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33-047

Sigma-Aldrich

PI 3-Kinase 3-step HTRF® Assay

The PI 3-Kinase 3-Step HTRF Assay is a high-performance assay kit that provides a universal method for testing all Class I PI3-Kinases in a homogeneous format.

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eCl@ss:
32161000
NACRES:
NA.84

Quality Level

100

species reactivity

human, mouse

manufacturer/tradename

HTRF®
Upstate®

technique(s)

activity assay: suitable (kinase)

NCBI accession no.

NM_006218.2

UniProt accession no.

P42336

detection method

fluorometric (HTRF)

shipped in

dry ice

Gene Information

human ... PIK3CA(5290)

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This Item
33-036SRP023314-792-M
Sigma-Aldrich

Sigma-Aldrich

33-047

PI 3-Kinase 3-step HTRF® Assay

Sigma-Aldrich

Sigma-Aldrich

33-036

PI 3-Kinase HTRF® Assay; 10,000 wells

PI3 kinase (p110a/p85a) Active human recombinant, expressed in baculovirus infected insect cells, ≥80% (SDS-PAGE)

Sigma-Aldrich

SRP0233

PI3 kinase (p110a/p85a) Active human

Sigma-Aldrich

Sigma-Aldrich

14-792-M

PI 3-Kinase (p110α(H1047R)/p85α), 10 µg

species reactivity

human, mouse

species reactivity

mouse, human

species reactivity

-

species reactivity

-

manufacturer/tradename

HTRF®

manufacturer/tradename

HTRF®, Upstate®

manufacturer/tradename

-

manufacturer/tradename

Upstate®

NCBI accession no.

NM_006218.2

NCBI accession no.

NM_006218.2

NCBI accession no.

U79143 (p110alpha), XM_043865 (p85alpha)

NCBI accession no.

-

UniProt accession no.

P42336

UniProt accession no.

P42336

UniProt accession no.

P42336

UniProt accession no.

P26450 (mouse), P27986, P42336, P42337 (mouse), U79143

detection method

fluorometric (HTRF)

detection method

fluorometric (HTRF)

detection method

-

detection method

-

General description

Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit α (PIK3CA) gene is mapped to human chromosome 3q26.32. This gene codes for the catalytic subunit p110α of class IA PI3-kinase. PI3K signaling pathways regulate various cellular activities and properties including proliferation, survival, apoptosis, motility, and morphology. Mutation or overexpression of the PIK3CA gene is implicated in the development of various human solid tumors including head and neck cancers or pharyngeal cancer and ovarian cancer.

Application

PI 3-Kinase 3-step HTRF® Assay has been used to determine the in vitro inhibitory potencies of phosphatidylinositol 3-kinase (PI3K) δ inhibitors such as MSD-496486311, MSD126796721, idelalisib, and duvelisib across PI3K α, β, γ, and δ isoforms.

Biochem/physiol Actions

Target Sub-Family: PI3K/PI4K

Packaging

Kit capacity: 10,000 wells

Components

4X Reaction Buffer

PIP2 (substrate, 1mM stock)

DM A Reaction Buffer

DM B Reaction Buffer

DM C Reaction Buffer

BPIP3

Stop Reagent

Storage and Stability

12 months at -70°C

Other Notes

Research Category
Apoptosis & Cancer
Research Sub Category
Oncology

Legal Information

HTRF is a registered trademark of Cis Bio International
UPSTATE is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

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 Class Code

11 - Combustible Solids

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Robbie L McLeod et al.
The Journal of pharmacology and experimental therapeutics, 369(2), 223-233 (2019-02-26)
We leveraged a clinical pharmacokinetic (PK)/pharmacodynamics (PD)/efficacy relationship established with an oral phosphatidylinositol 3-kinase (PI3K)δ inhibitor (Idelalisib) in a nasal allergen challenge study to determine whether a comparable PK/PD/efficacy relationship with PI3Kδ inhibitors was observed in preclinical respiratory models of
Andreas G Bader et al.
Nature reviews. Cancer, 5(12), 921-929 (2005-12-13)
There have long been indications of a role for PI3K (phosphatidylinositol 3-kinase) in cancer pathogenesis. Experimental data document a requirement for deregulation of both transcription and translation in PI3K-mediated oncogenic transformation. The recent discoveries of cancer-specific mutations in PIK3CA, the
Wanglong Qiu et al.
Clinical cancer research : an official journal of the American Association for Cancer Research, 12(5), 1441-1446 (2006-03-15)
Recent studies have reported high frequencies of somatic mutations in the phosphoinositide-3-kinase catalytic alpha (PIK3CA) gene in several human solid tumors. Although gene amplifications of PIK3CA have been reported in head and neck squamous cell carcinoma (HNSCC), small mutation of

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