Cayman Chemical

An inhibitor of the DNA damage sensor MRN, inhibiting MRN-dependent phosphorylation of histone H2AX (IC₅₀ = 66 μM); prevents activation of ATM by blocking the nuclease activity of Mre11; induces G2 arrest, abolishes the radiation-induced G2/M checkpoint, and prevents homology-directed...

A methyl derivative of uric acid and a product of C-8 oxidation of caffeine by cytochrome P450 enzymes.

A potent, cell-permeable inhibitor of aromatase (IC50 = 2 nM).

CAS Number: 1134803-18-1 Synonyms: CGP 57148-d₃; CGP57148B-d₃; Genfatinib-d₃; STI-571-d₃ Molecular Formula: C₂₉H₂₈D₃N₇O Formula Weight: 496.6

A small diffusible signaling molecule involved in quorum sensing, thereby controlling gene expression and affecting cellular metabolism in bacteria; activates NF-κβ in RAW 264.7 macrophages, increasing the expression of TNF-α, IL-1β, and IL-8; alters cell cycling and metabolism...

A polyphenolic antioxidant that is abundant in many fruits, vegetables, plant bark, and peels; has anti-carcinogenic, anti-mutagenic, anti-inflammatory, and organ-preserving properties; blocks methylation of H3R17 by CARM1 without significantly altering histone acetylase or DNA methyltransferase...

A selective, ATP-competitive inhibitor of the DNA damage control kinase, Chk2 (IC₅₀ = 15 nM); prevents apoptosis in human T-cells exposed to ionizing radiation (EC₅₀ = 3-7.6 µM).

Composes a significant portion of CNS gangliosides; concentration increases with maturation and may be related to nervous system degeneration.

A cell permeable analog of BAPTA that binds calcium only after the AM group is removed by cytoplasmic esterases; commonly used at 10-100 μM to evaluate the role of intracellular calcium in cell signaling; also inhibits Kv channels, including Kv1.3, Kv1.5, and Kv11.1 (Ki = 1.45, 1.23, and 1.30...

A phospholipid containing the long-chain (14:0) myristic acid inserted at the sn-1 and sn-2 positions.

trans-.DELTA.2-11-methyl-Dodecenoic acid is the conformational isomer of cis-.DELTA.2-11-methyl-dodecenoic acid, a diffusible signal factor (DSF) in extracellular microbial and fungal communication systems.

A synthetic intermediate useful for pharmaceutical synthesis; has mycobacteriostatic and mycobacteriocidal activities in vitro.

A small molecule stimulator of SRC-1, SRC-2, and SRC-3 that selectively induces paraptosis in a variety of cancer cells in vitro and reduces tumor growth in a xenograft mouse model; can increase the interaction of SRCs with the coactivators CBP and CARM1 and can induce ER stress coupled to the...

A BMI-1 inhibitor (IC₅₀ = ~ 0.5 μM) that irreversibly impairs CIC growth; reduces tumor growth in CIC xenograft assays and abrogates colorectal cancer cell self-renewal in vivo.

An activator of the ATP-sensitive K+ channels that displays anti-ischemic (EC25 = 8.9 μM) and cardioprotective (IC₅₀ = 0.03 μM) effects in rat hearts.

A potent, cell-permeable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki death proteins, leading to apoptosis.

A bacteriocin, a natural polycyclic antibacterial peptide, also called a lantibiotic; particularly effective against Gram-positive bacteria and commonly used as a food preservative.

A synthetic analog of natural PtdIns featuring C:18 fatty acid in the sn-1 position and arachidonic acid in the sn-2 position of the glycerol backbone; a critical phospholipid species that can served as an anchor for the binding of signal transduction proteins bearing pleckstrin homology (PH)...

A prodrug formulation of HPA which may be useful in various biochemical studies and as a reference standard in analytical work.

CAY10416 is a dual COX-2/5-LO inhibitor with IC₅₀ values of 50 and 3 nM, respectively. The selectivity of CAY10416 for COX is greater than 200-fold for COX-2 versus COX-1. COX-2/5-LO inhibitors such as CAY10416 are also apoptosis-inducing agents and are potentially useful in prostate...

A potent inhibitor of the CK1 isoforms CK1ε and CK1δ (IC₅₀ = 7.7 and 14 nM, respectively); less effectively inhibits a wide variety of related or common kinases; disrupts circadian rhythms in cells and animals; blocks the locomotor response to amphetamines in mice.

A potent inhibitor of IκB kinases (IKKs), displaying IC₅₀ values of 200, 40, and 70 nM for IKKα, IKKβ, and IKK complex, respectively, in cell-free assays; effective in cells and in animals.

A subtype-selective AMPA receptor antagonist that inhibits homomeric GluR1 and GluR3 as well as heteromeric GluR1/2 receptors (80-100% of glutamate-evoked currents inhibited at 100 µM); inhibits the GluR5(Q) receptor with a Ki value of 0.29 µM.

A natural product that has antioxidant and neuroprotective activity; promotes neurite outgrowth in cultured neurons and in rodents injected with Aβ(25-35); recovered Aβ(25-35)-induced memory deficit in mice; reverses hypoxia-mediated neurodegeneration by restoring hypoxia induced...