A Bcr-Abl kinase inhibitor (IC₅₀ = 5.8 nM) that is 25- to 55-fold more potent than imatinib in vitro and ≥10-fold more potent in vivo; inhibits 12 out of the 13 most frequent imatinib-resistant Bcr-Abl point mutations, but not the T315I mutation; also targets the Src family kinase Lyn…

Inhibits smooth MLCK (Ki = 0.3 µM) 10-fold more potently than its parent compound ML-9.

A cell-permeable dye that is cleaved by intracellular esterases, leaving membrane-impermeant calcein, a fluorescent indicator with absorption and emission maxima of 494 and 517 nm, respectively.

An inhibitor of PLC-dependent processes by an undefined mechanism; inhibits platelet aggregation induced by collagen or thrombin with IC₅₀ values of 0.6 and 5 µM, respectively.

A quinazoline that inhibits the tyrosine kinase activity of EGFR (IC₅₀ = 0.025 nM); inhibits the growth of SKOV3 and MDA-468 tumor cell lines (EC₅₀s = 6.5 and 30 µM, respectively).

A metabolite of the nucleoside reverse transcriptase inhibitor, zidovudine, formed by direct conjugation by UGT2B7.

A selective TRPM8 antagonist (IC₅₀s = 8.3 and 5.8 nM in human and rat, respectively); attenuates icilin-induced wet-dog shakes in rats (ED₅₀ = 0.65 mg/kg); reduces HSC3 and HSC4 oral squamous carcinoma cell migration and invasion in vitro.

A derivative of hydrochlorothiazide, which is a diuretic and antihypertensive agent that increases renal excretion of sodium, potassium, chloride, and bicarbonate ions by inhibiting tubular reabsorptive mechanisms.

A potent inhibitor of the TGF-β receptor 1 (TGF-β R1, ALK5) kinase (IC₅₀ = 14.36 nM); blocks TGF-β1-induced phosphorylation and nuclear translocation of SMAD2/3 as well as TGF-β1-directed gene expression; effective in vivo, preventing the development of fibrosis in animals.

A covalent Cdk7 inhibitor (IC₅₀s = 3.2-15.6 nM in vitro) that displays broad anti-proliferative activity against cancer cell lines, particularly T-ALL cell lines with characteristic misregulation of T cell lineage-specific transcription factors.

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).

11β-PGF2α-EA is the theoretical hepatic metabolite of PGD2-EA, produced during COX-2 metabolism of the endogenous cannabinoid AEA which is found in brain, liver, and other mammalian tissues. AEA can be used directly by COX-2 and specific PG synthase to produce ethanolamide congeners of…

An activator of the P2X receptors that exhibits 5-30-fold greater potency at the P2X7 receptor than ATP; activates the human, rat, and mouse receptors with EC₅₀ values of 0.7, 3.6, and 285 μM, respectively.

A potent and selective agonist of the human PGE2 receptor, EP4 with a Ki value of 0.38 nM and an EC50 value of 0.6 nM; induces thermal hyperalgesia when injected into guinea pig forepaw and increases vasodilation of human pulmonary vein.

A specific Akt inhibitor that has been shown to inhibit proliferation and to induce apoptosis of thyroid cancer cells (IC₅₀ = 30-60 nM in vitro); inhibits Akt, PDK1, and FLT3 in acute myelogenous leukemia cells, decreasing the colony-forming ability of these cells (IC₅₀…

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…

8-iso PGF1β is a potential autoxidation product of DGLA. There are no published reports on its isolation from any biological source or on its biological activity.

An inactive metabolite of PGE2 formed by 15-hydroxy PGDH PGs inactive.

A tight-binding, allosteric inhibitor of reverse transcriptase that is active against HIV-1 and HIV-2 (both EC₅₀s = 1 nM in vitro).

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.

PGF1β is the C-9 epimer of PGF1α. It was shown to enhance respiratory rate in experimental animals when administered intravenously.

A potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.

A corticosteroid prodrug that is converted to its active form, des-CIC, a glucocorticoid receptor agonist (Ki = 0.31 nM); used to ameliorate symptoms of airway inflammatory diseases.

A selective, short-acting adenosine A2A receptor agonist (Ki = 1.1 nM for pig striatum A2A receptor); used to induce hyperemia, particularly in the context of myocardial perfusion imaging.

An inactive metabolite of artemisinin.

A kaempferol glycoside that selectively inhibits RSK2 with an IC50 value of 89 nM (Ki = 1 μM) without interfering with upstream activators of RSK, including ERK, MEK, EGFR, and PKC; inhibits the proliferation of MCF-7 breast cancer cells at 100 μM and attenuates angiotensin II-induced cell…

ApNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity. FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its nominal endogenous substrate AEA (Item No. 90050). It also will hydrolyze…

A selective autotaxin inhibitor (IC50 = 5.7 nM) that has been shown to dose-dependently block thrombin-induced LPA secretion in platelets.

A selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC₅₀s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.

A staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC₅₀s ranging from 60-600 nM).

A Pim kinase inhibitor that blocks mTORC1 activity via activation of AMPK, killing a wide range of both myeloid and lymphoid cell lines (with IC50 values ranging from 0.8 to 40 μM); induces G1 phase cell-cycle arrest, dose-dependent induction of p27Kip1, apoptosis through the mitochondrial…

BW 245C is a selective agonist for the DP1 receptor. The Ki of BW 245C for the inhibition of [3H]-PGD2 binding to isolated human platelet membranes is 0.9 nM. It has a reported IC50 of 2.5 nM for the inhibition of ADP-induced human platelet aggregation and an IC50 of 250 nM for the inhibition of…