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PI 3-Kinase (p110α(H1047R)/p85α)
Description:
PI 3-Kinase (p110α(H1047R)/p85α)
Trade Name:
Upstate (Millipore)
Qty/Pk:
10 μg
Product Overview:
Complex of N-terminal 6His-tagged recombinant human p110α full length, containing the mutation H1047R, and untagged, recombinant, human p85α full length.
Background Information:
The H1047R substitution is a somatic mutation in p110α that has been associated with tumours of the colon, stomach, breast and brain. Combined in vitro and in vivo studies have shown that this mutation confers higher lipid kinase activity than wild type, and is able to induce oncogenic transformation. (Samuels Y. et al., Science, (2004); 304: 554; Kang S. et al., PNAS, (2005);102: 802-807 and Zhao J.J. et al., PNAS, (2005);102:18443-18448).
Species:
Human
Molecular Weight:
p110α(H1047R) MW = 125 kDa, p85α MW = 84 kDa.
Brand Family:
Upstate
Source:
Co-expressed by baculovirus in Sf21 insect cells.
Presentation:
50 mM Tris/HCl pH8.0, 300 mM NaCl, 0.1 mM EGTA, 0.03% Brij-35, 270 mM sucrose, 0.2 mM PMSF, 1 mM benzamidine, 0.1% 2-mercaptoethanol. Frozen solution.
Protein Target:
PI3Kα/p85α
UniProt Number:
Specific Activity:
For Specific Activity data, refer to the Certificate of Analysis for individual lots of this enzyme.
Storage Conditions:
Store at -70°C from date of shipment. For maximum recovery of product, centrifuge original vial prior to removing the cap.
Target Sub-Family:
PI3K/PI4K
Promotional Text:
This enzyme is part of KinaseProfiler™, a custom inhibitor selectivity discovery service.
Packaging:
Also available in 250μg size --call for pricing and availability and reference catalog number 14-792M when ordering the 250μg size.
Protein/Isoform Description:
Phosphoinositol-3-kinases (PI3 Kinases, PI3K) are a family of lipid kinases that mediate many intracellular signaling responses in both physiological and pathophysiological states. PI3 Kinase is a heteroduplex with three classes (I, II, & III) of catalytic domain. The class 1 PI3 Kinases are made up of a p85 regulatory protein and a p110 catalytic domain. There are 4 isoforms of the class 1 p110 catalytic domains. Class 1(A) include a, b, g and class 1(B) d. They are activated downstream via receptor tyrosine kinases or G-protein coupled receptors. Once activated, PI3Ks generate phosphatidylinositol 3,4,5-trisphosphate (PIP3) from PIP2. It was later found that PTEN, a lipid phosphatase, acts opposite to PI3K by dephosphorylating PIP3, converting it to PIP2, thus deactivating the effects of PI3K. Increased levels of PIP3 in the cell leads to the activation of many key signaling regulators including Akt and PDK as well as calcium release. One of the primary roles of PI3K is its regulation of cell growth and cell metabolism. Both of these play a critical role in cancer as some believe that a tumor’s shift to glycolysis is due to the activation of PI3K. PI 3-kinases have been linked with numerous disease states, including cancer, diabetes, allergic response, hypertension, cardiac contractility, atherosclerosis, sepsis and autoimmune/ inflammatory disorders.
Gene Symbol:
- PIK3CA
- PI3K
- PK3CA
Protein or Enzyme Type:
Kinases
Product Name:
PI 3-Kinase (p110α(H1047R)/p85α)
Entrez Gene Number:
Purification Method:
Ni2+/NTA-agarose