Biologically Active Small Molecules
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Genistein
Cayman ChemicalAn isoflavonoid phytoestrogenic compound found in soybeans, pea pods, and other legumes; acts as a tyrosine kinase inhibitor, has chemopreventive effects on breast, prostate, and other endocrine-dependent tumors.
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(Z-Ala-Ala-Ala-Ala)2Rh110
Cayman ChemicalA sensitive fluorogenic elastase substrate that is selectively cleaved by elastase to yield Rhodamine 110, which can be analyzed with an excitation wavelength of 485 nm and emission wavelength of 525 nm.
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3'-Azido-3'-deoxythymidine
LKT LabsAZT is a thymidine nucleoside analog that inhibits reverse transcriptase and is clinically used to treat HIV/AIDS. AZT inhibits viral DNA synthesis, preventing viral replication; at high doses, it may inhibit DNA polymerase. Use of AZT is often limited
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D-erythro-MAPP
Cayman ChemicalAn analog of ceramide that inhibits alkaline ceramidase (IC50 ~5 µM); suppresses growth of HL-60 cancer cells in culture.
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3-Methyladenine
Cayman ChemicalA specific inhibitor of PI3K activity and a widely used inhibitor of the autophagy; at 5 mM, inhibits protein degradation in rat hepatocytes by 65% and blocks class I, II, and III PI3Ks, including some downstream targets.
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NSC 405020
Cayman ChemicalFormal Name: 3,4-dichloro-N-(1-methylbutyl)-benzamide CAS Number: 7497-07-6 Molecular Formula: C12H15Cl2NO
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15(S)-15-methyl Prostaglandin F2a
Cayman Chemical15(S)-15-methyl PGF2α is a metabolically stable analog of PGF2α. It is a potent uterine stimulant and abortifacient which can be administered intramuscularly to induce labor. It induces luteolysis and reduces serum progesterone concentrations when given as an intramuscular injection in…
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5-trans Prostaglandin E2
Cayman Chemical5-trans PGE2 occurs naturally in some gorgonian corals and is a common impurity in commercial lots of PGE1. It is 18 times more potent than PGE2 in activating adenylate cyclase in NCB-20 cell homogenates. 5-trans PGE2 accelerates fibrinolysis by enhancing plasminogen activation mediated by…
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Unoprostone isopropyl ester
Cayman ChemicalUnoprostone isopropyl ester (Rescula) is the clinically approved, prodrug form of unoprostone, which is a free acid analog of PGF2α. Both latanoprost and Rescula have been approved for the treatment of ocular hypertension. Both analogs of PGF2α are believed to act by increasing the rate…
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ABT-199
LKT LabsBH3 mimetic and Bcl-2 inhibitor. It induces apoptosis in chronic lymphocytic leukemia cells
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MLCK Inhibitor Peptide 18
Cayman ChemicalA selective, cell permeable inhibitor of MLCK (IC50 = 50 nM).
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CH5132799
LKT LabsCH5132799 is an inhibitor of PI3K that is somewhat selective for p110a isoforms. This compound exhibits anticancer chemotherapeutic activity, inhibiting cell proliferation and tumor growth in breast cancer, ovarian cancer, prostate cancer, and endometrial cancer models.
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Ketoconazole
Cayman ChemicalAn orally active broad spectrum antifungal agent that blocks ergosterol biosynthesis by inhibiting the fungal CYP isoform CYP51; potently inhibits the mammalian analog CYP51A1 (IC50 = 63.5 nM), as well as a variety of other CYP isoforms.
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Omeprazole sulfone
Cayman ChemicalThe major metabolite of the gastric proton pump inhibitor, omeprazole; produced by CYP3A4 sulfoxidation of esomeprazole.
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Tivantinib
Cayman ChemicalA staurosporine derivative that binds to dephosphorylated c-Met kinase and to the colchicine binding site of tubulin; promotes mitotic arrest and apoptosis of various human tumor cell lines (EC50s ranging from 60-600 nM).
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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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Gly-Phe-ß-naphthylamide
Cayman ChemicalA substrate of cathepsin C that accumulates inside lysosomes causing lysosome degradation; 50 μM can inhibit the cathepsin-dependent activation of caspase-8.
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Acetylsalicylic Acid
LKT LabsNSAID and COX-1/2 inhibitor used to decrease inflammation. It inhibits platelet aggregation and prolongs bleeding time by decreasing levels of thromboxane A2. Chronic administration decreases risk of cancer and cardiovascular events.
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Cetrimide
LKT LabsCetrimide is a mix of quaternary ammonium salts that exhibits antiseptic and anticancer chemotherapeutic activities. Cetrimide acts as a cationic detergent, altering the mitochondrial membrane potential and inducing pore formation in membranes. Cetrimide bromide inhibits H+ ATP synthase, inducing…
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SB-258585 (hydrochloride)
Cayman ChemicalA potent, selective antagonist of the serotonin 5-HT6 receptor (pKi = 8.53); has been used in cells and in animals.
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Ionomycin (calcium salt)
Cayman ChemicalA selective calcium ionophore that mobilizes intracellular calcium stores. It is used as a research tool to raise the intracellular level of calcium, to study calcium transport across biological membranes, and to stimulate the intracellular production of cytokines.
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Fura-2 AM
Cayman ChemicalAnoninvasive, intracellular calcium indicator that is UV light-excitable; spectral properties in the presence of low calcium concentrations (excitation max = 362 nm, emission max = 512 nm) differ from those during high calcium conditions (excitation ma
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8-hydroxy Guanine (hydrochloride)
Cayman Chemical8-hydroxy Guanine is produced by oxidative damage of DNA or RNA by reactive oxygen and nitrogen species, including hydroxyl radical and peroxynitrite. It serves as a measure of oxidative stress in biological systems.
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Microcystin-RR
Cayman ChemicalA toxin produced by cyanobacteria that inhibits the catalytic activity of protein phosphatases PP1C, PP1γ, and PP2A with Ki values of 0.15, 0.24, and 0.018 nM, respectively.
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Prostaglandin A2-d4
Cayman ChemicalAn internal standard for the quantification of PGA2 by GC- or LC-MS.
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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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N-Palmitoyl Dopamine
Cayman ChemicalA “hybrid” analog which incorporates components of both the AEA-like and dopaminergic neurotransmitter pathways; is nearly inactive as a TRPV1 ligand and fails to elicit hyperalgesic or nocifensive responses in vivo; exhibits an “entourage” effect at concentrations of 0.1-10…
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SU 9516
Cayman ChemicalA potent inhibitor of several CDKs with selectivity for Cdk2 (IC50s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1); has anti-proliferative and pro-apoptotic activity in tumor cells.
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Alendronate Monosodium Trihydrate
LKT LabsAlendronate is a second generation bisphosphonate that exhibits anti-resorptive, anti-inflammatory, immunomodulatory, and anticancer chemotherapeutic activities. Alendronate inhibits bone resorption but does not have any effects on bone mineralization; it also inhibits osteoclast formation and…
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N-(3-hydroxyphenyl)-Arachidonoyl amide
Cayman Chemical3-HPA is an analog of AM404, which is a selective inhibitor of carrier-mediated transport of AEA. 3-HPA is metabolized by both COX-1 and COX-2 and also selectively and irreversibly inhibits COX-2 with an IC50 value of 2 µM.
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DY 131
Cayman ChemicalA selective ERRβ/γ receptor agonist (EC50 = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.