Biologically Active Small Molecules
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WH-4-023
Cayman ChemicalA selective inhibitor of the Src family of non-receptor tyrosine kinases (IC50s = 2 and 6 nM for Lck and Src, respectively); used in combination with PD 0325901, CHIR99021, and SB-590885 to support self-renewal of naïve human embryonic stem cells.
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Abacavir Sulfate
LKT LabsGuanosine analog and inhibitor of RT, guanylyl cyclase, and telomerase used to treat HIV infection. Grade: ≥98%
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Lenalidomide
Cayman ChemicalAn analog of thalidomide that, at 10 μM, alters gene expression and cell viability in a range of cancer cell lines; induces proliferation and enhances the functional capacity of T-lymphocytes, amplifying co-stimulatory signaling pathways.
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TIQ-A
Cayman ChemicalA PARP1 inhibitor (IC50 = 450 nM) that displays neuroprotective effects in cultured mouse cortical neurons; also inhibits eosinophilic infiltration into airways of OVA-challenged mice and induces the regression of atherosclerotic plaques in high-fat fed ApoE(-/-) mice.
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MLCK Inhibitor Peptide 18
Cayman ChemicalA selective, cell permeable inhibitor of MLCK (IC50 = 50 nM).
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CRT0066101 (hydrochloride)
Cayman ChemicalA pan inhibitor PKD (IC50s = 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively); blocks cell proliferation, induces apoptosis, and reduces the viability of pancreatic cancer cells both in vitro and in vivo.
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Chlorpromazine Hydrochloride
LKT LabsChlorpromazine is a phenothiazine that exhibits antipsychotic, antidepressant, anxiolytic, neuroprotective, and anticancer chemotherapeutic activities. Chlorpromazine inhibits D1/2/3/4 receptors, 5-HT1/2 receptors, a1/2-adrenergic receptors, and M1/2 muscarinic acetylcholine receptors (mAChRs).…
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ONO-8711
Cayman ChemicalA potent and selective competitive antagonist of the EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1, respectively); effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer; suppresses pain and acid-induced HCO3- secretion in the stomach.
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Tetrodotoxin
Cayman ChemicalA potent marine-derived neurotoxin that reversibly inhibits the inward sodium current through NaV channels (IC50s = 4.1 and 5.2 nM, respectively, in frog muscle and squid axon; Kd = 1.8 nM in rat brain), blocking nerve and muscle action potentials.
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Costunolide
Cayman ChemicalA natural sesquiterpene lactone that reduces growth (EC50 = 3-35 μM) and induces apoptosis in assorted cancer cell lines; inhibits the activation of Akt (15 μM) in endometriotic epithelial cells and STAT3 activation in THP-1 cells (EC50 = 10 μM); inhibits telomerase…
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KC7F2
Cayman ChemicalAn inhibitor of HIF-1α protein translation; suppresses phosphorylation of two key regulators of protein synthesis, eukaryotic translation initiation factor 4E binding protein 1 (4EBP1) and p70 S6 kinase; cytotoxic to a variety of cancer cell lines with an IC50 value of 15-25 µM.
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Biotin-XX hydrazide
Cayman ChemicalA biotinylating reagent that contains two aminohexanoic spacers to increase the efficiency of avidin-binding by alleviating steric hindrance.
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cis-ACCP
Cayman ChemicalA reversible and competitive inhibitor of type IV collagen-specific MMP-2 and MMP-9 with preference towards MMP-2 (IC50 = 4 and 20 µM, respectively).
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N-Acetyl-D-Leucine
LKT LabsN-acetyl-D-leucine is a D-amino acid that is deacylated in bacteria by d-aminoacylase enzymes. D-amino acids inhibit bacterial biofilm formation when they are incorporated into the cell wall. Compounds such as N-acetyl-D-leucine induce release of amyloid fibers that link cells together in the…
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ß-Amyloid Peptide (1-42), rat
LKT LabsAmyloid-ß (Aß) is a peptide cleavage product of amyloid precursor protein (APP) that is often used as a biomarker in Alzheimer’s disease. Misfolded Aß oligomers instigate conformation changes in other, normally folded Aß oligomers, increasing the number of misfolded proteins and eventually forming…
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Celecoxib
Cayman ChemicalAn anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits COX-2 (IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively; displays chemopreventive activity in multiple tumor types via proapoptotic effects independent of its capacity to block COX-2.
