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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6,931 – 6,945 of 60,533 results

6,931

Cayman Chemical BAY 11-7085, Purity: ≥98%, CAS: 196309-76-9, 25 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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6,932

Cayman Chemical Amlodipine, Purity: ≥98%, CAS: 88150-42-9, 5 g

An L-type calcium channel blocker; inhibits calcium influx in cardiac and vascular smooth muscle; inhibits calcium-induced contractions in depolarized rat aorta (IC50 = 1.9 nM), displaying a slow rate of association and dissociation in isolated vascular and cardiac tissues

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6,933

Cayman Chemical PF-573228, Purity: ≥95%, CAS: 869288-64-2, 50 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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6,934

Cayman Chemical PSI-7977, Purity: ≥98%, CAS: 1190307-88-0, 10 mg

A prodrug form of PSI-7411; inhibits HCV replication in an HCV replicon assay (EC50 = 0.092 µM); inhibits SARS-CoV-2 replication in iPSC-derived human brain cortical organoids at 20 µM

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6,935

Cayman Chemical CYT387, Purity: ≥95%, CAS: 1056634-68-4, 1 mg

An ATP-competitive inhibitor of JAK1 and JAK2 (IC50s = 11 and 18 nM, respectively); causes growth suppression and apoptosis in JAK2-dependent hematopoietic cell lines; is efficacious in a mouse model of JAK2V617F-dependent myeloproliferative neoplasms

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6,936

Cayman Chemical Meclizine (hydrochloride), Purity: ≥98%, CAS: 36236-67-6, 5 mg

A histamine H1 receptor antagonist (Ki = 250 nM); reduces ovalbumin-induced mast cell degranulation, edema and leukocyte influx in rat lung from 2.5-30 mg/kg

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6,937

Cayman Chemical Probenecid, Purity: ≥98%, CAS: 57-66-9, 10 g

An inhibitor of OATs and MRP1 and an agonist of TRPV2; inhibits OAT1, OAT3, and OAT6 (Kis = 6.3, 9.0, and 8.4 µM, respectively), as well as OAT2 (IC50 = 0.67 µM); selective for OATs over OCT1 and OCT2 (IC50s = 1,600 and 1,700 µM, respectively); decreases Fas antibody-induced GSH efflux and staurosporine-induced efflux of the MRP1 substrate calcein in Jurkat cells and decreases apoptotic progression at 7 mM; an agonist of TRPV2 (EC50 = 31.9 µM); induces nociceptive behavior in mouse models of carrageenan- or complete Freund’s adjuvant-induced inflammatory pain at 20 mM in drinking water in combination with doses of carrageenan or CFA that do not provoke pain responses alone

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6,938

Cayman Chemical Meloxicam, Purity: ≥95%, CAS: 71125-38-7, 25 mg

A selective inhibitor of COX-2 (IC50s = 11.8 and 143 μM for COX-2 and COX-1, respectively, in an enzyme activity assay) and an NSAID; reduces croton oil-induced increases in TNF-α and IL-1β mRNA levels and increases IL-10 mRNA levels in cornea in a rabbit model of acute ocular inflammation at 0.03%; inhibits pleural plasma exudation in a carrageenan-induced rat model of pleurisy at 3 mg/kg; reduces PGE2 levels in plasma and right stifle joint synovial fluid in a canine model of unilateral osteoarthritis of the right stifle joint at 0.2 mg/kg

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6,939

Cayman Chemical Dovitinib, Purity: ≥98%, CAS: 405169-16-6, 50 mg

A multi-kinase inhibitor; inhibits FLT3, CSF1R, c-Kit, FGFR1, FGFR3, VEGFR1, -2, and -3, PDFGRα, and PDGFRβ (IC50s = 1, 36, 2, 8, 9, 10, 13, 8, 27, and 210 nM, respectively); inhibits proliferation of human multiple myeloma cell lines expressing mutant, but not wild-type, FGFR3 (IC50s = 90-550 and >2,500 nM, respectively); decreases FGF-induced ERK1/2 phosphorylation and induces apoptosis in patient-derived multiple myeloma cells at 500 nM; inhibits bFGF-induced angiogenesis in a Matrigel™ plug assay in mice at 3-300 mg/kg for 8 days; reduces tumor growth in KM12L4A, DU145, and MV4-11 mouse xenograft models (ED50s = 17, 23, and 3 mg/kg per day, respectively)

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6,940

Cayman Chemical Dapivirine, Purity: ≥98%, CAS: 244767-67-7, 25 mg

A diarylpyrimidine derivative of the potent NNRTI efavirenz; inhibits HIV-1 reverse transcriptase (IC50= 24 nM: impedes the late stages of HIV-1 infection by interfering with HIV-1 Gag-Pol polyprotein processing

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6,941

Cayman Chemical Zanamivir, Purity: ≥98%, CAS: 139110-80-8, 5 mg

An inhibitor of influenza neuraminidase; inhibits neuraminidase activity in clinical isolates of influenza A subtypes H1N1 and H3N2 and influenza B (geometric mean IC50s = 0.73, 1.64, and 11.21 nM, respectively); inhibits replication of influenza A and B in isolated human respiratory epithelial cells (EC90s = <0.01 mg/L and 0.25-0.54 mg/L, respectively); reduces lung viral titers in mice infected with influenza A or B at 0.4 mg/kg intranasally

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6,942

Cayman Chemical Bikinin, Purity: ≥98%, CAS: 188011-69-0, 10 mg

An inhibitor of several ASK isoforms when given at a concentration of 10 µM, leaving residual kinase activity at less than 10% for ASKα, γ, ε, ζ, η, ι, and 20% for ASKθ, without inhibiting isoforms β and δ; activates signaling induced by brassinosteroids

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6,943

Cayman Chemical WAY-262611, Purity: ≥98%, CAS: 1123231-07-1, 1 mg

An inhibitor of Dkk1 that activates the Wnt signaling pathway, stimulating β-catenin/TCF-dependent transcription with an EC50 value of 0.63 µM; has good pharmacokinetic properties and increases trabecular bone formation in ovariectomized rats following oral administration

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6,944

Cayman Chemical Defactinib, Purity: ≥95%, CAS: 1073154-85-4, 5 mg

A dose-dependent inhibitor of FAK, with maximal inhibition of FAK autophosphorylation in cells achieved at 10 µM; restores the chemosensitivity of taxane-resistant cells to paclitaxel; orally bioavailable, inhibiting FAK and augmenting paclitaxel action against ovarian cancer cell tumors in mice

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6,945

Cayman Chemical Spermidine, Purity: ≥98%, CAS: 124-20-9, 10 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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Bioactive Small Molecules

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