1 mg, Biologically Active Small Molecules
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Oclacitinib
Cayman ChemicalAn orally bioavailable, specific, broad spectrum JAK inhibitor (IC50s = 10, 18, 99, and 84 nM for JAK1, JAK2, JAK3, and JAK4, respectively); blocks cell-based JAK signaling induced by IL-2, IL-4, IL-6, IL-13, or IL-31 with IC50 values ranging from 36 to 249 nM.
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(+)-Abscisic Acid
Cayman ChemicalA plant hormone with diverse roles in disease resistance, plant development, and response to stresses; regulates gene expression and may contribute to epigenetic changes at the chromatin level.
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Amphomycin
Cayman ChemicalAn antibacterial lipopeptide that targets Gram-positive bacteria and may be useful against drug resistant strains; also inhibits peptidoglycan synthesis.
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Adipokinetic Hormone, locust
LKT LabsAdipokinetic hormone is a neuropeptide hormone found in insects that is involved in the regulation of circadian rhythms. Adipokinetic hormone also increases activity of peptidase, lipase, amylase, and polygalacturonase in the salivary glands. In brain samples treated with H2O2, this peptide…
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Diphenyleneiodonium (chloride)
Cayman ChemicalDPI is an irreversible inhibitor of iNOS and eNOS with IC50 values of 50 nM and 0.3 µM, respectively. This inhibition is potent, irreversible, and time and temperature dependent. NADPH, NADP+, and 2'5'-ADP block the inhibitory action of DPI. Similarly, FAD or FMN protect…
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TMS
Cayman ChemicalCYP1B1 is mainly an extrahepatic enzyme which oxidatively metabolizes both endogenous (steroids; eicosanoids) and exogenous xenobiotics such as polyaromatic hydrocarbons. TMS is a potent and selective inhibitor of CYP1B1, with an IC50 of 6 nM. It is 50-fold selective for the inhibition of CYP1B1…
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Paxilline
Cayman ChemicalAn indole diterpene which potently and reversibly inhibits large conductance Ca2+-activated K+ (BKCa) channels, as shown in patch clamp (Ki = 1.9 nM) and whole smooth muscle cell studies (Ki = 35.7 nM).
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(-)-Indolactam V
Cayman ChemicalA tumor-promoting teleocidin compound that activates PKC (Ki = 3.4 nM and 1 μM for PKCη and PKCγ, respectively); induces differentiation of human embryonic stem cells into pancreatic progenitors.
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CAY10625
Cayman ChemicalAn antagonist of the interaction between survivin and the apoptosis-promoting protein Smac/DIABLO with an IC50 value of 2.2 µM; sensitizes cells to apoptotic stimuli.
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HT-2 Toxin
Cayman ChemicalAn active, deacetylated metabolite of T-2 toxin; inhibits protein synthesis and cell proliferation in plants; causes acute and chronic toxic effects in animals that ingest contaminated plant materials.
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Diclofenac-d4
Cayman ChemicalIntended for use as an internal standard for the quantification of diclofenac by GC- or LC-MS.
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U-73122
Cayman ChemicalAn inhibitor of PLC-dependent processes by an undefined mechanism; inhibits platelet aggregation induced by collagen or thrombin with IC50 values of 0.6 and 5 µM, respectively.
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(±)-ß-Hydroxybutyrate-d4 (sodium salt)
Cayman ChemicalAn internal standard for the quantification of (±)-β-hydroxybutyrate (sodium salt) by GC- or LC-MS.
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4-deoxy Nivalenol
Cayman ChemicalA natural type B trichothecene produced by certain species of the fungus Fusarium; inhibits protein biosynthesis, binds to peptidyl transferase, and inhibits the synthesis of RNA and DNA; passes the blood-brain barrier at different rates in different animals.
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10-Nitrolinoleate
Cayman ChemicalThe product of nitration of linoleate by NO-derived reactive species; activates PPARγ (Ki = 133 nM), inducing CD36 expression in macrophages, adipocyte differentiation, and glucose uptake; can also be metabolized to produce nitrite derivatives which in turn form NO, leading to increased cGMP production.
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15-deoxy-?12,14-Prostaglandin A1
Cayman ChemicalA synthetic PGA1 analog with structural features similar to 15-deoxy-Δ12,14-PGJ2, a ligand for PPARγ.
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Ophiobolin A
Cayman ChemicalA sesterterpenoid fungal phytotoxin that binds and irreversibly antagonizes calmodulin, blocking the activation of calmodulin-dependent phosphodiesterase with an IC50 value of 9 μM.
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8-iso Prostaglandin E2 isopropyl ester
Cayman Chemical8-iso PGE2 isopropyl ester is a more lipophilic form of the free acid, 8-iso PGE2. Prostaglandin esters have enhanced lipid solubility compared to their parent compounds. They are generally hydrolyzed to the free acid upon in vivo administration, making the esters useful prodrugs. In general, the…
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Eltrombopag
Cayman ChemicalEltrombopag is a small molecule, nonpeptide agonist of the thrombopoietin receptor. It selectively binds to the transmembrane domain of the receptor and stimulates megakaryocytopoiesis in primary human bone marrow cells through the JAK/STAT signaling pathway. Eltrombopag is reported to increase…
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R-1 Methanandamide Phosphate
Cayman ChemicalA water soluble prodrug analog of AEA with similar activity to that of AEA in the growth inhibition of C6 glioma cells; also a structural variant of LPA, however, its effects on the various LPA receptors have not been tested.
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Tin Mesoporphyrin IX (chloride)
Cayman ChemicalA potent, competitive inhibitor of HO activity in vitro (Ki = 14 nM); inhibits hepatic, renal, and splenic HO activity in vivo for extended periods of time; blocks bilirubin production in vivo, decreasing HO activity in animal models of hyperbilirubinemia.
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CYT387
Cayman ChemicalAn ATP-competitive inhibitor of JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively); causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines; is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms.
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13(S)-HODE-biotin
Cayman Chemical13(S)-HODE is the LO metabolite of linoleic acid. 13(S)-HODE modulates the PAF, LTB4, and fMLP-induced calcium influx in human PMNL. The mechanism by which 13(S)-HODE elicits its inhibitory effect is still unclear. The use of biotinylated 15(S)-HETE as a probe for detecting binding proteins and/or…
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RITA
Cayman ChemicalAn inhibitor of p53-HDM-2 interaction that can reactivate the tumor suppressor function of wild-type p53; binds to p53 with an apparent Kd value of 1.5 nM and prevents interaction with HDM-2 resulting in p53 stabilization, accumulation, and activation.
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Ampkinone
Cayman ChemicalA small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…
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Microcystin-LR
Cayman ChemicalMicrocystins are hepatotoxic cyclic heptapeptide toxins produced by cyanobacteria. They are responsible for periodic poisonings of humans and livestock drinking fresh water where the blue-green algae are endemic. Microcystin-LR is a selective inhibitor of protein phosphatase 2A (PP2A) (IC50= 0.04…
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Cdk5 Substrate
Cayman ChemicalA synthetic peptide (PKTPKKAKKL) corresponding to a sequence of histone H1; phosphorylated by Cdk5 with a Km value of 5 µM.
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Echinomycin
Cayman ChemicalA cell-permeable inhibitor of HIF-1-mediated gene transcription which acts by intercalating into DNA in a sequence-specific manner, blocking the binding of either HIF-1α or HIF-1β to the HRE; reversibly inhibits hypoxia-induced HIF-1 transcription activity in U215 cells with an EC50…