Biologically Active Small Molecules, 25 mg, Chemicals
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RVX-208
Cayman ChemicalA selective antagonist of BET bromodomains, binding with 10-100-fold higher affinity for BD2 (IC50 = 0.04-0.28 µM) over BD1 (IC50 = 1.8-3.1 µM), which causes selective release of BET proteins from chromatin; increases the expression of ApoA1 and reduces…
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A-967079
Cayman ChemicalA potent, selective, and bioavailable inhibitor of the TRPA1 channel, with IC50 values of 67 and 289 nM for the human and rat isoforms, respectively; attenuates cold allodynia following nerve injury and suppresses neuronal activity in response to mechanical stimulation.
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N-Decanoyl p-Nitroaniline
Cayman ChemicalDepNA is one of several nitroaniline fatty acid amides which can be used to measure FAAH activity.{8928} FAAH is a relatively unselective enzyme in that it accepts a variety of amide head groups other than the ethanolamine of its endogenous substrate AEA. It also will hydrolyze fatty acid amides…
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CAY10566
Cayman ChemicalA potent, selective inhibitor of Stearoyl-CoA desaturase 1 that demonstrates IC50 values of 4.5 and 26 nM in mouse and human enzymatic assays, respectively.
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(-)-Blebbistatin
Cayman ChemicalA selective cell-permeable inhibitor of non-muscle myosin II ATPases, inhibiting Mg-ATPase activity and in vitro motility of non-muscle myosin IIA and IIB for several species (IC50 = 0.5-5.0 μM), while poorly inhibiting smooth muscle myosin (IC50 = 80 μM).
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GNF-5
Cayman ChemicalA selective allosteric inhibitor of Bcr-Abl (IC50s = 4.52, 0.38, and 0.93 µM against Bcr-Abl mutants G250E, E255V, and M351T, respectively); displays additive inhibitory activity against T315I Bcr-Abl mutants both in in vitro assays and in a recalcitrant T315I Bcr-Abl mutant mouse…
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SR 49059
Cayman ChemicalA selective, nonpeptide antagonist of the vasopressin V1a receptor (Ki = 1.1-6.3 nM in human); inhibits arginine vasopressin-induced human platelet aggregation with an IC50 value of 3.7 nM.
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Phosphoramidon (sodium salt)
Cayman ChemicalA natural and potent inhibitor of NEP and NEP2, with Ki values of 2 nM for both enzymes; also a weak inhibitor of the related zinc metalloprotease ECE (Ki = 3.5 µM); has little or no effect on a variety of other proteases.
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Bazedoxifene acetate
Cayman ChemicalAn indole-based SERM that binds to both ERα (IC50 = 26 nM) and ERβ (IC50 = 99 nM); antagonizes 17β-estradiol-dependent and hormone-independent growth of breast cancer cell proliferation (80% reduction with 10 nM) in a manner related to cell cycle arrest and…
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ONX 0914
Cayman ChemicalA selective inhibitor of the β5i (LMP7) subunit of the immunoproteasome (IC50s = 65 and 73 nM for mouse and human, respectively) that demonstrates significantly weaker activity at the β5 subunit of the constitutive proteasome (IC50s = 0.92 and 1.04 µM for mouse…
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TBB
Cayman ChemicalAn 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.
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U-18666A
Cayman ChemicalA cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.
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trans-ISRIB
Cayman ChemicalA symmetric bis-glycolamide that inhibits the eIF2α phosphorylation-mediated unfolded protein response (IC50 = 5 nM in a cell-reporter assay); passes through the blood-brain barrier and significantly enhances learning and memory in mice and rats.
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PTC-124
Cayman ChemicalA nonaminoglycoside that has been reported to selectively induce ribosomes to read through premature nonsense stop signals on mRNA, thus allowing the production of full-length, functional proteins (IC50 = 7 nM); 60 mg/kg s.c. injection or 0.3-0.9 mg/ml orally has been shown to restore…
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A-23187
Cayman ChemicalA divalent cation ionophore, commonly used to facilitate the movement of Ca2+ into cells, triggering the activation of intracellular calcium-dependent pathways; also used to produce apoptosis through calcium overload, as occurs during hypoxic or oxidative stress.
