A selective SIP1 agonist (EC₅₀ = 1.35 nM); activates S1P1-mediated p42/p44 MAPK phosphorylation in CHO-K1 cells transfected with S1P1 (EC₅₀ = 46 nM); induces S1P1-dependent lymphopenia in mice, decreasing B and T cells by 65 and 85%, respectively, at 50 nM.

An irreversible inhibitor of carnitine palmitoyltransferase 1, a mitochondrial enzyme involved in fatty acid β-oxidation (IC50 = 5-20 nM in rat liver); also acts as a direct agonist of PPARα.

A mycotoxin produced in food and animal feeds; activates estrogen receptors, alters hormone levels, and hasten pre-pubertal development; can cause uterine, rectal, and vaginal prolapse, abortion, and infertility in older animals.

A dietary flavonoid which has diverse physiological activities through both direct and indirect effects; directly binds ERα and ERβ, acting as an inverse agonist or agonist; acts as an antioxidant; suppresses signaling through certain receptor tyrosine kinases, including EGFR and HGF.

A potent and selective inhibitor of DGAT-1 (IC₅₀ = 19 nM); has high oral bioavailability (100%) in rats with a moderate half-life of 6.8 hours; significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.

A nucleoside analog with antiviral activity, inhibiting thymidine kinases from herpes simplex virus types 1 and 2 with Ki values of 0.14 and 0.95 µM, while blocking green monkey Vero cell thymidine kinase less effectively (Ki = 53 µM).

An HDAC inhibitor that increases histone H3 acetylation levels in LoVo and HT-29 colon cancer cells at concentrations as low as 4 µM; dose-dependently decreases the activation of several oncogenic signaling kinases and induces cell cycle arrest in colon cancer cells.

A selective inhibitor of NLRP3, blocking the release of IL-1β in macrophages primed with LPS and activated with ATP or nigericin (IC₅₀ = 7.5 nM); active in vivo, blocking the production of IL-1β and enhancing survival in mouse models of multiple sclerosis and…

An inhibitor of PLC-dependent processes by an undefined mechanism; inhibits platelet aggregation induced by collagen or thrombin with IC₅₀ values of 0.6 and 5 µM, respectively.

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 natural sesquiterpene that inhibits the proliferation of a wide range of tumors and enhances the effects of various chemotherapies; 10-40 µg/ml dose-dependently induces apoptosis and cell cycle arrest in the G2/M phase in HepG2 cells, upregulating Fas/FasL expression.

A potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC₅₀ = 70 nM), compared to PI3Kα (IC₅₀ = 240 nM), PI3Kβ (IC₅₀ = 1.45 μM), and PI3Kδ (IC₅₀ =1.70 μM); shows little or no activity against 38 other…

An activator of sGC, stimulating activity at concentrations as low as 10-100 nM; inhibits platelet aggregation (IC50 = 36 nM), induces relaxation of preconstricted aorta rings (IC50 = 304 nM); effective in vivo, decreasing mean arterial blood pressure in hypertensive rats.

An orally bioavailable, reversible inhibitor of JAK1 and JAK2 (IC₅₀s = 5.9 and 5.7 nM, respectively) that has been shown to inhibit cytokine-induced phosphorylation of STAT3 in healthy human volunteers.

An ATP/GTP-competitive inhibitor of CK2 (IC₅₀ = 900 µM for rat liver CK2); less potently inhibits CCK2/cyclin A, GSK3β, and phosphorylase kinase (IC₅₀ = 15.6, 11.2, and 8.7 mM, respectively); much less effective against a range of other kinases.

A non-nucleoside reverse transcriptase inhibitor that binds to viral reverse transcriptase and blocks polymerase activity by preventing RNA plus-strand initiation (IC₅₀s = ~ 0.45 to 0.9 μM).

A fatty acid amide from T. titanicus that at 0.1 μg/ml protects against ER stress-dependent cell death in Neuro2a cells induced by tunicamycin.

A cell-permeable inhibitor of JMJD2E (KDM4DL; IC₅₀ = 920 nM); reduces the expression of immediate early genes of HSV (IC₅₀ = ~10 µM) and hCMV, blocks viral infection, and suppresses the level of viral reactivation in a ganglia explant model of latently infected mice.

A lipoic acid analog that inhibits α-ketoglutarate dehydrogenase, particularly in tumor cells; induces a strong mitochondrial burst of reactive oxygen species at 60-240 µM, resulting in cell death; demonstrates both in vitro and in vivo anti-tumor activity.

A non-symmetrically substituted indolylmaleimide that increases β-catenin levels by inhibiting GSK3β (IC₅₀ = 53 nM); reduces proliferation and increases differentiation of a ReNCell VM cell line derived from human ventral midbrain.

Selectively inhibits MEK1/2; potently inhibits growth and survival of human INA-6 multiple myeloma cells and cytokine-induced osteoclast differentiation (IC50s = 10 and 18.2 nM, respectively); 30 mg/kg reduced tumor growth significantly in mice bearing H929 MM xenografts.

A dual antagonist of TP and EP4 receptors; inhibits TxA2-induced platelet aggregation (IC₅₀ = 0.26 μM) and bronchial smooth muscle contraction; impairs PGE2-mediated relaxation of piglet saphenous vein, suppresses serum-induced proliferation of fibroblasts, and reduces metastasis in a…

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 reversible inhibitor of serine proteases such as trypsin (Ki = 0.06 pM), chymotrypsin (Ki = 9.5 nM), and kallikrein (Ki = 0.8 nM); widely used as a protein purification tool to prevent proteases present in tissue samples from degrading the protein of interest.

An aminopyridazine derivative that acts as a GABAA receptor antagonist that can be used as an intermediate in the synthesis of SR 95531.

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.

An intravenous β-lactam antibiotic that is effective against Gram-positive and Gram-negative bacteria (MICs range from 0.008-0.13 µg/ml); highly resistant to degradation by β-lactamases.

A specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.

A skeletal muscle relaxant that has applications in reducing muscle spasm, limitations in normal motion, and pain caused by musculoskeletal conditions.

A water-soluble receptor antagonist which targets both AMPA- and kainate-sensitive glutamate receptors (IC₅₀ = 0.15 and 4.8 µM, respectively); does not block the NMDA-sensitive glutamate receptor (IC₅₀ = ≥ 90 µM).

A derivative of glucose used to study carbohydrate metabolism, particularly in the identification, differentiation, and characterization of α-phosphoglucomutase, β-phosphoglucomutase, and α- and β-hexoglucomutases.

An inhibitor of p300 histone acetyltransferase (KAT3B; IC₅₀ = 1.98 µM in vitro); blocks acetylation of histones and p53 in cells treated with trichostatin A or etoposide, respectively, and reduces STAT3 phosphorylation.