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Key Documents

681675

Sigma-Aldrich

Wortmannin

≥98% (HPLC), solid, PI3-kinase inhibitor, Calbiochem

Synonyme(s) :

Wortmannin, KY 12420, MLCK Inhibitor II

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About This Item

Formule empirique (notation de Hill):
C23H24O8
Numéro CAS:
Poids moléculaire :
428.43
Numéro MDL:
Code UNSPSC :
12352200
Nomenclature NACRES :
NA.77

product name

Wortmannin, Wortmannin, CAS 19545-26-7, is a cell-permeable, potent, selective, and irreversible inhibitor of PI3-Kinase (IC₅₀ = 5 nM). Does not affect any upstream signaling events.

Niveau de qualité

Pureté

≥98% (HPLC)

Forme

solid

Fabricant/nom de marque

Calbiochem®

Conditions de stockage

OK to freeze
protect from light

Couleur

white to off-white

Solubilité

DMSO: 25 mg/mL

Conditions d'expédition

ambient

Température de stockage

−20°C

InChI

1S/C23H24O8/c1-10(24)30-13-7-22(2)12(5-6-14(22)25)16-18(13)23(3)15(9-28-4)31-21(27)11-8-29-20(17(11)23)19(16)26/h8,12-13,15H,5-7,9H2,1-4H3/t12-,13+,15+,22-,23-/m0/s1

Clé InChI

QDLHCMPXEPAAMD-QAIWCSMKSA-N

Description générale

A cell-permeable, fungal metabolite that acts as a potent, selective, and irreversible inhibitor of phosphatidylinositol 3-kinase in purified preparations and cytosolic fractions (IC50 = 5 nM). Blocks the catalytic activity of PI 3-kinase without affecting the upstream signaling events. Preincubation of fibroblasts with wortmannin abolishes PDGF-mediated Ins(3,4,5)P3 formation (IC50 = 5 nM). Also blocks the metabolic effects of insulin in isolated rat adipocytes without affecting the insulin receptor tyrosine kinase activity. Inhibits MAP kinase activation induced by platelet activating factor in guinea pig neutrophils (200 - 300 nM). Also inhibits other kinases such as myosin light chain kinase (IC50 = 200 nM) and PI 4-kinase at concentrations higher than that required for inhibition of PI 3-kinase. Also blocks phospholipase D. A 10 mM (1 mg/233 µl) solution of Wortmannin (Cat. No. 681676) in DMSO is also available.
A fungal metabolite that acts as a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) in purified preparations and cytosolic fractions (IC50 = 5 nM). Preincubation of fibroblasts with wortmannin abolishes PDGF-mediated Ins(3,4,5)P3 formation (IC50 = 5 nM). Blocks the catalytic activity of PI 3-kinase without affecting the upstream signaling events. Also blocks the metabolic effects of insulin in isolated rat adipocytes without affecting the insulin receptor tyrosine kinase activity. Inhibits MAP kinase activation induced by platelet activating factor in guinea pig neutrophils (0.2-0.3 µM). Inhibits osteoclastic bone resorption. Inhibits other kinases, such as myosin light chain kinase (IC50 = 200 nM) and PI 4-kinase at concentrations 100-fold higher than that required for the inhibition of PI 3-kinase. Also blocks phospholipase D.

Actions biochimiques/physiologiques

Cell permeable: yes
Primary Target
phosphatidylinositol-3-kinase
Product does not compete with ATP.
Reversible: no
Target IC50: 5 nM against phosphatidylinositol 3-kinase; 5 nM against PDGF-mediated Ins(3,4,5)P3 formation; 200 nM against myosin light chain kinase

Conditionnement

Packaged under inert gas

Avertissement

Toxicity: Highly Toxic (H)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 2 months at -20°C.

Autres remarques

Cross, M.J., et al. 1995. J. Biol. Chem. 270, 25352.
Nakamura, I., et al. 1995. FEBS Lett. 361, 79.
Ferby, I.M., et al. 1994. J. Biol. Chem. 269, 30485.
Okada, T., et al. 1994. J. Biol. Chem. 269, 3568.
Wymann, M.P. and Arcaro, A. 1994. Biochem. J.298, 517.
Arcaro, A. and Wymann, M.P. 1993. Biochem. J.296, 297.
Nakanishi, S., et al. 1992. J. Biol. Chem. 267, 2157.
Bonser, R.W., et al. 1991. Br. J. Pharmacol.103, 1237.
Due to the nature of the Hazardous Materials in this shipment, additional shipping charges may be applied to your order. Certain sizes may be exempt from the additional hazardous materials shipping charges. Please contact your local sales office for more information regarding these charges.

Informations légales

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Pictogrammes

Skull and crossbones

Mention d'avertissement

Danger

Mentions de danger

Classification des risques

Acute Tox. 1 Inhalation - Acute Tox. 1 Oral - Acute Tox. 2 Dermal

Code de la classe de stockage

6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


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