Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • GSK5959

    Cayman Chemical

    A potent, selective, and cell-permeable inhibitor of the BRPF1 bromodomain (IC50 = 80 nM); disrupts chromatin binding of BRPF1 in a cellular assay by blocking the interaction of BRPF1 with histone H3.3.

  • ethyl-2-amino-4-phenyl Thiophene-3-Carboxylate

    Cayman Chemical

    A synthetic intermediate useful for pharmaceutical synthesis.

  • 2-amino-4-phenyl Thiazole

    Cayman Chemical

    A synthetic intermediate useful for pharmaceutical synthesis.

  • ATB-346

    Cayman Chemical

    ATB-346 is a non-steroidal anti-inflammatory drug (NSAID), derived from naproxen but coupled to an H2S-releasing moiety. At 30 µmol/kg in rats, it suppressed COX and gastric PGE2 synthesis to the same level as naproxen but reduced COX-2 expression and accelerated…

  • DG-172 (hydrochloride)

    Cayman Chemical

    An orally available inverse agonist of PPARβ/δ (IC50 = 27 nM), down-regulating transcription of ANGPTL4 in mouse myoblasts (IC50 = 9.5 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.

  • GW 9578

    Cayman Chemical

    A potent, selective PPARα agonist that activates murine and human PPARα with EC50 values of 0.005 and 0.05 µM, respectively; 0.2 mg/kg given orally once daily for three days decreased serum total LDL cholesterol 40-60% in male Sprague-Dawely rats.

  • REV 5901

    Cayman Chemical

    REV 5901 is an antagonist of cysteinyl-leukotriene receptors with a Ki value of 0.7 µM for guinea pig lung membranes. It is also an inhibitor of rat neutrophil 5-LO with an IC50 value of 0.12 µM.

  • N-(2-hydroxyethyl)-Naphthalimide

    Cayman Chemical

    An N-substituted 1,8-naphthalimide used as a fluorescent probe for various studies and as a precursor for protection of amine groups.

  • 10-POHSA

    Cayman Chemical

    A FAHFA in which palmitoleic acid is esterified to 10-hydroxy stearic acid.

  • Leukotriene B4-3-aminopropylamide

    Cayman Chemical

    An analog of LTB4 that binds to the BLT1 and BLT2 receptors with Ki values of 5.1 and 1,227 nM, respectively.

  • Tolazoline (hydrochloride)

    Cayman Chemical

    A competitive α1- and α2-adrenergic receptor antagonist with peripheral vasodilator and histamine-like effects in animal models.

  • Dihomo-y-Linolenic Acid

    Cayman Chemical

    An elongation product of γ-linolenic acid (18:3), rapidly metabolized by fatty acid desaturases to produce arachidonic acid (20:4); metabolized through the cyclooxygenase pathway to produce 1-series prostaglandins; can reduce atopic dermatitis and atherosclerosis when added to the diet of mice.

  • Caspase-3 Inhibitor VII

    Cayman Chemical

    CAS Number: 745046-84-8 Synonyms: Ivachtin Molecular Formula: C20H21N3O7S

  • Ispinesib

    Cayman Chemical

    The kinesin-like spindle protein Eg5 (also known as kinesin-5, kinesin family protein 11, or Kif11) is a motor protein that is essential for establishing a bipolar spindle during mitosis both in normal and tumor cells. Ispinesib is a cell-permeable, allosteric inhibitor of Eg5 (Ki app = 2.3 nM)…

  • 13-Docosenamide

    Cayman Chemical

    An amide of docosenoic acid first identified in the CSF of sleep-deprived cats; causes reduced mobility and slightly lessened awareness in rats.

  • Vancomycin (hydrochloride)

    Cayman Chemical

    A glycopeptide antibiotic identified for its utility in the treatment of gram-positive bacteria, including penicillin-resistant staphylococci; binds to bacterial cell wall precursors, interfering with their synthesis.

  • Pentosidine

    Cayman Chemical

    A well-characterized natural advanced glycation end (AGE) that is often used as a biomarker for the production of all AGEs.

  • Inauhzin

    Cayman Chemical

    A cell-permeable, selective SIRT1 inhibitor (IC50 = 0.7-2 µM) that reactivates p53 by inhibiting SIRT1 deacetylation activity; inhibits cell proliferation by inducing p53-dependent apoptosis in various human cancer cells (IC50s = 5.4, 51.9, 3.2, 33.9, and 85.4 µM…

  • Capsaicin, natural

    LKT Labs

    Capsaicin is an agonist of transient receptor potential vanilloid (TRPV) channels that was originally found in peppers of the Capsicum genus. Capsaicin exhibits analgesic, anti-inflammatory, anti-obesity, and anticancer chemotherapeutic activity. Capsaicin also displays bronchoconstrictive activity…

  • ß-D-Glucose

    Cayman Chemical

    One of two cyclic forms of D-glucose that is the monomer unit in cellulose.

  • Aflatoxin B2

    Cayman Chemical

    The dihydro derivative of Aflatoxin B1.

  • ProClin™ 300

    MilliporeSigma

    ProClin biocides are immediately microstatic upon contact with microbial organisms as a result of their ability to quickly penetrate cell membranes and inhibit specific enzymes crucial to cellular respiration. Multiple specific sites of ProClin toxicity prevent microorganisms from developing high…

  • Echinomycin

    Cayman Chemical

    A 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…

  • Juvenile Hormone III

    Cayman Chemical

    An acyclic sesquiterpenoid that regulates diverse processes in insects; activates the juvenile hormone receptor, known as methoprene-tolerant, with a Kd value of 2.9 nM.

  • Fluconazole

    Cayman Chemical

    A triazole antifungal agent that is effective against most Candida strains.

  • Apigenin

    LKT Labs

    Apigenin is a flavonoid found in various plant sources that exhibits anticancer, antioxidative, anti-inflammatory, cognition enhancing, and neuroprotective activities. In gastric cancer cells, apigenin inhibits cell proliferation, decreases mitochondrial membrane potential, increases expression of…

  • Aldicarb

    Cayman Chemical

    A carbamate pesticide that reversibly inhibits acetylcholinesterase.

  • Prostaglandin E1

    Cayman Chemical

    PGE1 is the theoretical COX metabolite of DGLA, but it is virtually undetectable in the plasma of normal humans or other animals. Its pharmacology includes vasodilation, hypotension, and anti-platelet activities. The IC50 of PGE1 for the inhibition of ADP-induced human platelet…

  • AX 048

    Cayman Chemical

    A potent group IVA cPLA2 inhibitor (XI(50) = 0.022); reduces thermal hyperalgesia evoked by carrageenan injection of rat hind paw (ED50 = 1.2 mg/kg); does not inhibit COX activity or interfere with CB1 receptor signaling.

  • Bumetanide

    Cayman Chemical

    A loop diuretic with good absorption and pharmacodynamic properties; acts as an inhibitor of NKCC1 and the kidney-specific NKCC2 (Ki = 0.5 and 59 μM for human and rabbit NKCC1, respectively).

  • Aristolochic Acid C

    LKT Labs

    Aristolochic acid C is a carcinogenic compound found in Aristolochia and Radix that has commonly been used in traditional Chinese medicine.

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