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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
332 Results for "
specific substrate
" in MedChemExpress (MCE) Product Catalog:
Products (332)
332 Results for "specific substrate" in MCE Product Catalog:
Cat. No.: HY-A0003A
CAS No.: 1243329-97-6
Synonyms: CC-5013 hydrochloride
Lenalidomide hydrochloride (CC-5013 hydrochloride) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide hydrochloride induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide hydrochloride promotes IL-2 release and effector functions of CD8 + T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide hydrochloride can be used in research related to hematological malignancies, acute liver failure and acute kidney injury .
Cat. No.: HY-E70400
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Thermostable T7 RNA Polymerase is a thermostable version of T7 RNA Polymerase (HY-E70090). Compared with T7 RNA Polymerase, it has high temperature resistance and stable activity. T7 RNA polymerase is a polymerase expressed by Escherichia coli from the RNA polymerase gene of T7 bacteriophage. T7 RNA polymerase is highly specific and involved in in vitro transcription (IVT) of mRNA. In the presence of Mg 2+, T7 RNA polymerase only uses the single-stranded or double-stranded DNA containing the T7 promoter sequence as a template, and uses NTP as a substrate to synthesize RNA complementary to the single-stranded DNA downstream of the promoter .
Cat. No.: HY-L081
185 compounds
Protein phosphorylation is a key post-translational modification underlying the regulation of many cellular processes. Phosphatases and kinases contribute to the regulation of protein phosphorylation homeostasis in the cell. This reversible regulation of protein phosphorylation is critical for the proper control of a wide range of cellular activities, including cell cycle, proliferation and differentiation, metabolism, cell-cell interactions, etc.
Protein phosphatases have evolved in separate families that are structurally and mechanistically distinct. Based on substrate specificity and functional diversity, protein phosphatases are classified into two superfamilies: Protein serine/threonine phosphatases and Protein tyrosine phosphatases. Ser/Thr phosphatases are metalloenzymes belonging to two major gene families termed PPP (phosphoprotein phosphatase) and PPM (metal-dependent protein phosphatases), whereas protein tyrosine phosphatases (PTPs) belong to distinct classes of enzymes that utilize a phospho-cysteine enzyme intermediate as a part of their catalytic action.
MCE supplies a unique collection of 185 phosphatase inhibitors that mainly targeting protein tyrosine phosphatases (PTPs) and serine/threonine-specific protein phosphatases. MCE Phosphatase Inhibitor Library is a useful tool for phosphatase drug discovery and related research.
Cat. No.: HY-117747
CAS No.: 151867-81-1
Synonyms: JCR 424; XM 323
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DMP 323 is a potent, nonpeptide cyclic urea inhibitor of HIV protease, effective against both HIV type 1 and type 2. Designed using structural information and database searching, it competitively inhibits the cleavage of both peptide and HIV-1 gag polyprotein substrates. DMP 323 shows comparable potency to other highly effective HIV protease inhibitors like A-80987 and Ro-31-8959. Importantly, its efficacy against HIV protease remains unaffected by human plasma or serum, suggesting low affinity for plasma proteins. Furthermore, DMP 323 demonstrates minimal inhibition of various mammalian proteases at concentrations much higher than those needed for HIV protease inhibition, highlighting its specificity for viral targets .
Cat. No.: HY-131025
CAS No.: 1811539-88-4
Synonyms: JF585, SE; JF585, NHS
Synonyms: JF646, Tetrazine
Cat. No.: HY-178018
CAS No.: 1269110-12-4
Synonyms: iOXCT1
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D574-0246 is a dual-activity inhibitor of OXCT1, inhibiting both the ketolytic and succinyltransferase activities of OXCT1. D574-0246 reduces substrate-specific (LACTB K284) and global protein succinylation and decreases OXCT1 ketolytic activity in HepG2 cells. D574-0246 inhibits the viability of HCC cells (IC50: 16.49 μM in PLC cells, 6.656 μM in HepG2 cells). D574-0246 exerts anti-tumor efficacy in nude mice bearing OXCT1-overexpressing HepG2 xenograft tumors. D574-0246 can be used for the study of hepatocellular carcinoma (HCC) .
Cat. No.: HY-184556
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dCBP-30 is an orally active, selective and dual-acting CBP/p300 PROTAC degrader with DC50 values of 0.05 nM (CBP) and 0.04 nM (p300), respectively. dCBP-30 reduces the acetylation levels of histone substrates H3K27, H3K18, H2BK5 and H2BK20, downregulates multiple myeloma-specific dependency programs, and induces multiple myeloma cell apoptosis. dCBP-30 triggers tumor regression and prolongs survival in multiple myeloma xenograft mouse models, and exhibits synergistic antiproliferative activity with dexamethasone. dCBP-30 can be used for the research of multiple myeloma .
