Biologically Active Small Molecules, 1.0 mg
-
CX-5461
Cayman ChemicalA selective inhibitor of RNA polymerase I-driven transcription of rRNA (IC50s = 142, 113, and 54 nM in HCT116, A375, and MIA PaCa-2 tumor cells, respectively); demonstrates in vivo antitumor activity against human solid tumors in mouse xenograft models.
-
DAPI (hydrochloride)
Cayman ChemicalA fluorescent probe which is commonly used to stain DNA and chromosomes for fluorescent microscopy and flow cytometry applications; characterized by ultraviolet (max 358 nm) excitation and blue (max 461 nm) emission wavelengths.
-
2-Chloroadenosine
Cayman ChemicalA metabolically stable adenosine analog that binds to adenosine A1, A2A, and A3 receptors with Ki values of 300, 80, and 1,900 nM, respectively; anticonvulsive activity in a rat model of generalized seizures.
-
Eggmanone
Cayman ChemicalA selective inhibitor of PDE4 (IC50 = 72 nM) that antagonizes the Hedgehog signaling pathway; activates localized PKA signaling, which, in turn, regulates Gli processing and translocation.
-
-
Valsartan
Cayman ChemicalA nonpeptide angiotensin II receptor antagonist which selectively and insurmountably inhibits the angiotensin II AT1 receptor subtype (IC50 = 2.7 nM); does not alter PPARγ activity.
-
7-keto Cholesterol
Cayman ChemicalA bioactive sterol that can affect cholesterol homeostasis, membrane properties and cell survival; inhibits CYP7A1 with an IC50 = ~ 1 µM; can be used as a standard in the determination of cholesterol derivatives by GC-MS or HPLC.
-
11-keto-ß-Boswellic Acid
Cayman Chemical11-keto-β-Boswellic acid is a naturally occurring pentacyclic triterpene isolated from the gum resin exudate from the stem of the tree B. serrata (frankincense). Boswellic acids are specific, non-redox inhibitors of leukotriene synthesis via 5-lipoxygenase that demonstrate anti-inflammatory…
-
(S)-p38 MAP Kinase Inhibitor III
Cayman ChemicalA methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 µM in vitro); potently blocks the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 µM, respectively).
-
(±)-Cromakalim
Cayman ChemicalAn activator of the ATP-sensitive K+ channels that displays anti-ischemic (EC25 = 8.9 μM) and cardioprotective (IC50 = 0.03 μM) effects in rat hearts.
-
IQ-1
Cayman ChemicalA cell-permeable compound that maintains long-term mouse ESC pluripotency; allows ESCs to form embryoid bodies that continue to express markers of pluripotency when used at 4 µg/ml with Wnt3a; blocks the interaction of Nkd with a subunit of PP2A.
-
N-Arachidonyl Maleimide
Cayman ChemicalNAM is a potent, irreversible inhibitor of MAGL or MAGL-like activity in rat cerebellar membranes, exhibiting an IC50 value of 140 nM. Inhibition of MAGL by the sulfhydryl-reactive maleimide group of NAM suggests a critical cysteine residue is present in the substrate-binding site of the enzyme.
-
Ochratoxin A
Cayman ChemicalA mycotoxin produced by A. ochraceus, A. carbonarius, and P. verrucosum that is commonly found as a food contaminant (Tolerable Weekly Intake = 100 ng/kg body weight per day); triggers nephropathy, induces renal adenomas, and initiates skin tumors through events involving oxidative stress,…
-
Ac-YVAD-pNA
Cayman ChemicalA colorimetric substrate whose amino acids YVAD have been shown to be a preferred cleavage site for caspase-1 and -4.
-
-
RAD140
Cayman ChemicalAD140 is an orally bioavailable, nonsteroidal selective androgen receptor modulator (SARM) that binds to the androgen receptor with a Ki value of 7 nM. At 0.03-0.3 mg/kg, it has been shown to stimulate muscle weight increase without affecting prostate or seminal vesicle in castrated male rats. At…
-
U-18666A
Cayman ChemicalA cell permeable drug that inhibits cholesterol trafficking from late endosomes/lysosomes to the ER, but not to the plasma membrane.
