
Modulatori enzimatici
Sottocategorie di "Modulatori enzimatici"
Trovati 693 prodotti di "Modulatori enzimatici"
GSK3 (3-13)/crosstide-[S]
A glycogen synthase kinase 3β- (GSK3β-) / crosstide fragment representing the phosphorylation site on GSK3β-. GSK3β- is a serine/threonine kinase which regulates glycogen synthase activity and is a key mediator of vertebrate development, tumourigenesis and cell differentiation. GSK3β- is phosphorylated by activated AKT/protein kinase B on serine 9- promoting its inactivation.Purezza:Min. 95%Colore e forma:PowderPeso molecolare:1,193.6 g/molSRT2104
CAS:Activator of SIRT1 deacetylaseFormula:C26H24N6O2S2Purezza:Min. 95%Colore e forma:PowderPeso molecolare:516.64 g/molPHA 793887
CAS:Inhibitor of cyclin dependend kinases
Formula:C19H31N5O2Purezza:Min. 95%Colore e forma:SolidPeso molecolare:361.24778Fluvastatin lactone
CAS:HMG-CoA reductase inhibitorFormula:C24H24FNO3Purezza:Min. 95%Colore e forma:PowderPeso molecolare:393.45 g/molNrf2 (69-84)
Nuclear Factor Erythroid 2-Related Factor 2 (Nrf2) and its negative regulator Kelch-Like ECH-Associated Protein 1 (Keap1) provide vital protection in maintaining cellular redox. In parallel, Nrf2 also aids the resolution of inflammation and also tissue repair. In homeostatic conditions, the transcription factor Nrf2 is controlled in a cytoplasmic complex with Keap1 with ubiquitination and protein degradation. Nrf2 has been linked to numerous cancers due to mutations affecting the binding region of Nrf2 to Keap1, resulting in Nrf2 dissociating from the complex. Nrf2 constitutively accumulates in the nucleus and activation of prosurvival genes that promote cancer cell proliferation.The Neh2 region of Nrf2 interacts with Keap1, as shown by nuclear magnetic resonance spectroscopy. The 16 amino acid peptide (AFFAQLQLDEETGEFL) (69-84) flanks the conserved ETGE motif and can replicate the binding to keap1.Therapeutics targeting the Nrf2 signalling pathway and activation of Nrf2 is a keen area of research, with many cancers being linked to Nrf2, particularly pancreatic cancer. Additionally, activation of Nrf2 has become a possible target as a treatment for COVID. Nrf2 (69-84) replicating full-length Nrf2 binding has been helpful in all cases.Purezza:Min. 95%Colore e forma:PowderPeso molecolare:1,856.9 g/mol[G]-JAK1 peptide (1015-1027) p(Y1022)
This peptide is phosphorylated by Janus kinase 1 (JAK1) and is an ideal substrate for use in kinase assays. The JAK family of kinases is essential for the signalling of a host of immune modulators in tumour, stromal, and immune cells where they are highly expressed. JAK family proteins mediate the signalling of the interferon (IFN), IL-6, and IL-2 families of cytokines.JAK kinases are associated with cytokine receptors. Cytokine binding to these receptors results in activation of JAK kinases and receptor phosphorylation. Phosphorylated cytokine receptors recruit STAT proteins, which are then phosphorylated by the activated JAK kinases. Phosphorylated STAT proteins form homo- and hetero-dimers that translocate into the nucleus and function as transcription factors.This JAK1 substrate peptide contains an N-terminal Glycine-residue and a phospho-tyrosine-residue.Purezza:Min. 95%Colore e forma:PowderPeso molecolare:1,710.7 g/molAZD 2098
CAS:A potent and selective agonist of CCR4 chemokine receptor with IC50 values ranging from 10 to 25 nM across different species. CCR4 is involved in activation and migration of Th2 lymphocytes to the lungs in response to allergens. Treating sensitised rats results in reduced inflammation of lung tissue.Formula:C11H9Cl2N3O3SPurezza:Min. 95%Colore e forma:PowderPeso molecolare:334.18 g/molSorafenib tosylate - Bio-X ™
CAS:Sorafenib is a drug that belongs to the class of multikinase inhibitors. It inhibits a number of kinases, including the Mcl-1 protein, which is involved in apoptosis along with blocking picolinic acid (PA), an endogenous metabolite involved in apoptosis signal transduction. Sorafenib also binds to epidermal growth factor receptor (EGFR) on the surface of cancer cells, inhibiting the production of proteins that are required for angiogenesis, thus blocking the formation of new blood vessels. Sorafenib may also inhibit P-glycoprotein (Pgp) activity. Overall, these cytotoxic effects give Sorafenib anti-tumor properties, inhibiting angiogenesis and cellular transformation, which are the two main processes of tumor growth and metastasis. Sorafenib tosylate has been shown to be effective against a range of solid tumors such as breast, prostate and lung cancers and is also used for the treatment of metastatic colorectal cancer and renal cell carcinoma. A combination therapy group found that sorafenib was more effective when used with interferon alfa-2b for the treatment of advanced renal cell carcinoma. Sorafenib tosylate also has the potential for drug interactions with other drugs that are metabolized by cytochrome P450 enzymes.
