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A tumor vascular disrupting agent, inducing apoptosis in tumor vascular endothelium resulting in necrosis at the tumor core; potently activates the STING/TBK1/IRF3 signaling pathway in mouse leukocytes, inducing type-I-IFN production; inhibits VEGFR1 and VEGFR2 (IC50 = 119 and 11...
A cell-permeable, potent inhibitor of FABP4 (Ki is = 250 and 350 nM, respectively); reduces atherosclerosis in mice lacking ApoE and protects against the development of insulin resistance associated with genetic or diet-induced obesity in mice.
An indole plant alkaloid used as a peripheral vasodilator to increase blood flow to the brain; contracts excised human cerebrovascular smooth muscle in vitro with an EC50 value of 30 μM.
Ro 3-1314 is an inhibitor of both COX and lipoxygenase. Ro 3-1314 inhibits ram seminal vesicle COX with a Ki of 0.6 µM. It is a more effective inhibitor of COX-1 than of 15-LO, inhibiting 95% and 68%, respectively, of these enzymatic activities when used at a concentration of 48 µM.
A lipophilic and non-hydrolyzable cAMP analog that acts as a site-selective inhibitor of PKA type I and II, with preference towards site A of type I and site B of type II.
A cell-permeable inhibitor of HDAC activity (IC50 = 100 nM).
CAS Number: 1134163-29-3 Molecular Formula: C19H16D4N2O3S Formula Weight: 360.5
A muscarinic M1 and M2 mACh receptor agonist (pKB = 5 and 3.7, respectively) that is typically used as an animal model for temporal lobe epilepsy.
A cell-permeable bis-indolo (indirubin) compound that acts as a highly potent, selective, reversible, and ATP-competitive inhibitor of GSK3α/β (IC50 = 5 nM); inhibition of GSK activates the Wnt-signaling pathway and sustains pluripotency in human and mouse ESCs; maintains...
A reversible, time-dependent NOS inhibitor which binds more tightly to iNOS (Ki = 0.56 µM) than nNOS (Ki = 6 µM).
A synthetic ligand specific for RORα and RORγ (Kis = 172 and 111 nM, respectively) that functions as an inverse agonist; inhibits TH17 cell differentiation and IL-17A secretion in cultured splenocytes and human PBMCs at 5 μM; 25 mg/kg twice/day delays onset and severity of...
The Fatty Acid Screening Library contains more than 75 compounds of fatty acids with diverse biological activities in a 96-well Matrix tube rack format as 2 mM stocks in DMSO. The library may also include some of the most commonly-ordered fatty acids, including arachidonic, linoleic,...
Molecular Formula C22H26ClNO4 • HCl Formula Weight 440.4
Source: Recombinant protein expressed in E. coli WDR5 has been demonstrated to bind histone H3 by recognizing the first three amino acids of the N-terminal tail. Binding of WDR5 to a conserved arginine-containing motif in MLL-1, the so-called WDR5 interaction (“Win”) motif, promotes the...
cis-.DELTA.2-11-methyl-Dodecenoic acid is a diffusible signal factor (DSF) in extracellular microbial and fungal communication systems. In a DSF bioassay, the minimum concentration of cis-.DELTA.2-11-methyl-dodecenoic acid required for induction of a DSF biosensor was about 0.5 µM, which is...
An inhibitor of PHGDH, inhibiting serine synthesis from 3-PG in cells (IC50 = 33 µM); inhibits the proliferation of cancer cells by blocking de novo serine synthesis.
An aminoglycoside antibiotic that shows potent activity against a broad spectrum of bacteria.
A bioactive monohydroxylated metabolite of the cholinesterase inhibitor, tacrine that has less acute liver toxicity than tacrine in both animal and clinical studies of Alzheimer’s disease.
An inhibitor of the dopachrome tautomerase activity of MIF in vitro (IC50 = 7 µM) and in cells (IC50 = 25 µM); blocks the activation of NF-κB and TNF-α secretion from LPS-treated macrophages and improves the survival of mice following sepsis.
Acidic PEAase is an enzyme that promotes the hydrolysis of palmitoylethanolamide. A selective inhibitor of acidic PEAase (IC50 = 4.5 µM) that fails to inhibit FAAH even at a concentration of 100 µM.
A water-soluble form of the endogenous hormone cortisol that can bind to glucocorticoid receptors, initiating the transcription of anti-inflammatory and immunosuppressive mediators and inhibiting proinflammatory cytokine activity (IC50 = 6.7 µM for IL-6); commonly used to supplement...
A certified reference material categorized as a phytocannabinoid; produced by the oxidocyclization of cannabigerolic acid by cannabidiolic acid synthase; intended for research and forensic applications,,
A metabolite of propranolol.
A competitive antagonist of muscarinic (M) receptors (Ki = 1.4, 2.7, 3.6, 3.1, and 2.2 nM for M1 through M5, respectively).