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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7,111 – 7,125 of 60,533 results

7,111

Cayman Chemical VU0361737, Purity: ≥98%, CAS: 1161205-04-4, 10 mg

A selective PAM of mGluR4, displaying EC50 values of 110 and 240 nM for rat and human receptors, respectively; passes the blood-brain barrier to act centrally in rats

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7,112

Cayman Chemical Purvalanol A, Purity: ≥98%, CAS: 212844-53-6, 5 mg

A potent, cell-permeable, and selective inhibitor of CDKs (IC50s = 4, 70, 35, 850, and 75 nM for cdc2/cyclin B, Cdk2/cyclin A, Cdk2/cyclin E, Cdk4/cyclin D1 and Cdk5-p35, respectively); reversibly arrests synchronized cells in the G1 and G2 phase of the cell cycle, inhibiting both cell proliferation and cell death

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7,113

Cayman Chemical Stattic, Purity: ≥98%, CAS: 19983-44-9, 25 mg

A selective inhibitor of STAT3 activation, dimerization and nuclear translocation (IC50 = 5.1 μM at 37°C); 10 μM induces apoptosis in STAT3-dependent breast cancer cells

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7,114

Cayman Chemical Phleomycin, Purity: ≥95% (mixture of phleomycins), CAS: 11006-33-0, 50 mg

A glycopeptide antibiotic with diverse biological activities; induces chromosomal breaks in S. cerevisiae at 1 to 2 µM; reduces proliferation, DNA synthesis, and the percentage of cells entering mitosis in HeLa cells at 5 or 10 µg/ml; increases survival time in combination with LS34 in an Ehrlich mouse ascites tumor model at 1 mg/kg per day; has been used as an antibiotic selection agent for successfully transformed cells in genetic engineering experiments

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7,115

Cayman Chemical 9-cis Retinoic Acid, Purity: ≥90%, CAS: 5300-03-8, 10 mg

Potently activates all isoforms of RAR (Ki = 0.5-27 nM) as well as RXR isoforms (Ki = 3.8-12 nM)

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7,116

Cayman Chemical Loratadine, Purity: ≥98%, CAS: 79794-75-5, 5 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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7,117

Cayman Chemical (R)-PFI-2 (hydrochloride), Purity: ≥95%, CAS: 1627607-87-7, 5 mg

A potent, cell-permeable inhibitor of SET7/9 (IC50 = 2 nM) that demonstrates greater than 1,000-fold selectivity over a panel of 18 other methyltransferases

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7,118

Cayman Chemical UNC0379, Purity: ≥95%, CAS: 1620401-82-2, 10 mg

A selective inhibitor of the lysine methyltransferase SET8 (IC50 = 7.3 µM; Kd = 18.3 µM)

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7,119

Cayman Chemical MLS-573151, Purity: ≥98%, CAS: 10179-57-4, 1 mg

A specific, cell permeable inhibitor of Cdc42 (IC50 = 2 μM); has no effect on other GTPases, including the related Rho family members RhoA, Rac1, and Rac2

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7,120

Cayman Chemical Ezetimibe, Purity: ≥98%, CAS: 163222-33-1, 25 mg

An inhibitor of NPC1L1 (Ki = 220 nM); reduces cholesterol absorption in hamsters fed a high-cholesterol diet (ED50 = 0.04 mg/kg per day); reduces the levels of helper T cells and memory T cells from the blood of heart transplant recipients at 346 nM

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7,121

Cayman Chemical GIT 27, Purity: ≥98%, CAS: 6501-72-0, 50 mg

An immunomodulatory compound that inhibits inflammatory antigen presentation both in vitro and in preclinical in vivo models of autoimmune diseases; targets macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, macrophage migration inhibitory factor, and inducible nitric oxide synthase-mediated nitric oxide generation

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7,122

Cayman Chemical ML-243, Purity: ≥98%, CAS: 1426576-80-8, 5 mg

An inhibitor of cancer stem cells, displaying 32-fold selective inhibition of a breast cancer stem cell-like cell line (EC50 = 2.0 µM) over a control (mammary epithelial) cell line (EC50 = 64 µM)

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7,123

Cayman Chemical ML-179, Purity: ≥98%, CAS: 1883548-87-5, 1 mg

A potent inverse agonist of LRH-1 (IC50 = 320 nM) with maximum efficacy of 40% repression; inactive at the related SF1 transcriptional activator; alters the expression of haptoglobin, SAA1, and SAA4, induces the death of MDA-MB-231 breast cancer cells, and inhibits the StAR promoter (IC50 = 2.12 µM)

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7,124

Cayman Chemical TPT-260 (hydrochloride), Purity: ≥95%, CAS: 2076-91-7, 5 mg

A thiophene thiourea derivative that acts as a chaperone to stabilize the retromer complex against thermal denaturation (Kd = ~5 µM); dose-dependently increases the level of retromer proteins, redirects APP from the endosome, and reduces the formation of pathogenic APP in cultured hippocampal neurons

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7,125

Cayman Chemical XCT790, Purity: ≥98%, CAS: 725247-18-7, 10 mg

A selective inverse agonist of ERRα (IC50 = ~300-500 nM); blocks ERRα/PGC-1α-dependent signaling, suppressing the expression of MAO A and B; induces proteasomal degradation of ERRα and potentiates the degradation of ERα by fulvestrant

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Bioactive Small Molecules

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