Cayman Chemical

Epoxyeicosatrienoic acid (EpETrE; EET) metabolites of arachidonic acid such as 11(12)-EET and 14(15)-EET have been identified as endothelium derived hyperpolarizing factors with vasodilator activity. Soluble epoxide hydrolase (sEH) catalyzes the conversion of EETs to the corresponding dihydroxy...

A selective FLT3 inhibitor (Kd = 1.6 nM) that inhibits the proliferation of MV4-11 cells both in vitro (IC₅₀ = 0.56 nM) and in in vivo mouse models of FLT3-ITD acute myeloid leukemia.

A tetrachloro indandione that acts as a potent inhibitor of UCH-L3 and demonstrates 125-fold selectivity over UCH-L1 (IC₅₀s = 0.6 and 75 µM, respectively).

A selective antagonist of NMDA receptors that contain NR2B subunits (IC₅₀ = 0.3 µM) with 150-fold weaker activity at those bearing NR2C or NR2D subunits; also acts as a potent ligand at receptors for σ1, emopamil binding proteins, and their σ-like, fungal counterpart...

A structural analog of capsaicin, which is the noxious active component of hot peppers of the Capsicum genus, and the amide of vanillylamine and oleic acid; acts as an agonist at TRPV1, inducing desensitization analgesia in rat and mouse models of pain; potentiates the agonist activity of endogenous...

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.

Dampens excessive neutrophil trafficking to sites of inflammation; reduces neutrophil infiltration by 70% at doses as low as 10 pg per mouse and significantly reduces leukocyte adherence and emigration at 1 nM.

Applications: (+) FC, IF, and WB

β-Hydroxybutyrate (β-HB; 3-hydroxybutyric acid) is produced in the liver, mainly from the oxidation of fatty acids, and exported to peripheral tissues for use as an energy source. Measurement of β-HB can provide a reliable index of the level of normal ketosis as well as detect...

(±)8-HDHA is an autoxidation product of DHA in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. (±)8-HDHA is a potential marker of oxidative stress in brain and retina where DHA is an abundant PUFA.

An intermediate in the synthesis of dasatinib.

A potent, selective inhibitor of FGFR tyrosine kinase activity, blocking autophosphorylation of FGFR1 (IC₅₀ = 21.5 nM); impairs angiogenesis, as well as self-renewal of stem cells via ERK1/2 activation.

A negative allosteric modulator of the mGlu5a receptor subtype (Ki = 42 nM; IC₅₀ = 110 nM); produces antidepressant, and anxiolytic effects.

Inhibits glycolysis though the inactivation of mitochondria-bound hexokinase; decreases oxygen consumption as well as aerobic and anaerobic glycolysis in Ehrlich ascites tumor cells (IC₅₀s = 90 and 45 μM, respectively).

Source: recombinant N-terminal hexahistidine-tagged protein expressed in E. coli Mr: 18.3 kDa

13,14-dihydro PGE1 is a biologically active metabolite of PGE1 with comparable potency to the parent compound. It is an inhibitor of ADP-induced platelet aggregation in human PRP and washed platelets with IC50 values of 31 and 21 nM, respectively. 13,14-dihydro PGE1 is a slightly more potent...

A thioester substrate analog of 2-AG that can be utilized for the measurement of MAGL activity; hydrolysis of the thioester bond by MAGL generates a free thiol that reacts rapidly with the chromogenic reagent DTNB resulting in a yellow product with an absorbance maximum at 412 nm.

A potent inhibitor of TNKS1 and TNKS2 (IC₅₀s = 6 and 72 nM, respectively); inhibits signaling along the Wnt/β-catenin pathway in a cell-based reporter assay.

A natural demethoxy derivative of curcumin; activates macrophage phagocytosis and, with 1α,25-dihydroxyvitamin D3, stimulates amyloid-β clearance by macrophages (optimal stimulation at 100 nM BDMC); suppresses proliferation in cancer cells; down-regulates p300 and inhibits LPS-induced...

An intermediate for the synthesis of glucosylceramide synthase inhibitors such as 1-dNM, a glucose analog that potently inhibits α-glucosidase I and II.

A small molecule inhibitor of the TGF-β receptor type 1/type II kinases (IC₅₀ = 69 nM); used to study the role of TGF-β signaling in tumor cell migration and metastasis; disrupts Smad-2 phosphorylation, an immediate downstream target of the kinase activity.

A minor alkaloid produced in plants of the Solanaceae family, including tobacco; detection in urine is used as an indicator of tobacco use; diminishes Aβ production, reduces the transcription and protein levels of β-secretase, and dose dependently inhibits NF-κB activation.

A biotin-tagged analog of FTY720; methanol side chain of FTY720 that is targeted for phosphorylation by sphingosine kinases is retained, suggesting that it would likewise be phosphorylated in vivo.

An abundant secondary metabolite of ?9-THC