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 HSL compound produced in the marine bioluminescence bacterium V. fischeri.

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…

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

A competitive antagonist of muscarinic receptors that potently blocks signaling through M1, M2, and M3 (Kis = 25, 125, and 10 nM, respectively), resulting in muscle relaxation.

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.

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 broad spectrum, orally available kinase inhibitor that targets primarily tyrosine kinases, including VEGFR and EGFR, with IC₅₀ values in the nanomolar range; also potently blocks non-receptor tyrosine kinases, including ABL, RET, and SRC, as well as several serine/threonine kinases.

A natural isoflavone which is biotransformed by intestinal bacteria to give the phytoestrogens daidzein and equol, resulting in antithrombotic, antiallergic, and other salutary effects; modulates serotonin receptors when given intraperitoneally; suppresses LPS-mediated activation of NF-κB in…

A receptor antagonist acting at the muscarinic receptors (Ki = 5.5, 47, 0.84, 8.6, and 2.3 nM for M1 through M5, respectively); effective in treating problems related to the lower urinary tract.

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.

An antibacterial and coccidiostat compound that shows selective toxicity for HMLER breast cancer stem cells (IC₅₀ = ~24 μM); 8 μM treatment of 4T1 and MCF-7-Ras breast cancer cell lines decreases cancer stem cell growth ~2-fold and ~3-fold, respectively; 5 mg/kg inhibits mammary…

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.

A quinone which inhibits topoisomerase I at 25 μM and transglutaminase (IC₅₀ = 5 μM); reduced to β-lapachone hydroquinone by NQO1, generating ROS during its reversion to β-lapachone; sensitizes cancer cells to radiation, suppresses NF-κB activation, and drives apoptosis.

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).