-
Ponasterone A
Cayman ChemicalAn insect hormone used as an inducer of ecdysone-inducible mammalian expression systems.
-
BSI-201
Cayman ChemicalAn irreversible, noncompetitive inhibitor of PARP1 that disrupts binding between PARP1 and DNA by interacting with the DNA binding domain; produces rapid apoptosis in the various cancer cell (IC50s = 40-128 μM).
-
ML-204
Cayman ChemicalML-204 selectively blocks transient receptor potential canonical 4 (TRPC4) channels (IC50s = 0.96 and 2.6 μM in fluorescent and electrophysiological assays, respectively). It exhibits 19-fold selectivity against TRPC6 and 9-fold selectivity against TRPC5 and does not affect TRPV1,…
-
MRS1523
Cayman ChemicalA selective adenosine A3 receptor antagonist (Kis = 18.9 and 113 nM for human and rat A3 receptors, respectively, versus Kis = 15.6 and 2.05 µM for rat A1 and A2A receptors, respectively).
-
Olmesartan Medoxomil
Cayman ChemicalA prodrug that is metabolized in vivo to RNH-6270, a nonpeptide angiotensin II antagonist that potently inhibits angiotensin binding to the AT1 receptor (IC50 = 7.7 nM) without affecting binding to the AT2 receptor; reduces blood pressure.
-
Verteporfin
Cayman ChemicalA photosensitizer used during photodynamic therapy to eliminate abnormal blood vessels in the eye that are associated with conditions such as macular degeneration; also inhibits autophagosome formation by directly targeting and modifying p62, a scaffold and adaptor protein that binds both…
-
N-Oleoyl Dopamine
Cayman ChemicalA selective, endogenous TRPV1 agonist that is a “hybrid” analog, which incorporates components of both the AEA-like and dopamine neurotransmitter pathways; binds to the human recombinant TRPV1 (Ki = 36 nM) with equipotency to that of capsaicin and slightly more potency than that of…
-
Resminostat (hydrochloride)
Cayman ChemicalAn orally bioavailable inhibitor of HDAC1, HDAC3, and HDAC6 (IC50s = 43-72 nM), resulting in hyperacetylation of histone H4 in multiple myeloma cells; abrogates cell growth and strongly induces apoptosis in multiple myeloma cells (IC50s = 2.5-3 µM); dose-dependently…
-
-
CAY10512
Cayman ChemicalCAY10512 is a substituted trans-stilbene analog of resveratrol that is 100-fold more potent as measured by antioxidant activity. The IC50 value for inhibition of TNFα-induced activation of NF-κB by CAY10512 is 0.15 µM compared to 20 µM by resveratrol.
-
DY 131
Cayman ChemicalA selective ERRβ/γ receptor agonist (EC50 = 130 nM); used to potentiate ERRγ-induced growth inhibition in LNCaP and DU145 prostate cancer cell lines.
-
Ampkinone
Cayman ChemicalA small molecule activator of AMPK that stimulates functional activation of AMPK in cultured muscle cells (EC50 = 4.3 μM), enhancing glucose uptake by 3.2-fold; 10 mg/kg up-regulates the activity of AMPK in the liver and muscle of diet-induced obese mice, enhancing insulin sensitivity and…
-
CWHM12
Cayman ChemicalCWHM12 is an analog of RGD peptide (Item No. 14501), a tripeptide that inhibits integrin-ligand interactions in studies related to cell adhesion, migration, growth, and differentiation. CWHM12 selectively inhibits αv integrins (IC50s = 1.8, 0.8, 61, 1.5, and 0.2 nM for…
-
Ingenol-3-angelate
Cayman ChemicalA hydrophobic diterpene ester that rapidly induces cell death in proliferating keratinocytes through plasma membrane and mitochondrial disruption; causes inflammation due, at least in part, to activation of PKC, leading to antibody-dependent cellular cytotoxicity.
-
N-(2-phenylethyl)-Indomethacin amide
Cayman ChemicalN-2PIA is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2. N-2PIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.06 and 0.125 µM, respectively. It is over 400 times less potent as an inhibitor of…