Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Cafestol Palmitate

    LKT Labs

    Cafestol is a diterpene initially found in brewed, unfiltered coffee that exhibits anti-angiogenic, anticancer, chemopreventive, neuromodulatory, anti-inflammatory, and hyperlipidemic activities. Cafestol inhibits proliferation, migration, and tube formation in vitro, potentially through decreasing…

  • Ginkgolic Acid C15:1

    Cayman Chemical

    A 2-hydroxy-6-alkylbenzoic acid in which the alkyl chain contains 15 carbons and is unsaturated at the 8 position; inhibits SUMOylation in vitro (IC50 = 3 µM) and in cells without affecting protein ubiquitination; directly binds the SUMO-activating enzyme E1, blocking the formation…

  • Perlapine

    Cayman Chemical

    An atypical neuroleptic that blocks dopamine and serotonin (5-HT) receptors (Kis = 60, 30, and 30 nM for D2, D4, and 5-HT2A, respectively); an agonist for hM3Dq, a DREADD, with >10,000-fold selectivity for hM3Dq over hM3.

  • CI-1040

    Cayman Chemical

    A potent inhibitor of MEK in (IC50 = 2.3 nM; Kd = 74 nM when activated with ATP) that suppresses phosphorylation of ERK in mouse colon 26 tumors (IC50 = 35 nM).

  • Prostratin

    Cayman Chemical

    Potently induces HIV-1 reactivation in latent reservoirs of infected Jurkat-LAT-GFP cells (IC50 = ~0.5 µM); activates NF-κB via PKC and downregulates HIV-1 receptor CD4 expression and its co-receptors CXCR4 and CCR5.

  • 15(R),19(R)-hydroxy Prostaglandin E2

    Cayman Chemical

    19(R)-Hydroxylated prostaglandins occur in µg/ml concentrations in the semen of certain mammalian species, especially primates. In the case of humans, the compounds are primarily of the PGE series, and the hydroxyl stereochemistry is 15(S),19(R). 19(R)-Hydroxylated prostaglandins are also…

  • Nitrocefin

    Cayman Chemical

    A chromogenic cephalosporin substrate commonly used to detect β-lactamases in bacteria and other microbes.

  • a-Linolenic Acid

    Cayman Chemical

    ALA is an essential fatty acid found in leafy green vegetables. ALA, as part of a low saturated fat diet, helps prevent cardiovascular disease. ALA decreases blood pressure, serum cholesterol levels, and platelet aggregation.

  • Oxalomalic Acid (sodium salt)

    Cayman Chemical

    Formed by the condensation of oxaloacetate with glyoxylate; inhibits aconitase activity at 1 mM, which interferes with IRP1 binding and decreases glutamate secretion in lens and retinal pigment epithelial cells.

  • C-6 Ceramide

    Cayman Chemical

    C-6 ceramide is a cell-permeable analog of naturally occurring ceramides. With a longer carbon chain than C-2 ceramide, it is somewhat more hydrophobic, and may more closely mimic the effects of natural ceramides. C-6 ceramide mediates many diverse biological activities including apoptosis,…

  • CVT-10216

    Cayman Chemical

    A selective, reversible inhibitor of ALDH2 (IC50 = 29 nM); reduces excessive alcohol drinking in alcohol-preferring rats, prevents self-administration of alcohol in Long-Evans rats, and produces anxiolytic effects.

  • Bleomycin Sulfate

    LKT Labs

    This product is a mixture of bleomycin sulfate salts; bleomycin A2 is pictured. Bleomycin is an anticancer chemotherapeutic that binds DNA and induces DNA cleavage and strand breaks; it is highly toxic. Bleomycin A5 is clinically used to treat lymphomas, squamous cell carcinomas, and testicular…

  • PDM 11

    Cayman Chemical

    A structural analog of several resveratrol derivatives which act as a potent and selective AhR antagonists and agonist.

  • tert-butyl p-Toluate

    Cayman Chemical

    tert-butyl p-Toluate is a synthetic intermediate useful for pharmaceutical synthesis.

  • AZD 4547

    Cayman Chemical

    A selective inhibitor of the fibroblast growth factor receptor tyrosine kinase (IC50s = 0.2, 2.5, and 1.8 nM for FGFR1, 2, and 3, respectively); demonstrates antiproliferative activity in tumor cell lines expressing deregulated FGFRs (IC50s = 18-281 nM) and in an FGFR-driven…

  • Budesonide

    Cayman Chemical

    A glucocorticoid steroid that activates the glucorcorticoid receptor with an EC50 value of 12.4 nM; reduces inflammation and has utility in inflammatory diseases, like asthma and inflammatory bowel disease; may be abused by athletes.

