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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
14 Results for "
dissociation rates
" in MedChemExpress (MCE) Product Catalog:
Products (14)
14 Results for "dissociation rates" in MCE Product Catalog:
1
1 Cited Publications
Cat. No.: HY-P10495A
Target:
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Cat. No.: HY-NP143
CAS No.: 93928-24-6
Cat. No.: HY-150085
CAS No.: 2393881-77-9
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GSK951 is a highly potent, selective, and reversibly covalent KLK5 inhibitor, with an IC50 of approximately 250 pM and a pIC50 of 9.6 against hKLK5. It exhibits over 100-fold selectivity over KLK7, KLK14, matriptase, and elastase. GSK951 binds to the catalytic site of KLK5 via covalent interaction with the catalytic serine, with a slow dissociation rate. GSK951 improves skin barrier function, reduces transepidermal water loss, decreases the expression of proinflammatory cytokines, and inhibits the elevated KLK5 protease activity in the stratum corneum. GSK951 can be used in studies related to skin barrier dysfunction.
Cat. No.: HY-P10495
CAS No.: 1778685-49-6
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Cat. No.: HY-175872
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14-3-3σ/ERα stabilizer-2 (Compound 41) is a covalent 14-3-3σ/ERα stabilizer with a Kd of 10.1 nM. 14-3-3σ/ERα stabilizer-2 significantly decreases the dissociation rate of ERα, stabilizing the binary ERα/14-3-3σ interaction. 14-3-3σ/ERα stabilizer-2 can be used for molecular glues research .
Cat. No.: HY-126829
CAS No.: 1260635-77-5
Coumarin-SAHA is a fluorescent probe for determining the binding affinities (kd) and the dissociation off-rates (koff) of the HDAC8-inhibitor complexes .
Cat. No.: HY-161810
CAS No.: 2991693-72-0
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MRS8247 is a positive allosteric modulator (PAM) of the A3 adenosine receptor (A3AR) that can also slow the dissociation rate of agonists .
Cat. No.: HY-182423
CAS No.: 1310817-94-7
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RO5328673 is an orally active, blood-brain barrier permeable neurokinin receptor antagonist that effectively targets human NK3 receptors (Ki=0.4 nM, Ka=0.1 nM), human NK2 receptors (Ki=1.1 nM, Ka=0.9 nM), and guinea pig NK3 receptors (Ka=0.1 nM and 0.13 nM). RO5328673 acts as an insurmountable antagonist of NK3 receptors with a slow dissociation rate, while it shows rapid association and dissociation rates at human NK2 receptors. RO5328673 potently inhibits senktide (HY-P0187)-induced enhancement of spontaneous activity in dopaminergic neurons and reverses senktide-induced changes in motor activity of gerbils. RO5328673 is widely applicable to research related to schizophrenia .
Cat. No.: HY-P11770
CAS No.: 1352117-55-5
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α-Tubulin (residues 440-451) (α-Tubulin Tail) is a Microtubule growth inhibitor. α-Tubulin (residues 440-451) transiently interacts with the longitudinal polymerization interface of α-tubulin, regulating the apparent association and dissociation rates of tubulin at the microtubule growing end. α-Tubulin (residues 440-451) inhibits microtubule growth .
Cat. No.: HY-187811
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MAO-B-IN-62 is a MAO-B inhibitor with an IC50 of 0.8 μM against MAO-B. MAO-B-IN-62 also acts as a PPARγ agonist with an EC50 of 14.6 μM. MAO-B-IN-62 binds to the active site of free MAO-B and activates PPARγ, both with a slow dissociation rate and sustained target-binding capacity. MAO-B-IN-62 exhibits antioxidant and anti-inflammatory activities. MAO-B-IN-62 can be used in the research of neurodegenerative diseases .
Cat. No.: HY-187082
CAS No.: 587879-32-1
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P552-02 is an epithelial sodium channel (ENaC) inhibitor. P552-02 blocks ENaC function in humans, guinea pigs, rats and sheep, exhibits the characteristic of reduced dissociation rate after binding to ENaC, inhibits ENaC-mediated short-circuit current, and slows the absorption of airway surface liquid (ASL). P552-02 induces hyperkalemia in guinea pigs and rats, blocks the activity of airway ENaC in guinea pigs, and enhances mucociliary clearance in sheep both in vivo and in vitro. P552-02 is applicable to cystic fibrosis-related research .
Cat. No.: HY-W097223
CAS No.: 135-57-9
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PD-1/PD-L1-IN-58 (compound 2) is a novel inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-58 selectively binds to PD-L1 over PD-1, with a dissociation rate constant (KD) value of 77.60 nM. PD-1/PD-L1-IN-58 has oral activity. PD-1/PD-L1-IN-58 can be used in the research of influenza A virus .
Cat. No.: HY-182513
CAS No.: 459842-29-6
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ONO-8539 is an orally active prostanoid EP1 receptor antagonist with competitive, insurmountable binding and slow receptor dissociation for long-duration inhibition. ONO-8539 modulates afferent nerve function related to bladder activity, inhibits detrusor overactivity-related contractions, decreases nonvoiding contractions and voiding duration, and increases uroflow rate with ATP (HY-B2176)-induced detrusor overactivity. ONO-8539 attenuates acid-induced heartburn symptoms, extends time to first heartburn sensation, and prevents primary hypersensitivity after distal esophageal acidification. ONO-8539 can be used for the research of overactive bladder and gastroesophageal reflux disease .
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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