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5'-Deoxy-5'-methylthioadenosine
Cayman ChemicalAn intermediate in the generation of adenine and methionine that is produced by the decarboxylation of SAM; a potent agonist of adenosine receptors (Kis = 0.15, 1.13, 13.9, and 0.68 μM for A1, A2A, A2B, and A3, respectively); inhibits several enzymes at higher concentrations.
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SU 9516
Cayman ChemicalA potent inhibitor of several CDKs with selectivity for Cdk2 (IC50s = 22, 40, and 200 nM for Cdk2/cyclin A, Cdk1/cyclin B, and Cdk4/cyclin D1); has anti-proliferative and pro-apoptotic activity in tumor cells.
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Meropenem
Cayman ChemicalAn intravenous β-lactam antibiotic that is effective against Gram-positive and Gram-negative bacteria (MICs range from 0.008-0.13 µg/ml); highly resistant to degradation by β-lactamases.
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SNC 80
Cayman ChemicalA selective non-peptide agonist of the δ-opioid receptor (Ki = 0.18 nM, IC50 = 2.73 nM) that is over 2,000-fold less effective at the μ-opioid receptor; effectively activates µ/δ receptor heteromers (EC50 = 52.8 nM) but not κ/δ or μ/κ heteromers.
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AG-370
Cayman ChemicalA selective inhibitor of PDGF receptor kinase with an IC50 value of20 µM in human bone marrow; inhibits the EGF receptor with an IC50 value of 820 µM.
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CYM 5541
Cayman ChemicalA selective agonist of S1P3 (EC50 = 72-132 nM); less effectively activates S1P1 (EC50 = 28-38 µM) and is ineffective at S1P2, S1P4, and S1P5 as well as a panel of other receptors, ion channels and transporters.
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Cyclothiazide
Cayman ChemicalA benzothiadiazide that acts as a potentiator of AMPA receptors, positively modulating its response to glutamic acid (EC50 = 3.8 µM); also a negative modulator of GABAA receptors, reversibly inhibiting both evoked and spontaneous inhibitory postsynaptic currents (IC50 =…
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Propidium Iodide
Cayman ChemicalA fluorescent probe commonly used to identify dead cells; excitation at 488-535 nm and emission maximum of 617 nm.
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Nevirapine
Cayman ChemicalA non-nucleoside reverse transcriptase inhibitor that binds to viral reverse transcriptase and blocks polymerase activity by preventing RNA plus-strand initiation (IC50s = ~ 0.45 to 0.9 μM).
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DMXAA
Cayman ChemicalA tumor vascular disrupting agent, inducing apoptosis in tumor vascular endothelium resulting in necrosis at the tumor core; potently activates the STING/TBK1/IRF3 signaling pathway in mouse leukocytes, inducing type-I-IFN production; inhibits VEGFR1 and VEGFR2 (IC50 = 119 and 11…
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NASPM (hydrochloride)
Cayman ChemicalA synthetic analog of Joro spider toxin that blocks GluR2-lacking, Ca2+-permeable AMPA receptors (IC50 = 0.33 µM) at -60 mV but not at +40 mV; protects against ischemia-induced neuronal cell death by preventing influx of toxic levels of Ca2+ into injured neurons.
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1-Octadecyl Lysophosphatidic Acid (sodium salt)
Cayman ChemicalA LPA analog containing stearyl alcohol at the sn-1 position; exhibits platelet aggregating activity with an EC50 value of 9 nM versus an EC50 value of 177 nM for 1-octadecanoyl LPA.
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TG101348
Cayman ChemicalA small molecule inhibitor of JAK2 (IC50 = 6 nM) and the related kinases FLT3 (IC50 = 25 nM) and RET (IC50 = 17 nM) with significantly less potent activity against JAK3 (IC50 = 169 nM); inhibits the growth of Ba/F3 cells expressing JAK2V617F or MPLW515L…
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Carmustine
Cayman ChemicalA nitrogen mustard β-chloro-nitrosourea compound used as an alkylating agent to form interstrand crosslinks in DNA, which leads to cancer cell cytotoxity and apoptosis; also reported to inhibit glutathione reductase, thioredoxin reductase, and lipoamide dehydrogenase.
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(S)-Duloxetine (hydrochloride)
Cayman ChemicalA potent inhibitor of serotonin and norepinephrine reuptake (Kis = 4.6 and 15.6 nM, respectively, for rat synaptosomes); less effectively inhibits dopamine reuptake (Ki = 369 nM); effective in cells, tissues, and in vivo.