Cayman Chemical

A negative allosteric modulator of CaSR that blocks calcium-mediated activation (IC₅₀ = 0.39 µM); attenuates the activation of CaSR by calcimimetics.

The pharmacologically inactive optical enentiomer of (R)-LSF.

A lipophilic analog of 16-phenoxy tetranor PGF2α.

DNA methylation is an important epigenetic process regulating gene expression. Methylation occurs on carbon 5 of 2-deoxy cytidine yielding the modified base 5-methyl-2-deoxy cytidine. The methylation pattern of cells is tightly regulated during development with the methylation profile being...

A stable, cell-permeable cGMP analog that competitively inhibits cGMP-dependent protein kinases (cGKs), including cGK Iα and cGK II (IC₅₀s = 18.3 and 0.16 µM, respectively); blocks the relaxation of rat tail arteries induced by the nitric oxide donor SIN-1.

PGF2α-OH is an analog of PGF2α in which the C-1 carboxyl group has been reduced to a primary alcohol. Biological studies on rat uterus show it to be a weak agonist. The compound is reported to retain ocular hypotensive properties, but the nature of the receptors which mediate these...

An LPA analog containing palmitic acid at the sn-1 position.

Source: Active recombinant N-terminal Strep II-tagged protein expressed in E. coli Mr: 42.6 kDa JMJD2D catalyzes the demethylation of di- and tri-methylated forms of histone H3 at lysine residue 9 (me2/3), leading to transcriptional repression and activation, respectively. JMJD2D is an...

A naturally-occurring anthraquinone with diverse effects, including the suppression of inflammation, dyslipidemia, and cancer; directly and selectively inhibits CK2 (IC₅₀ = 0.89 μM) and the COP9 signalosome; acts as a phytoestrogen, blocking 17β-estradiol binding to ER with Ki...

A propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC₅₀ = 50 nM); does not inhibit other NMDA subunits, AMPA receptors, or kainate receptors; has neuroprotective effects in vitro and in vivo.

A cell-permeable carbazolic compound which directly interacts with and stabilizes CRY1 and CRY2, preventing ubiquitin-dependent degradation while lengthening the circadian period (IC₅₀ = 0.82-14 μM); inhibits glucagon-induced gluconeogenesis in primary hepatocytes.

13,14-dh PGE1-d4 contains four deuterium atoms at the 3, 3', 4, and 4' positions. It is intended for use as an internal standard for the quantification of 13,14-dh PGE1 by GC- or LC-mass spectrometry.

Molecular Formula C₁₈H₂₇N₃O₃ • HCl Formula Weight 369.9

An uncharged, 1,4-di-substituted, phenyl-linked bis-TFMS phosphate mimetic that acts as a reversible, competitive, and active-site directed inhibitor of SHP-2, PTP1B, PTP-ε, PTP-Meg-2, PTP-σ, PTP-β, and PTP-µ (IC₅₀s = 1.8, 2.5, 8.4, 13, 20, 6.4, and 6.7 µM,...

A non-lipid agonist of LPA2 (EC₅₀ = 0.10 µM) that is without effect at other LPA receptor subtypes; protects IEC-6 cells against caspase activation and apoptosis following irradiation; increases the survival of mice suffering from hematopoietic acute radiation syndrome after...

A phospholipid containing the medium-chain (12:0) lauric acid inserted at the sn-1 and sn-2 positions.

A lipid peroxidation product; actively modifies histidine and lysine residues on proteins and causes protein cross-linking.

Antigen: 5,5-dimethyl-2-(8-octanoic acid)-1-pyrroline N-oxide coupled to ovalbumin Host: rabbit Cross-reactivity: species independent Applications: WB, ICC, and ELISA Proteins with endogenous peroxidase activity are susceptible to forming radical adducts. Immunodetection of spin trap products allows...

N-acetyl LTE4 is the major inactive metabolite of LTE4 found in bile. This route of metabolism is prominent in the rat, but of minor importance in humans. N-acetyl LTE4 is 100 times less potent than LTC4 as a vasoconstricting agent. In healthy human subjects urinary excretion of N-acetyl LTE4 is...

Aminoguanidine is equipotent to L-NMMA and L-NNA as an inhibitor of iNOS. The IC₅₀ values for inhibition of mouse iNOS and rat nNOS are 5.4 and 160 µM, respectively. Aminoguanidine also inhibits induction of iNOS protein expression by endotoxin in rat macrophages.

The COX Colorimetric Inhibitor Screening Assay measures the peroxidase component of cyclooxygenases. The peroxidase activity is assayed colorimetrically by monitoring the appearance of oxidized N,N,N',N'-tetramethyl-p-phenylenediamine (TMPD) at 590 nm. Inhibition of COX activity, measured by...

A potent, ATP-competitive inhibitor of JAK2 that less effectively inhibits JAK3 (IC₅₀s = 3 and 48 nM, respectively); inhibits JAK2 containing the V617F mutation (IC₅₀ = 20 nM); reduces the growth of Ba/F3 pro-B-cells in SCID mice without affecting erythroid progenitors,...

Selectively and competitively blocks T3 binding to both TRα and TRβ (IC₅₀s = 1.5 µM), demonstrating ~1000-fold lower affinity for TRα in intact cells compared with T3.

An antagonist of the kainate receptor, an ionotropic glutamate receptor (apparent Kd = 5.94 µM).