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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
37 Results for "
substrate binding pockets
" in MedChemExpress (MCE) Product Catalog:
Products (37)
37 Results for "substrate binding pockets" in MCE Product Catalog:
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 .
Adamantanone (2-Adamantone; 2-Oxoadamantane) serves as a substrate for some alcohol dehydrogenases and also acts as a probe for characterizing substrate-binding pockets. Adamantanone can be reduced by 3α-hydroxysteroid dehydrogenase and 3β-17β-hydroxysteroid dehydrogenase derived from Pseudomonas testosteroni, and it can fit into the conformationally flexible substrate-binding pockets of these enzymes that undergo substrate-induced fit .
Cat. No.: HY-152214
CAS No.: 2883730-60-5
SIRT5 inhibitor 5 is a potent SIRT5 inhibitor with an IC50 value of 0.21 µM. SIRT5 inhibitor 5 does not occupy the NNAD + -binding pocket and acts as a substrate-competitive inhibitor .
PS423 is a prodrug of PS210, acting as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K. PS210 is a potent and selective PDK1 activator targeting the PIF binding pocket of PDK1 .
Cat. No.: HY-168634
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SJ46421 is a BRD3BD2 PROTAC degrader. SJ46421 induces a cooperative ternary complex of KLHDC2 and BRD3BD2 with an IC50 of 7.8 nM. SJ46421 binds to the substrate-binding pocket of KLHDC2, forms cooperative ternary complexes with BRD3BD2, BRD2BD2 and BRD4BD2, disrupts the autoinhibitory tetramer assembly of KLHDC2, drives selective ubiquitination of BRD3BD2, and inhibits the ubiquitination of endogenous KLHDC2 diglycine substrates. SJ46421 can be used in cancer research .
Cat. No.: HY-134136B
CAS No.: 799812-82-1
Synonyms: S-Octanoate-CoA triammonium; S-Octanoate-coenzyme A triammonium
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Octanoyl coenzyme A triammonium is an enoyl-CoA hydratase binder. Octanoyl coenzyme A triammonium binds to the active site of enoyl-CoA hydratase, occupies the binding pocket for the fatty acid tail of the enzyme's substrate, and induces a conformational shift in a flexible protein loop via its longer octanoyl chain, forming an open channel leading to the inter-trimer gap .
Cat. No.: HY-W013724S
Synonyms: IDP-15N4 dilithium; Inosine-5'-diphosphoric acid-15N4 disodium
Cat. No.: HY-W490804
CAS No.: 2971-36-0
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HPTE is the active in vivo metabolite of Methoxychlor (HY-B1873), and acts as an inhibitor of 3β‑HSD and 17β‑HSD3. HPTE binds to the substrate-binding pocket of 3β‑HSD in a non-competitive manner, but competitively occupies the coenzyme NAD +-binding site, thereby inhibiting the conversion of pregnenolone to progesterone. HPTE binds to the androstenedione-binding pocket (the substrate pocket) of 17β‑HSD3 in a non-competitive manner, and competitively occupies the coenzyme NADPH-binding site, thus blocking the conversion of androstenedione to testosterone. HPTE interferes with androgen biosynthesis in Leydig cells by inhibiting the activities of these two key steroidogenic enzymes. HPTE can be used in studies related to androgen biosynthesis .
Cat. No.: HY-141764S
CAS No.: 1794780-53-2
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2,2-Bis(p-hydroxyphenyl)-1,1,1-trichloroethane-d8 is the deuterated-labeled HPTE (HY-W490804). HPTE is the active in vivo metabolite of Methoxychlor (HY-B1873), and acts as an inhibitor of 3β‑HSD and 17β‑HSD3. HPTE binds to the substrate-binding pocket of 3β‑HSD in a non-competitive manner, but competitively occupies the coenzyme NAD +-binding site, thereby inhibiting the conversion of pregnenolone to progesterone. HPTE binds to the androstenedione-binding pocket (the substrate pocket) of 17β‑HSD3 in a non-competitive manner, and competitively occupies the coenzyme NADPH-binding site, thus blocking the conversion of androstenedione to testosterone. HPTE interferes with androgen biosynthesis in Leydig cells by inhibiting the activities of these two key steroidogenic enzymes. HPTE can be used in studies related to androgen biosynthesis .
