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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
63 Results for "
substrate binding site
" in MedChemExpress (MCE) Product Catalog:
Products (63)
63 Results for "substrate binding site" in MCE Product Catalog:
12
12 Publications Verification
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NNMTi is a potent nicotinamide N-methyltransferase (NNMT) inhibitor (IC50=1.2 μM) and selectively binds to the NNMT substrate-binding site residues . NNMTi promotes myoblast differentiation in vitro and enhances fusion and regenerative capacity of muscle stem cells (muSCs) in aged mice .
3
3 Cited Publications
Synonyms: YH25448; GNS-1480
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Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
3
3 Cited Publications
Cat. No.: HY-163316
CAS No.: 3030697-87-8
Research Areas:
SIRT4-IN-1 is a selective and potent Sirtuin 4 (Sirt4) inhibitor with an IC50 of 16 μM for hSirt4. SIRT4-IN-1 also inhibits hSirt1, hSirt2, hSirt3, hSirt4 and hSirt6. SIRT4-IN-1 competes with acyl peptide substrate for Sirt4's acyl binding site, and is noncompetitive with NAD +. SIRT4-IN-1 increases glutamate dehydrogenase (GDH) activity and rescues pyruvate dehydrogenase (PDH) activity. SIRT4-IN-1 inhibits adipocyte differentiation and suppresses Sirt4 overexpression-induced increased differentiation. SIRT4-IN-1 can be used for the researches of cancer and metabolic disease .
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3 Cited Publications
Cat. No.: HY-109061B
CAS No.: 2247995-37-3
Synonyms: YH25448 mesylate; GNS-1480 mesylate
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
2
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2
2 Cited Publications
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7-Azido-4-methylcoumarin is a selective coumarin-based fluorescent probe for hydrogen sulfide (H2S). In the presence of H2S, the aromatic azido group of 7-Azido-4-methylcoumarin is selectively reduced to produce the fluorescently active 7-amino-4-methylcoumarin (AMC). 7-Azido-4-methylcoumarin binds to the coumarin/phenol-binding site of BSA, the aglycone-binding site of UGT1A6, and the substrate-binding site of SULT1A1, respectively. 7-Azido-4-methylcoumarin retains its fluorescent properties after covalent binding, acts as a fluorescent H2S probe, and does not react with cysteine, homocysteine or glutathione (Ex/Em = 340/445 nm) .
1
1 Cited Publications
Cat. No.: HY-48999A
CAS No.: 3033987-42-4
FSK hydrochloride is fluorosulfonyloxybenzoyl-L-lysine, which features a long, flexible aryl fluorosulfate-containing side chain that can reach protein sites inaccessible to covalent conjugation. FSK hydrochloride modifies nanomolecules to target epidermal growth factor receptor (EGFR), resulting in irreversibly bound covalent interactions. Through genetically encoded chemical crosslinking, FSK hydrochloride captures unknown enzyme-substrate interactions in living cells, targets residues other than Cys, and mediates crosslinking at the binding periphery. FSK hydrochloride enables the construction of a bioreactive SuFEx system for generating covalent bonds in various proteins both in vitro and in vivo .
Cat. No.: HY-P1315
CAS No.: 70195-20-9
Synonyms: Glycylglycyl-L-tyrosyl-L-arginine
Cat. No.: HY-W003969
CAS No.: 695-34-1
Synonyms: Ascensil; 2-Amino-4-methylpyridine
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Aminopicoline (Ascensil) is a potent and non-selective inhibitor of nitric oxide synthase (NOS) isoenzymes (iNOS, nNOS, eNOS). Aminopicoline competes with arginine at the substrate-binding site of nitric oxide synthase, reduces cellular nitric oxide production, inhibits the elevation of plasma nitrate, increases mean arterial pressure at high doses, and also serves as a basis for radiolabeled ligands to localize nitric oxide synthase binding sites. Aminopicoline can be used in the research of diseases associated with septic shock, joint inflammation, intestinal inflammation, and CNS inflammation .
Cat. No.: HY-134136A
CAS No.: 324518-20-9
Cat. No.: HY-D1078
CAS No.: 127770-45-0
Cat. No.: HY-P10856
CAS No.: 3085809-95-3
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GSK 366 is a type II kynurenine-3-monooxygenase (KMO) inhibitor with IC50 values of 2.3 nM and 0.7 nM for human KMO and P. fluorescens-KMO (Pf-KMO). GSK 366 binds to KMO’s substrate site, prevents productive NADPH association, substrate binding, and FAD hydroperoxy species formation. GSK 366 does not stimulate hydrogen peroxide (H2O2) production and reduces H2O2 levels. GSK 366 can be used for the researches of inflammation and neurological disease, such as acute pancreatitis multiple organ dysfunction syndrome and Alzheimer’s disease .
Cat. No.: HY-146248B
Purity: 98.02%
Research Areas:
TFMU-ADPr diammonium is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr diammonium can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr diammonium binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr diammonium can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr diammonium is also applicable to COVID-19-related research .
Cat. No.: HY-178124
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Huib32 is a potent small-molecule inhibitor of USP32 (IC50 = 21.2 nM), exhibiting high selectivity over other closely related deubiquitinating enzymes (DUBs), such as USP8/10/16, UCHL1 and OTUB2. Huib32 reversibly inhibits USP32 by covalently binding to the active site Cys743, which enhances substrate ubiquitination, alters endosomal morphology, and mimics USP32 depletion. Huib32 can be used for breast, ovarian, and lung cancer and Alzheimer's and Parkinson’s diseases research .
Cat. No.: HY-146248
CAS No.: 2412923-11-4
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Glutathione sulfonate (S-Sulfoglutathione) is a multifunctional bioactive compound that inhibits angiogenesis and tumor growth. Glutathione sulfonate is a competitive inhibitor of glutathione S-transferase and is involved in the detoxification process and the binding of a variety of exogenous and endogenous compounds. Glutathione sulfonate acts in the substrate binding site of Escherichia coli glutathione S-transferase, affecting the catalytic mechanism. The structural characteristics of Glutathione sulfonate contribute to its inhibitory effect by hydrogen bonding in the active center of the enzyme .
Cat. No.: HY-150510
CAS No.: 2866408-21-9
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MS8511 is a selective G9a/GLP covalent irreversible inhibitor by targeting a cysteine residue at the substrate binding site, with IC50 values of 100 nM (G9a) and 140 nM (GLP), and Kd values of 44 nM (G9a) and 46 nM (GLP). MS8511 reduces the cellular H3K9me2 level and enhances antiproliferation activity. MS8511 can be used for the research of several types of cancers including brain, breast, ovarian, lung, bladder, melanoma, colorectal cancer, and other disease such as Alzheimer’s disease (AD), sickle cell disease, Prader−Willi syndrome (PWS) .
Cat. No.: HY-175597
CAS No.: 2363753-48-2
ClpP modulator-1 (Compound BC8a), a peptidomimetic, is an allosteric ClpP modulator. ClpP modulator-1 is a ClpP activator at low concentration with EC50s of 0.35 and 0.58 μM for for Neisseria meningitides ClpP (NmClpP) and Escherichia coli ClpP (EcClpP), resepectively. ClpP modulator-1 also inhibits peptidase activity at high concentration by competitively inhibiting substrate protein (LY-AMC) binding to ClpP C sites. ClpP modulator-1 has antibacterial activity. ClpP modulator-1 can be used for bacterial infections 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
