθ-IN-12 shows low CACO-2 permeability and acts as a modest efflux substrate .
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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
