Biologically Active Small Molecules

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Biologically Active Small Molecules

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  • Paliperidone

    Cayman Chemical

    A potent antagonist of dopamine receptors (IC50s = 1.0 and 0.9 nM for D2 and D3, respectively);,also avidly binds α1- and α2-adrenergic receptors, histamine H1 receptor, and serotonin (5-HT) receptors 5-HT1D and 5-HT2A (Kis = 10, 80, 3.4, 19, 1.2 nM, respectively).

  • Triptolide

    Cayman Chemical

    The major bioactive constituent of T. wilfordii Hook F., with known antiproliferative, immunosuppressive, anti-inflammatory, antifertility, and antipolycystic kidney disease effects; inhibits human DCTPP1 (Ki = 168 μM; IC50 = 7-10 nM) and COX-2 (IC50 = 0.04 μM).

  • 2-Arachidonoyl Glycerol

    Cayman Chemical

    An endogenous agonist of the CB1 and CB2 receptors; it is the most abundant molecular species of monoacylglycerol found in rat brain.

  • MK-2206 (hydrochloride)

    Cayman Chemical

    An orally active, allosteric Akt inhibitor (IC50s = 5, 12, and 65 nM for Akt1, 2, and 3, respectively); inhibits cell proliferation of human cancer cell lines synergistically in combination with other topoisomerase inhibitors, antimetabolites, antimicrotubule agents, DNA cross-linkers or growth…

  • JC-1

    Cayman Chemical

    A membrane-permeable cationic dye that is used to study mitochondrial integrity in the context of cellular apoptosis; changes fluorescence characteristics with alteration in mitochondrial transmembrane potential, a very early event in apoptosis.

  • A-769662

    Cayman Chemical

    A small molecule thienopyridone that activates AMPK directly in cell-free assays (EC50 = 116 nM) and intact cells by allosterically activating AMPK and inhibiting its dephosphorylation on Thr172.

  • 7-Methylguanine

    Cayman Chemical

    A metabolite of the natural purine base that is generated by DNA methylation and has been used as a probe of protein-DNA interactions and for DNA sequencing methods; carcinogenic biomarker for cigarette smoking that is detectable in urine.

  • Streptavidin:SureLight® B-PE

    Cayman Chemical

    Spectral Characteristics: Visible absorption maximum = 545 nm, Emission maximum = 572 nm; This streptavidin with a SureLight® B-Phycoerythrin probe, binds biotinylated targets.

  • Nicardipine (hydrochloride)

    Cayman Chemical

    A dihydropyridine L-type calcium channel antagonist that displays antihypertensive and antianginal activity; selectively inhibits adenosine A3 receptors (Ki = 3.25 µM) and CYP3A4 catalytic activity (IC50 = 0.148 µM); activates TRPA1 channels, producing an increase in Ca2+…

  • TBB

    Cayman Chemical

    An ATP/GTP-competitive inhibitor of CK2 (IC50 = 900 µM for rat liver CK2); less potently inhibits CCK2/cyclin A, GSK3β, and phosphorylase kinase (IC50 = 15.6, 11.2, and 8.7 mM, respectively); much less effective against a range of other kinases.

  • Aureusimine B

    Cayman Chemical

    A natural pyrazinone produced by certain fungi and by Staphylococcus spp. that inhibits calpain in a casein hydrolysis assay (IC50 = 1.3 µM), contributes to S. aureus infection in mice, and alters human keratinocyte gene expression.

  • Finasteride

    Cayman Chemical

    A 4-azasteroid analog of testosterone that competitively blocks type II 5α-reductase activity (IC50 = 4.2 nM) with 100-fold greater affinity than for the type I enzyme; used in the treatment of benign prostatic hyperplasia, decreasing human prostatic dihydrotestosterone levels by…

  • Bicyclo Prostaglandin E1

    Cayman Chemical

    Bicyclo Prostaglandin E1 (bicyclo PGE1) is a stable, base-catalyzed transformation product of the PGE1 metabolite 13,14-dihydro-15-keto PGE1. Bicyclo PGE1 is a stable, base-catalyzed transformation product of the PGE1 metabolite 13,14-dihydro-15-keto PGE1. 13,14-dihydro-15-keto PGE1 itself is a…

  • 16-phenoxy Prostaglandin F2a ethyl amide

    Cayman Chemical

    A prodrug of a potent FP receptor agonist.

  • FK-409

    Cayman Chemical

    FK-409 is a NO donor. It liberates NO in a time-dependent manner with a half-life of approximately 40 minutes in phosphate buffer (pH 7.4) at 37°C. The IC50 for the inhibition of platelet aggregation is 4.9 µM.

