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Inhibits BMP type 1 receptor-induced phosphorylation of SMAD1/5/8 (IC50 = 4.9 nM); shows specificity for ALK1, 2, 3, and 6 (IC50s = 0.8, 0.8, 5.3, and 16.7 nM, respectively) over ALK4 and 5 (IC50s = 101 and 350 nM, respectively).
A substituted diamine that produces rapid bactericidal activity against both Gram-positive and Gram-negative bacteria; displays MIC99 values of 2.9, 11.5, 2.9, and 2.9 µM against S. aureus RN4220, P. aeruginosa PAO1, E. coli ANS1, and MRSA 10082B, respectively.
A potent fluoroquinolone antibiotic.
A substrate for 5’-nucleotide phosphodiesterases.
A potent α1A-adrenoceptor antagonist (Ki = 0.036 nM).
A reversible competitive inhibitor of squalene synthase (Ki = 78 pM in vitro); reduces cholesterol synthesis in HepG2 cells (IC50 = 6 µM) and inhibits hepatic cholesterol synthesis in mice (ED50 = 0.2 mg/kg); also inhibits FPTase and GGPTase-I (IC50s = 216 and...
A fungal toxin that demonstrates selective inhibition of HDAC3/NcoR over HDAC6 (IC50s = 15.8 and 665.1 nM, respectively); has broad spectrum activity against Apicomplexan parasites and exhibits antiproliferative activity against various cancer cell lines (IC50s = 0.13-2.36 μM).
A potent antagonist of the muscarinic M3 receptor (pKi = 9.3); also has a high affinity for the M5 receptor (pKi = 8.9).
A prodrug of the potent, long-acting, and selective AT1 receptor antagonist, candesartan; 4-16 mg/day effectively reduces diastolic blood pressure and has proved useful in the treatment of hypertension and diabetes.
An inhibitor NF-κB activation in vitro and in vivo (IC50 = 5 µM).
An orally active, selective inhibitor of Cdk4 (IC50 = 11 nM) and Cdk6 (IC50 = 16 nM) with antiproliferative activity against retinoblastoma-positive tumor cells, blocking retinoblastoma phosphorylation and inducing G1 arrest; used to demonstrate a role for insulin-activated...
An inhibitor of HMG-CoA reductase (IC50 = 5 nM) that has been shown to be more effective than atorvastatin, simvastatin, or pravastatin in decreasing LDL cholesterol and increasing HDL cholesterol.
CYP1B1 is mainly an extrahepatic enzyme which oxidatively metabolizes both endogenous (steroids; eicosanoids) and exogenous xenobiotics such as polyaromatic hydrocarbons. TMS is a potent and selective inhibitor of CYP1B1, with an IC50 of 6 nM. It is 50-fold selective for the inhibition of CYP1B1...
Antigen: mouse PCSK9 amino acids 152-163 Host: rabbit Cross Reactivity: (+) human, mouse, and rat PCSK9 Applications: ICC and WB PCSK9 is a member of the subtilisin serine protease family with an important role in lipoprotein metabolism. Several gain of function mutations in the PCSK9 gene are...
Formal Name: N-[(1S)-2-hydroxy-1-phenylethyl]-N'-[4-(4-pyridinyl)phenyl]-urea CAS Number: 928320-12-1 Molecular Formula: C20H19N3O2
NAM 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.
A secondary metabolite produced by fungi; inhibits IgE production by mouse B cells in culture (IC50 = 3.6 μM) and dose-dependently (0.4-25 μg/ml) stimulates neuritogenic activity in rat pheochromocytoma PC12 cells; demonstrates nematicidal activity at 300 μg/ml.
An internal standard for the quantification of 12-OAHSA by GC- or LC-MS.
A potent HDAC inhibitor that inhibits HDAC2 and HDAC6 with IC50 values of 0.119 and 434 nM; ineffective against HDAC4 (IC50 = >1,000 nM); inhibits the growth of HCT116 cells and HuT-78 cells (GI50 = 29.4 and 1.4 μM, respectively) more effectively than human dermal...
An SGK1 inhibitor (IC50s = 62 and 103 nM for SGK1 and SGK2, respectively) that demonstrates greater than 30-fold selectivity for SGK1 over Akt and other related kinases; inhibits the androgen-stimulated growth of human prostate carcinoma LNCaP cells (IC50 ~ 1 μM).
A derivative of the natural product artemisinin which effectively kills the malarial parasites P. falciparum and P. vivax (IC50 = 1.3 nM); kills trematodes of the species Schistosoma, providing protection against schistosomiasis.
A proposed anti-inflammatory EPA metabolite that has been shown to promote inflammatory resolution in numerous disease models, including experimental colitis, asthma, atherosclerosis, type 2 diabetes, and HSV-1-induced stromal keratitis.
Antigen: internal central human Bim amino acids Host: rabbit Cross Reactivity: (+) human, mouse, and rat Bim/BOD (IN) Applications: IHC and WB Bim/BOD interacts with diverse members in the pro-survival Bcl-2 sub-family including Bcl-2, -xL, and -w and induces apoptosis.
A noncompetitive allosteric agonist of S1P2 (EC50 = 0.48 μM) that does not display agonist activity towards S1P1, S1P3, S1P4, or S1P5.