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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
488 Results for "
Conformational constraint
" in MedChemExpress (MCE) Product Catalog:
Products (488)
488 Results for "Conformational constraint" in MCE Product Catalog:
Cat. No.: HY-110168R
CAS No.: 913830-15-6
Target:
NS 9283 (Standard) is the analytical standard of NS 9283 (HY-110168). This product is intended for research and analytical applications. NS 9283 (A-969933) is a α4β2 nicotinic acetylcholine receptor (α4β2 nAChR) positive allosteric modulator that preferentially targets the (α4)3 (β2)2 stoichiometric conformation. NS 9283 increases the potency of ACh-induced currents without enhancing the maximal effect of ACh. NS 9283 also enhances prefrontal glutamate release, modulates attention-related electrophysiological responses, and potentiates the antinociceptive effects associated with α4β2 nAChR agonists. NS 9283 can be used in research related to inflammatory pain, postoperative pain, osteoarthritis pain, and Parkinson's disease .
Cat. No.: HY-110168S
Target:
NS 9283-d4 is the deuterated-labeled NS 9283 (HY-110168). NS 9283 (A-969933) is a α4β2 nicotinic acetylcholine receptor (α4β2 nAChR) positive allosteric modulator that preferentially targets the (α4)3 (β2)2 stoichiometric conformation. NS 9283 increases the potency of ACh-induced currents without enhancing the maximal effect of ACh. NS 9283 also enhances prefrontal glutamate release, modulates attention-related electrophysiological responses, and potentiates the antinociceptive effects associated with α4β2 nAChR agonists. NS 9283 can be used in research related to inflammatory pain, postoperative pain, osteoarthritis pain, and Parkinson's disease .
Cat. No.: HY-113298R
CAS No.: 498-23-7
Synonyms: Methylmaleic acid (Standard); Citraconate (Standard)
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MFN2 agonist-1 is an allosteric agonist of mitofusin 2 (MFN2) with an EC50 of 3 nM. MFN2 agonist-1 mimics the MFN2 HR1 peptide to compete for HR2, disrupt the HR1-HR2 autoinhibitory interaction, stabilize the open conformation of MFN2, and promote GTP hydrolysis and mitochondrial fusion. MFN2 agonist-1 acts in a manner dependent on endogenous MFN1 or MFN2, and does not impair cell viability. MFN2 agonist-1 reverses mitochondrial fragmentation, depolarization, aggregation and axonal transport defects, restores bidirectional movement and improves enhanced autophagy. MFN2 agonist-1 is used in studies related to Charcot-Marie-Tooth disease type 2A, Alzheimer's disease, Parkinson's disease and Huntington's disease .
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AM-001 is a selective Epac1 inhibitor with an IC50 value of 47.8-53.7 μM. AM-001 blocks cAMP (Cyclic AMP) (HY-B1511)-induced conformational changes of Epac1, inhibits Epac1-dependent activation of Rap1, and does not compete with cAMP for binding to Epac1. AM-001 disrupts the formation of the Epac1-GRK5 complex, blocks nuclear import of GRK5, and inhibits GRK5-mediated nuclear export of HDAC5 and activation of MEF2. AM-001 can be used in research related to heart disease, myocardial ischemia/reperfusion injury, SARS-CoV-2 infection, influenza A virus infection, atrial fibrillation and idiopathic pulmonary fibrosis .
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GNE-274 is a non-degrading estrogen receptor α (ERα/ESR1) modulator structurally similar to GDC-0927 (HY-111484). GNE-274 competes for binding to the ligand-binding domain of ERα and induces a coregulator-binding conformation similar to that of antagonists, yet retains partial agonistic transcriptional activity and does not promote ERα turnover. GNE-274 effectively inhibits E2-stimulated proliferation of ER-positive, HER2-negative breast cancer cells. GNE-274 promotes the recruitment of ERα to the nucleus and chromatin, increases chromatin accessibility, while largely maintaining the intranuclear mobility of ERα. GNE-274 can be used in research on ER-positive breast cancer and ERα transcriptional dynamics .
Cat. No.: HY-159520
CAS No.: 2731294-23-6
Synonyms: Ofirnoflast; HT-6184
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Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC50 of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia .
Cat. No.: HY-16782R
CAS No.: 945614-12-0
Synonyms: ARRY-614 (Standard)
Pexmetinib (Standard) (ARRY-614 (Standard)) is the analytical standard of Pexmetinib (HY-16782). This product is intended for research and analytical applications. Pexmetinib (ARRY-614) is an orally active dual Tie-2 and p38 MAPK inhibitor. Pexmetinib binds to Tie-2 and p38 MAPK in a "DFG-out" conformation, attenuates the phosphorylation of p38, inhibits STAT3 activation, reduces the promoter-binding activity of NFATc1, and decreases the expression of MMPs. Pexmetinib inhibits leukemia cell proliferation, abrogates TNF-α-mediated myelosuppression of healthy hematopoietic stem cells, stimulates hematopoiesis in primary myelodysplastic syndrome (MDS) samples, inhibits RANKL-induced osteoclast formation and bone resorption, and suppresses migration, invasion and induced osteolysis of breast cancer cells. Pexmetinib can be used in research related to myelodysplastic syndrome, acute myeloid leukemia and breast cancer-induced osteolysis .
Cat. No.: HY-181420A
CAS No.: 3029443-36-2
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BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS), non-covalent pan-KRAS inhibitor (IC50=28-120 nM). BBO-11818 specifically binds to the Switch-II/Helix 3 pocket, disrupts the KRAS:RAF1 interaction by inducing conformational changes, and blocks the MAPK signaling pathway. BBO-11818 exhibits significant anti-tumor activity, which not only inhibits cell proliferation and induces apoptosis, but also drives tumor regression in xenograft models. BBO-11818 produces synergistic effects when combined with Cetuximab (HY-P9905), anti-PD-1 antibody or PI3Kα inhibitor. BBO-11818 is used in the research of KRAS mutation-related malignancies such as pancreatic cancer, non-small cell lung cancer and colorectal cancer .
