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.

Formal Name: 6-amino-1,4-dihydro-1,3-dimethyl-4-[4-(trifluoromethyl)phenyl]-pyrano[2,3-c]pyrazole-5-carbonitrile CAS Number: 1637739-82-2 Molecular Formula: C₁₆H₁₃F₃N₄O Formula Weight: 334.3

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

A natural isoflavone which acts as a phytoestrogen; stimulates the growth of estrogen-dependent breast cancer cells in vivo; promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover; increases bone formation in collagen matrix in vivo.

Binds avidly and selectively to the structurally-similar bromodomains of SMARCA4 and PB1(domain 5) with Kd values of 89 and 48 nM, respectively; also interacts with the bromodomain of SMARCA2; does not interact with other bromodomains or with a panel of kinases.

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.

A potent inhibitor of chymotrypsin and chymase (Ki = 9.36 and 13.1 nM, respectively), that less effectively blocks the activity of cathepsins, papain, and leukocyte elastase.

A positive allosteric modulator of the M1 mAChR; dose-dependently reduces the concentration of acetylcholine required to activate M1; the effective range for potentiation is 0.1 to 100 μM with 3 nM acetylcholine; restores impairment in reversal learning in a mouse model of Alzheimer’s disease.

A flavonoid isolated from the root of the traditional Chinese herb S. baicalensis with anti-inflammatory, antioxidant, antitumor, and neuroprotective activities at concentrations from 5-75 μM.

A potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO₃- secretion in the stomach.

A cell-permeable ACL inhibitor (IC₅₀ = 0.13 µM) that has been reported to reduce weight gain and lower plasma cholesterol, triglycerides, and glucose in a mouse model of hyperlipidemia.

A synthetic adrenal hormone, an androstanediol analog, that acts as an androgen receptor antagonist; inhibits androstenediol-dependent LNCaP cell tumor growth both in vitro (IC₅₀ = 6 nM) and in vivo.

A nonpurine inhibitor of xanthine oxidoreductase (Ki = 0.7 nM) that has proven effective in lowering serum urate levels when administered to manage hyperuricemia in patients with gout.

A form of PS that contains the abundant long-chain (16:0) palmitic acid inserted at the sn-1 and sn-2 positions; commonly used in the generation of liposomes and other types of artificial membranes.

CAS Number: 883986-34-3 Molecular Formula: C₂₄H₂₅N₅O₄ Formula Weight: 447.5

A side-chain substituted oxysterol derived from dietary cholesterol that inhibits the cleavage of SREBPs; has been implicated in a variety of metabolic events including cholesterol homeostasis and atherosclerosis as well as antitumor and immunomodulating activities.

CB-5083 is an orally bioavailable inhibitor of p97 (IC₅₀ = 11 nM), a transitional endoplasmic reticulum ATPase also known as valosin-containing protein (VCP). It disrupts cellular protein homeostasis and demonstrates anti-tumor activity in hematological and solid tumor models. CB-5083…

An inhibitor of the HATs p300 and pCAF (IC50 = 7 and 5 μM, respectively) that also inhibits the HAT Gcn5; promotes neurogenesis and ex vivo expansion of human hematopoietic stem cells; induces apoptosis in several types of cancer cells and has anti-inflammatory actions.

An activated fluorescent molecule (excitation: 494 nm, emission: 519 nm) used for labeling proteins; reacts optimally with sulfhydryl groups on cysteine side chains at pH 7, forming a stable thioether bond.

A potent activator of KCNQ1 (Kv7.1) channels (EC₅₀ = 260 nM); EC₅₀ > 30 µM for KCNQ2, KCNQ4, and hERG; potentiates both homomultimeric KCNQ1 channels and unsaturated heteromultimeric (KCNQ1/KCNE1) channels in model cardiomyocytes and augments IKs current in cultured…

A selective serotonin reuptake inhibitor (Ki = 6.2 nM in rat hypothalamus) with comparatively little effect on noradrenaline reuptake (Ki = 1,100 nM); potentiates the pharmacological effects of serotonin and its precursor, 5-hydroxy tryptophan, in the CNS resulting in antidepressant effects.

A cell-permeable, potent inhibitor of both SHP-1 and SHP-2 (IC₅₀ = 355 and 318 nM, respectively); much less effective against other protein tyrosine phosphatases and DUSP26.

An immune response modifier that acts as a ligand of TLR7 and 8; demonstrates potent anti-tumor and anti-viral properties and has been used to study the innate immune response to viral infections.

A potent, reversible, ATP-competitive, and selective inhibitor of the Src family of protein tyrosine kinases: p56lck (IC₅₀ = 4 nM), p59fynT (IC₅₀ = 5 nM), Hck (IC₅₀ = 5 nM).

Formal Name: N-[(1S)-2-hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]-urea CAS Number: 928320-12-1 Molecular Formula: C₂₀H₁₉N₃O₂

CAS Number: 1000998-59-3 Molecular Formula: C₂₂H₂₁ClN₂O₆ Formula Weight: 444.9

An orally active inhibitor of PI3Kg that suppresses joint inflammation in mouse models of rheumatoid arthritis; inhibits human recombinant PI3Kg, a, b, and d in an ATP-competitive manner with IC50 values of 8, 60, 270, and 300 nM, respectively.

A naturally occurring agonist for the nuclear receptor Nur77 (IC₅₀ = 0.278 nM); induces apoptosis in cancer cells and retards xenograft tumor growth; induces genes related to gluconeogenesis and decreases atherosclerosis progression in mice fed a high fat/high cholesterol diet.

An apigenin flavone C-glycoside isolated from various tropical plant species that demonstrates broad antioxidant, anti-inflammatory, anticancer, and antinociceptive activities.

WS3 is a non-specific proliferative molecule that modulates the activity of Erb3 binding protein-1 and the IκB kinase pathway. It has been used to mediate proliferation of primary retinal pigment epithelial cells ex vivo in order to provide a renewable source of cells for transplantation in a…

An N-cyanosulphonamide that selectively blocks the sodium/bicarbonate cotransporter (NBC, also known as SLC4A7) with a Ki value of 1.7 µM, with full inhibition occurring at ~30 µM in myocytes; prevents changes in pH associated with depolarization and hyperpolarization of ventricular myocytes.

Myriocin is an amino fatty acid antibiotic derived from certain thermophylic fungi, in this case Mycelia sterilia. It is a potent immunosuppressant having 10- to 100-fold more activity than cyclosporin A. Myriocin is a potent inhibitor of serine palmitoyltransferase (Ki = 0.28 nM), the enzyme that…