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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
21 Results for "
threonine residue
" in MedChemExpress (MCE) Product Catalog:
Products (21)
21 Results for "threonine residue" in MCE Product Catalog:
280
280 Cited Publications
Synonyms: PS-341; LDP-341; NSC 681239
Research Areas:
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .
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1 Cited Publications
Cat. No.: HY-KE7057
O-Glycosidase is highly specific and can release Galβ1-3GalNAc from serine, threonine residues or as part of a glycopeptide or glycoprotein. Applied to glycoprotein biosynthesis analysis, O-glycan bioactive protein O-glycosylation detection and binding site analysis.
Synonyms: 4-Nitrobenzyl mesylate; para-Nitrobenzyl mesylate; PNBM
Target:
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
p-Nitrobenzyl mesylate (4-Nitrobenzyl mesylate) is an alkylating reagent. p-Nitrobenzyl mesylate alkylates thiophosphorylated serine, threonine, tyrosine residues and cysteine thiols, without modifying hydroxyl, amino or carboxylic acid functional groups. p-Nitrobenzyl mesylate generates thiophosphate epitopes on thiophosphorylated substrate proteins for recognition by thiophosphate-specific antibodies. p-Nitrobenzyl mesylate facilitates the identification and purification of kinase substrates. p-Nitrobenzyl mesylate is applicable to studies related to cerebral ischemia-reperfusion injury .
Cat. No.: HY-10227R
CAS No.: 179324-69-7
Synonyms: PS-341 (Standard); LDP-341 (Standard); NSC 681239 (Standard)
Research Areas:
Bortezomib (Standard) is the analytical standard of Bortezomib. This product is intended for research and analytical applications. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Bortezomib can be used for the study of multiple myeloma (MM) . Bortezomib effectively inhibits TREM2 expression in tumor-associated macrophages (TAMs) .
Cat. No.: HY-P5979
CAS No.: 1071466-49-3
Target:
Research Areas:
Cat. No.: HY-10227S
Purity: ≥98.0%
Synonyms: PS-341-d8; LDP-341-d8; NSC 681239-d8
Target:
Research Areas:
Protein serine/threonine kinase (Ser/Thr protein kinase) is a signal transduction molecule. Protein serine/threonine kinase phosphorylates specific residues on target substrates, regulates phosphorylation-dependent signal cascades, modulates cellular processes of mycobacteria, blocks phagosome-lysosome fusion, promotes meiotic maturation of Xenopus laevis (African clawed frog) oocytes, rescues the phenotype of Saccharomyces cerevisiae (budding yeast) CDC5 mutants, and exhibits cell cycle phase-specific kinase activity. Protein serine/threonine kinase maintains a tightly regulated cell cycle expression pattern, and sustains the growth and survival of mycobacteria. Protein serine/threonine kinase can be used in studies related to tuberculosis .
Cat. No.: HY-E70290
Synonyms: GALNT1
Target:
Research Areas:
N-Acetylgalactosaminyltransferase 1 (GALNT1) is a glycosyltransferase that initiates mucin-type O-glycosylation by transferring α-GalNAc from UDP-GalNAc to serine (Ser) or threonine (Thr) residues in proteins. Overexpression of N-Acetylgalactosaminyltransferase 1 in gastric cancer can promote abnormal O-glycosylation of CD44, thereby activating the Wnt/β-catenin signaling pathway and regulating the malignant behavior of gastric cancer cells. Additionally, N-Acetylgalactosaminyltransferase 1 plays a crucial role in cancer growth and metastasis by modifying the O-glycosylation of various glycoproteins, such as mucin (MUC1), osteopontin (OPN), matrix metalloproteinase-14 (MMP14), and integrin α3 .
Cat. No.: HY-10227G
Synonyms: PS-341 (GMP); LDP-341 (GMP); NSC 681239 (GMP)
Cat. No.: HY-P5444
CAS No.: 149924-99-2
Cat. No.: HY-P5954
Target:
Research Areas:
Cat. No.: HY-E70691
CLK1 is one of the dual specificity kinases and is the founding member of the 'LAMMER' family of kinases. CLK1 activity is positively regulated by phosphorylation on either tyrosine residues or serine/threonine residues, and is negatively regulated by steric constraints mediated by the N-terminal domain, as well as, by phosphorylation on a subset of serine/threonine residues within the catalytic domain. CLK1 Recombinant Human Active Protein Kinase is a recombinant CLK1 protein that can be used to study CLK1-related functions .