Sorafenib tosylate is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.Formula:C21H16ClF3N4O3•C7H8O3SPurezza:Min. 95%Colore e forma:PowderPeso molecolare:637.03 g/molTTK 21
CAS:CBP/p300 histone acetyltransferase activatorFormula:C17H15ClF3NO2Purezza:Min. 95%Colore e forma:PowderPeso molecolare:357.76 g/molErlotinib mesylate
CAS:EGFR tyrosine kinase inhibitorFormula:C23H27N3O7SPurezza:Min. 95%Colore e forma:White PowderPeso molecolare:489.54 g/molLGK 974
CAS:Inhibits Wnt signaling pathway by targeting porcupine, a membrane-bound O-acyltransferase involved in the palmitoylation and secretion of Wnt. Anti-cancer properties of LGK 974 have been demonstrated in various tumor models of breast cancer, head and neck squamous cell carcinoma and glioblastoma. Blocks LPS-mediated inflammatory response in epithelial and endothelial cells.
Formula:C23H20N6OPurezza:Min. 98 Area-%Colore e forma:White PowderPeso molecolare:396.40 g/molNitric oxide synthase, endothelial (492-507)
Peptide derived from the endothelial nitric oxide synthase which synthesises nitric oxide in order to protect endothelial cells from vascular diseases, atherosclerosis and thrombosis.Purezza:Min. 95%Colore e forma:PowderPeso molecolare:1,788.1 g/molFluvastatin sodium salt - Bio-X ™
CAS:Fluvastatin is a statin that lowers blood cholesterol and triglycerides by inhibiting HMG-CoA reductase, an enzyme that plays a critical role in the synthesis of cholesterol. Fluvastatin has also been shown to reduce the incidence of myocardial infarction, and to reduce atherosclerotic lesions in animal models, reducing the incidence of cardiovascular disease. Fluvastatin also has been shown to inhibit the activation of toll-like receptor 4 (TLR4) by lipopolysaccharide (LPS), which may be related to its anti-inflammatory effects. Furthermore, through lowering blood cholesterol, Fluvastatin also inhibits tubulointerstitial injury and prevents renal damage caused by high concentrations of the lipid.Formula:C24H25FNNaO4Purezza:Min. 98%Peso molecolare:433.45 g/molTAK 243
CAS:A potent inhibitor of ubiquitin activating enzyme E1. Lowers ubiquitin conjugates in cells, thereby disrupting cell signalling, cell cycle progression and repair of DNA damage. Anti-tumor effects have been demonstrated in vitro and in vivo. TAK 243 has been used to study the biology of ubiquitins and its potential as anti-cancer therapy.Formula:C19H20F3N5O5S2Purezza:Min. 95%Colore e forma:White Off-White PowderPeso molecolare:519.52 g/molN-[3-(1,3-Benzodioxol-5-yl)pyrazolo[1,5-a]pyrimidin-5-yl]-N',N'-dimethyl-propane-1,3-diamine
Selective inhibitor of the mutated RET variant RETV804M, which is the anticipated drug-resistant RET mutant that can occur in tumours treated with kinase inhibitors. The compound has a biochemical IC50 of 0.02 µM and selectivity for purified RETV804M over purified RET and KDR of 3.7 and 110, respectively. The efficacy of the compound was shown also in cell cultures with IC50 of 4.4 µM, and cell assay selectivity for RETV804M over RET and KDR of 0.89 and 2.3, respectively.Formula:C18H21N5O2Purezza:Min. 98 Area-%Colore e forma:PowderPeso molecolare:339.39 g/molI-RW
