Biologically Active Small Molecules

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Cayman Chemical Biologically Active Small Molecules

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  • D-myo-Inositol-1,2,3,4-tetraphosphate (sodium salt)

    Cayman Chemical

    Ins(1,2,3,4)-P4 is one of the many InsP isomers that could act as small, soluble second messengers in the transmission of cellular signals. Ins(1,2,3,4)-P4 exhibits agonist activity at the Ins(1,4,5)-P3 receptor expressed in CHO cells where it induces Ca2+ mobilization with an ED50 value of 18.1…

  • GW 441756

    Cayman Chemical

    A potent, selective inhibitor of TrkA (IC50 = 2 nM); used to clarify the role of TrkA in regulating cell function.

  • Tris-HCl Stock Solution (1 M, pH 7.0)

    Cayman Chemical

    Tris-HCl Stock Solution (1 M, pH 7.0) contains filtered Tris-HCl (1 M, pH7.0). It is ready to use as supplied.

  • KIN-59

    Cayman Chemical

    An allosteric inhibitor of TPase (IC50s = 44 and 67 µM for purified E. coli and human enzymes, respectively); inhibits TPase-induced angiogenesis in a CAM assay; also inhibits the binding of FGF2 to FGFR1.

  • 4-amino Benzamidoxime

    Cayman Chemical

    A synthetic intermediate for pharmaceutical synthesis.

  • CDDO-TFEA

    Cayman Chemical

    A trifluoroethylamide derivative of CDDO that enhances Nrf2 expression and signaling in various models of neurodegeneration; demonstrates anticancer activity against several neuroblastoma cell lines with IC50s = 85-170 nM.

  • Ivermectin B1a aglycone

    Cayman Chemical

    An acid degradation product produced by hydrolysis of the disaccharide unit of ivermectin; inhibits nematode larval development.

  • 1-Aminocyclopropanecarboxylic Acid

    Cayman Chemical

    An intermediate in the synthesis of the plant hormone ethylene; acts as a partial agonist at the glycine-binding site on NMDA receptors (EC50 = 0.7-0.9 µM) and, in the presence of high levels of glutamate, as a competitive antagonist at the glutamate-binding site on NMDA receptors…

  • 3'-Deoxyguanosine

    Cayman Chemical

    A ligand that can be complexed with enzymes, such as purine nucleoside phosphorylase, and receptors, such as G-coupled receptors, in order to study structure-activity relationships; also used to selectively impair transcription.

  • ALLO-1

    Cayman Chemical

    A SMO antagonist that inhibits both wild-type (IC50 = 50 nM) and mutant SMO, including the D473H SMO mutant (IC50s = 300-1000 nM).

  • TH287

    Cayman Chemical

    A selective inhibitor of the nucleotide pool sanitizing enzyme MTH1 (IC50 = 0.8 nM) that kills cancer cell lines (IC50s = 0.8-3.06 µM).

  • trans-2-Decenoic Acid

    Cayman Chemical

    An unsaturated fatty acid found in royal jelly produced from the hypopharyngeal and mandibular gland secretions of honeybees; isolated in conjunction with 10-HDA (Item No. 10976) and both demonstrate weak estrogenic activity, inhibiting binding of 17β-estradiol (Item No. ISO60155) to estrogen…

  • Tetradecyl Phosphonate

    Cayman Chemical

    A pan-antagonist of LPA1-3 receptors (IC50 = 10, 5.5, and 3.1 µM, respectively)

  • BH3I-1

    Cayman Chemical

    A cell permeable inhibitor that blocks the binding of BH3 peptides to Bcl-xL, inducing apoptosis; inhibits interactions of BH3 domain-containing proteins with Bcl-xL, Bcl-2, and Bcl-W, inducing apoptosis in Bcl-2 or Bcl-W expressing cells with Ki values of 43.4 and 124 µM, respectively.

  • RI-2

    Cayman Chemical

    A reversible inhibitor of RAD51 (IC50 = 44.2 µM); inhibits DNA repair and sensitizes cancer cells to cross-linking chemotherapy in vitro at 150 µM.

  • 1-Octadecyl Lysophosphatidic Acid

    Cayman Chemical

    A LPA analog containing stearic acid at the sn-1 position; has potent platelet aggregating activity with an EC50 value of 9 nM.

