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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6,901 – 6,915 of 60,533 results

6,901

Cayman Chemical Ibotenic Acid, Purity: ≥98%, CAS: 2552-55-8, 5 mg

A neuroexcitatory amino acid that functions as a NMDA and metabotropic glutamate receptor agonist; used to induce brain lesions in animal models of cognitive dysfunction

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6,902

Cayman Chemical MLN2238, Purity: ≥95%, CAS: 1072833-77-2, 10 mg

A 20S proteasome inhibitor (IC50 = 3.4 nM in a cell-free assay for the β5 subunit) and an active metabolite of MLN9708; selective for the β5 subunit over the β1 and β2 subunits (IC50s = 31 and 3,500 nM, respectively); binds caseinolytic protease P (Kd = 5,700 nM); prevents MRSA-induced hemolysis of isolated ovine erythrocytes (EC50 = 3,600 nM); inhibits the proliferation of A375, H460, HCT116, and HT-29 cells (IC50s = 20, 58, 19, and 52 nM, respectively); inhibits osteoclastogenesis in PBMCs isolated from patients with multiple myeloma (IC50 = 4.8 nM); reduces tumor growth in a CWR22 prostate cancer mouse xenograft model at 14 mg/kg

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6,903

Cayman Chemical XE 991 (hydrochloride), Purity: ≥98%, CAS: 122955-13-9, 5 mg

A blocker of KCNQ channels that potently inhibits KCNQ1 and 2 homomeric channels (IC50 = 0.75 and 0.71 µM, respectively) as well as KCNQ2+3 heteromultimers (IC50 = 0.6 µM); shows good in vivo potency and duration of action

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6,904

Cayman Chemical LT175, Purity: ≥98%, CAS: 862901-87-9, 5 mg

A dual PPARα/γ ligand that displays partial agonism toward PPARγ (EC50s = 0.22, 0.26, and 0.48 µM for hPPARα, mPPARα, and hPPARγ, respectively); improves glucose homeostasis in diet-induced insulin resistant mice

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6,905

Cayman Chemical 11-deoxy Prostaglandin E2, Purity: ≥99%, CAS: 35536-53-9, 5 mg

11-deoxy PGE2 is a stable, synthetic analog of PGE2. In contrast to PGE2 which has bronchodilation effects, 11-deoxy PGE2 is a powerful bronchoconstrictor and is 5 to 30 times more potent than PGF2α in the contraction of human respiratory tract smooth muscle in vitro.{483}

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6,906

Cayman Chemical UNC0642, Purity: ≥95%, CAS: 1481677-78-4, 1 mg

A selective inhibitor of G9a and GLP methyltransferases that competitively inhibits binding of H3K9 substrates with a Ki = 3.7 nM; reduces H3K9 dimethylation levels in MDA-MB-231 and PANC-1 cells (IC50s = 110 and 40 nM, respectively); displays improved pharmacokinetic properties relative to UNC0638

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6,907

Cayman Chemical Zinquin ethyl ester, Purity: ≥98%, CAS: 181530-09-6, 5 mg

A cell-permeable, quinolone-based fluorescent probe used as a zinc indicator (excitation 368 nm, emission 490 nm); used to monitor intracellular zinc fluxes associated with apoptosis

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6,908

Cayman Chemical MKT-077, Purity: ≥95%, CAS: 147366-41-4, 1 mg

A cationic rhodacyanine dye that inhibits the Hsp70 family of chaperones; demonstrates antiproliferative activity against cancer cell lines (EC50s = 1.4-2.2 µM in vitro) through its ability to abrogate the interaction of the chaperone with the tumor suppressor p53

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6,909

Cayman Chemical Nevirapine, Purity: ≥98%, CAS: 129618-40-2, 25 mg

An NNRTI; binds to HIV-1 reverse transcriptase and inhibits RNA plus-strand initiation (IC50 = 0.45 μM); prevents seroconversion and viremia in a chimpanzee model of HIV-1 infection

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6,910

Cayman Chemical JNJ-26854165, Purity: ≥98%, CAS: 881202-45-5, 5 mg

An antagonist of MDM2 that suppresses the growth of cancer cell lines expressing wild-type p53 (IC50 values range from 240-440 nM); orally bioavailable, having anti-proliferation as well as apoptotic actions in various tumor models; affects multiple signaling pathways

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6,911

Cayman Chemical Coelenterazine 400a, Purity: ≥95%, CAS: 70217-82-2, 5 mg

A bisdeoxy derivative of coelenterazine that produces an emission maximum of 395 nm following conversion by Renilla luciferase; commonly used in BRET2 protocols to evaluate protein-protein interactions

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6,912

Cayman Chemical Z-FA-FMK, Purity: ≥98%, CAS: 197855-65-5, 5 mg

An irreversible inhibitor of cysteine proteases, including cathepsins B, L, and S, cruzain, and papain; inhibits effector caspases-2, -3, -6, and -7 (IC50 = 6-32 µM) without affecting the initiator caspases-8 and -10; can be used both in cells and in vivo

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6,913

Cayman Chemical SCH 79797 (hydrochloride), Purity: ≥98%, CAS: 1216720-69-2, 5 mg

A non-peptide antagonist of PAR1; blocks binding of haTRAP (IC50 = 70 nM) as well as platelet aggregation induced by either haTRAP or α-thrombin (IC50 = 0.3 and 3 µM, respectively); has no activity against PAR2, PAR4, or other receptors involved in platelet activation

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6,914

Cayman Chemical R-848, Purity: ≥98%, CAS: 144875-48-9, 10 mg

An immune response modifier that acts as a ligand of TLR7 and 8; demonstrates potent anti-tumor and anti-viral properties and has been used to study the innate immune response to viral infections

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6,915

Cayman Chemical IPBT-5CA, Purity: ≥98%, CAS: 306935-41-1, 50 mg

A selective agonist of GPR109B (HCA3; EC50 = 400 nM) that displays no activity at GPR109A (HCA2)

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Bioactive Small Molecules

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