The peptide IRW, characterised from egg protein, exhibits inhibitory properties against the angiotensin converting enzyme (ACE2) and could be used to prevent cardiovascular disease with further research. Treatment of hypertensive mice with IRW induced endothelium-dependent vasorelaxation and reduced vascular inflammation. The IRW tripeptide acts as anti-hypertensive by upregulating ACE2 activity via the Mas receptor (MasR) and upregulating Akt/eNOS signalling in the aorta. IRW also induces superoxide dismutase (SOD), catalase (CAT), and glutathione peroxidase (GPx) activity. These may play a factor in IRW's role as an anti-inflammatory. IRW shows promise as a nutraceutical for inflammatory conditions and a tool for drug development in cardiovascular disease.Purezza:Min. 95%Peso molecolare:1,830.9 g/molMEK162
CAS:Inhibitor of MEK1/2 kinase enzymes; antineoplasticFormula:C17H15BrF2N4O3Purezza:Min. 95%Colore e forma:White/Off-White SolidPeso molecolare:441.23 g/molIQVPL (EYGF-56)
During extraction of lecithin from egg yolk, peptide by-products can be isolated and purified by gel filtration. Within the by-products this has led to the discovery of biologically active value-added products. The egg yolk gel filtration (EFGF) fractions were analysed for their antioxidant and angiotensin converting enzyme (ACE) inhibitory activities. EYGF-56 predominantly contained 3 peptides - SDNRNQGY, IQVPL, and KGLWE. IQVPL in EYGF-56 was found to have minimal antioxidant activity. YPSPV showed some angiotensin converting enzyme (ACE) inhibitory activity.Purezza:Min. 95%Peso molecolare:567.4 g/molDanusertib
CAS:Inhibitor of aurora kinases
Formula:C26H30N6O3Purezza:Min. 95%Colore e forma:White PowderPeso molecolare:474.57 g/molK252c
CAS:Inhibitor of protein kinase PKCFormula:C20H13N3OPurezza:Min. 95%Colore e forma:PowderPeso molecolare:311.34 g/molPemetrexed disodium salt - Bio-X ™
CAS:Pemetrexed is an antifolate drug that is used to treat mesothelioma and non-small cell lung cancer. It is used during chemotherapy and sometimes used in conjunction with cisplatin. This drug disrupts folate-dependent metabolic activities essential for cell replication. In vitro studies have shown that Pemetrexed inhibits thymidylate synthase.Formula:C20H19N5Na2O6Purezza:Min. 95%Colore e forma:PowderPeso molecolare:471.37 g/molMoexipril HCl - Bio-X ™
CAS:Moexipril is an angiotensin converting enzyme inhibitor that is used for the treatment of hypertension. This drug is a prodrug for moexiprilat and works by relaxing the blood vessels causing them to widen and lowering blood pressure. Moexipril has been shown to be effective in treating metabolic disorders such as congestive heart failure.Formula:C27H34N2O7Purezza:Min. 95%Colore e forma:PowderPeso molecolare:498.57 g/molNVP AAM 077 tetrasodium hydrate
CAS:NMDA receptor antagonistFormula:C17H13BrN3Na4O5P·xH2OPurezza:Min. 95%Colore e forma:Light yellow to light green solid.Peso molecolare:542.14Pazopanib - Bio-X ™
CAS:Pazopanib is an antineoplastic agent that is used to treat advanced renal cell cancer and advanced soft tissues sarcoma. This drug is a multitargeted tyrosine kinase inhibitor against vascular endothelial growth factor receptor 1, 2, 3 and c-kit. As a result, it increases tumor apoptosis and decreases tumor blood flow.