Cat. No.: HY-181888
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GRL-142 is a potent HIV-1 protease inhibitor capable of crossing the blood-brain barrier. GRL-142 exhibits extremely high inhibitory activity against both wild-type and multidrug-resistant strains (IC50=0.0094 nM). GRL-142 acts synergistically with the P2/P2' segments via a unique scaffold binding mechanism, utilizes fluorine-mediated stable interactions to maintain its bioactive conformation, adapts to p51 HIV-1 protease mutants, and maintains the flap-closed state by directly acting on the flap tip residues. GRL-142 disrupts the flap-water hydrogen bond network of wild-type protease, thereby effectively blocking viral replication. GRL-142 can be used to study HIV-1 infection and the associated neurocognitive disorder (HAND) .
Cat. No.: HY-183400
CAS No.: 195450-11-4
Target:
Neurotensin Receptor MMP EGFR Toll-like Receptor (TLR) Wnt Caspase PARP MyD88 NF-κB TNF Receptor Apoptosis
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BIM-46174 is a heterotrimeric G protein complex inhibitor. BIM-46174 blocks GPCR downstream signaling by trapping Gα proteins in a nucleotide-free pocket conformation, thereby inhibiting Gαq-mediated calcium release, Gαs-mediated cAMP production, and GPCR-regulated cancer cell invasion. In vitro, BIM-46174 effectively suppresses a variety of clinically multidrug-resistant cell lines and induces tumor cell apoptosis through activation of caspase-3 and PARP cleavage. BIM-46174 also inhibits activation of the Neu1-MMP-9-GPCR signaling platform and downstream NF-κB signaling, and is widely used in the study of cancer signaling pathways and inflammation-related research, including lung cancer, pancreatic cancer, breast cancer, melanoma, and leukemia .
Cat. No.: HY-184717
Atg4B-IN-3 (compound a25) is a ATG4B inhibitor with a Kd value of 18.01 nM against the human target. Atg4B-IN-3 stably regulates the closed conformation of the loop, prevents substrates from accessing the catalytic site Cys74, and thereby inhibits the proteolytic activity of ATG4B. Atg4B-IN-3 blocks autophagic flux, reduces LC3-II levels, promotes p62 accumulation, disrupts autophagy homeostasis and enhances cell death. Atg4B-IN-3 inhibits cell proliferation, migration and clonogenic survival capacity. Atg4B-IN-3 can be used in studies related to esophageal squamous cell carcinoma .
Cat. No.: HY-187096
ERα/RAD51 degrader 1 is a ERα and RAD51 HyT degrader as well as an apoptosis (Apoptosis) inducer. ERα/RAD51 degrader 1 induces conformational changes in helices 11-12 of ERα, promotes the recruitment of Hsp70, and drives the degradation of ERα and RAD51 via the ubiquitin-proteasome pathway. ERα/RAD51 degrader 1 downregulates the expression of BRCA1/2. ERα/RAD51 degrader 1 acts on tamoxifen (HY-13757A)-sensitive and tamoxifen-resistant breast cancer in both in vitro and in vivo models. ERα/RAD51 degrader 1 is applicable to breast cancer-related research (hydrophobic tag: (HY-B0402)) .
Cat. No.: HY-D3102
CAS No.: 1015251-87-2
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CGTDP is a fluorescent probe used for selective labeling of active-site arginine residues, detection of local polarity, and monitoring of conformational changes in enzyme active sites. CGTDP contains a neutral red moiety serving as a polarity-sensitive fluorophore, and a phenylglyoxal unit acting as an arginine-specific labeling group; it undergoes a selective reaction via its α-dicarbonyl moiety with the guanidyl group of arginine residues in enzyme active sites to form a covalent linkage, thereby enabling the reporting of the local microenvironment at the labeled site. The excitation/emission wavelengths are Ex/Em = 398/607 nm and Ex/Em = 507/607 nm; these wavelengths blue-shift in organic solvents, such as Ex/Em = 375/569 nm and Ex/Em = 469/569 nm in THF, and Ex/Em = 375/587 nm and Ex/Em = 470/587 nm in acetonitrile. When labeled onto creatine kinase, its excitation/emission wavelengths are Ex/Em = 493/590 nm .
Cat. No.: HY-P1609
CAS No.: 105116-61-8
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Cat. No.: HY-P1793
CAS No.: 83471-50-5
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Cat. No.: HY-P1793A
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Cat. No.: HY-P992024
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Cat. No.: HY-P99899
CAS No.: 2052591-32-7
Synonyms: PR-1498487
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Cat. No.: HY-W004812
CAS No.: 161660-94-2
Synonyms: (1S,3S)-3-[(tert-Butoxycarbonyl)amino]cyclopentanecarboxylic acid
Target:
Research Areas:
BOC-(1R,3S)-3-aminocyclopentane carboxylic acid ((1S,3S)-3-[(tert-Butoxycarbonyl)amino]cyclopentanecarboxylic acid) is a conformationally constrained peptide building block and a key component of SARS-CoV-2 main protease (Mpro) inhibitors. When incorporated into macrocyclic peptides, BOC-(1R,3S)-3-aminocyclopentane carboxylic acid not only helps generate high-affinity Mpro inhibitors by preorganizing the secondary structure of peptides, but also exerts sequence-dependent functional inhibition on the hydrolytic activity of Mpro. BOC-(1R,3S)-3-aminocyclopentane carboxylic is widely used in COVID-19-related research .
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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
