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A biotin-tagged analog of FTY720; methanol side chain of FTY720 that is targeted for phosphorylation by sphingosine kinases is retained, suggesting that it would likewise be phosphorylated in vivo.
An abundant secondary metabolite of ?9-THC
A copper and zinc chelator and an irreversible inhibitor of aldehyde dehydrogenase (IC50 = 0.1 mM) that has been indicated for the treatment of alcohol dependence; targets the ubiquitin-proteasome pathway, induces ROS, activates JNK and p38 pathways, and inhibits NF-κB activity in...
An analog of the oral anticoagulant warfarin; functions as a vitamin K antagonist and has a half-life in plasma of about eight hours.
The Prostaglandin Screening Library I contains more than 70 “F-series” of prostaglandins and isoprostanes in a 96-well Matrix tube rack format as 2 mM stocks in DMSO.
An intermediate in the synthesis of cysteine that is produced from homocysteine and serine by the action of cystathionine-β-synthase; excess cystathionine in the urine is a hallmark of cystathioninuria.
An orally available, selective inhibitor of both free and prothrombinase-bound factor Xa (Ki = 0.8 nM); effective anticoagulant in both preclinical and clinical models of venous and arterial thrombosis.
A potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM); shows little or no activity against 38 other...
A fluorescent probe that reacts stoichiometrically and rapidly with ONOO- (rate constant (k) = 1.1 μM/s); excitation of 332 nm and emission > 400 nm.
An analog of PGF2α containing a 17-phenoxy group on the lower side chain and an isopropyl ester at the C-1 position.
A selective antagonist of EBI2 (IC50s = 11 and 15 nM for human and mouse receptors, respectively); blocks the oxysterol-induced migration of U937 monocytic cells.
A CYP450 ω-oxidation metabolite of PGF2α.
Blocks Cav1.2 channels and acts an antagonist of muscarinic acetylcholine receptors; inhibits contraction of detrusor myocytes and prevents activation of the micturition center in the brain, resulting in muscle relaxation (IC50 = 2 µM for relaxation of human bladder precontracted by...
A chemical probe for the bromodomains of the BRPF family of proteins; binds BRPF1B, BRPF2, and BRPF3 with Kd values of 0.1, 0.,5 and 2.4 µM, respectively, as determined by ITC.
A widely used antifungal imidazole that interferes with ergosterol synthesis in fungal cell membranes; induces reactive oxygen species in fungal biofilms, demonstrating a MIC value of ≥256 μM against Candida spp.
Selectively activates hM3Dq (EC50 = 1.7 nM), a DREADD derived from the human muscarinic acetylcholine M3 receptor.
A reversible inhibitor of the H2S synthesizing enzyme cystathionine-γ-lyase; blocks H2S synthesis in rat liver preparations with an IC50 value of 6.5 µM.
CAS Number: 67469-81-2 Molecular Formula: C28H34N2O • 2HCl Formula Weight: 487.5
A b,b'-dimethyl hexadecanedioic acid that exhibits hypolipidemic and antidiabetogenic effects.
A divalent crosslinker of SAP that causes rapid depletion of circulating SAP via hepatic clearance.
A DNA alkylating agents that induces DNA interstrand and intrastrand crosslinks, cytotoxicity, and apoptosis; inhibits the growth of PC-3 prostate cancer cells with IC50 values of 0.074 or 0.77 μM for sequential dosing or single dosing, respectively.
A selective, potent inhibitor of PHD2 (IC50 = 1.6 nM); active in vivo, inhibiting prolyl hydroxylation and increasing HIF1α levels in cells (IC50 values range from 5.6 to 11.7 µM) and inducing HIF1α and HIF2α expression in mice; penetrates the...
An ATP-competitive, second-generation ALK inhibitor (IC50 = 3.5 nM) that also inhibits ROS (IC50 = 8.9 nM) and ACK (IC50 = 5.8 nM); demonstrates antitumor activity in xenograft mouse models and has been shown to overcome crizotinib resistance in non-small cell lung...
17,20-dimethyl PGF1α is an analog of the limaprost family with structural modifications intended to give it a prolonged half-life and greater potency. Limaprost is an analog of PGE1 which is orally active in both rats and guinea pigs. The additional methyl groups in the lower side chain confer...