Formula:C21H23N7O2SPurezza:Min. 95%Colore e forma:PowderPeso molecolare:437.52 g/molCobimetinib
CAS:Inhibitor of MEK kinase
Formula:C21H21F3IN3O2Purezza:Min. 95%Colore e forma:White PowderPeso molecolare:531.31 g/molSunitinib malate - Bio-X ™
CAS:Sunitinib is a receptor tyrosine kinase inhibitor and a chemotherapeutic agent used for the treatment of renal cell carcinoma. This drug can also be used to treat gastrointestinal tumors that are resistant to imatinib. Sunitinib inhibits VEGFR1, VEGFR2, VEGFR3, PDGFR and KIT tyrosine kinases.Formula:C22H27FN4O2·C4H6O5Purezza:Min. 95%Colore e forma:PowderPeso molecolare:532.56 g/molKGLWE (EYGF-56)
During extraction of lecithin from egg yolk, peptide by-products can be isolated and purified by gel filtration. Within the by-products this has led to the discovery of biologically active value-added products. The egg yolk gel filtration (EFGF) fractions were analysed for their antioxidant and angiotensin converting enzyme (ACE) inhibitory activities. EYGF-56 predominantly contained 3 peptides - SDNRNQGY, KGLWE, and IQVPL. KGLWE in EYGF-56 was found to have very strong antioxidant activity. KGLWE showed minimal angiotensin converting enzyme (ACE) inhibitory activity.Purezza:Min. 95%Peso molecolare:630.3 g/mol(-)-Huperzine A
CAS:Acetylcholinesterase inhibitor; therapy for Alzheimer's diseaseFormula:C15H18N2OPurezza:(%) Min. 98%Colore e forma:PowderPeso molecolare:242.32 g/molPimasertib
CAS:A selective inhibitor of MEK1/2 kinase. Anti-proliferative and pro-apoptotic in multiple myeloma (MM) cells via G0/G1 cell cycle arrest and caspase 3 and PARP cleavage, respectively. Synergistic with other anti-MM therapies. Has anti-tumor effects in some solid tumors, such as in K-ras mutated colorectal cancer.Formula:C15H15FIN3O3Purezza:Min. 95%Colore e forma:White To Yellow SolidPeso molecolare:431.2 g/molCP 43
CAS:Inhibitor of TAOK1 and TAOK2 kinasesFormula:C25H24N2O2Purezza:Min. 95%Colore e forma:SolidPeso molecolare:384.47 g/molDexrazoxane - Bio-X ™
CAS:Dexrazoxane is a cytoprotective drug that is used in chemotherapy to provide cardio-protection against anthracycline toxicity. It is an antimitotic agent with immunosuppressive properties. Dexrazoxane works by binding to iron in the cell, preventing it from being released. Dexrazoxane is also a catalytic inhibitor of topoisomerase II.Formula:C11H16N4O4Purezza:Min. 95%Colore e forma:PowderPeso molecolare:268.27 g/molERKtide amide
ERKtide Substrate Peptide.Purezza:Min. 95%Colore e forma:PowderPeso molecolare:1,674.9 g/molD 4476
CAS:Inhibitor of protein kinase CK1Formula:C23H18N4O3Purezza:Min. 95%Peso molecolare:398.41 g/molRucaparib
CAS:Inhibitor of poly (ADP-ribose) polymerase enzyme; antineoplastic
Formula:C19H18FN3OPurezza:Min. 98 Area-%Colore e forma:Yellow PowderPeso molecolare:323.36 g/molPYK2 peptide substrate
Substrate for proline-rich tyrosine kinase 2 (Pyk2)- can be used for substrate phosphorylation assays. Pyk2 is a member of the focal adhesion kinase (FAK) subfamily of cytoplasmic tyrosine kinases. Pyk2 is also known as: calcium-dependent tyrosine kinase (CADTK)- cellular adhesion kinase β- related adhesion focal tyrosine kinase (RAFTK)- or FAK2.Pyk2 functions as a scaffold protein, and it interacts with cytoplasmic proteins at focal adhesion sites to integrate different environmental signals. Pyk2 is activated by several stimuli, including elevated intracellular calcium levels, protein kinase C activation, and exposure to stress factors. Recently, Pyk2 has become a potentially important new therapeutic target or prognostic marker because overexpression of Pyk2 has been found in many human tumours.Purezza:Min. 95%Peso molecolare:1,938.9 g/molS-Rolipram
