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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
38 Results for "
tight binding
" in MedChemExpress (MCE) Product Catalog:
Products (38)
38 Results for "tight binding" in MCE Product Catalog:
29
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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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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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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4 Cited Publications
Synonyms: HMTase Inhibitor IX
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MM-102 (HMTase Inhibitor IX) is a cell-permeable and tightly binding inhibitor of MLL1-WDR5 interaction (IC50=2.4 nM). MM-102 can specifically inhibit the growth and induce apoptosis of leukemia cells containing MLL1 fusion protein, and reduce renal fibrosis and inflammation in mice with ischemia-reperfusion injury. In addition, MM-102 also acts as an H3K4 histone methyltransferase inhibitor to improve the development of porcine somatic cell nuclear transfer (SCNT) embryos .
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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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1 Cited Publications
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Amastatin hydrochloride is a slow, tight binding, competitive aminopeptidase (AP) inhibitor with Ki values of 0.26 nM, 30 nM, 52 nM for Aeromonas aminopeptidase, cytosolic leucine aminopeptidase, microsomal aminopeptidase .
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1 Cited Publications
Cat. No.: HY-D2468
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Sulfonylurea Receptor HRP-Streptavidin is a biotin-binding signal amplifier designed to bind tightly with biotinylated anti-TSH monoclonal antibodies, thereby constituting a key component of the signal amplification system in immunoassays. HRP-Streptavidin is formed by the covalent coupling of Horseradish Peroxidase (HRP) with Streptavidin; it combines the highly efficient catalytic activity of the enzyme with the high affinity of Streptavidin for biotin, making it a potent and sensitive tool for signal amplification. HRP-Streptavidin is suitable for use in Western Blotting, ELISA, and other detection techniques .
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Opelconazole (PC945), a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. Opelconazole is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively .
Cat. No.: HY-B0306
CAS No.: 14222-60-7
Synonyms: Protionamide
Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
Cat. No.: HY-P991200
Cat. No.: HY-P11446
CAS No.: 254729-66-3
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ONO-0300302 is an orally active and potent LPA1 (lysophosphatidic acid receptor 1) antagonist, with an IC50 of 0.086 μM. ONO-0300302 is a slow tight binding inhibitor, and its binding affinity increases with time, with Kd of 0.34 nM (37 °C, 2 h). ONO-0300302 can be used for benign prostatic hyperplasia (BPH) research .
QStatin is a potent and selective inhibitor of SmcR (V. harveyi LuxR homologue) with an EC50 of 208.9 nM, binding tightly to SmcR and changes the flexibility of the protein, thereby altering its transcription regulatory activity. QStatin shows pan-QS (Vibrio quorum sensing) inhibitor activity in diverse Vibrio species and attenuates their virulence in an aquatic host. QStatin may be a sustainable antivibriosis agent useful in aquacultures .
Cat. No.: HY-125475
CAS No.: 927881-99-0
Synonyms: GMI-1070
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Rivipansel is a small-molecule glycomimetic pan-selectin antagonist with inhibitory activity against E-selectin and P-selectin. Rivipansel binds tightly to the lectin domain of E-selectin, and selectively blocks the recognition of CD62L by E-selectin without affecting the binding of PSGL-1 to E-selectin. Rivipansel functionally inhibits the adhesion of hematopoietic cells to endothelial cells, and is applicable to research related to sickle cell disease .
Cat. No.: HY-161304
CAS No.: 2444302-23-0
HDAC6-IN-33 (compound 6) is a selective and irreversible HDAC6 inhibitor with an IC50 of 193 nM. HDAC6-IN-33 shows no activity against HDAC1-4. HDAC6-IN-33 is a tight-binding HDAC6 inhibitor capable of inhibiting HDAC6 via a two-step slow-binding mechanism .
Cat. No.: HY-P3828
CAS No.: 923949-88-6
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Cat. No.: HY-125969
CAS No.: 852935-07-0
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Rtt109 inhibitor 1 (Compound 1) is an inhibitor for histone acetyltransferase Rtt109 through a tight binding, uncompetitive system. Rtt109 inhibitor 1 exhibits antifungal activity through acetylation at H3K56 site .
Cat. No.: HY-P2713
CAS No.: 314266-76-7
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Cat. No.: HY-P11446A
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Cat. No.: HY-113646
CAS No.: 1013621-70-9
Shield-2 is an efficient stabilizing ligand binding to the FKBP (F36V) protein with a dissociation constant of 29 nM. Shield-2 binds tightly to the FKBP mutants destabilizing domains and prevents degradation, thus providing small molecule regulation over intracellular protein levels .
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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
