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Wortmannin Catalog No.GC12338

A PI3K inhibitor,selective and irreversible

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10mM (in 1mL DMSO)
$80.00
In stock
5mg
$61.00
In stock
10mg
$88.00
In stock
20mg
$142.00
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Sample solution is provided at 25 µL, 10mM.

Quality Control

Quality Control & SDS

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Protocol

Cell experiment [1]:

Cell lines

v-sis NIH 3T3 cells

Preparation method

The solubility of this compound in DMSO is > 21.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

1.3 μM

Applications

In PDGF-stimulated v-sis NIH 3T3 cells, Wortmannin almost completely inhibited the formation of Ptdlns-3-phosphates. However, in resting cells, Wortmannin showed no effect on the pattern of phospholipids.

Animal experiment [2]:

Animal models

Immunodeficient mice bearing orthotopic human pancreatic cancer xenografts

Dosage form

0 ~ 0.7 mg/kg; i.v.; 0 ~ 4 hrs

Applications

In orthotopic human pancreatic cancer xenografts, PKB/Akt phosphorylation was inhibited by Wortmannin in a time- and dose-dependent manner, and reached a plateau at 4 hrs and at 0.7 mg/kg. Meanwhile, the levels of PKB/Akt phosphorylation were decreased maximally by ~ 50%.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Powis G, Bonjouklian R, Berggren M M, et al. Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Research, 1994, 54(9): 2419-2423.

[2]. Ng SS, Tsao MS, Nicklee T, Hedley DW. Wortmannin inhibits pkb/akt phosphorylation and promotes gemcitabine antitumor activity in orthotopic human pancreatic cancer xenografts in immunodeficient mice. Clin Cancer Res. 2001 Oct;7(10):3269-75.

Chemical Properties

Cas No. 19545-26-7 SDF
Chemical Name (1S,6bR,9aS,11R,11bR)-1-(methoxymethyl)-9a,11b-dimethyl-3,6,9-trioxo-3,6,6b,7,8,9,9a,10,11,11b-decahydro-1H-furo[4,3,2-de]indeno[4,5-h]isochromen-11-yl acetate
Canonical SMILES O=C1[C@](C([H])([H])[C@@]2([H])OC(C([H])([H])[H])=O)(C([H])([H])[H])[C@](C([H])([H])C1([H])[H])([H])C(C3=O)=C2[C@]4(C([H])([H])[H])C5=C3OC([H])=C5C(O[C@]4([H])C([H])([H])OC([H])([H])[H])=O
Formula C23H24O8 M.Wt 428.43
Solubility ≥ 21.42mg/mL in DMSO Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
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Background

Wortmannin is a selective and irreversible inhibitor of phosphatidylinositol-3-kinase with IC50 value of 1.9nM [1].

Wortmannin is a microbial product. It is produced by a fungal strain, Talaromyces wortmannin KY12420 and is screened out as a potent inhibitor of myosin light chain kina (MLCK). Wortmannin inhibits MLCK as directly interacting with the catalytic domain but not the calmodulin or the regulatory domains. It is found to be a non-competitive inhibitor. The IC50 value of wortmannin for MLCK is 1.9μM. Wortmannin inhibits the phosphorylation and contraction of myosin light chain in rat aort. As an inhibitor of MLCK, wortmannin is developed as vasodilators and anti-inflammatory agent [2].

Wortmannin is also found to be an inhibitor of PI3K with IC50 of 1.9nM in antiphosphotyrosine immunoprecipitates from Swiss 3T3 cells. The inhibition mode is noncompetitive with respect to ATP. Wortmannin is a highly selective inhibitor of PI3K. It has no inhibition effect on Ptdlns-4-kinase, protein kinase C, c-src protein tyrosine kinase and phosphoinositide-specific phospholipase C [1].

References:
[1] Powis G, Bonjouklian R, Berggren M M, et al. Wortmannin, a potent and selective inhibitor of phosphatidylinositol-3-kinase. Cancer Research, 1994, 54(9): 2419-2423.
[2] Nakanishi S, Kakita S, Takahashi I, et al. Wortmannin, a microbial product inhibitor of myosin light chain kinase. Journal of Biological Chemistry, 1992, 267(4): 2157-2163.