An extract from A. lappa, a burdock plant traditionally used in Japanese Kampo medicine for its antioxidant, anti-inflammatory, antiproliferative, and antiviral activity.

A sulfonyl hydrazide that inhibits BCATc (IC₅₀s = 0.81 and 0.2 µM in human and rat, respectively) with 15-fold selectivity over BCATm; blocks calcium influx into neurons (IC₅₀ = 4.8 µM) following inhibition of glutamate uptake and demonstrates neuroprotective…

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.

An endogenous CB neurotransmitter that binds to both CB1 and CB2 receptors.

A selective IGF-1R inhibitor (IC₅₀ = 0.17 µM); inhibits tumor proliferation both in vitro and in a mouse model of multiple myeloma.

A non-steroidal androgen receptor antagonist (IC50 = 36 nM); reduces the efficiency of nuclear translocation of the androgen receptor and impairs both its binding to DNA and the recruitment of coactivators.

An organic polysulfide compound found in garlic that acts as an H2S donor; reduces the survival of prostate cancer PC-3 cells (IC50 = 22 μM) and inhibits the growth of human colon adenocarcinoma HCT15 cells (IC50 = 11.5 μM); suppresses the growth of PC-3 xenografts in vivo in mice and induces…

GSK2606414 is an orally available, selective protein kinase R-like ER kinase (PERK) inhibitor with an IC₅₀ value of 0.4 nM. It can inhibit thapsigargin-induced PERK phosphorylation in lung carcinoma A549 cells and attenuates subcutaneous pancreatic human tumor xenograft growth in mice.…

A melatonin metabolite first identified in rat brain that has antioxidant and free radical scavenging activities in several experimental models; may be measured in plasma as an index of melatonin synthesis and metabolism.

The racemic version of the selective NMDA receptor antagonist, D-AP5 that competitively inhibits the glutamate binding site of NMDA receptors (Kd = 1.4 μM); D-AP5 is the active (−)-stereoisomer, while L-AP5, the(+)-isomer, demonstrates considerably less potent NMDA receptor antagonist activity.

A prodrug that is metabolized in vivo to RNH-6270, a nonpeptide angiotensin II antagonist that potently inhibits angiotensin binding to the AT1 receptor (IC50 = 7.7 nM) without affecting binding to the AT2 receptor; reduces blood pressure.

A naturally-occurring dimethyl ether analog of resveratrol; acts as a powerful antioxidant, suppresses the synthesis of PGE2 from LPS-stimulated human peripheral blood mononuclear cells (IC₅₀ = 1.0 μM), and inhibits cell proliferation (IC₅₀ = ~60 μM); evokes effects that…

An N-hydroxysuccinimide ester of the nitroxide spin label tempyo; an active acylating agent that preferentially targets α-amino groups, used to spin label proteins and aminoacylated RNA species.

A fluorescent probe that can react with ONOO-, HOCl, and H2O2 in a similar manner to CBA, yet is formulated for improved solubility.

The Rho family of GTPases regulates diverse signal transduction pathways. One member, the cell division control protein 42 homolog (Cdc42), is involved in filopodia function, cell polarity, cell cycling, and other processes. CASIN is an indole-based small molecule that inhibits activation of the…

A structural analog of sphingosine and a novel immune modulator; inhibits lymphocyte emigration from lymphoid organs; becomes phosphorylated by sphingosine kinase in vivo to act as a potent agonist at S1P1, S1P3, S1P4, and S1P5.

A fluorescent indicator of peroxynitrite formation; neither NO, superoxide, nor hydrogen peroxide alone appear to oxidize DCFH.

A potent inhibitor of kynurenine 3-hydroxylase (IC₅₀ = 37 nM), preventing the conversion of kynurenine to 3-hydroxy kynurenine; reduces ischemia-mediated neuronal damage in tissues; can be used in vivo by direct injection.

A potent, cell-permeable inhibitor of all JAK isoforms (IC50 = 6.1, 12, and 8.0 nM for JAK1, JAK2, and JAK3, respectively); useful in ameliorating inflammatory or autoimmune components of a host of diseases.

An ATP-competitive inhibitor of JAK1 and JAK2 (IC₅₀s = 11 and 18 nM, respectively); causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines; is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms.

An HNF4α antagonist that can repress the expression of known HNF4α target genes, inhibiting endogenous insulin expression in vitro (IC50 = 930 nM).

An ERβ Selective agonist; exhibits 70-fold higher relative binding affinity for ERβ versus ERα.

A major metabolite of histamine used as a biomarker of histaminergic system activity.

A catatoxic steroid that acts as an agonist of the rodent PXR at µM concentrations; mediates induction of hepatic CYP3A, Oatp2, and Cyp7a1, regulating both xenobiotic and bile acid homeostasis.

A substrate for the synthesis of RNA during the transcription process and the synthesis of DNA during DNA replication; participates in G-protein-related signal transduction where it is converted to GDP through the action of GTPases.

A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd value of 43 nM.

A potent ATP-competitive inhibitor of ATM kinase (IC₅₀ = 13 nM; Ki = 2.2 nM); sensitizes cells to both ionizing radiation and chemotherapeutic agents; induces senescent breast, lung, and colon carcinoma cells to undergo cell death; inhibits HIV-1 replication in C8166 human T-lymophocyte…

Unoprostone isopropyl ester (Rescula) is the clinically approved, prodrug form of unoprostone, which is a free acid analog of PGF2α. Both latanoprost and Rescula have been approved for the treatment of ocular hypertension. Both analogs of PGF2α are believed to act by increasing the rate…

Carboxy-PTIO is a NO scavenger. It reacts stoichiometrically with NO and can be used for EPR detection of NO.

An inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC₅₀ value of 15-25 µM.

A reversible and competitive inhibitor of type IV collagen-specific MMP-2 and MMP-9 with preference towards MMP-2 (IC50 = 4 and 20 µM, respectively).

A selective inhibitor of PI3Kγ