  • Single-Use Docosahexaenoic Acid (peroxide free)

    Cayman Chemical

    Single-use docosahexaenoic acid (peroxide free) consists of 10 sealed ampules, each containing >1 ml of ethanolic solution of fatty acid at a concentration of 500 µg/ml. Peroxides were removed by silicic acid chromatography. The headspace in each ampule is purged with argon. Single-use…

  • 11-dehydro-2,3-dinor Thromboxane B2

    Cayman Chemical

    11-dehydro-2,3-dinor TXB2 has been identified as a TXB2 metabolite in human urine by GC/MS. The relative abundance is only about one-tenth that of 11-dehydro TXB2, making it unlikely that 11-dehydro-2,3-dinor TXB2 will be used widely as an index of thromboxane synthesis.

  • KRN 633

    Cayman Chemical

    A selective inhibitor of VEGFR kinase activity (IC50s = 170, 160, and 125 nM for VEGFR1, 2, and 3, respectively); suppresses VEGF-dependent activation of MAPK and cell proliferation and demonstrates antitumor and antiangiogenic activity.

  • PtdIns-(5)-P1 (1,2-dioctanoyl) (ammonium salt)

    Cayman Chemical

    A synthetic analog of natural PtdIns featuring C8:0 fatty acids at the sn-1 and sn-2 positions; contains the same inositol and DAG stereochemistry as the natural compound.

  • D-erythro-Sphingosine C-18

    Cayman Chemical

    D-erythro-Sphingosine is formed primarily from the breakdown of ceramide. Sphingosine inhibits PKC and phosphatic acid phosphohydrolase, whereas it activates PLD and DAG kinase. Phosphorylation of sphingosine by SPHK 1 and SPHK 2 produces sphingosine-1-phosphate, a potent bioactive lipid that…

  • BW 755C

    Cayman Chemical

    A dual inhibitor of 5-LO and COX pathways, inhibiting 5-LO, COX-1, and COX-2 (IC50s = 0.75 μM, 0.65 μg/ml, and 1.2 μg/ml, respectively); may also inhibit other LO pathways in vivo.

  • Pterostilbene

    Cayman Chemical

    A naturally-occurring dimethyl ether analog of resveratrol; acts as a powerful antioxidant, suppresses the synthesis of PGE2 from LPS-stimulated human peripheral blood mononuclear cells (IC50 = 1.0 μM), and inhibits cell proliferation (IC50 = ~60 μM); evokes effects that…

  • 5-bromo-3-phenyl Salicylic Acid

    Cayman Chemical

    Selective inhibitor of aldo-keto reductase 1C1 (AKR1C1; Ki = 140 nM) versus AKR1C2 and AKR1C3 (Ki = 1.97 and 21 µM, respectively); does not inhibit AKR1C4 at 100 µM.

  • 4-Methylumbelliferyl Oleate

    Cayman Chemical

    A fluorogenic substrate for acid and alkaline lipases.

  • Fusaric Acid

    Cayman Chemical

    A picolinic acid derivative first isolated from fungi of the genus Fusarium; transformed to an N-methylamide derivative by many plant species.

  • Agomelatine

    Cayman Chemical

    A melatonin receptor MT1 and MT2 agonist and competitive antagonist of human and porcine 5-HT2Creceptors (pKi = 6.2 and 6.4, respectively) as well as human 5-HT2B receptors (pKi = 6.6).

  • CC-401

    Cayman Chemical

    A potent, selective inhibitor of all three JNK isoforms (Ki values range from 25 to 50 nM); bioavailable when delivered by gavage, blocking JNK signaling and renal fibrosis in a rat obstructed kidney model; decreases hepatic necrosis and apoptosis after orthotopic liver transplantation in rats.

  • E-64c

    Cayman Chemical

    A synthetic analog of E-64, a potent and irreversible cysteine protease inhibitor; inhibits cathepsin B and L from rat liver with IC50 values of 8.7 and 3.5 nM, respectively.

  • 4-(1-piperazinyl)-1H-Indole (hydrochloride)

    Cayman Chemical

    4-(1-piperazinyl)-1H-Indole (hydrochloride) is a synthetic intermediate useful for pharmaceutical synthesis.

  • CeMMEC13

    Cayman Chemical

    A selective inhibitor of TAF1 bromodomain 2 (IC50 = 2.1 µM); synergizes with (+)-JQ1 to inhibit the proliferation of THP-1 and H23 lung adenocarcinoma cells.

  • 12-epi Leukotriene B4

    Cayman Chemical

    An isomer of LTB4 which would not be expected to occur in either non-enzymatic hydrolysis products, or in the enzymatic products of LTA4 hydrolase; has significantly reduced activity compared to LTB4.

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