Cat. No.: HY-180846
CAS No.: 3119375-08-2
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NT32 is a selective METTL13 stabilizer with a Kd value of 14 μM. NT32 could occupy both the SAM/SAH-binding pocket and the peptide substrate-binding site of METTL13 simultaneously. NT32 specifically targets and stabilizes METTL13. NT32 shows no inhibitory activity against non-small cell lung cancer .
Cat. No.: HY-137744
CAS No.: 148821-01-6
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MANT-GppNHp is a competitive adenyl cyclase (AC) inhibitor. MANT-GppNHp is a fluorescently labeled GTP (HY-113225) analogue. MANT-GppNHp interacts with the hydrophobic pocket near the AC catalytic site through its MANT group, thereby directly blocking the binding of the substrate ATP. MANT-GppNHp can be used to study diseases related to the increased activity of AC (such as cholera) .
Cat. No.: HY-110287R
CAS No.: 300815-04-7
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Apcin (Standard) is the analytical standard of Apcin (HY-110287). This product is intended for research and analytical applications. Apcin, a ligand of Cdc20, is a potent and competitive anaphase-promoting complex/cyclosome (APC/C(Cdc20)) E3 ligase activity inhibitor. Apcin competitively inhibits APC/C-dependent ubiquitylation by binding to Cdc20 and preventing substrate recognition. Apcin occupes the D-box-binding pocket on the side face of the WD40-domain and can prolong mitosis .
Cat. No.: HY-110197A
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6bK formate is a selective insulin-degrading enzyme (IDE) inhibitor with an IC50 of 50 nM. 6bK formate binds to the distal pocket of IDE, thereby blocking substrate binding, peptide unfolding and cleavage processes, and reducing the degradation of insulin, glucagon and amylin. 6bK formate improves oral glucose tolerance but impairs intraperitoneal glucose tolerance. 6bK formate can be used in research related to type 2 diabetes .
Cat. No.: HY-180548
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MRC37 is a high-affinity TRIM21 ligand with a Kd of 0.4 µM. MRC37 targets the IgG Fc-binding pocket in the PRYSPRY domain of TRIM21, mimics the "HHNY" epitope, and inhibits substrate-induced aggregation and activation of TRIM21 via competitive blockade of antibody binding. MRC37 effectively blocks TRIM21-mediated antiviral immunity (such as adenovirus neutralization) and Trim-Away targeted protein degradation without cytotoxicity. MRC37 antagonizes TRIMTAC activity, and its multiple modification sites do not affect target binding, making it suitable as a degrader warhead for research on viral immunity and neurodegenerative diseases such as tauopathies .
Cat. No.: HY-111175
CAS No.: 905978-63-4
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IG-105 is an orally active and potent tubulin inhibitor that competitively inhibits [ 3H] colchicine binding to tubulin with an IC50 of 0.6 μM and inhibits tubulin polymerization with an IC50 of 3 μM. IG-105 inhibits microtubule polymerization by binding to the colchicine pocket of tubulin, induces G2-M phase arrest, and subsequently activates the caspase cascade through Bcl-2 inactivation and p53 upregulation, inducing apoptosis. IG-105 effectively overcomes multidrug resistance as a non-Pgp substrate. IG-105 can be used for research on leukemia, breast cancer, liver cancer, prostate cancer, lung cancer, melanoma, pancreatic cancer, and colon cancer .
Cat. No.: HY-187178
CAS No.: 1966932-74-0
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KDM2A/7-IN-1 is a lysine demethylase 2A (KDM2A) inhibitor with a human IC50 of 11 nM. KDM2A/7-IN-1 requires co-factor 2-oxoglutarate (2OG) for binding and occupies the H3K36me2 substrate pocket via a dimethylated lysine 36-mimicking group. KDM2A/7-IN-1 represses E2F-regulated genes, induces epithelial-mesenchymal transition, DNA repair, and mTOR pathways in specific cells, and selectively inhibits proliferation of ALT-positive cancer cell lines. KDM2A/7-IN-1 can be used for the research of ALT-positive cancers .
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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
