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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
20 Results for "
competitive noncovalent inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (20)
20 Results for "competitive noncovalent inhibitor" in MCE Product Catalog:
15
15 Publications Verification
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GRL0617 is a selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLpro), with an IC50 of 0.6 μM and a Ki value of 0.49 μM. GRL0617 also inhibits SARS-CoV with an EC50 of 14.5 μM. GRL0617 can be used for the research of severe acute respiratory syndrome .
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1 Cited Publications
Cat. No.: HY-155108B
Purity: 99.88%
OATD-02 hydrochloride is the hydrochloride salt form of OATD-02 (HY-155108). OATD-02 hydrochloride an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and Arginase2. OATD-02 hydrochloride is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 hydrochloride bolishes tumor immunosuppression induced by both arginases. OATD-02 hydrochloride can be used for melanoma study .
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1 Cited Publications
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JNJ-42226314, a chemical probe, is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain .
Cat. No.: HY-W012817
CAS No.: 95-71-6
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Cat. No.: HY-159829
CAS No.: 1803346-98-6
Synonyms: NBI-1117568; HTL-0016878
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Direclidine (NBI-1117568, HTL-0016878) is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. It binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .
Cat. No.: HY-155108
CAS No.: 2146132-73-0
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study .
CH7233163 is a noncovalent ATP-competitive inhibitor for EGFR-Del19/T790M/C797S. CH7233163 can overcome Osimertinib (HY-15772)-Resistant EGFR-Del19/T790M/C797S mutation. CH7233163 blocks the EGFR phosphorylation in the Del19/T790M/C797S_NIH3T3 cells. CH7233163 has antitumor activities .
Cat. No.: HY-10243
CAS No.: 923590-37-8
Synonyms: MK-7009
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Vaniprevir (MK-7009) is a non-covalent competitive inhibitor of the hepatitis C virus (HCV) NS3/4A protease.
Cat. No.: HY-169422A
CAS No.: 3064599-37-4
Synonyms: IDE275 (enantiomer)
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GSK4418959 enantiomer is an enantiomer of GSK4418959 (HY-169422). GSK4418959 (IDE275) is a non-covalent, reversible, selective and orally active WRN helicase inhibitor. GSK4418959 inhibits ATPase and DNA unwinding functions in an ATP-competitive manner. GSK4418959 can be used for the study of microsatellite instability-high (MSI-H) cancer .
Cat. No.: HY-177936
CAS No.: 951950-33-7
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NAE-IN-3 (compound 1) is a potent, selective and non-covalent competitive NEDD8-activating enzyme (NAE) inhibitor (IC50 = 0.8 μM). NAE-IN-3 inhibits NAE by blocking the ATP-binding domain. NAE-IN-3 exhibits selectivity over analogous E1 enzymes UAE and SAE. NAE-IN-3 can be used for cancer research .
Cat. No.: HY-149929
CAS No.: 2872672-18-7
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EBL-3183, an indole-2-carboxylate, is a potent metallo-β-lactamase (MBL) inhibitor. EBL-3183 is reversibly binding, non-covalent, competitive NDM-1 inhibitor with a pIC50 of 7.7 .
Cat. No.: HY-156029
CAS No.: 2755685-19-7
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IA1-8H2 is a non-covalent, non-competitive inhibitor of PHPT1 (IC50: 3.4 μM). IA1-8H2 can be used for research of lung cancer, hepatocarcinoma, and renal cancer .
Cat. No.: HY-W012817R
CAS No.: 95-71-6
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Cat. No.: HY-176219
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Bcl-2-IN-23 (compound 5) is a selective inhibitor targeting Bcl-2. The IC50 of Bcl-2-IN-23 in HTB-140, HeLa and SW620 cells is 25.7-33.7 μM. Bcl-2-IN-23 can non-covalently competitively bind to Bcl-2 protein, significantly reduce its expression, and induce late apoptosis and necroptosis of cancer cells. Bcl-2-IN-23 enhances the sensitivity of cancer cells to apoptosis and reduces the release of IL-6 inflammatory factors by disrupting the Bcl-2-mediated mitochondrial apoptosis inhibition pathway. Bcl-2-IN-23 can be used for anti-apoptosis research of malignant tumors such as melanoma, cervical cancer, and colorectal cancer .
Cat. No.: HY-170399
CAS No.: 3053753-61-7
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SARS-CoV-2 PLpro-IN-1 (Compound 85) is a non-covalent and competitive inhibitor of SARS-CoV-2 PLpro with an IC50 of 15.06 μM and a Ki of 22.93 μM. SARS-CoV-2 PLpro-IN-1 inhibits the proliferation of Vero cell with an IC50 of 7.47 μM .
Cat. No.: HY-173305
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Mpro/PLPro-IN-2 (Compound 22l) is a non-covalent competitive dual inhibitor of the papain-like protease and main protease of SARS-CoV-2, with a Ki of 0.2 μM for the papain-like protease and a Ki of 1.1 μM for the main protease . Mpro/PLPro-IN-2 can be used in the research field of anti-SARS-CoV-2 .
Cat. No.: HY-189095
CAS No.: 57323-76-9
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KLK6-IN-2 is a reversible non-covalent and selective KLK6 inhibitor, with an IC50 of 2.1 μM against hKLK6. KLK6-IN-2 acts as a reversible competitive inhibitor of boar Spermatozoa acrosin, with a Ki of 2.6 μM against porcine acrosin. KLK6-IN-2 exhibits trypanocidal activity against Trypanosoma brucei rhodesiense, with an IC50 of 3.71 μM .
Cat. No.: HY-181912
CAS No.: 1461756-61-5
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D-DT/MIF-1-IN-1 (Compound 4h) is a non-competitive, non-covalent inhibitor of MIF-1 and D-DT, with IC50 values of 2.4 μM and 4.0 μM against D-DT, and an IC50 value of 9.8 μM against MIF-1. D-DT/MIF-1-IN-1 inhibits D-DT-induced phosphorylation of ERK and exerts antiproliferative activity in non-small cell lung cancer cells .
Cat. No.: HY-159829A
CAS No.: 3028447-14-2
Synonyms: NBI-1117568 citrate; HTL-0016878 citrate
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Direclidine (NBI-1117568, HTL-0016878) citrate is a selective orthosteric agonist targeting the muscarinic acetylcholine M4 receptor, exhibiting very low affinity for M1, M2, M3, and M5 receptors. Direclidine citrate binds to the orthosteric site of the M4 receptor in a non-covalent, competitive manner. Direclidine citrate specifically activates the M4 receptor, inhibiting the release of acetylcholine from striatal cholinergic interneurons, thereby regulating the balance of the dopaminergic system and reducing psychiatric symptoms associated with excessive dopamine release. Direclidine citrate can improve symptoms associated with neuropsychiatric disorders and is used in research on schizophrenia and other neuropsychiatric disorders .
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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
