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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
3540 Results for "
m6A substrate
" in MedChemExpress (MCE) Product Catalog:
Products (3540)
3540 Results for "m6A substrate" in MCE Product Catalog:
Synonyms: 5,6-EET; (±)5,6-EpETrE
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5,6-Epoxyeicosatrienoic acid (5,6-EET; (±)5,6-EpETrE) is a fully racemic version of the enantiomeric forms biosynthesized from arachidonic acid by cytochrome P450 enzymes. In solution, 5,6-Epoxyeicosatrienoic acid degrades into 5,6-DiHET and 5,6-δ-lactone, which can be converted to 5,6-DiHET and quantified by GC-MS. In neuroendocrine cells, such as the anterior pituitary and pancreatic islets, 5,6-Epoxyeicosatrienoic acid has been implicated in the mobilization of calcium and hormone secretion. 5,6-Epoxyeicosatrienoic acid is an inhibitor of T-type voltage-gated calcium channels (Cav3) that inhibits isoforms Cav3.1, Cav3.2 (IC50=0.54 μM), and Cav3. and decreases nifedipine-resistant phenylephrine-induced vasoconstriction in isolated mouse mesenteric arteries via Cav3.2 blockade when used at a concentration of 3 μM. In addition, it is a substrate of COX-1 and COX-2.
Cat. No.: HY-13687R
CAS No.: 873225-46-8
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IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.
Cat. No.: HY-146248A
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TFMU-ADPr triethylamine 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 triethylamine 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 triethylamine 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 triethylamine 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 triethylamine is also applicable to COVID-19-related research .
Cat. No.: HY-146248B
Purity: 98.02%
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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-16265A
CAS No.: 2514957-81-2
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JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .
Cat. No.: HY-183118
CAS No.: 3064485-16-8
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CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. CID-078 binds cyclin hydrophobic patches, disrupting interactions of cyclin A-Cdk2 with E2F1 and cyclin B-Cdk1 with Myt1, and selectively targets RxL binding motifs to block complex-substrate interactions. CID-078 induces DNA damage, G2/M cell cycle arrest, apoptosis, mitotic catastrophe, spindle assembly checkpoint activation, and neomorphic cyclin B-CDK2 complex formation, driving synthetic lethality in E2F-driven cancer cells. CID-078 can be used for the research of small cell lung cancer, non-small cell lung cancer, triple negative breast cancer, advanced solid tumors, luminal HR +/HER 2- breast cancer, RB1-altered solid tumors, and neuroblastoma .
Cat. No.: HY-D3187
CAS No.: 2484831-02-7
Cat. No.: HY-W013724
CAS No.: 54735-61-4
Synonyms: IDP disodium; Inosine-5'-diphosphoric acid disodium
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Inosine-5'-diphosphate disodium (IDP disodium) is a decoy substrate of NM23-H2. Inosine-5'-diphosphate disodium has a superior bond capacity on GDP-binding pocket of NM23-H2 (KD: 5.0 μM). Inosine-5'-diphosphate disodium abrogates c-MYC transcription, induces apoptosis and G2/M cell cycle arrest by disrupting NM23-H2-Pu27-GQ interactions without affecting NM23-H2-mediated kinase properties. Inosine-5'-diphosphate disodium has antihypoxic, antihyperthermic and antiarrhythmic activity and protects animals against the noxious effects of γ-irradiation. Inosine-5'-diphosphate disodium can be used for cancers like Burkitt's lymphoma and cardiovascular diseases research .
Cat. No.: HY-W740027
CAS No.: 1160707-78-7
Synonyms: 5-Methyldeoxycytidine-d3
Cat. No.: HY-101488R
CAS No.: 1010100-07-8
CC-885 (Standard) is the analytical standard of CC-885 (HY-101488). This product is intended for research and analytical applications. CC-885, a cereblon (CRBN) modulator, acts as a molecular glue degrader targeting GSPT1 with a Kd of 350 nM. CC-885 binds to CRBN to alter the substrate specificity of the CRL4 E3 ligase, promoting the ubiquitination and proteasomal degradation of GSPT1, BNIP3L, PLK1, CDK4, IKZF1/3, GSPT2, WIZ, CHD7, GOLM1, CK1α and ETS1. CC-885 induces apoptosis, cell cycle arrest, transcriptional downregulation and antiproliferation in cancer cells. CC-885 is applicable to research related to relapsed/refractory acute myeloid leukemia, MYC-driven tumors, metastatic castration-resistant prostate cancer, multiple myeloma, hepatocellular carcinoma, glioblastoma, VHL-deficient clear cell renal cell carcinoma and non-small cell lung cancer [6] .