  • N-Benzylacetamidine (hydrobromide)

    Cayman Chemical

    A potent inhibitor of iNOS (IC50 = 0.20 μM), with over 1,000-fold selectivity compared to eNOS (IC50 = 350 μM).

  • VS-5584

    Cayman Chemical

    A purine analog that inhibits mTOR (IC50 = 37 nM) and PI3K (IC50s = 16, 68, 25, and 42 nM for the α, β, γ, and δ isoforms, respectively); demonstrates broad anti-proliferative sensitivity leading to tumor growth inhibition in human tumor models.

  • Dihomo-?-Linolenoyl PAF C-16

    Cayman Chemical

    Dihomo-γ-linolenoyl PAF C-16 is a PAF analog which contains dihomo-γ-linolenoate at the sn-2 position rather than the acetate moiety found in PAF C-16. The biological activities of dihomo-γ-linolenoyl PAF C-16 are not known at present, but may be similar to arachidonoyl PAF C-16…

  • Prothionamide

    Cayman Chemical

    A bactericidal thioamide effective against M. tuberculosis (MIC = ~0.5 µg/ml), M. leprae (MIC = 0.8-1.6 mg/L), and M. avium; inhibits mycolic acid biosynthesis (Ki = 2 nM).

  • JAK2 Inhibitor V

    Cayman Chemical

    A selective inhibitor of the autophosphorylation of wild type and V617F mutant forms of JAK2, displaying IC50 values between 10 and 30 µM; blocks the proliferation of erythroleukemia cells and human hematopoietic progenitor cells expressing JAK2-V617F.

  • Pseudolaric Acid B

    Cayman Chemical

    A diterpene acid isolated from the bark of P. kaempferi, a traditional Chinese medicinal plant; has anti-fungal activities and diverse effects that are relevant to cancer therapy.

  • LEE011

    Cayman Chemical

    A selective cyclin D1/CDK4 and cyclin D3/CDK6 inhibitor (nm IC50) that inhibits retinoblastoma protein phosphorylation, which prevents CDK-mediated G1-S phase transition, arresting the cell cycle in the G1 phase, suppressing DNA synthesis, and inhibiting cancer cell growth; reduces…

  • SB 202190

    Cayman Chemical

    A selective, potent, cell-permeable inhibitor of p38 MAP kinases, inhibiting p38α (SAPK2A, MAPK14) and p38β (SAPK2B, MAPK11) with IC50 values of 50 and 100 nM, respectively; at 10 μM, has negligible effects on a range of other kinases, including other MAP kinases (ERKs, JNKs).

  • Rucaparib (phosphate)

    Cayman Chemical

    A potent, cell-permeable inhibitor of PARP-1 (Ki = 5.5 μM); arrests tumor growth in mice bearing epigenetically silenced BRCA1 UACC3199 xenograft tumors.

  • Sp-8-bromo-Cyclic AMPS (sodium salt)

    Cayman Chemical

    A cell-permeable cAMP analog with improved lipophilicity compared to the PKA activators, 8-bromo-cAMP and Sp-cyclic AMPS; not readily degraded by PDE.

  • (±)-4-hydroxy Propranolol (hydrochloride)

    Cayman Chemical

    An active metabolite of propranolol, inhibiting β1- and β2-adrenergic receptors with KD values of 2.4 and 5.8 nM, respectively; comparable to propranolol in potency in antagonizing the effects of isoprenaline on heart rate and blood pressure in cats and dogs.

  • cis,cis-Octadeca-9,12-dienol

    Cayman Chemical

    A polyunsaturated fatty alcohol produced by the reduction of linoleic acid.

  • PHOME

    Cayman Chemical

    A fluorogenic, sensitive substrate for human sEH which displays good aqueous stability and solubility making it ideal for high throughput screening programs.

  • 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…

  • KL002

    Cayman Chemical

    A cell-permeable carbazolic compound which directly interacts with and stabilizes CRY1 and CRY2, preventing ubiquitin-dependent degradation while lengthening the circadian period (IC50 = 1.2-5.9 μM).

  • GW 441756

    Cayman Chemical

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

  • Tephrosin (synthetic)

    Cayman Chemical

    A rotenoid that exhibits antineoplastic and piscicidal activities; inhibits the NADH:ubiquinone oxidoreductase (IC50 = 98 nM) and induces ornithine decarboxylase activity (IC50 = 147 nM).

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