CAS:Inhibitor of PDE4 enzyme; anti-inflammatoryFormula:C16H21NO3Purezza:Min. 95%Colore e forma:White To Off-White SolidPeso molecolare:275.34 g/molAxltide Peptide substrate
Axltide-is a substrate peptide for use in kinase assays and is based on the mouse insulin receptor substrate 1 (IRS1) (amino acid 979-989).IRS1 is a membrane-proximal adaptor protein, which binds to, and is phosphorylated by, the insulin receptor (IR) at its tyrosine residue. IRS1 transmits the extracellular signal for insulin to serine/threonine kinases, such as Akt which then deliver the signal into the cell to mediate the various actions of insulin.Purezza:Min. 95%Colore e forma:PowderPeso molecolare:1,513.7 g/molMilrinone - Bio-X ™
CAS:Milrinone has an application for use in the treatment of heart failure. It has been shown to increase cardiac output and decrease left ventricular end diastolic pressure (LVEDP). Milrinone also increases the amount of oxygen delivered to the tissues by increasing cardiac contractility. Milrinone is part of our Bio-X ™ Range. These products are aimed at life science researchers who need high quality ready to use products for assay development, screening or other R&D work. With a solubility datasheet and convenient vials, all of our Bio-X ™ products are in stock across our global warehouses for rapid delivery and ease of use.Formula:C12H9N3OPurezza:(%) Min. 95%Colore e forma:PowderPeso molecolare:211.22 g/molDAPKtide Substrate Peptide
DARKtide is a substrate peptide for death-associated protein kinase (DAPK) for use in kinases assays. DAPK is involved in several cellular pathways including: apoptosis, tumour suppression, stress response, anti-viral immunity and IL-1-associated inflammatory diseases. In C. elegans DAPK-1 regulates epidermal morphogenesis, innate immunity and wound repair.Purezza:Min. 95%Colore e forma:PowderPeso molecolare:1,577.9 g/molA15
A15 also known as alpha2-Antiplasmin is a serine/protease inhibitor which inactivates plasmin in the blood. To inhibit plasmin in the blood alpha2-Antiplasmin forms a protease serpin complex with plasmin due to interactions of kringle 1 or 3 of plasmin and the lysine residues of alpha2-Antiplasmin's C-terminus. Although synthesised in the Liver A15 is also present within the neurons of the human brain and its expression has been found to be enhanced in Aβ plaques of Alzheimer's disease and during myocardial infarction. A high concentration of alpha2-Antiplasmin in the blood may also contribute to an increased risk of Ischemic strokes. Alternatively its expression appears to be diminished in patients with cirrhosis and acute liver failure. A further function of A15 is its ability to regulate fibrinolysis through crosslinking to fibrin.Purezza:Min. 95%Colore e forma:PowderPeso molecolare:1,755.9 g/molYPSPV (EYGF-33)
During extraction of lecithin from egg yolk, peptide by-products can be isolated and purified by gel filtration. Within the by-products this has led to the discovery of biologically active value-added products. The egg yolk gel filtration (EFGF) fractions were analysed for their antioxidant and angiotensin converting enzyme (ACE) inhibitory activities. EYGF-33 predominantly contained 3 peptides - KLSDW, YPSPV, and MPVHTDAD). YPSPV in EYGF-33 was found to have minimal antioxidant activity. However, YPSPV showed notably high angiotensin converting enzyme (ACE) inhibitory activity, it exceeded the positive control captopril.Purezza:Min. 95%Peso molecolare:560.3 g/molNitazoxanide - Bio-X ™
