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12-338 Wortmannin, (PI3 Kinase inhibitor)

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12-338
1 mg  
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Overview

Replacement Information
Description
Catalogue Number12-338
Brand Family Upstate
Trade Name
  • Upstate
DescriptionWortmannin, (PI3 Kinase inhibitor)
OverviewWortmannin, a fungal metabolite, is a cell-permeable, irreversible inhibitor of phosphatidylinositol 3 kinase (PI3 Kinase) with an IC50 of 5nM. It blocks the catalytic activity of PI3-Kinase without affecting upstream signaling events such as insulin receptor tyrosine kinase activity. Wortmannin also inhibits the activities of myosin light chain kinase and PI4-Kinase at concentrations a hundred times higher than those required to inhibit PI3-Kinase.
References
Product Information
HS Code3822 19 90
Presentation1mg of lyophilized powder packaged under inert gas. White to off-white powder.
Quality LevelMQ100
Applications
ApplicationThe Wortmannin, (PI3 Kinase inhibitor) controls the biological activity of PI3 Kinase. This small molecule/inhibitor is primarily used for Biochemicals applications.
Key Applications
  • Kinase Assay
Biological Information
Entrez Gene Number
Entrez Gene SummaryReceptor-regulated class I phosphoinositide 3-kinases (PI3Ks) phosphorylate the membrane lipid phosphatidylinositol 4,5-bisphosphate (PtdIns(4,5)P2) to PtdIns(3,4,5)P3, which in turn recruits and activates cytosolic effectors involved in proliferation, survival, or chemotaxis. PIK3R5 is a PI3K regulatory subunit (Brock et al., 2003 [PubMed 12507995]).[supplied by OMIM]
Gene Symbol
  • PIK3R5
  • P101-PI3K
  • FOAP-2
  • F730038I15Rik
Protein TargetPI3Kγ
Target Sub-FamilyPI3K/PI4K
UniProt Number
UniProt SummaryFUNCTION: SwissProt: Q8WYR1 # Regulatory subunit of the PI3K gamma complex.
SIZE: 880 amino acids; 97348 Da
SUBUNIT: Heterodimer of a catalytic subunit (PIK3CG/p120) and a regulatory (PIK3R5a/p101) subunit. Interacts with G beta gamma proteins.
SUBCELLULAR LOCATION: Nucleus (By similarity). Cytoplasm (By similarity). Membrane; Peripheral membrane protein (By similarity).
TISSUE SPECIFICITY: Highly expressed in leukocytes, followed by spleen, lymph node, thymus ans bone marrow.
DOMAIN:SwissProt: Q8WYR1 The heterodimerization region allows the binding to the catalytic subunit.
SIMILARITY:
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Quality AssuranceRoutinely evaluated by kinase assay.
Purity: ≥95% by HPLC.
Molecular Formula: C23H24O8
Molecular Weight: 428.4
Usage Statement
  • Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
Storage and Shipping Information
Storage ConditionsProtect from light. Stable for 2 years as supplied at -20°C. Following reconstitution aliquot and store at -20°. The DMSO/ethanol stock solutions are stable for 1-3 months at -20°C.
Packaging Information
Material Size1 mg
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalog Number GTIN
12-338 04053252405112

Documentation

Wortmannin, (PI3 Kinase inhibitor) SDS

Title

Safety Data Sheet (SDS) 

Wortmannin, (PI3 Kinase inhibitor) Certificates of Analysis

TitleLot Number
Wortmannin (PI3 Kinase inhibitor) - 2153577 2153577
Wortmannin (PI3 Kinase inhibitor) - 2375500 2375500
Wortmannin (PI3 Kinase inhibitor) 2930507
Wortmannin (PI3 Kinase inhibitor) 2960506
Wortmannin (PI3 Kinase inhibitor) 3098899
Wortmannin (PI3 Kinase inhibitor) 2475643
Wortmannin (PI3 Kinase inhibitor) 2886360
Wortmannin (PI3 Kinase inhibitor) - 2202511 2202511
Wortmannin (PI3 Kinase inhibitor) - 2290358 2290358
Wortmannin (PI3 Kinase inhibitor) - 2558391 2558391

References

Reference overviewApplicationPub Med ID
Akt/protein kinase B isoforms are differentially regulated by epidermal growth factor stimulation
Okano, J., et al
J Biol Chem, 275:30934-42 (2000)  2000

Immunoblotting (Western)10908564 10908564
Wortmannin, a specific inhibitor of phosphatidylinositol-3 kinase, blocks osteoclastic bone resorption.
Nakamura, I, et al.
FEBS Lett., 361: 79-84 (1995)  1995

Show Abstract
7890044 7890044
Wortmannin and its structural analogue demethoxyviridin inhibit stimulated phospholipase A2 activity in Swiss 3T3 cells. Wortmannin is not a specific inhibitor of phosphatidylinositol 3-kinase.
Cross, M J, et al.
J. Biol. Chem., 270: 25352-5 (1995)  1995

Show Abstract
7592698 7592698
Wortmannin as a unique probe for an intracellular signalling protein, phosphoinositide 3-kinase.
Ui, M, et al.
Trends Biochem. Sci., 20: 303-7 (1995)  1995

Show Abstract
7667888 7667888
Platelet-derived growth factor-induced phosphatidylinositol 3-kinase activation mediates actin rearrangements in fibroblasts.
Wymann, M and Arcaro, A
Biochem. J., 298 Pt 3: 517-20 (1994)  1994

Show Abstract
8141762 8141762
Wortmannin inhibits mitogen-activated protein kinase activation induced by platelet-activating factor in guinea pig neutrophils.
Ferby, I M, et al.
J. Biol. Chem., 269: 30485-8 (1994)  1994

Show Abstract
7982965 7982965
Essential role of phosphatidylinositol 3-kinase in insulin-induced glucose transport and antilipolysis in rat adipocytes. Studies with a selective inhibitor wortmannin
Okada, T, et al
J Biol Chem, 269:3568-73 (1994)  1994

8106400 8106400

Technical Info

Title
Unlocking the Mystery of Cancer: Do the Mutant p110α Subunits of PI3-Kinase Hold the Key?

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Categories

Life Science Research > Proteins and Enzymes > Substrate & Control Proteins > Kinase & Phosphatase Substrates
Life Science Research > Drug Discovery and Development > Kinase & Phosphatase Screening > Kinase & Phosphatase Substrates