Cat. No.: HY-E70568
Target:
Research Areas:
Protease (O-glycan Cleaving) is recombinantly expressed from E.coli and contains a His tag. Protease (O-glycan Cleaving) is an O-glycan-dependent protease that digests proteins carrying mucin-type O-glycans, including sialylated substrates, glycosylated Ser and Thr residues at the N terminus. Protease (O-glycan Cleaving) digests a variety of O-glycan structures, including sialylated glycosylated core 1 and core 2 structures and Tn antigen. Protease (O-glycan Cleaving) does not digest terminally modified serine or threonine residues, nor does it digest N-glycosylation sites on glycoproteins.
Cat. No.: HY-E70569
Target:
Research Areas:
α-N-acetylgalactosidase (EC 3.2.1.4) is a highly specific exoglycosidase that efficiently hydrolyzes α-N-acetylgalactosamine (GalNAc) linked to serine or threonine residues in glycoproteins (Tn antigen). α-N-acetylgalactosidase shows activity against α 1-3 linked terminal GalNAc . α-N-acetylgalactosidase is suitable for use in the pH range of 6.0-7.6 and does not require cofactors or special buffer systems.
Cat. No.: HY-160478
CAS No.: 839708-29-1
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .
Cat. No.: HY-L164
2,276 compounds
Protein serine/threonine kinases (PSKs) are protein kinases that use ATP as a high-energy donor molecule to transfer phosphate groups to serine/threonine residues of target protein. As an important signal transduction regulator, serine/threonine kinases can affect the function of target proteins by disrupting enzyme activity or binding of target proteins to other proteins. Serine/threonine kinases are involved in the regulation of immune response, cell proliferation, differentiation, apoptosis and other physiological processes. Serine/threonine kinase inhibitors are an important class of compounds that have been widely studied in cancer, chronic inflammation, autoimmune diseases, aging and other diseases.
MCE designs a unique collection of 2,276 serine/threonine kinase inhibitors, mainly targeting the receptor PKA, Akt, PKC, MAPK/ERK, etc, which is an effective tool for development and research of anti-cancer, anti-chronic inflammatory diseases, anti-autoimmune diseases and anti-aging compounds.
Cat. No.: HY-E71300
Target:
Research Areas:
The acceptor for β-galactoside α-2,3-sialyltransferase (EC 2.4.99.4) is Galβ1,3GalNAc-R, where R is H, a threonine or serine residue in a glycoprotein, or a glycolipid. Lactose can also serve as an acceptor.
Cat. No.: HY-E70949
Target:
Research Areas:
Protein Kinase C,Rat (EC 2.7.1.37) is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins. Protein Kinase C in turn are activated by signals such as increases in the concentration of diacylglycerol (DAG) or calcium ions (Ca 2+).
Cat. No.: HY-10654
CAS No.: 1192216-03-7
Target:
Research Areas:
EphB4-IN-2 is a tyrosine kinase inhibitor targeting the Eph family and Src family. EphB4-IN-2 binds to the ATP-binding site of the kinase domain of EphB4, and exhibits high affinity for tyrosine kinases with threonine as the gatekeeper residue, such as Abl, Lck and Src. EphB4-IN-2 can be used in research related to tumor-associated angiogenesis .
Cat. No.: HY-L914
3,211 compounds
In the research of covalent inhibitors targeting serine and threonine, scientists have found that the nucleophilicity of these hydroxyl groups is significantly enhanced due to the influence of their surrounding environment. This results in higher activity during catalytic reactions. Aspirin, which targets the non-catalytic domain serine (Ser529 in human COX1) of cyclooxygenase, exerts its anti-inflammatory effect through covalent binding. β-lactam antibiotics, which targets the catalytic domain serine of penicillin-binding proteins, interferes with bacterial cell wall synthesis.
Through careful selection, we constructed a structural filter containing over 110 electrophilic groups. By analyzing the electrophilic fragments selected by the structural filter, we removed any molecules with trivial or undesirable structural features. Ultimately, we obtained 3,300 fragment molecules which can target serine and threonine residues and can be used for fragment-based covalent drug discovery.
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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
