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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
17 Results for "
ligand dissociation
" in MedChemExpress (MCE) Product Catalog:
Products (17)
17 Results for "ligand dissociation" in MCE Product Catalog:
1
Research Areas:
Synonyms: CPHPC; Ro63-8695; GSK2315698
Target:
Research Areas:
Miridesap is a ligand for serum amyloid P component (SAP) and intends to inhibit and dissociate SAP binding to amyloid fibrils and tangles.
Cat. No.: HY-D1092
CAS No.: 63560-89-4
Cat. No.: HY-P10495A
Target:
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UNC3474 is a small molecule ligand, binding with 53BP1. UNC3474 binds the aromatic methyl-lysine binding cage of 53BP1 TT, with a dissociation constant (Kd) of 1.0 ± 0.3 μM. UNC3474 inhibits the recruitment of 53BP1 to DSBs by stabilizing a pre-existing autoinhibited state of 53BP1 in cells .
Cat. No.: HY-168440
CAS No.: 2541626-73-5
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Aurora-A ligand 1 is a high-affinity and specific Aurora-A inhibitor with a dissociation constant (Kd) value of 0.85 nM. Aurora-A ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC Aurora-A degraders with antitumor activity. Aurora-A ligand 1 can be used for the synthesis of HLB-0532259 (HY-168439). HLB-0532259 shows anti-tumor activity against neuroblastoma .
Cat. No.: HY-173291
CAS No.: 3063166-64-0
Target:
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Tau ligand-1 (Compound 75) is a ligand for aggregated tau protein that can penetrate the blood-brain barrier . In tissues from patients with Alzheimer's disease, progressive supranuclear palsy, corticobasal degeneration, and Pick's disease, Tau ligand-1 exhibits high affinity for aggregated tau protein, with equilibrium dissociation constant (KD) values ranging from 1 to 3.8 nM . Tau ligand-1 can serve as a potential positron emission tomography (PET) tracer and holds promise for application in positron emission tomography imaging studies of tau-related diseases in the central nervous system .
Cat. No.: HY-157558
Synonyms: 8SGE
Target:
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KDRLKZ-1 (8SGE) is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 0.36 μM), with an IC50 of 0.21 μM and 0.31 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-1 binds to the substrate-binding pocket of the KLHDC2 kelch domain, mimics the interaction of natural substrates and displaces them. KDRLKZ-1 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-1 can be used in scaffold ligand research for PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-157559
Target:
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KDRLKZ-2 is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 95 nM), with an IC50 of 68 nM and 0.1 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-2 binds to the substrate-binding pocket of the kelch domain of KLHDC2, mimics the interaction of natural substrates and displaces them. KDRLKZ-2 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-2 can be used in scaffold ligand studies of PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-P10495
CAS No.: 1778685-49-6
Target:
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 .
Cat. No.: HY-14863
CAS No.: 250384-82-8
Synonyms: CTA-018
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Lunacalcipol (CTA-018), as a vitamin D analogue, has a dual role in the pathogenesis of Chronic Kidney Disease (CKD), as an agonist of vitamin D receptor and an antagonist of cytochrome P450 enzyme 24-hydroxylase. Lunacalcipol binds to VDR and regulates transcriptional activity of VDR by influencing ligand binding affinity, ligand-dependent coactivator recruitment or inhibitory factor dissociation, efficiency of ligand entry into target cells, tissue specificity and different metabolism of ligand. Lunacalcipol can be used in the study of CKD, especially Secondary Hyperparathyroidism (sHPT) .
Cat. No.: HY-180554
CAS No.: 300587-89-7
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UCB1244283 is a synaptic vesicle glycoprotein 2A (SV2A) allosteric modulator. UCB1244283 binds to a secondary ligand-binding site in SV2A and enhances orthosteric ligand engagement when the orthosteric site is occupied, by stabilizing the occluded state and slowing ligand dissociation. UCB1244283 shows a clear protective effect against both tonic and clonic convulsions in sound-sensitive mice. UCB1244283 can be used for epilepsy research .
Cat. No.: HY-P10332
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Cat. No.: HY-101861R
CAS No.: 224624-80-0
Synonyms: CPHPC (Standard); Ro63-8695 (Standard); GSK2315698 (Standard)
Target:
Research Areas:
Miridesap (Standard) is the analytical standard of Miridesap (HY-101861). This product is intended for research and analytical applications. Miridesap is a ligand for serum amyloid P component (SAP) and intends to inhibit and dissociate SAP binding to amyloid fibrils and tangles.
Cat. No.: HY-183984
Target:
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G-quadruplex ligand 6 is a G-quadruplex ligand targeting the c-MYC promoter with anti-tumor activity. G-quadruplex ligand 6 forms a non-covalent complex with Pu22, a G-quadruplex model of the c-MYC promoter, with a microscopic dissociation constant Kd of 0.202 μM. G-quadruplex ligand 6 selectively inhibits tumor cell proliferation, blocks the binding of transcription factors by stabilizing the G-quadruplex in the c-MYC promoter, and thereby regulates the expression of proto-oncogenes. G-quadruplex ligand 6 can be used in the research of pancreatic cancer, non-small cell lung cancer, colorectal cancer, and triple-negative breast cancer .
Cat. No.: HY-W686762
CAS No.: 219704-16-2
Target:
Research Areas:
m,p-Dimethyl PPE is a D4 dopamine receptor ligand. m,p-Dimethyl PPE promotes GDP/GTP exchange of the G protein α-subunit, dissociates the receptor-G protein complex, stabilizes the low-affinity receptor state, and inhibits adenylate cyclase activity. m,p-Dimethyl PPE inhibits Forskolin (HY-15371)-induced melatonin synthesis in retinal photoreceptor cells and reduces the efficacy of full agonists when used in combination. m,p-Dimethyl PPE can be used in studies related to attention-deficit hyperactivity disorder .
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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