Cat. No.: HY-112624H
CAS No.: 9004-54-0
Synonyms: Dextran 2; Dextran D2; Dextran T2(MW 1600-2400)
Cat. No.: HY-113225S1
Synonyms: GTP-13C10,15N5 tetraammonium
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Guanosine triphosphate- 13C10, 15N5 tetraammonium solution (100 mM) (GTP- 13C10, 15N5 tetraammonium) is the 15N, 13C-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate (GTP) is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism .
Cat. No.: HY-113225S4
Purity: 98.4%
Synonyms: GTP-15N5,d14 dilithium
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Guanosine triphosphate- 15N5,d14 dilithium (GTP- 15N5,d14 dilithium) is the deuterated, 15N-labeled Guanosine triphosphate (HY-113225). Guanosine triphosphate (GTP) is a critical nucleotide and regulator of cellular metabolism. Guanosine triphosphate promotes ribosomal DNA localization, pre-rRNA transcription and ribosome biogenesis by binding to RNA polymerase I and GPN proteins (GPN1/3). Guanosine triphosphate links MYC-dependent ribosome biogenesis to nucleotide sufficiency, acts as a metabolic gatekeeper supporting protein synthesis, DNA/RNA synthesis and cellular signal transduction, while also participating in the physiological activities of pancreatic β-cells and serving as an oxidative substrate for reactive oxygen species. In small cell lung cancer with high MYC expression, Guanosine triphosphate accumulates through the IMPDH-driven synthetic pathway, thereby affecting apoptosis and mitotic processes. Guanosine triphosphate is used in the research of small cell lung cancer, hepatoblastoma and cellular metabolism .
Cat. No.: HY-129242S
CAS No.: 80404-14-4
Synonyms: 4-Oxo-Tempo-15N,d16
Tempone- 15N,d16 (4-Oxo-Tempo 15N,D16) is the deuterated, 15N-labeled Tempone (HY-129242). Tempone (4-Oxo-Tempo) is a nitroxide radical spin label and ROS scavenger. Tempone induces cytotoxicity in lymphoma cells. Tempone serves as a substrate for intracellular reduction to hydroxylamine, rapidly equilibrates between intracellular and extracellular compartments, reduces nitroxide radical spin labels at the ubiquinol site of the respiratory chain, and acts as an alternative terminal electron acceptor when electron flow to oxygen is blocked. Tempone serves as a superoxide sensor, a T2-weighted MRI contrast agent, and a dynamic nuclear polarization polarizing agent for 13C. Tempone inhibits superoxide and peroxynitrite, hydroxyl radical generation, nitrotyrosine formation, and poly (ADP-ribose) formation, and alleviates renal dysfunction and injury in ischemia/reperfusion and hydrogen peroxide-induced injury. Tempone can be used for research on ischemia-reperfusion injury, acute renal failure, and lymphoma [6] .
Cat. No.: HY-130046R
CAS No.: 547-81-9
Synonyms: 16-epi-Estriol (Standard); 16β,17β-Estriol (Standard)
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16-Epiestriol (Standard) is the analytical standard of 16-Epiestriol (HY-130046). This product is intended for research and analytical applications. 16-Epiestriol (16-epi-Estriol; 16β,17β-Estriol) is a natural stereoisomer of estriol and an anti-inflammatory agent that targets UGT. The Ki values of 16-Epiestriol against human UGT1A10 and UGT2B7 are 98.1 μM and 162 μM, respectively. As a glucuronidation substrate, 16-Epiestriol can be modified at the 3-OH, 16-OH and 17-OH sites by various UGT enzymes; in liver microsomes, the modification mainly occurs at the 16-OH and 17-OH sites, while reactions take place at all three sites in intestinal microsomes. 16-Epiestriol acts on the phase II inflammatory process by blocking edema mediated by prostaglandins and leukocyte infiltration. It lacks glycogenic activity or any effect on blood glucose levels, and serves as an important candidate molecule in the research of inflammatory diseases .
