An analog of scriptaid that lacks scriptaid’s HDAC inhibitory effects; used as a negative control in experiments involving scriptaid.

A thioester substrate analog of 2-AG that can be utilized for the measurement of MAGL activity; hydrolysis of the thioester bond by MAGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB resulting in a yellow product with an absorbance maximum at 412 nm.

An immunosuppressant used to prevent transplant rejection; potent inhibitor of IL-2 activation of lymphocytes (IC50 = 5 pM); specifically interacts with FKBP12 to form a complex which inhibits mTORC1.

A γ-secretase inhibitor that blocks Notch processing (IC₅₀ = 1.7 nM); reduces Aβ40 levels by 71% in an APP transgenic mouse model within 4 hours after a single 100 μM/kg dose.

A non-steroidal androgen receptor antagonist (IC50 = 36 nM); reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.

An N-acylethanolamide that inhibits dietary-restriction-induced lifespan extension in wild type and TOR pathway mutant nematodes; also has anti-inflammatory properties, suppressing the expression of IL-6 and MCP-1 in 3T3-L1 adipocytes in response to lipopolysaccharide.

An analog of geldanamycin which has potent in vivo activity and reduced toxicity; has diverse anti-tumor actions; promotes the degradation of HER2 and induces growth arrest and apoptosis in breast cancer cells overexpressing HER2 (IC50 = 4-72 nM).

An alkaloid metabolite of nicotine as well as a major product of its pyrolysis; binds comparably to CYP2A6 and CYP2A13 (Kis = 7.5 and 5.6 µM, respectively), but appears to more effectively inactivate CYP2A6.

A selective inhibitor of the Src family of non-receptor tyrosine kinases (IC₅₀s = 2 and 6 nM for Lck and Src, respectively); used in combination with PD 0325901, CHIR99021, and SB-590885 to support self-renewal of naïve human embryonic stem cells.

Unoprostone isopropyl ester (Rescula) is the clinically approved, prodrug form of unoprostone, which is a free acid analog of PGF2α. Both latanoprost and Rescula have been approved for the treatment of ocular hypertension. Both analogs of PGF2α are believed to act by increasing the rate…

A selective inhibitor of the TGF-β type1 receptor ALK5 (IC₅₀s = 4, 18, and 23 nM for ALK5 autophosphorylation, TGF-β cellular assay, and ALK5 binding in HepG2 cells, respectively); used to induce stem cell pluripotency by replacing the reprogramming transcription factor Sox2…

Molecular Formula: C₅₇H₉₂O₆ Formula Weight: 873.4

A melatonin metabolite first identified in rat brain that has antioxidant and free radical scavenging activities in several experimental models; may be measured in plasma as an index of melatonin synthesis and metabolism.

A major metabolite of sulforaphane that has been shown induce ARE-driven gene expression with roughly 8-fold less potency than sulforaphane.

A potent blocker of HCN channels that inhibits HCN4 more potently than HCN1 (IC₅₀s = 32 and 158 nM, respectively); modulates the sinoatrial node and slows heart rate; reduces neuropathic pain in several animal models.

A potent and selective inhibitor of Wip1 (IC₅₀ = 6 nM); increases phosphorylation of Wip1 substrates and blocks cell cycling in cancer cells; orally bioavailable, causing inhibition of lymphoma xenograft growth in mice.

An agonist for mCAR (EC₅₀ = 20 nM) that is effective for the mouse receptor but not for human or rat CAR receptors; potently induces cytochrome P450 monooxygenases and multidrug resistance and xenobiotic efflux proteins.

An indole-based SERM that binds to both ERα (IC₅₀ = 26 nM) and ERβ (IC₅₀ = 99 nM); antagonizes 17β-estradiol-dependent and hormone-independent growth of breast cancer cell proliferation (80% reduction with 10 nM) in a manner related to cell cycle arrest and…

A purine derivative that reversibly antagonizes aryl hydrocarbon receptor signaling (IC₅₀ = 127 nM in CD34+ cells); induces a 50-fold increase in human embryonic stem cells expressing CD34 (EC₅₀ = 120 nM) and a 17-fold increase in stem cells that retain the ability to engraft…

A protopanaxadiol that has diverse in vitro and in vivo effects, including cardioprotective, neuroprotective, and anti-inflammatory actions.

An LDH inhibitor (Kis = 5.46 and 15.06 µM, for the A and B isoforms, respectively) that prevents proliferation of many different cancer cells by blocking glycolysis and ATP production.

A potent lipid signaling molecule that exhibits a wide range of biological activities; it enhances cell growth and inhibits the normal apoptotic response to a variety of stimuli.

ACAT is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of ACAT with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide…

A natural isoflavone which acts as a phytoestrogen; stimulates the growth of estrogen-dependent breast cancer cells in vivo; promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover; increases bone formation in collagen matrix in vivo.

A natural nitroaryl-substituted polyketide that exhibits antitumor, antifungal, and insecticidal activities; non-competitive inhibitor NADH:ubiquinone oxidoreductase of bovine heart, N. crassa, and E. coli (IC₅₀s = 0.07, 0.08, and 22 nmol/mg protein, respectively).

A selective EP1 antagonist that inhibits PGE2 signaling in a guinea pig ileum muscle strip assay (pA2 = 8.1); demonstrates analgesic activity in a mouse writhing assay (ED50 = 0.9 mg/kg); potentiates the vasorelaxation of human pulmonary vein induced by PGE2 (EC50 = 7.75 µM).

An allosteric, reversible inhibitor of PAR1 on platelets, preventing surface expression of P-selectin induced by the peptide SFLLRN with an IC₅₀ value of 0.26 µM; also blocks platelet activation induced by thrombin but not by PMA, U-46619, or collagen.

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 sensitive fluorogenic elastase substrate that is selectively cleaved by elastase to yield Rhodamine 110, which can be analyzed with an excitation wavelength of 485 nm and emission wavelength of 525 nm.

A selective, reversible inhibitor of V-ATPases in mammalian, plant, or fungal cells with an IC₅₀ value in the 4-400 nM range; at 100 nM, the related bafilomycin A1 blocks V-ATPase-mediated acidification of lysosomes during autophagy, preventing protein degradation.

A verapamil derivative that dose-dependently blocks calcium uptake via Na+/Ca2+ exchange in diverse types of cells (Ki = 28 µM); also prevents calcium release from mitochondria induced by Ruthenium Red but not by uncouplers, respiratory inhibitors, or a chelating agent.

A cell-permeable inhibitor of Arp2/3 complex action that inhibits actin polymerization in vitro, using human, bovine and fission yeast proteins (IC₅₀s = 4, 32, and 24 µM, respectively); prevents the formation of actin filament comet tails by Listeria in infected SKOV3 cells…