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Key Documents

681675

Sigma-Aldrich

Wortmannin

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

Sinônimo(s):

Wortmannin, KY 12420, MLCK Inhibitor II

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About This Item

Fórmula empírica (Notação de Hill):
C23H24O8
Número CAS:
Peso molecular:
428.43
Número MDL:
Código UNSPSC:
12352200
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.

Nível de qualidade

Ensaio

≥98% (HPLC)

forma

solid

fabricante/nome comercial

Calbiochem®

condição de armazenamento

OK to freeze
protect from light

cor

white to off-white

solubilidade

DMSO: 25 mg/mL

Condições de expedição

ambient

temperatura de armazenamento

−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

chave InChI

QDLHCMPXEPAAMD-QAIWCSMKSA-N

Descrição geral

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.

Ações bioquímicas/fisiológicas

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

Embalagem

Packaged under inert gas

Advertência

Toxicity: Highly Toxic (H)

Reconstituição

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

Outras notas

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.

Informações legais

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

Pictogramas

Skull and crossbones

Palavra indicadora

Danger

Frases de perigo

Classificações de perigo

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

Código de classe de armazenamento

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

Classe de risco de água (WGK)

WGK 3

Ponto de fulgor (°F)

Not applicable

Ponto de fulgor (°C)

Not applicable


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