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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
122 Results for "
Competitive interactions
" in MedChemExpress (MCE) Product Catalog:
Products (122)
122 Results for "Competitive interactions" in MCE Product Catalog:
Cat. No.: HY-110196
CAS No.: 1627607-88-8
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(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2 .
Cat. No.: HY-160478
CAS No.: 839708-29-1
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .
Cat. No.: HY-133233
CAS No.: 116457-99-9
Synonyms: 1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
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Thioetheramide-PC (1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine) is a structurally modified phospholipid that acts as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). Thioetheramide-PC has an IC50 value of 2 μM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, Thioetheramide-PC also binds to the activation site of the enzyme. Thioetheramide-PC binds more tightly to the activation site than to the catalytic site. As a result of this dual interaction, at low concentrations, Thioetheramide-PC may activate phospholipase activity rather than inhibit it.
Cat. No.: HY-100834R
CAS No.: 131123-76-7
Synonyms: 5,7-DCKA (Standard)
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5,7-Dichlorokynurenic acid (Standard) is the analytical standard of 5,7-Dichlorokynurenic acid (HY-100834). This product is intended for research and analytical applications. 5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
Cat. No.: HY-W457608
CAS No.: 34330-04-6
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CU7218 competitively binds to the phosphopeptide-binding pocket of 14-3-3ε and blocks its interaction with the 9J10 peptide. CU7218 can be used in cancer research .
Cat. No.: HY-101503R
CAS No.: 682741-29-3
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HTS01037 (Standard) is the analytical standard of HTS01037 (HY-101503). This product is intended for research and analytical applications. HTS01037 is an inhibitor of fatty acid binding; and a competitive antagonist of protein-protein interactions mediated by AFABP/aP2 with a Ki of 0.67 μM.
Cat. No.: HY-187677
CAS No.: 94159-34-9
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PCSK9-IN-36 is a PCSK9 inhibitor and a flavonoid glycoside derivative. PCSK9-IN-36 binds stably within the surface groove of PCSK9 through hydrophobic interactions involving its flavonoid scaffold and an electrostatic hydrogen-bonding network formed by its polar glycosidic group, thereby competitively blocking the interaction between PCSK9 and the low-density lipoprotein receptor (LDLR). PCSK9-IN-36 can be used for research on hypercholesterolemia .
Cat. No.: HY-P11841
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Cat. No.: HY-110147
CAS No.: 922732-52-3
SSM-3 is a potent furin inhibitor with an EC50 of 54 nM. SSM-3 uses its positively charged guanidyl group to form strong electrostatic interactions with the negatively charged residues in the catalytic center of furin, thereby competitively occupying and blocking the active site. SSM-3 can be used in the research of anthrax and avian influenza .
Cat. No.: HY-180222
KGA-4066 is a novel non-ATP-competitive CDK2 inhibitor. KGA-4066 inhibits CDK2/Cyclin A2 with an IC50 value of 236.7 nM, disrupts their interaction, promots CDK2 degradation via the lysosomal pathway. KGA-4066 has anticancer activity against hepatocellular carcinoma .
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Gallocyanine (NCI8642) is a DKK/LRP interaction inhibitor and Wnt/β-catenin signaling pathway activator. Gallocyanine binds to the YWTD repeat domains of LRP5/6, competitively blocks the interaction between DKK and LRP5/6, with an IC50 of approximately 3 μM for inhibiting DKK1 binding to LRP5, an IC50 of 6.38 μM for inhibiting DKK1 binding to LRP6, and a Ki of 14 μM for inhibiting the DKK2C/LRP6-E3E4 interaction. Gallocyanine reverses the inhibitory effect of DKK1 on WNT3A signaling, with an EC50 of approximately 5 μM. Gallocyanine can be used in studies related to Alzheimer's disease, bone formation and glucose metabolism .
Cat. No.: HY-P11842
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Cat. No.: HY-179091
CU-TZD-20 is a PARP-1 inhibitor. CU-TZD-20 has a high affinity for binding to the PARP-1 catalytic domain and good structural stability. CU-TZD-20 competitively occupies NAD + binding sites and forms stable interactions with key catalytic residues. CU-TZD-20 can be used for cancer research .
Cat. No.: HY-107597R
CAS No.: 40045-50-9
Synonyms: SU3327 (Standard)
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Halicin (Standard) is the analytical standard of Halicin (HY-107597). This product is intended for research and analytical applications. Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt Kinase .
Cat. No.: HY-187394
CAS No.: 1425050-80-1
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hIgG-hFc receptor-IN-3 is a protein-protein interaction inhibitor of human immunoglobulin G-human neonatal Fc receptor (hIgG-hFcRn). Identified via virtual ligand screening and optimized through structure-activity relationship studies, hIgG-hFc receptor-IN-3 competitively inhibits the binding of IgG to FcRn, thereby accelerating the clearance of endogenous IgG. hIgG-hFc receptor-IN-3 can be used for the research of autoimmune diseases .
Cat. No.: HY-183344
CAS No.: 3056856-56-2
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IL-1β-IN-4 is a selective IL-1β competitive binder. IL-1β-IN-4 interferes with the interaction between IL-1β and its cognate receptor IL-1R1, with an IC50 of 8.3 μM. IL-1β-IN-4 can be used in studies related to inflammatory and immune diseases .
Cat. No.: HY-171172
CAS No.: 2493080-16-1
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GSC-718 is a CD22 inhibitor with an IC50 of 0.161 μM against mouse CD22. GSC-718 competitively blocks the binding of mouse CD22 to natural glycan ligands, and inhibits the interaction between CD22 and α2,6-sialylated ligands. GSC-718 promotes B cell proliferation and enhances antibody production. GSC-718 can be used in the research of B cell lymphoma and rheumatoid arthritis .
Cat. No.: HY-111126R
CAS No.: 2046250-48-8
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K67 (Standard) is the analytical standard of K67 (HY-111126). This product is intended for research and analytical applications. K67 is a selective the interaction between Keap1 and S349 phosphorylated p62 inhibitor, with an IC50 of 1.5 μM. K67 has a weaker inhibitory effect on the interaction between Keap1 and Nrf2 (IC50 is 6.2 μM). K67 competitively binds to the binding site of Keap1 with p-p62, blocKing the abnormal activation of the p62-dependent Nrf2 pathway. K67 inhibits tumor cell proliferation and enhances the sensitivity of hepatocellular carcinoma (HCC) to chemotherapeutic drugs by restoring Keap1-mediated ubiquitination and degradation of Nrf2 .
Cat. No.: HY-187642
CAS No.: 303059-39-4
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IGGi-11 is a competitive Gαi inhibitor with a Kd of 5.3 μM for sGαi3. IGGi-11 binds to the GIV interaction region of Gαi3, blocks non-canonical G protein signaling, and does not interfere with Gαi nucleotide processing, Gβγ binding, GPCR activation, or effector regulation. IGGi-11 inhibits the pro-invasive properties of metastatic breast cancer. IGGi-11 can be used in related studies on metastatic breast cancer .
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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