CAS:Nitazoxanide acts as a noncompetitive inhibitor of the pyruvate: ferredoxin/flavodoxin oxidoreductases of various microorganism with Ki values between 2 and 10 μM. Nitazoxanide is clinically relevant for its broad-spectrum action to reduce the growth of bacteria, various parasites, and especially for its efficacy against the pathogen Helicobacter pylori. Nitazoxanide also has been shown to be effective in treating inflammatory bowel disease and acute enteritis caused by bacteria. In 2021, nitazoxanide was tested for the treatment of COVID-19 patients with mild symptoms due to its broad antiviral action.Formula:C12H9N3O5SPurezza:Min. 90 Area-%Colore e forma:PowderPeso molecolare:307.28 g/mol4-5-(4-Pyridylmethylamino)pyrazolo1,5-apyrimidin-3-ylbenzamide
CAS:Selective inhibitor of the mutated RET variant RETV804M, which is the anticipated drug-resistant RET mutant that can occur in tumours treated with kinase inhibitors. The compound has a biochemical IC50 of 0.02 µM and selectivity for purified RETV804M over purified RET and KDR of 3.7 and 110, respectively. The efficacy of the compound was shown also in cell cultures with IC50 of 4.4 µM, and cell assay selectivity for RETV804M over RET and KDR of 0.89 and 2.3, respectively.Purezza:Min. 98 Area-%Colore e forma:PowderPeso molecolare:344.37 g/molA 1070722
CAS:High affinity inhibitor of glycogen synthase kinase GSK-3 with Ki of 0.6 nM. A 1070722 showed favourable characteristics for the penetration across blood brain barrier. A 1070722 was also shown to reduce the phosphorylation of microtubule-associated protein Tau.Formula:C17H13F3N4O2Purezza:Min. 95%Colore e forma:SolidPeso molecolare:362.31 g/molNintedanib ethanesulfonate
CAS:Used for treatment of idiopathic pulmonary fibrosisFormula:C31H33N5O4•C2H6O3SPurezza:Min. 98 Area-%Colore e forma:PowderPeso molecolare:649.76 g/molGSK 1904529A
CAS:Inhibitor of IGF1 receptorFormula:C44H47F2N9O5SPurezza:Min. 95%Peso molecolare:851.33889Bragsin 2
CAS:Inhibitor of BRAG2-mediated activation of Arf GTP-ase. In vitro experiments showed that Bragsin2 inhibits the Arf GTP-ase activation that is mediated by a nucleotide exchange factor BRAG2 in a membrane-dependent manner. Bragsin2 interacts with the PH domain of BRAG2 protein as well as membrane, which prevents the activation of lipidated Arf. Bragsin2 affects the trans-Golgi network and was shown to affect the tumour sphere in breast cancer cell lines.Formula:C11H6F3NO5Purezza:Min. 95%Colore e forma:SolidPeso molecolare:289.16 g/molGC376 sodium
CAS:GC 376 is an inhibitor of the main protease Mpro (3CLpro) in coronaviruses as well as picornaviruses. This broad-spectrum antiviral compound has been used as investigational veterinary drug for treatment of feline infectious peritonitis virus (FIPV) infections. Recent studies also showed that GC 376 inhibits the main protease Mpro (3CLpro) from SARS-CoV-2 with IC50 of 0.03 μM and EC50 of 3.37 μM.
Formula:C21H30N3NaO8SPurezza:Min. 95 Area-%Colore e forma:White PowderPeso molecolare:507.53 g/molSD 0006
CAS:SD 0006 is a small-molecule inhibitor, which is synthesized through specialized chemical processes. It functions by selectively inhibiting the cyclooxygenase-2 (COX-2) enzyme, which plays a significant role in the inflammatory pathway. This inhibition reduces the production of pro-inflammatory prostaglandins, ultimately leading to a decrease in inflammation.Formula:C20H20ClN5O2Purezza:Min. 95%Peso molecolare:397.86 g/molEverolimus
CAS:mTOR kinase inhibitor; rapamycin analog; immunosuppressantFormula:C53H83NO14Purezza:90%Colore e forma:White Off-White PowderPeso molecolare:958.23 g/mol
