Biologically Active Small Molecules

Laboratory Chemicals - Life Science - Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Cayman Chemical

    A potent and selective PPARγ ligand. It binds to the PPARγ ligand-binding domain with a Kd of 43 nM.

  • Cayman Chemical

    An analgesic and antipyretic compound; inhibits COX-2 activity by more than 80%, albeit at relatively high doses, while it is less effective against COX-1.

  • Cayman Chemical

    A selective inhibitor of PAD4 (IC50 = 200 nM in the absence of calicum); inhibits the citrullination of PAD4 target proteins and diminishes NET formation in mouse neutrophils.

  • Cayman Chemical

    An 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.

  • A pyrazine derivative that is used as a flavoring agent in the food and tobacco industry; has DNA strand breakage activity and strongly inhibits IL-2 production by Jurkat cells stimulated with phytohemagglutinin (IC50 = ~1.25 mM).

  • Cayman Chemical

    A flavone that modulates xenobiotic metabolism; antagonizes AhR at nanomolar concentrations, although it agonizes AhR at higher concentrations (10 µM); inhibits CYP19, CYP1A1, CYP1A2, and CYP1B1 (IC50s = 500, 60, 6, and 5 nM, respectively), whereas it activates CYP3A4 (Kd = 7.4 µM).

  • LKT Labs

    Aspartame is a dipeptide ester that is used as an artificial sweetener in commercial food production. Aspartame exhibits antibacterial efficacy against Porphyromonas, a periodontal pathogen. In vivo, aspartame also displays antinociceptive activity, increasing latency times in tail flick and paw…

  • Cayman Chemical

    A natural oxidative metabolic product of the mycotoxin aflatoxin B2.

  • Cayman Chemical

    A non-ionic, water-soluble X-ray contrast agent for intravascular administration; can cause acute kidney injury and is used in animal models of contrast-induced nephropathy.

  • Cayman Chemical

    A cell-permeable, stable free radical that is commonly used to evaluate the ability of compounds to act as free radical scavengers or hydrogen donors and to measure the antioxidant activity of tissue extracts; followed by color change from purple (absorbance at 515-528 nm) to yellow.

  • Cayman Chemical

    A potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC50 values of 67 and 289 nM for the human and rat isoforms, respectively; attenuates cold allodynia following nerve injury and suppresses neuronal activity in response to mechanical stimulation.

  • Aminoguanidine is equipotent to L-NMMA and L-NNA as an inhibitor of iNOS. The IC50 values for inhibition of mouse iNOS and rat nNOS are 5.4 and 160 µM, respectively. Aminoguanidine also inhibits induction of iNOS protein expression by endotoxin in rat macrophages.

  • Cayman Chemical

    Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of sPLA2. The IC50 value for thioetheramide-PC is 2 µM at a substrate concentration of 0.5 mM. In addition to binding to the catalytic site of sPLA2, thioetheramide-PC…

  • A major metabolite of sulforaphane that has been shown induce ARE-driven gene expression with roughly 8-fold less potency than sulforaphane.

  • Cayman Chemical

    (±)11-HDHA is an autoxidation product of DHA in vitro. It is also produced from incubations of DHA in rat liver, brain, and intestinal microsomes. DHA is metabolized to 11(S)-HDHA by human platelets and canine retina. In addition to 11(S)-HDHA, 14(S)-HDHA is also produced by platelets.…

  • Cayman Chemical

    An inhibitor of RIP1 kinase that prevents the death of TNF-α-treated FADD-deficient Jurkat cells with an EC50 value of 490 nM.

  • Cayman Chemical

    Caffeic 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.

  • Cayman Chemical

    An analog of thalidomide that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines; induces proliferation and enhances the functional capacity of T-lymphocytes, amplifying co-stimulatory signaling pathways.

  • Cayman Chemical

    (±)15-HETE is one of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid. The biological activity of (±)15-HETE is similar to that of its constituent enantiomers (Item Nos. 34720 and 34710).

  • Cayman Chemical

    A cyclic hexapeptide mycotoxin that binds β-tubulin in a vinca domain; blocks microtubule growth, modulates the dynamics of microtubules, and interferes with mitosis.

  • A potential metabolite of 8-iso PGF2β via the 15-hydroxy PGDH pathway.

  • Cayman Chemical

    Enzymatically-derived PGE2 is an optically pure compound whereas PGE2 derived from the free radical-catalyzed peroxidation of arachidonate is a racemic mixture. Ent-PGE2 is the opposite enantiomer of PGE2. Significant amounts of racemic PGE2 (rac-PGE2) are generated in vitro and in vivo in settings…

  • 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.

  • Benzyl isothiocyanate (BITC) is an isothiocyanate originally found in cruciferous vegetables that exhibits immunomodulatory, anti-parasitic, antibiotic, antioxidative, anti-atherosclerotic, anti-angiogenic, anti-metastatic, anticancer chemotherapeutic, and chemopreventive activities. BITC inhibits…

  • Nicotinic acetylcholine receptor agonist isolated from Nicotiana tabacum and Nicotiana rustica. Nicotine Tartrate finds an application as the nicotine active in a wide range of smoking cessation products such as nicotine lozenges and nicotine sub-lingual tablets. (-)-Nicotine ditartrate is a…

  • Cayman Chemical

    A selective and competitive inhibitor of NAD+-dependent type-I 15-PGDH (IC50 = 26.4 nM; Ki = 5 nM).

  • LKT Labs

    C59 is a PORCN inhibitor that exhibits anticancer chemotherapeutic activity, inhibiting the progression of mammary tumors in vivo by downregulating Wnt signaling. Grade: ≥98%

  • Cayman Chemical

    A reversible, selective, allosteric antagonist of mGluR7 that blocks agonist-induced calcium mobilization (IC50 = 26 nM).

  • Cayman Chemical

    Formal Name: N-?[[(4-?aminophenyl)?amino]?thioxomethyl]?-?4-?(1,?1-?dimethylethyl)?-benzamide CAS Number: 1011301-27-1 Molecular Formula: C18H21N3OS

  • Cayman Chemical

    A polysulfonated naphthylurea that inhibits the binding of calmodulin to recognition sites on the ryanodine receptor-1 (IC50 = 4.9 μM), blocks G protein coupling to GPCRs, and non-selectively antagonizes P2 purinergic receptors (10-100 μM); acts as a non-specific competitor of…

  • Cayman Chemical

    A thiol-reactive fluorogenic probe; used to evaluate or quantify a variety of compounds containing reactive sulfur or thiol groups, including H2S, glutathione, proteins, and nucleotides.

  • Cayman Chemical

    A potent, competitive inhibitor of HMG-CoA reductase (Ki = 0.12 nM).

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