  • AG-879

    Cayman Chemical

    A tyrphostin compound that inhibits nerve growth factor (NGF)-dependent TrkA tyrosine phosphorylation in PC-12 cells (IC50 = ~40μM), HER2-ErbB2 kinase in several breast and ovarian cancer cell lines (IC50 = ~0.5 μM), and the VEGF receptor FLK1 (IC50 = ~1 μM).

  • Rubratoxin A

    Cayman Chemical

    A natural mycotoxin and selective inhibitor of PP2A (IC50 = 170 nM); causes suppression of tumor metastasis and reduction of primary tumor volume in mouse xenografts.

  • S-ethyl N-[4-(trifluoromethyl)phenyl] Isothiourea (hydrochloride)

    Cayman Chemical

    EPIT is a selective, competitive inhibitor of nNOS having a Ki of 0.32 µM for the purified human enzyme. EPIT exhibits 115-fold and 29-fold selectivity for nNOS compared to iNOS and eNOS, respectively. It exhibits reduced inhibitory potency in whole-cell assays, possibly due to reduced…

  • Angiotensin II (1-4), Human

    LKT Labs

    Angiotensin II (AT II) is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). AT II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca2+ levels; this results in contraction and vasoconstriction,…

  • Betamethasone 21-Phosphate Sodium

    LKT Labs

    Betamethasone is a glucocorticoid receptor agonist that exhibits anti-inflammatory, immunosuppressive, and anti-ulcerative activities. Betamethasone is clinically used to treat skin irritations such as psoriasis and to accelerate preterm fetal lung development.

  • 4-hydroxy Nonenal Mercapturic Acid-d3

    Cayman Chemical

    An internal standard for the quantification of 4-HNE mercapturic acid by GC- or LC-MS.

  • NSC 245214

    Cayman Chemical

    A thienyl cycloalkanone that is part of the NCI small molecule repository.

  • Forskolin

    Cayman Chemical

    A naturally occurring diterpene that directly activates adenylyl cyclase to raise levels of cAMP in a wide variety of cell types; binds to type 1 adenylyl cyclase membranes with an IC50 value of 41 nM and demonstrates an EC50 value of 0.5 μM in an activation assay.

  • Naringenin-7-O-ß-D-Glucuronide

    Cayman Chemical

    A main phase II metabolite of naringenin that is detectable in urine.

  • E7046

    Cayman Chemical

    A specific antagonist of the type 4 PGE2 receptor EP4; possesses significant anti-tumor growth activity in multiple preclinical tumor models through modulating myeloid cells.

  • Diflunisal

    Cayman Chemical

    An NSAID that inhibits both COX-1 (IC50 = 113 µM) and COX-2 (IC50s = 8.2 and 134 µM for human whole blood assay and human-modified whole blood assays, respectively).

  • S-isopropyl Isothiourea (hydrobromide)

    Cayman Chemical

    IPTU is a potent inhibitor of NOS in vitro but may lack good in vivo efficacy due to poor cellular penetration. The Ki values are 9.8, 22, and 37 nM using purified human iNOS, eNOS, and nNOS, respectively.

  • 3-bromo-7-Nitroindazole

    Cayman Chemical

    3-Bromo-7-nitroindazole is a more potent inhibitor of nNOS than 7-nitroindazole in vitro, but unlike 7-nitroindazole, it is also potent against iNOS. The IC50 values for inhibition of rat nNOS, bovine eNOS, and rat iNOS are 0.17, 0.86, and 0.29 µM, respectively.

  • Bis(3,5-dibromosalicyl) Succinate

    LKT Labs

    Bis(3,5-dibromosalicyl) succinate is an aspirin analog that is used to induce hemoglobin chain crosslinks at lysine residues. This compound is used to study hemoglobin function in research models and may be used to develop treatments for sickle-cell anemia. This compound may exhibit…

  • 15(S)-Fluprostenol

    Cayman Chemical

    (+)-15(R)-Fluprostenol isopropyl ester is a prodrug (Travoprost) which is converted by esterase enzymatic activity in the cornea to yield the corresponding free acid. The free acid, (+)-15(R)-fluprostenol, is a potent FP receptor agonist. The 15(R)-epimers of most PGs are about 100 times less…

  • NSC 12

    Cayman Chemical

    An FGF inhibitor.

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