Catalog No.S2758 Synonyms: KY 12420
Molecular Weight(MW): 428.43
Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.
Cited by 18 Publications
5 Customer Reviews
L3.6pl cells at 6,000 cells per well were incubated in MEM with 5% FBS in triplicate in a 96-well culture plate and then treated alone with 5 umol/L BMS-777607, 10 umol/L wortmannin, or with BMS-777607 in combination with individual inhibitors. Polyploidy was examined under BK71 Olympus microscope and photographed 72 hours after treatment.
Mol Cancer Ther 2014 13(1), 37-48. Wortmannin purchased from Selleck.
The effects of KITL on the differentiation of stem Leydig cells. Seminiferous tubules were cultured in the presence of various concentrations of KITL (K) without (C) or with PI3K inhibitor wortmannin (W) for 21 days. Panel A, KITL (0-100 ng/ml); Panel B, KITL (K) alone or with W (100 nM), K1 = KITL 1 ng/ml, K100 = 100 ng/ml. Medium testosterone (T) levels were measured. Mean ± SEM, n = 4-8. Identical letters indicate no significant difference between two groups at P < 0.05. W:Wortmannin
Mol Cell Endocrinol, 2017, 444:1-8. Wortmannin purchased from Selleck.
Cell growth inhibition of non-small cell lung carcinoma (NSCLC) by inhibitor of phosphoinositide 3-kinases (PI3Ks) Wortmannin. NCI-H460 and its multi-drug resistant (MDR) counterpart NCI-H460/R were subjected to Wortmannin. According to the results obtained, the effect of Wortmannin is dependent on the existence of MDR in the range of tested concentrations.
2014 Dr.Milica Pesic from Institute for Biological Research. Wortmannin purchased from Selleck.
Purity & Quality Control
Choose Selective PI3K Inhibitors
|Description||Wortmannin is the first described PI3K inhibitor with IC50 of 3 nM in a cell-free assay, with little selectivity within the PI3K family. Also blocks autophagosome formation and potently inhibits DNA-PK/ATM with IC50 of 16 nM and 150 nM in cell-free assays.|
The inhibition of MLCK by Wortmannin is not affected by calmodulin or peptide substrat, while reduced by high concentration of ATP. Wortmannin directly interacts with the catalytic domain of MLCK and leads to an irreversible loss of the enzyme activity. Wortmannin has no inhibitory to cAMP-dependent protein kinase, cGMP-dependent protein kinase, and calmodulin-dependent protein kinase II, and has little effect on protein kinase C activity.  Wortmannin inhibits N-formylmethionyl-leucylphenylalanine (fMLP)-stimulated PtdInsP3 (phosphatidylinositol 3,4,5-trisphosphate) formation with IC50 of 5 nM and this inhibition is completely abolished when pretreated with 100 nM Wortmannin in human neutrophils, with increased PtdInsP2 levels and no effects on cellular PtdInsP and PtdIns contents. Wortmannin could develop oscillatory changes in F-actin content and does not inhibit fMLP-stimulated actin polymerization in neutrophils.  Wortmannin irreversibly inhibits phosphatidylinositol 3-kinase (PI3-kinase) activity with binding to the 110-kDa protein (IC50 of 3 nM) and has no effect PI4-kinase in RBL-2H3 cells. Wortmannin also inhibits both Fc epsilon RI-mediated histamine secretion and leukotriene release, with no effect on the activation of the tyrosine kinase Lyn.  Wortmannin completely abolishes the insulin-induced hexose uptake in isolated rat adipocytes at 0.1 μM, without impairing isoproterenol-stimulated lipolytic activity.  Wortmannin suppresses insulin-induced production of nitric oxide by 50% at 500 nM in human umbilical vein endothelial cells, which is in response to IGF-1.  Wortmannin suppresses DNA double strand break (DSB) repair and has no effect on DSB levels or the kinetics of single strand break (SSB) repair in Chinese hamster ovary cells at 50 μM. Wortmannin could potentiate ionizing radiation (IR)-induced cytotoxicity with no toxicity by itself.  Wortmannin inhibits polo-like kinase (PLK1) activity IC50 of 24 nM in intact G2/M-arrested cells.  Wortmannin increases Toll-like receptor (TLR)-mediated accumulation of IL-6 in human macrophages with EC50 of 50 nM. Meanwhile Wortmannin significantly enhances TLR-mediated inducible nitric-oxide synthase (iNOS) expression and nitrite accumulation in mouse macrphages. Wortmannin activates the nuclear factor-κB and up-regulates the cytokine mRNA production.  Wortmannin also inhibits Polo-like kinase (PlK) 1 and PlK3, which play important roles in mitosis. Wortmannin treatment could lead to a reduction in phosphorylation of p53 on serine 20 induced by DNA damage.  Wortmannin suppresses hyaluronan-induced Akt phosphorylation and cell motility/migration in SW1990 cells. 
|In vivo||Wortmannin inhibits peritoneal metastasis of SW1990 in mice at 1 mg/kg, without any weight loss.  Wortmannin inhibits phosphatidylinositide 3-kinase-protein kinase B (PKB)/Akt phosphorylation in both normal tissues (lung, heart and brain homogenates) and tumor tissue in mice, without mortality or acute toxicity at 0.7 mg/kg. Combination with LY188011, Wortmannin significantly increases apoptosis and inhibit tumor growth in orthotopic tumor, while both monotherapy could not. |
-  Nakanishi S, et al. J Biol Chem, 1992, 267(4), 2157-2163.
-  Arcaro A, et al. Biochem J, 1993, 296(Pt 2), 297-301.
-  Yano H, et al. J Biol Chem, 1993, 268(34), 25846-25856.
-  Okada T, et al. J Biol Chem, 1994, 269(5), 3568-3573.
-  Zeng G, et al. J Clin Invest, 1996, 98(4), 894-898.
-  Boulton S, et al. Carcinogenesis, 1996, 17(11), 2285-2290.
-  Liu Y, et al. Chem Biol, 2005, 12(1), 99-107.
-  Hazeki K, et al. Mol Pharmacol, 2006, 69(5), 1717-1724.
-  Liu Y, et al. J Biol Chem, 2007, 282(4), 2505-2511.
-  Teranishi F, et al. Cancer Sci, 2009, 100(4), 770-777.
-  Ng SS, et al. Clin Cancer Res, 2001, 7(10), 3269-3275.
-  Sarkaria JN, et al. Cancer Res, 1998, 58(19), 4375-4382.
|In vitro||DMSO||85 mg/mL (198.39 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )
* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
Molecular Weight Calculator
Enter the chemical formula of a compound to calculate its molar mass and elemental composition:
Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2
Instructions to calculate molar mass (molecular weight) of a chemical compound:
To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.