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IBMX
Cayman ChemicalA widely-used non-specific inhibitor of cAMP and cGMP PDEs (IC50 = 19, 50, 18, 13, 32, 7, and 50 μM for PDE1, PDE2, PDE3, PDE4, PDE5, PDE7, and PDE11, respectively).
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Spiro-MeOTAD
Cayman ChemicalA stable and efficient hole-transport material in organic light-emitting devices and in ssDSSCs; yields high ssDSSC efficiency due to its excellent pore-filling property into mesoporous titania films.
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Cefaclor Monohydrate
LKT LabsCefaclor is a second generation β-lactam cephalosporin antibiotic. Cefaclor exhibits antibacterial efficacy against gram positive and gram negative bacteria, inhibiting penicillin binding proteins to prevent peptidoglycan synthesis and bacterial cell wall formation. Cefaclor also displays…
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Bafilomycin A1
Cayman ChemicalA selective, reversible inhibitor of vacuolar H+-ATPases (V-ATPases), blocking these proton pumps in mammalian, plant, or fungal cells with an IC50 value in the 4-400 nM range; also inhibits autophagy by preventing vacuolar acidification necessary for autophagosome maturation.
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cis-trismethoxy Resveratrol
Cayman ChemicalA potent anti-mitotic drug that is 100-fold more active than resveratrol at inhibiting the growth of human colon cancer Caco-2 cells; inhibits tubulin polymerization in a dose-dependent manner (IC50 = 4 μM) and enzymes involved in the synthesis of the polyamines, putrescine, and spermidine.
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2-Hydroxypropyl-ß-cyclodextrin
Cayman ChemicalA cyclic oligosaccharide containing seven D-(+)-glucopyranose units that is widely used to improve the aqueous solubility of various compounds, especially those containing a phenyl group.
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Adefovir
LKT LabsAdefovir is an antiviral prodrug that displays immunomodulatory activity. Adefovir is an acyclonucleotide analog that inhibits viral DNA polymerase, acting as a DNA chain terminator. Adefovir is primarily used to treat hepatitis B infection, but also displays activity against retroviruses. Adefovir…
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Nullscript
Cayman ChemicalAn analog of scriptaid that lacks scriptaid’s HDAC inhibitory effects; used as a negative control in experiments involving scriptaid.
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5-fluoro 203
Cayman ChemicalA cytotoxic compound that at 1 µM activates aryl hydrocarbon receptor signaling, inducing transcription of cytochrome P450 1A1, which leads to the formation of DNA adducts and cell cycle arrest; can increase the levels of ROS as well as activate JNK, ERK, and p38MAPK in certain ovarian,…
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Tunicamycin
Cayman ChemicalA specific inhibitor of N-linked glycoslylation that blocks the first step of glycoprotein synthesis and induces protein unfolding; impairs the function of several receptor tyrosine kinases, including EGFR, ErbB2, ErbB3, IGF-IR, and ALK; radiosensitizes glioma and pancreatic adenocarcinoma cells to…
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CAY10505
LKT LabsCAY10505 is an inhibitor of p110? PI3K. CAY10505 increases endothelial relaxation, normalizes levels of glutathione, nitrate, and nitrite, and alters the vascular endothelial lining in hypertensive rats, improving vascular endothelial dysfunction. Grade: ≥98%
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Ciprofloxacin is a second generation fluoroquinolone antibiotic that exhibits antibacterial activity against both gram negative and gram positive bacteria. Ciprofloxacin inhibits DNA gyrase and topoisomerase IV, preventing DNA replication.
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Spectinomycin (hydrochloride hydrate)
Cayman ChemicalAn aminocyclitol antibiotic active against Gram-negative and Gram-positive bacteria; inhibits protein synthesis by binding to the 30S ribosomal subunit and interfering with peptidyl tRNA translocation.
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2-hydroxy Flutamide
Cayman ChemicalThe major metabolite formed during the metabolism of the non-steroidal antiandrogen flutamide by cytochrome P450 isoforms CYP1A2 and CYP3A4; inhibits the binding of testosterone to the nuclear androgen receptor (IC50 = ~300-900), blocking the expression of AR target genes.
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BMS 833923
Cayman ChemicalAn orally bioavailable inhibitor of Smo; blocks binding of BODIPY cyclopamine (IC50 = 21 nM) and inhibits Gli activation in cell lines that express wild-type Smo or activated mutant forms of Smo (IC50s = 6-35 nM); inhibits Shh pathway activity and prevents tumor growth in…