Bioactive Small Molecules

A vast array of small, non-peptide, organic compounds that are biologically active. Products include receptor antagonists, molecular probes, metabolites, GPCR ligands, neurotransmitters, ion channel modulators, and signaling activators and inhibitors.

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7,411 – 7,425 of 60,533 results

7,411

Cayman Chemical TTNPB, Purity: ≥98%, CAS: 71441-28-6, 1 mg

An analog of retinoic acid that potently and selectively activates retinoic acid receptors (EC50s = 21, 4, and 2.4 nM for RARα, RARβ, and RARγ, respectively); used to study RAR action in epidermal cell proliferation, embryogenesis, and stem cell differentiation

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7,412

Cayman Chemical BAY 11-7085, Purity: ≥98%, CAS: 196309-76-9, 5 mg

An irreversible inhibitor of IκBα phosphorylation, preventing activation of NF-κB by cytokines and lipopolysaccharide (IC50 = 10 μM); blocks gene expression that is regulated through the classical pathway of NF-κB activation and in this way blocks apoptosis, cell adhesion, and inflammation

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7,413

Cayman Chemical PF-573228, Purity: ≥95%, CAS: 869288-64-2, 10 mg

A selective FAK inhibitor (IC50s = 4 and 30-100 nM for a purified recombinant catalytic fragment of FAK and in cultured cells, respectively) that can inhibit chemotactic and haptotactic migration of cells as well as prevent focal adhesion turnover

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7,414

Cayman Chemical Aprepitant, Purity: ≥98%, CAS: 170729-80-3, 1 mg

An antiemetic and NK1 antagonist (Ki = 3 nM; IC50 = 0.09 nM for the human receptor); selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3); prevents substance P-induced plasma extravasation into the esophagus of guinea pigs at 1 mg/kg; reduces NK1-agonist-induced foot tapping in gerbils

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7,415

Cayman Chemical JNJ-7706621, Purity: ≥98%, CAS: 443797-96-4, 10 mg

A dual inhibitor of Cdks and Aurora kinases; inhibits Cdk1/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk3/cyclin E, Cdk4/cyclin D1, Cdk6/cyclin D1, Aurora A, and Aurora B in vitro (IC50s = 9, 4, 3, 58, 253, 175, 11, and 15 nM, respectively); blocks the growth of cancer cells in vitro and in vivo

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7,416

Cayman Chemical CASIN, Purity: ≥95%, CAS: 425399-05-9, 5 mg

A Cdc42 GTPase inhibitor (IC50 = 2 µM for inhibiting actin assembly in PIP2-stimulated actin polymerization assays) that has been used to explore the role of Cdc42 in the division, survival, and differentiation of hematopoietic stem cells

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7,417

Cayman Chemical FK-3311, Purity: ≥98%, CAS: 116686-15-8, 1 mg

A COX-2 inhibitor; inhibits LPS-induced TxB2 production (IC50 = 316 nM) in vitro; inhibits adjuvant-induced arthritis (ED50 = 0.29 mg/kg) in rats without causing gastrointestinal irritation; alleviates ischemia-repurfusion injury in canine liver and rat lung in vivo

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7,418

Cayman Chemical ML-178, Purity: ≥95%, CAS: 1355026-47-9, 5 mg

A selective S1P4 agonist (EC50 = 46.3 nM)

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7,419

Cayman Chemical ML-211, Purity: ≥95%, CAS: 2205032-89-7, 25 mg

A dual inhibitor of LYPLA1 (IC50 = 17 nM) and LYPLA2 (IC50 = 30 nM); also inhibits the serine hydrolase ABHD11 (IC50 = 10 nM)

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7,420

Cayman Chemical ELR510444, Purity: ≥95%, CAS: 1233948-35-0, 25 mg

An inhibitor of tubulin polymerization (IC50 = 10 μM); binds to tubulin at the colchicine binding site; induces microtubule depolymerization in A-10 cells (EC50 = 21 nM); inhibits growth in a cancer cell line panel (IC50s = 9-43 nM) via formation of multiple spindles and induction of mitotic arrest; reduces tumor size in an MDA-MB-231 breast cancer mouse xenograft model in a dose-dependent manner; inhibits HIF-1α in RCC4 cells in a concentration-dependent manner

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7,421

Cayman Chemical NVP-ADW742, Purity: ≥98%, CAS: 475488-23-4, 1 mg

A selective IGF-1R inhibitor (IC50 = 0.17 µM); inhibits tumor proliferation both in vitro and in a mouse model of multiple myeloma

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7,422

Cayman Chemical BI-D1870, Purity: ≥95%, CAS: 501437-28-1, 10 mg

A cell permeable, ATP-competitive inhibitor of the four vertebrate isoforms of RSK, RSK1-4 (IC50s = 31, 24, 18, and 15 nM, respectively); also significantly inhibits PLK1, Aurora B, MELK, and MST2 at 100 nM

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7,423

Cayman Chemical Spermidine, Purity: ≥98%, CAS: 124-20-9, 25 g

An endogenous polyamine; inhibits the activity of the human inward-rectifying potassium channel Kir2.3 in a patch-clamp assay at 25 µM; induces autophagy in HeLa cells at 100 µM; increases the lifespan of D. melanogaster, yeast, and C. elegans; reduces demyelination of the optic nerve and disease severity in a mouse model of EAE when administered in the drinking water at 30 mM; reduces increases in blood pressure, left ventricular posterior wall thickness, and heart weight in salt-sensitive Dahl rats fed a high-salt diet

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7,424

Cayman Chemical Loratadine, Purity: ≥98%, CAS: 79794-75-5, 50 mg

A non-sedating antihistamine that acts as a selective inverse agonist of peripheral histamine H1 receptors (Ki = 35 nM); inhibits the release of LTC4 (IC50 = 8 µM) and histamine (IC50 = 11 µM) from rodent mast cells and inhibits allergic bronchospasm in guinea pigs (ED50 = 0.40 mg/kg)

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7,425

Cayman Chemical Remodelin (hydrobromide), Purity: ≥98%, CAS: 1622921-15-6, 5 mg

A 2-thiazolylhydrazone derivative that, at 10 µM, improves nuclear architecture, chromatin organization, and survival of both cells lacking lamin A and cells from patients with progeria; inhibits NAT10

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Bioactive Small Molecules

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