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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
15 Results for "
Conformational transition
" in MedChemExpress (MCE) Product Catalog:
Products (15)
15 Results for "Conformational transition" in MCE Product Catalog:
2
2 Cited Publications
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Iperoxo is a potent superagonist of muscarinic acetylcholine receptor (mAChR) that activates M1, M2 and M3 receptors with pEC50 of 9.87, 10.1 and 9.78. Iperoxo can be used for direct probing activation-related conformational transitions of muscarinic receptors when labeled with tritium .
Cat. No.: HY-P5423
CAS No.: 107658-43-5
Cat. No.: HY-W007729
CAS No.: 79069-13-9
Cat. No.: HY-145416
G247 is a specific MsbA inhibitor. G247 acts as a transmembrane domains (TMDs) wedge, symmetrically increasing nucleotide-binding domains (NBDs) separation and preventing conformational transition of MsbA. G247 suppresses ATPase activity by increasing inter-NBD distance .
Cat. No.: HY-172403
CAS No.: 25608-40-6
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Poly-L-aspartic acid is an acidic polypeptide that functions via pH-dependent conformational changes. Poly-L-aspartic acid is promising for research of pH-responsive structural transitions in biological systems .
Cat. No.: HY-P10534
CAS No.: 873582-78-6
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Cat. No.: HY-P11353
CAS No.: 117138-19-9
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Cat. No.: HY-175761
Riboswit-modulator-1 (Compound A1), a covalent RNA ligand, is a bacterial Flavin mononucleotide (FMN) riboswitch modulator. Riboswit-modulator-1 modifies unpaired guanine residues (G11 and G62) proximal to the FMN-binding site through a proximity-driven mechanism, and interferes with its conformational transitions. Riboswit-modulator-1 acts as a negative antagonist by eliciting the opposite effect of the natural effector molecule .
Cat. No.: HY-P1609
CAS No.: 105116-61-8
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Cat. No.: HY-182098
Cat. No.: HY-182098A
Cat. No.: HY-182098B
Cat. No.: HY-182098C
Cat. No.: HY-179506
P53 Activator 16 (Compound JC16) is a p53 activator. P53 Activator 16 exhibits selective cytotoxicity and pro-apoptotic (apoptosis) activity towards p53-Y220C mutant cancer cells, while having little effect on wild-type or P53-deficient cells. P53 Activator 16 induces the conformational transition of cell p53-Y220C from the mutant form to the wild-type form, accompanied by the transcriptional activation of p53 target genes, without increasing the overall level of p53 protein. P53 Activator 16 can be used for the study of p53 mutant cancers .
Cat. No.: HY-184501
CAS No.: 486440-74-8
UE01 is an orally active, selective small-molecule modulator targeting both ULK1/ERK1/2. UE01 activates hULK1 with an EC50 of 695.30 nM and a KD of 114.3 nM for ULK1; it inhibits hERK1 with an IC50 of 179.90 nM and a KD of 114 nM for ERK1; it shows weak binding to ERK2 with a KD of 2.8 mM. UE01 induces the conformational transition of ULK1 from an inactive to an active state, enhances the phosphorylation of ULK1 Ser317 and mAtg13 Ser355, and reduces the phosphorylation of ULK1 Ser757. UE01 competitively occupies the ATP-binding pocket of ERK1, inhibits ERK1 kinase activity, and reduces the activity of the ERK1/2 signaling pathway. UE01 induces complete autophagy flux and apoptosis, upregulates Atg5, Atg7, LC3-II/LC3-I, Bax, cytochrome C (Cyt c), Cleaved-Caspase 3, Cleaved-PARP1 and E-cadherin, downregulates p62, Bcl-2, MMP-2 and MMP-9, reduces the phosphorylation of Exo70 Ser250, and promotes the proteasome-dependent degradation of Cav-1, thereby inhibiting EMT-related phenotypes and extracellular matrix degradation. UE01 can be used in studies related to triple-negative breast cancer .
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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!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