Cat. No.: HY-170316
Ibetazol is a Importin β1 (KPNB1) inhibitor and nucleocytoplasmic transport disruptor. Ibetazol binds covalently to Cys585 of Importin β1, blocks both Importin β1-mediated direct transport and Importin α-dependent nuclear import processes, without affecting transport mediated by other nucleocytoplasmic transport proteins. Ibetazol induces cytoplasmic accumulation of Importin α1, and inhibits nuclear import of substrates carrying nuclear localization signals (NLS), including the NLS-cMyc reporter gene, RelA/p65 and SREBP1. Ibetazol triggers spindle malformation and chromosome misalignment by disrupting the mitotic function of Importin β1. Ibetazol inhibits the proliferation of cells expressing wild-type Importin β1. Ibetazol has a high activity-cytotoxicity window, lacks intrinsic fluorescence, and acts rapidly on nucleocytoplasmic transport processes. Ibetazol serves as a tool compound for investigating nuclear import processes specifically mediated by Importin β1 .
Cat. No.: HY-189126
CAS No.: 1240580-64-6
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YL064 is a multi-target STAT3-c-MYC inhibitor that directly binds to ATXN3 and inhibits its deubiquitinating activity, thereby promoting the ubiquitination and proteasomal degradation of oncogenic substrates of ATXN3. YL064 inhibits the phosphorylation of STAT3-Tyr705 without altering the total protein level of STAT3; meanwhile, it directly binds to the SH2 domain of STAT3 to block the dimerization, nuclear translocation, and DNA-binding activity of STAT3. YL064 directly targets the C-terminal HLH-Zip domain of c-Myc, upregulates the phosphorylation of c-Myc at the Thr58 site, and induces the ubiquitination and proteasome-dependent degradation of c-Myc. YL064 suppresses tumor cell proliferation, induces G2/M cell cycle arrest, reduces cell migration and invasion capacities, and triggers cancer cell apoptosis. YL064 can be used in related research on breast cancer, prostate cancer, diffuse large B-cell lymphoma, and multiple myeloma .
Cat. No.: HY-W021016
CAS No.: 824395-67-7
Synonyms: (S,S)-Ph-BPE
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(+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane ((S,S)-Ph-BPE) is a chiral bisphosphine ligand and catalyst. (+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane acts as a chiral ligand in rhodium-catalyzed reductive hydroformylation of alkenyl boronic esters, enabling enantiodivergent synthesis of chiral γ-boryl alcohols. (+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane forms chiral nickel-phosphine complexes to mediate asymmetric hydrogenation of aliphatic γ- and δ-keto acids; protons promote substrate C=O bond activation and stereoselectivity control via hydrogen bonding. (+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane forms a monodentate nickel complex, which serves as the active species for asymmetric hydrogenation of aliphatic keto acids .
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-112817A
Synonyms: 8-Oxo-Deoxyguanosine triphosphate trisodium
8-Oxo-dGTP (8-Oxo-Deoxyguanosine triphosphate) trisodium solution (100mM) is an oxidized guanine nucleotide formed by ROS-mediated oxidative modification of dGTP, and it also serves as a key substrate for 8-oxo-dGTP pyrophosphohydrolases (such as hMTH1 and E. coli MutT). 8-Oxo-dGTP trisodium solution (100mM) acts as a DNA mutagen, inserts into nascent DNA and pairs with adenine and cytosine, inducing A:T to C:G transversion mutations. Furthermore, 8-Oxo-dGTP trisodium solution (100mM) causes oxidative DNA base modification, strand breakage and S-phase arrest, and ultimately triggers AIF-mediated apoptosis and promotes spontaneous carcinogenesis in mth1-deficient mice. Accumulation of 8-Oxo-dGTP trisodium solution (100mM) in cells induces genomic instability, but it exhibits a tumor-suppressive effect that reduces tumor incidence in mouse models instead. 8-Oxo-dGTP trisodium solution (100mM) is widely used in studies related to spontaneous carcinogenesis, Parkinson's disease, Alzheimer's disease, heart failure and tumor mechanisms .
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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
