Biologically Active Small Molecules
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Guaiacol
Cayman ChemicalGuaiacol is a phenolic natural product first isolated from Guaiac resin and the oxidation of lignin. Guaiacol is readily oxidized by the heme iron of peroxidases including the peroxidase of COX enzymes. It can therefore serve as a reducing co-substrate for COX reactions. The one-electron oxidation…
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Mecamylamine (hydrochloride)
Cayman ChemicalA noncompetitive nicotinic acetylcholine receptor antagonist with preferential activity at the α3β4 subtype (IC50 = 90-640 nM) compared to α4β2, α3β2, and α7 subtypes (IC50s range from 1-7 μM).
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Flumazenil
Cayman ChemicalAn imidazobenzodiazepine derivative that competitively inhibits benzodiazepine binding to GABAA receptors (IC50 = 2 nM); used to reverse sedation induced by benzodiazepine drugs and is effective in the treatment of benzodiazepine overdose or withdrawal.
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Olaparib
Cayman ChemicalA potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 µM); can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.
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4-bromo-A23187
LKT LabsNon-fluorescent halogenated A23187 analog and Ca2+ ionophore. It induces formation of endothelial microvesicles, increasing leakage of lactate dehydrogenase and decreasing cell viability. It also induces mast cell degranulation and stimulates the acros
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VER-49009
Cayman ChemicalAn Hsp90 inhibitor with an IC50 value of 47 nM; induces the expression of HSP27 and Hsp72 while reducing the client proteins c-Raf, B-Raf, survivin, and PRMT5, causing cell cycle arrest and apoptosis.
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AMT (hydrochloride)
Cayman ChemicalAMT is a potent, relatively selective inhibitor of iNOS with a Ki of 4.2 nM in mouse macrophages. It inhibits other isoforms of NOS, but at higher concentrations; the IC50 values for rat nNOS and bovine eNOS are 34 and 150 nM, respectively.
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15(R)-17-phenyl trinor Prostaglandin F2a isopropyl ester
Cayman ChemicalA latanoprost-related isomer containing both a double bond at C-13,14 and an invered (b) hydroxyl group at C-15; a potential impurity in most commercial preparations of the lantanoprost bulk drug product.
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CeMMEC1
Cayman ChemicalA selective inhibitor of TAF1 bromodomain 2 (Kd = 1.8 µM; IC50 = 0.9 µM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.
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SMER3
Cayman ChemicalA selective inhibitor of SCFMET30 ubiquitin ligase, an E3 ligase that regulates transcription, cell-cycle control, and immune response; at 5 μM, upregulates a set of methionine biosynthesis genes by altering the SCFMET30 complex, preventing ubiquitination of target proteins, including Met4.
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Abiraterone
Cayman ChemicalBlocks CYP17A1 by potently inhibiting both the 17α-hydroxylase and the 17,20 lyase activities (IC50 = 18 and 17 nM, respectively); essentially eliminates plasma testosterone while producing a 3- to 4-fold increase in plasma luteinizing hormone.
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Azithromycin Dihydrate
LKT LabsAzithromycin is an azalide macrolide antibiotic derived from erythromycin. Azithromycin binds the bacterial 50S ribosomal subunit, inhibiting protein translation. Azithromycin displays antibacterial, anti-fibrotic, and anti-inflammatory activities. In epithelial cells, azithromycin inhibits the…
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Docosahexaenoic Acid
Cayman ChemicalAn essential fatty acid and the most abundant ω-3 fatty acid in neural tissues, especially in the retina and brain; constitutes as much as 40% of the total PUFA pool in retinal and neuronal membranes; dietary supplementation via fish oil inhibits the progression of atherosclerosis and delays…
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Bexarotene
Cayman ChemicalA high-affinity ligand for retinoid X receptors (RXRs)(EC50 = 28, 25, and 20 nM for RXRα, β, and γ, respectively); inhibits cell cycle progression, induces apoptosis, and blocks angiogenesis and metastasis; stimulates clearance of soluble Aβ, reduces plaque area, and reverses…
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2,3-dinor-11ß-Prostaglandin F2a
Cayman ChemicalKey urinary metabolite of PGD2; represents approximately 1% and 4% of the infused radiolabeled dose in monkeys and humans, respectively.
