Selectively inhibits ALK1 (IC₅₀ = 46 nM) and ALK2 (IC₅₀ = 32 nM) with >300-fold selectivity over ALK3, ALK6, and VEGF type 2 receptor; inhibits BMP4 signaling with an IC₅₀ value of 152 nM in a functional assay.

Initiates glycogen synthesis in hepatocytes by causing inactivation of phosphorylase a and activation of glycogen synthase a (maximal effects with ~20 µM Itu); potent inhibitor of ERK2 (Ki = 525 nM).

A potent, selective chemical probe for the methyl lysine reading function of L3MBTL3 (Kd = 120 nM; IC₅₀ = 40 nM) that competitively displaces mono- or dimethyl-lysine containing peptides.

A analog of tenovin-1; elevates p53 activity in MCF-7 cells at 10 µM and reduces growth of ARN8 melanoma xenograft tumors in SCID mice at a dose of 50 mg/kg.

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 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 colchicine derivative that inhibits tubulin polymerization (IC₅₀ = 2.1 μM) with low toxicity; suppresses microtubule dynamicity, inhibits cell migration, blocks microtubule assembly, and arrests cells in metaphase; used to synchronize cells and for karyotyping in cytogenetic studies.

A selective slow off-rate inhibitor of Raf kinases (IC₅₀s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively); shows significant antiproliferative activity against mutated BRAF or mutated NRAS cancer cell lines and xenograft models.

A mammalian pheromone used to prime sexual behavior of sows in estrus for mating or artificial insemination; also used to study receptor-mediated odorant detection and the genetic basis for anosmias.

15(S)-15-methyl PGF2α methyl ester is a derivative of 15(S)-15-methyl PGF2α with increased membrane permeability. Hydrolysis of the methyl ester in vivo releases the biologically active 15(S)-15-methyl PGF2α, which is a potent uterine stimulant and abortifacient.

A non-selective bromodomain inhibitor that at 1 µM has been shown to accelerate FRAP recovery of BRD4 and CREBBP bromodomains in HeLa cells.

A selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC₅₀ = 0.04-0.28 µM) over BD1 (IC₅₀ = 1.8-3.1 µM), which causes selective release of BET proteins from chromatin; increases the expression of ApoA1 and reduces…

11β-PGE2 is the C-11 epimer of PGE2. It is a moderate inhibitor of PGE2 binding to rat hypothalamic membranes with a Ki value of 53 nM. 11β-PGE2 also stimulates bone resorption in rats at concentrations of 10-8 to 10-6 M which is similar to PGE2. 11β-PGE2 inhibits PGE2 binding to the…

A non-cholestatic regioisomer of E217G that acts as a substrate for MRP2, competing with E217G for MRP2-mediated transport (IC₅₀ = 14.2 µM).

A competitive inhibitor of nucleotide binding by Ras-related GTPases; binds Rab7 (Ki = 13 nM), preventing BODIPY-linked GTP and GDP binding with EC₅₀ values of 11.2 and 21 nM, respectively.

A potential metabolite of bimatoprost when administered to animals; potential minor impurity in commercial preparations of bimatoprost.

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…

An endogenous, maturation-inducing steroid that at 1 µg/ml induces germinal vesicle breakdown in oocytes from several teleost species; can also influence spermiation by stimulating milt production when administered at 5 mg/kg to various male teleosts.

A PKCα and PKCβ1 inhibitor with IC₅₀ values of 2.3 and 6.2 nM, respectively; also inhibits the checkpoint kinases Chk1/2 and abrogates DNA damage-induced cell cycle arrest, leading to cytotoxicity in p53 mutant tumor cells.

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

A metabolite of estradiol 3-sulfate that has been modified by a UDP-glucuronosyltransferase; enhances utilization by anion transporters, most commonly leading to excretion in urine and bile.

A phosphonic analog of ATP and agonist of P2X1 and P2X3 (EC50 = ~1 µM); ~1,000-fold less potent at P2X2, P2X receptors 4-7, and P2Y receptors; used as a stable analog of ATP to study the interaction of ATP with kinases and other proteins.

8-iso-17-phenyl PGF2β is an isomer of bimatoprost (free acid) that is epimerized at the 8 and 9 positions. There are no published reports on the biological activity of 8-iso-17-phenyl PGF2β.

A hepatic metabolite of zearalenone that is a less potent agonist of estrogen receptors than the parent compound.

A homolog of EPEA, characterized by the addition of an (R)-α-methyl group at the methylene carbon adjacent to the amide nitrogen.

A mycotoxin produced from F. moniliforme that functions as an inhibitor of ceramide synthase (sphingosine N-acyltransferase).

A resorcylic acid lactone with antiviral and antiprotozoan activity; used as negative control for MAPKKK inhibitor (5Z)-7-oxo zeaenol (Item No. 17459).

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.

6-keto prostaglandin F_1α (6-keto PGF_1α) is the inactive, non-enzymatic hydrolysis product of PGI₂. 6-keto PGF_1α serves as a useful marker of PGI₂ biosynthesis in vivo. When [ 3 H]-PGI₂ is injected into healthy human…

A potent inhibitor of PI3K isoforms α, δ, and γ (IC₅₀s = 0.28, 0.12, and 0.97 nM, respectively) that is 31 times less potent at PI3Kβ; has increased potency in cancer cell lines harboring PIK3CA-activating alterations, and is effective in vivo.

An inhibitor of CETP; inhibits plasma CETP with an IC₅₀ value of 9 µM; in rabbits given an atherogenic diet, increases HDL, decreases VLDL, and attenuates induced atherosclerosis; in humans, inhibits CETP activity and increases HDL levels but does not reduce the risk of recurrent…

A dihydropteridinone that inhibits Plk1, Plk2, and Plk3 (IC₅₀s = 0.87, 5, and 56 nM, respectively), inducing mitotic arrest and apoptosis; inhibits proliferation of multiple cancer cell lines (EC₅₀s = 11-37 nM) and prevents the growth of various human carcinoma xenografts in mice.