A selective small molecule activator of SIRT1 that is 1,000-fold more potent than resveratrol; improves insulin sensitivity, lowers plasma, glucose and increases mitochondrial capacity in diet-induced obese and diabetic leptin-deficient ob/ob mice after one week of treatment with an oral dose of…

A microbial metabolite that binds the TCR on Vγ9Vδ2 peripheral blood lymphocytes with high affinity (EC50 = 0.39 nM); induces the expansion of human memory Vγ9Vδ2 T cells.

A potent and selective inhibitor of PLD1, both in vitro (IC₅₀ = 46 nM) and in cells (IC₅₀ = 11 nM); also effective as a PLD2 inhibitor at higher concentrations (IC₅₀ = 933 nM in vitro; 1,800 nM in cells); strongly inhibits the invasive migration of several breast…

An enantiomer of C75, which in racemic form is a stable FAS inhibitor that when administered leads to profound weight loss and feeding inhibition in both high-fat diet wild type obese and leptin-deficient ob/ob mice.

A synthetic analog of natural PtdIns featuring C8:0 fatty acids at the sn-1 and sn-2 positions; contains the same inositol and DAG stereochemistry as the natural compound.

Largely acts a cell signaling intermediate; serving as substrate to produce IP5s, which can be further phosphorylated to produce Ins(1,2,3,4,5,6-)P6; also phosphorylated to produce phytic acid, which serves diverse roles in eukaryotic tissues; a poor activator of the Ins(1,4,5)-P3 receptor in vitro.

A competitive inhibitor of CBX7 chromodomain binding to H3K27me3 (Ki = 43 µM); derepresses transcription of the polycomb repressive complex target gene p16/CDKN2A in prostate cancer cells at 250 µM.

Formal Name: 3,4-dichloro-N-(1-methylbutyl)-benzamide CAS Number: 7497-07-6 Molecular Formula: C₁₂H₁₅Cl₂NO

An active metabolite of propranolol, inhibiting β1- and β2-adrenergic receptors with KD values of 2.4 and 5.8 nM, respectively; comparable to propranolol in potency in antagonizing the effects of isoprenaline on heart rate and blood pressure in cats and dogs.

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 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.

An inhibitor of ALK5, ALK4, and ALK7 (IC₅₀s = 12, 45, and 7.5 nM, respectively); blocks the phosphorylation of Smad2/3 and inhibits TGF-β-induced epithelial-to-mesenchymal transition; used to reprogram fibroblasts into alternative lineages.

A cell-permeable derivative of 2-HG.

An AM ester of the red fluorescent calcium indicator rhod-2; accumulates within mitochondria.

RD162 is a second-generation androgen receptor (AR) antagonist. It inhibits binding of 18 F-FDHT to AR in human prostate cancer cells with an IC₅₀ value of 30.9 nM. RD162 completely suppresses VCaP cell proliferation at 1 µM and induces apoptosis of VCaP cells at 10 µM.…

A selective inhibitor of TAF1 bromodomain 2 (Kd = 1.8 µM; IC₅₀ = 0.9 µM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.

An analog of suramin that selectively inhibits P2X1 receptors (pIC50 = 6.3); selectively antagonizes the Gsα-subunit G protein, which suppresses the association rate of GTPγS binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks G protein coupling to…

A cell-permeable, reversible inhibitor of a mitochrondrial glutaminase splice variant, glutaminase C (IC₅₀ = ~2.5 µM), which is commonly found in cancer cells; blocks transformation induced by Rho GTPases and inhibits the proliferation of cancer cell lines without affecting normal cells.

A non-nucleoside pyridopyrimidine compound that selectively blocks the action of adenosine kinase in an adenosine-competitive manner (IC₅₀ = 1.7 nM in cell-free assays); suppresses nociception in various rodent pain models.

A Gcn5 and pCAF HAT inhibitor.

TXA2 receptor agonist; causes platelet shape change (EC₅₀ ~6 nM) and aggregation (EC₅₀ ~97 nM).

An analog of (−)-blebbistatin that is stable to prolonged irradiation at 450-490 nm and has been successfully used in fluorescent live cell imaging.

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

CWHM12 is an analog of RGD peptide (Item No. 14501), a tripeptide that inhibits integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation. CWHM12 selectively inhibits αv integrins (IC₅₀s = 1.8, 0.8, 61, 1.5, and 0.2 nM for…

Formal Name: N-[(1S)-2-hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]-urea CAS Number: 928320-12-1 Molecular Formula: C₂₀H₁₉N₃O₂

A potent, selective antagonist of TRPV4 channels, blocking the influx of calcium induced by the TRPV4 agonist GSK634775 with IC₅₀ values of 2, 5, and 40 nM for rat, mouse, and human isoforms, respectively; effective in vivo, as it resolves pulmonary edema resulting from myocardial…

A small molecule inhibitor of tankyrase 1 and 2 (IC₅₀ = 11 and 4 nM, respectively); increases the protein levels of the axin-GSK3β complex and promotes the degradation of β-catenin; inhibits colony formation of APC-deficient colorectal cancer cells at 0.33 µM.

PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral/antitumor activity. At a 25 µM concentration, PGA2 blocks the cell…

A potent, selective inhibitor of aldose reductase (IC₅₀ = 47 nM in vitro) used to improve the cytotoxic effects certain anticancer agents; inhibits PGF2α and PGE2 production in human endometrial cells (EC₅₀ = 10 μM).

A prenylflavonoid with potent estrogenic activity that inhibits both ERα and ERβ (IC₅₀s = 57 and 68 nM, respectively); effective in vivo, suppressing bone loss and temperature changes in rat models of osteoporosis and postmenopausal hot flashes.

A selective and competitive inhibitor of NAD+-dependent type-I 15-PGDH (IC₅₀ = 26.4 nM; Ki = 5 nM).

A potent, selective, and orally bioavailable inhibitor of PRMT5 (Ki = 5 nM); blocks the growth of mantle cell lymphoma Z-138 xenografts, without significant body weight loss, in mice.