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A potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through NaV channels (IC50s = 4.1 and 5.2 nM, respectively, in frog muscle and squid axon; Kd = 1.8 nM in rat brain), blocking nerve and muscle action potentials.
A selective PI3K inhibitor with an IC50 value of 1.4 µM.
A cell-permeable, fluorescent probe for DNA that is useful as a marker of nuclei for cell cycle studies in combination with BrdU and to distinguish nuclear morphology in apoptotic cells.
A form of palmitic acid with an ω-terminal alkyne for use in click chemistry to isolate palmitoylated proteins.
A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC50 = 4 nM), p59fynT (IC50 = 5 nM), Hck (IC50 = 5 nM).
A non-peptide antagonist of PAR1; blocks binding of haTRAP (IC50 = 70 nM) as well as platelet aggregation induced by either haTRAP or α-thrombin (IC50 = 0.3 and 3 µM, respectively); has no activity against PAR2, PAR4, or other receptors involved in platelet...
Pargyline is an irreversible inhibitor of monoamine oxidase (MAO) that is used clinically to treat moderate hypertension. At 10 mg/kg iv, pargyline induces a moderate decrease of systolic blood pressure in unanaesthetized hypertensive rats but not normotensive WKR or Sprague-Daley rats. The...
A glycopeptide antitumor antibiotic that produces single and double-strand DNA breaks in tumor cells to interrupt their cell cycle; has been used for the treatment of Hodgkin’s lymphoma in combination with doxorubicin, squamous cell carcinomas, testicular cancer, as well as in animal models of...
A potent inhibitor of GSK3β (IC50 = 30 nM) that induces neurogenesis in mouse embryonic stem cells.
An orally active, allosteric Akt inhibitor (IC50s = 5, 12, and 65 nM for Akt1, 2, and 3, respectively); inhibits cell proliferation of human cancer cell lines synergistically in combination with other topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth...
An irreversible antitumor agent that induces non-apoptotic cell death selectively in tumor cells expressing the small T oncoprotein and oncogenic Ras (IC50s = 1.25-5 µg/ml).
An imidazoquinoline compound that activates TLR7 (EC50 = 2.1 µM) on immune cells, inducing the production of IFN-α, IL-12, and other mediators; up-regulates the OGF receptor on cancer cells, blocking cell proliferation (IC50 = 2 µM).
A non-sedating ophthalmic antihistamine that antagonizes histamine H1 receptors (IC50 = 1.58 nM) and prevents the release of pro-inflammatory mediators from mast cells and eosinophils.
A lipid peroxidation product; actively modifies histidine and lysine residues on proteins and causes protein cross-linking.
A calcimimetic that allosterically activates the calcium-sensing receptor (CaSR; pEC50 = 7.3 in HEK293T cells expressing CaSR) inhibiting parathyroid hormone secretion.
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