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Pyroxamide
Cayman ChemicalAn inhibitor of HDAC, including HDAC1 (IC50 = 0.1-0.2 μM); induces growth suppression and cell death of certain types of cancer cells in culture.
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Nullscript
Cayman ChemicalAn analog of scriptaid that lacks scriptaid’s HDAC inhibitory effects; used as a negative control in experiments involving scriptaid.
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13,14-dihydro-19(R)-hydroxy Prostaglandin E1
Cayman Chemical13,14-dihydro-19(R)-hydroxy PGE1 is the theoretical metabolite of 13,14-dihydro PGE1 by ω-1 hydroxylase. There are no known reports on its biosynthesis or biological activity.
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Caffeic Acid
Cayman ChemicalCaffeic acid is an inhibitor of 5-LO with an IC50 value of 3.7-72 µM and 12-LO with an IC50 value of 5.1-30 µM.
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11ß-Prostaglandin F2a
Cayman ChemicalPrimary plasma metabolite of PGD2; levels increase nearly 3-fold upon allergan-induced bronchoconstriction in asthmatics.
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GSK-J4 (hydrochloride)
Cayman ChemicalAn ethyl ester prodrug of the JMJD3 selective histone demethylase inhibitor GSK-J1; reduces LPS-induced proinflammatory cytokine production, including that of TNFα (IC50 = 9 µM) in human primary macrophages.
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Methylpiperidino pyrazole
Cayman ChemicalA highly selective ERα receptor antagonist (Ki = 5.6 nM; IC50 = 80 nM).
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PI-103
Cayman ChemicalA potent, cell-permeable, ATP-competitive inhibitor of PI3K family members (IC50 = 2, 8, 20, 26 nM for DNA-PK, p110α, mTORC1, and PI3-KC2β, respectively).
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YS-035 (hydrochloride)
Cayman ChemicalA verapamil derivative that dose-dependently blocks calcium uptake via Na+/Ca2+ exchange in diverse types of cells (Ki = 28 µM); also prevents calcium release from mitochondria induced by Ruthenium Red but not by uncouplers, respiratory inhibitors, or a chelating agent.
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Chlorzoxazone
Cayman ChemicalA benzoxazolone derivative that causes skeletal muscle relaxation and blocks spasticity in clinical studies; enhances KCa2.2 and KCa3.1 channels (EC50s = 87 and 98 µM, respectively); urinary excretion of its 6-hydroxy metabolite is often used as a probe of CYP2E1 activity in…
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7-Piperazin-1-yl-thieno[2,3-c] Pyridine (hydrochloride)
Cayman Chemical7-Piperazin-1-yl-thieno[2,3-c] pyridine (hydrochloride) is a synthetic intermediate useful for pharmaceutical synthesis.
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Aflatoxin B1
LKT LabsAflatoxins are mycotoxins found in foods and livestock feeds that were initially produced by species of Aspergillus. Aflatoxin B1 is the most cytotoxic of all aflatoxins; it inhibits DNA synthesis and induces cell cycle arrest.
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PAF C-16 Carboxylic Acid
Cayman ChemicalModified with a carboxylic acid group terminating the C-16 alkyl chain, providing a convenient site for chemical crosslinking.
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(±)-4-hydroxy Propranolol (hydrochloride)
Cayman ChemicalAn active metabolite of propranolol, inhibiting β1- and β2-adrenergic receptors with KD values of 2.4 and 5.8 nM, respectively; comparable to propranolol in potency in antagonizing the effects of isoprenaline on heart rate and blood pressure in cats and dogs.
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Methyl y-Linolenyl Fluorophosphonate
Cayman ChemicalAn analog of MAFP, which has been widely studied as an inhibitor of phospholipases, FAAH, and as a CB receptor ligand; pharmacology of the γ-linolenyl analog of MAFP has not been completely investigated.
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Carbadox
LKT LabsCarbadox is an antibiotic compound used to treat livestock; it exhibits antibacterial activity against Lawsonia and Treponema. Carbadox is also used as a growth promoter and may be mutagenic.
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AZD 2932
Cayman ChemicalCAS Number: 883986-34-3 Molecular Formula: C24H25N5O4 Formula Weight: 447.5