Wortmannin, (PI3 Kinase inhibitor)

Wortmannin, (PI3 Kinase inhibitor)

Upstate (Millipore)

1 mg

Wortmannin, 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.

Kinase Assay

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.

Receptor-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]

FUNCTION: 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:

Routinely evaluated by kinase assay.
Purity: ≥95% by HPLC.
Molecular Formula: C₂₃H₂₄O₈
Molecular Weight: 428.4

Upstate

1mg of lyophilized powder packaged under inert gas. White to off-white powder.

PI3Kγ

Q8WYR1

Protect 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.

PI3K/PI4K

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.

Kinase

• PIK3R5
• P101-PI3K
• FOAP-2
• F730038I15Rik

Inhibitors

Wortmannin, (PI3 Kinase inhibitor)

NM_014308.2