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 .
Cat. No.: HY-D0180
CAS No.: 17455-13-9
Synonyms: 18C6; 1,4,7,10,13,16-Hexaoxacyclooctadecane
Cat. No.: HY-N8279
CAS No.: 62213-14-3
Synonyms: Endo-β-1,3-1,4-glucanase
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β-1,3-1,4-glucanase (Endo-β-1,3-1,4-glucanase) is a glycoside hydrolase family 16 enzyme (some members belong to subfamily 25). β-1,3-1,4-glucanase shows high substrate specificity toward mixed‑linked β‑glucans and cleaves β‑1,4 glycosidic bonds adjacent to β‑1,3 linkages in an endo‑type pattern. β-1,3-1,4-glucanase can be used in industrial enzyme applications and monogastric animal feed supplementation .
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Cat. No.: HY-138660
CAS No.: 2376841-30-2
Synonyms: HM-JF526 NHS
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HM Janelia Fluor 526, SE (HM-JF526 NHS) is a derivative of hydroxymethyl JF526 (HM-JF526). SMLM (single-molecule localization microscopy) imaging in standard phosphate-buffered saline (pH 7.4) revealed that the HM-JF526 label showed spontaneous blinking behavior throughout the imaging session and did not require short-wavelength activation light . Janelia Fluor fluorescent dyes can be chemically conjugated to the specific HaloTag substrate (a chloroalkane ligand) to form a fluorescent ligand, rather than binding directly to the HaloTag protein itself. Janelia Fluor products are licensed under U.S. Pat. Nos. 9,933,417, 10,018,624 and 10,161,932 and other patents from Howard Hughes Medical Institute.
Cat. No.: HY-160841
CAS No.: 2567941-52-8
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Biotin-16-dCTP is a biotinylated deoxycytidine triphosphate that serves as an important DNA labeling substrate. Biotin-16-dCTP can be enzymatically incorporated into the 3' end of DNA probes via terminal deoxynucleotidyl transferase, forming a 1-3 nucleotide-long tail to achieve biotinylation of the probes. Biotin-16-dCTP enhances chemiluminescent detection of low-abundance targets such as specific tRNA isoacceptors through Northern blotting. Biotin-16-dCTP can also replace conventional dCTP to be integrated into single-stranded DNA generated by asymmetric polymerase chain reaction, which is applicable for bioconjugation or pull-down assays. Repeated freeze-thaw cycles of Biotin-16-dCTP should be avoided to prevent degradation of its function for probe biotinylation .
Cat. No.: HY-A0003R
CAS No.: 191732-72-6
Synonyms: CC-5013 (Standard)
Lenalidomide (Standard) (CC-5013 (Standard)) is the analytical standard of Lenalidomide (HY-A0003). This product is intended for research and analytical applications. Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8 + T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury .
Cat. No.: HY-P4551
CAS No.: 31373-65-6
Synonyms: N-Benzoyl-Gly-His-Leu
Research Areas:
Cat. No.: HY-W035133
CAS No.: 14527-51-6
Synonyms: 5,10,15,20-Tetra-p-tolyl-21H,23H-porphine
Cat. No.: HY-L906
646 compounds
On May 15, 2024, "Dimerization and antidepressant recognition at noradrenaline transporter" was published online by Nature. The research findings were an effort from Shanghai Institute of Materia Medica, Chinese Academy of Sciences. This study unraveled the important neural system target - the noradrenaline transporter (NET), obtaining the binding modes of human NET homodimers with the natural substrate norepinephrine (NE) and six selective antidepressants. It laid an important theoretical foundation for understanding the physiological regulation mechanisms of NET and other monoamine transporters.
The Norepinephrine Transporter (NET) Compound Library is obtained by computer-aided virtual screening based on the HY-L901 compound library . The specific screening process includes molecular docking screening, key pharmacophore screening, and CNS-MPO screening, which can be used for new drug discovery targeting the noradrenaline transporter.
Cat. No.: HY-120247
CAS No.: 1520893-08-6
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TASP0434299 (Compound 10) is a labeled ligand for the vasopressin V1b receptor. TASP0434299 exhibits high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and shows potent antagonistic activity against the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 is a substrate for human and rhesus monkey P-glycoprotein, resulting in low brain uptake in rhesus monkeys. TASP0434299 binds to V1B receptors in rat and monkey pituitary tissues in a saturable and specific manner both in vitro and in vivo. When radiolabeled with tritium or 11C, TASP0434299 serves as a prototype V1B receptor radiotracer to visualize V1B receptor in the pituitary gland of anesthetized monkeys via positron emission tomography .
Cat. No.: HY-137325A
CAS No.: 301334-89-4
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2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
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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
