Cayman Chemical

A less potent IWP-2 derivative that has been used to determine which structural features of IWP-2 are essential for impairing Wnt/ β-catenin pathway activity.

A potent inhibitor of both MEK 1 and 2 that works in an ATP-noncompetitive fashion (IC₅₀s = 0.7 and 0.9 nM, respectively); blocks dual phosphorylation of ERK1/2 and stops cell cycling in cancer cell lines, both in vitro and in multiple tumor models in mice.

PtdIns-(4,5)-P2-biotin is an affinity probe which allows the PIP2 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(4,5)-P2 to serve as a general probe for any protein with a high affinity binding interaction with inositol-(4,5)-diphosphate phospholipids, such...

Saline sodium phosphate EDTA stock solution (20X, pH 6.5) contains a concentrated solution of filtered saline sodium phosphate EDTA (SSPE) buffer.

An inhibitor of CXCR4 activation by SDF-1 (IC50 = 4.5 nM) which also blocks HIV-induced cytopathogenicity (EC50 = 73 nM).

PGF2α-NEt is an analog of PGF2α in which the C-1 carboxyl group has been modified to an N-ethyl amide. PG esters have been shown to have ocular hypotensive activity. PG N-ethyl amides were recently introduced as alternative prostaglandin ocular hypotensive prodrugs. Although it has been...

A cell-permeable dipeptide that potently antagonizes PPARγ (Kd = 8.34 µM); reversibly and competitively blocks activation of PPARγ by rosiglitazone (IC₅₀ = 8-32 µM); active in vivo, abolishing the protective effects of rosiglitazone in experimental spinal cord...

A selective, potent agonist of EP4 with an IC₅₀ value of 3 nM (versus 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors) and an EC₅₀ value of 0.19 nM in functional assays; induces the differentiation of bone marrow stem cells from both young and aged rats...

An irreversible inhibitor of GAPDH (Ki = 1.6 µM); selectively induces apoptosis in high-glycolytic cancer cells by inhibiting the generation of ATP in the glycolytic pathway; also inhibits mammalian DNA polymerases β and λ as well as terminal deoxynucleotidyl transferase in family...

Antigen: human optineurin amino acids 115-130 Host: rabbit Cross-Reactivity: (+) human optineurin; (−) murine, rat, and porcine optineurin Application(s): WB

A tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p (IC₅₀s = 7 and 2 µM, respectively); inhibits the growth of S. cerevisiae (GI50 = 30 µM).

An inhibitor of α-D-galactosidase; also inhibits the ceramide-specific glucosyltransferase (IC₅₀ = 41.4 µM) without affecting α-glucosidase I and II or β-glucocerebrosidase (IC₅₀s > 1 mM); sensitizes CLL cell lines to chemotherapeutic agents.

An antimicrotubule drug used to treat Hodgkin’s lymphoma, non-small cell lung, breast, head and neck, and testicular cancer; inhibits steady-state tubulin addition to microtubules (Ki = 0.18 μM) and inhibits B16 melanoma cell proliferation (IC50 = 1 nM).

A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor (nm IC₅₀) that inhibits retinoblastoma protein phosphorylation, which prevents CDK-mediated G1-S phase transition, arresting the cell cycle in the G1 phase, suppressing DNA synthesis, and inhibiting cancer cell growth; reduces...

A bulky purine analog that acts as a selective, ATP-competitive, analog-sensitive Plk1 allele inhibitor; blocks mitotic progression in cells expressing analog-sensitive Plk1 alleles at 10 µM and selectively sensitizes Plk1 to small-molecule inhibitors.

A small molecule lethal to mutant RAS-expressing cells (IC50s = 71 and 272 nM in HRASG12V-expressing and non-expressing BJeH cells, respectively). CAS #: 1360705-96-9

A potent, selective inhibitor of the kinase activity of fibroblast growth factor receptors (FGFRs) 1, 2, and 3 (IC₅₀s = 9.3, 7.6, and 22 nM, respectively); inhibits the growth of cancer cells expressing FGFR genetic alterations both in vitro and in xenograft mouse models.

A close analog of SGC707 that is completely inactive against PRMT3 at concentrations as high as 100 µM.

A decomposition product of the macrolide antibiotic, erythromycin A that has been identified as a β-turn mimic of the peptide hormone motilin; used to determine the binding characteristics of ligands of the motilin receptor.

A bile acid and FXR ligand (EC50 = 13-34 μM) that is a key regulator of cholesterol homeostasis; exhibits toxicity that is linked to increased glutathione and increased oxidative stress; excess CDCA contributes to liver and intestinal cancers.

A peripherally acting, selective and reversible COMT inhibitor with IC₅₀ values of 150-300 nM in rat liver (Ki = 145 nM) and 10-20 nM in rat brain tissues; decreases 3-OMD levels in the rat brain by 16-52% and prolongs the bioavailability of L-DOPA in patients with Parkinson’s...

A naturally occurring steroid alkaloid that acts as a potent histamine H3 receptor antagonist (Kis = 5.2 and 24.5 nM for rat and human, respectively) that efficiently crosses the blood-brain barrier but has a poor rate of CNS clearance.

A neutral, lipid soluble form of the free acid; increases cytosolic Ca2+ concentration leading to pancreatic acinar cell injury due to excessive consumption of ethanol.

(±)12(13)-EpOME-d4 contains four deuterium atoms at the 9, 10, 12, and 13 positions. It is intended for use as an internal standard for the quantification of latanoprost by GC- or LC-MS.