A cell-permeable, fluorescent probe for DNA that is useful as a marker of nuclei for cell cycle studies in combination with BrdU and to distinguish nuclear morphology in apoptotic cells.

A metabolite of vinclozolin, a dicarboximide fungicide, that acts as an effective antagonist of the androgen receptor (Ki = 9.7 µM in rat).

An aminopyrimidine derivative that inhibits GSK3α and GSK3β (IC50s = 10 and 6.7 nM, respectively); activates glycogen synthesis in CHO-IR cells (EC50 = 0.8 μM) and in isolated type 1 diabetic rat skeletal muscle; has been shown to promote self-renewal of embryonic stem cells.

A prodrug for A-771726 that regulates T lymphocyte progression through the cell cycle by selectively inhibiting de novo pyrimidine synthesis; used to slow the disease progression of rheumatoid arthritis and as an immunosuppressive agent to prevent rejection of transplant allografts and xenografts.

A competitive, non-NMDA glutamate receptor antagonist (IC₅₀s = 0.3 and 1.5 μM for AMPA and kainate receptors, respectively, versus IC₅₀ = 25 μM for NMDA receptors).

An analog of trimethoxy resveratrol; inhibits the growth of a variety of human tumor cell lines at concentrations form 0.4 to 2 µg/ml, which is 5-6 times more potent than resveratrol

SC-560 is a member of the diaryl heterocycle class of COX inhibitors which includes celecoxib (Celebrex™) and rofecoxib (Vioxx™). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC₅₀ value for…

CAS Number: 444932-31-4 Molecular Formula: C₂₀H₁₉N₃O₄ Formula Weight: 365.4

A naturally-occurring but uncommon form of sphingosine, accounting for approximately 13% of the sphingosine in human skin; can be phosphorylated by sphingosine kinases to produce C-17 sphingosine-1-phosphate.

An imidazole that potently antagonizes the α2-adrenoceptor (Ki = 1.6 nM); shows selectivity over the α1-adrenoceptor (Ki = 13,300 nM) and is a poor antagonist at a wide variety of other receptors and channels.

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 2' deoxy analog of 5-azacytidine which is incorporated into DNA and causes hypomethylation by inhibiting DNA methyltransferases in a concentration-dependent manner; useful in conditions characterized by DNA hypermethylation, as is found in myelodysplastic syndromes.

A metabolite produced during GCDH deficiency and used as a biomarker of glutaric acidemia type 1.

A CYP450 metabolite of estradiol with low affinity for estrogen receptors; rapidly metabolized to 2-ME2 with a half-life of approximately ten minutes in rat.

A major phase I metabolite of tamoxifen, a well-known estrogen receptor antagonist in breast but partial estrogen receptor agonist in endometrium; has at least a 100-fold higher affinity for estrogen receptors than tamoxifen.

A selective inhibitor of STAT3 activation, dimerization and nuclear translocation (IC₅₀ = 5.1 μM at 37°C); 10 μM induces apoptosis in STAT3-dependent breast cancer cells.

A small molecule that stimulates the expression of PGC-1α and downstream genes in skeletal muscle cells, improving glucose utilization and fatty acid oxidation at a concentration of 20 μM; 15 mg/kg/day administered to diabetic db/db mice improved glucose tolerance, pyruvate tolerance, and…

A selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC₅₀s = 65 and 73 nM for mouse and human, respectively) that demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC₅₀s = 0.92 and 1.04 µM for mouse…

8-hydroxy Guanine is produced by oxidative damage of DNA or RNA by reactive oxygen and nitrogen species, including hydroxyl radical and peroxynitrite. It serves as a measure of oxidative stress in biological systems.

A less potent IWP-2 derivative that has been used to determine which structural features of IWP-2 are essential for impairing Wnt/ β-catenin pathway activity.

A selective, nonpeptide AT2R antagonist (IC₅₀ = 5.6 nM vs. 100 nM for AT1R) that has been used to selectively examine the specific roles for AT1R and AT2R in hypertensive and other vascular research-related models.

An irreversible, mechanism-based inhibitor of LSD1 (IC₅₀ = 16 nM); induces gene expression changes in various cancer cell lines, inhibiting their proliferation (EC₅₀s <5 nM).

A GABAA receptor agonist whose potency varies depending on the receptor subunit composition (partial agonist at α1β2γ2 (ED50 = 143 µM), full agonist at α5 (ED50 = 28-129 µM), and super agonist at α4β3δ (ED50 = 6 µM)); acts as an antagonist…

A conjugate of biotin and lysine used for derivatization or conjugation to proteins and other molecules with a medium-chain length spacer; also used as an anterograde, retrograde, or intracellular neuroanatomical tracer that is fixable with aldehyde-based fixatives.

A small molecule inhibitor of JAK2 (IC₅₀ = 6 nM) and the related kinases FLT3 (IC₅₀ = 25 nM) and RET (IC₅₀ = 17 nM) with significantly less potent activity against JAK3 (IC₅₀ = 169 nM); inhibits the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L…

Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of sPLA2. The IC₅₀ value for thioetheramide-PC is 2 µM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, thioetheramide-PC…

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.

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.

A selective non-peptide agonist of the δ-opioid receptor (Ki = 0.18 nM, IC₅₀ = 2.73 nM) that is over 2,000-fold less effective at the μ-opioid receptor; effectively activates µ/δ receptor heteromers (EC₅₀ = 52.8 nM) but not κ/δ or μ/κ heteromers.

A mixture of moenomycins A, A12, C1, C3 and C4, which are antibiotics isolated from several strains of Streptomyces that directly inhibit bacterial peptidoglycan glycosyltransferases; minimal inhibitory concentration of moenomycin A against various Gram-positive bacteria ranges from 1-100 nM.

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.

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.…