AKT1, Unactive (GWB-885085)





Application Note: Kinase assay Recombinant full-length human inactive AKT1 was expressed in Sf9 cells using an N-terminal GST tag.

Function: General protein kinase capable of phosphorylating several known proteins. Phosphorylates TBC1D4. Signals downstream of phosphatidylinositol 3-kinase (PI(3)K) to mediate the effects of various growth factors such as platelet-derived growth factor (PDGF), epidermal growth factor (EGF), insulin and insulin-like growth factor I (IGF-I). Plays a role in glucose transport by mediating insulin-induced translocation of the GLUT4 glucose transporter to the cell surface. Mediates the antiapoptotic effects of IGF-I. Mediates insulin-stimulated protein synthesis, partly by playing a role in both insulin-induced phosphorylation of 4E-BP1 and in insulin-induced activation of p70 S6 kinase. Promotes glycogen synthesis by mediating the insulin-induced activation of glycogen synthase.

Catalytic Activity: ATP + a protein = ADP + a phosphoprotein.

Subunit: Interacts with CENTG1 isoform 2 (PIKE-A) in the presence of guanine nucleotides.

Subcellular Location: Cytoplasm. Nucleus. Nucleus after activation by integrin-linked protein kinase 1 (ILK1).

Tissue Specificity: In all human cell types so far analyzed.

Domain: Binding of the PH domain to the phosphatidylinositol 3-kinase alpha (PI(3)K) results in its targeting to the plasma membrane.

Ptm: Phosphorylation on Thr-308, Ser-473 and Tyr-474 is required for full activity. Ser-473 phosphorylation by the Rictor-mTor complex favors Thr-308 phosphorylation by PDPK1. Ser-473 phosphorylation is enhanced by interaction with CENTG1 isoform 2 (PIKE-A).

Similarity: Belongs to the Ser/Thr protein kinase family. RAC subfamily.

Similarity: Contains 1 PH domain.

Similarity: Contains 1 protein kinase domain.

Summary: The serine-threonine protein kinase encoded by the AKT1 gene is catalytically inactive in serum-starved primary and immortalized fibroblasts. AKT1 and the related AKT2 are activated by platelet-derived growth factor. The activation is rapid and specific, and it is abrogated by mutations in the pleckstrin homology domain of AKT1. It was shown that the activation occurs through phosphatidylinositol 3-kinase. In the developing nervous system AKT is a critical mediator of growth factor-induced neuronal survival. Survival factors can suppress apoptosis in a transcription-independent manner by activating the serine/threonine kinase AKT1, which then phosphorylates and inactivates components of the apoptotic machinery. Multiple alternatively spliced transcript variants have been found for this gene. [1] Brunt,K.R., Fenrich,K.K., Kiani,G., Tse,M.Y., Pang,S.C., Ward,C.A. and Melo,L.G.
Protection of human vascular smooth muscle cells from H2O2-induced apoptosis through functional codependence between HO-1 and AKT
[2] Foster,K.S., McCrary,W.J., Ross,J.S. and Wright,C.F., et al.
Members of the hSWI/SNF chromatin remodeling complex associate with and are phosphorylated by protein kinase B/Akt
[3] Yang,H., Zhang,Y., Zhao,R., Wen,Y.Y., Fournier,K., Wu,H.B., Yang,H.Y., Diaz,J., Laronga,C. and Lee,M.H.
Negative cell cycle regulator 14-3-3sigma stabilizes p27 Kip1 by inhibiting the activity of PKB/Akt
[4] Peter,A.K. and Crosbie,R.H., et al.
Hypertrophic response of Duchenne and limb-girdle muscular dystrophies is associated with activation of Akt pathway
[5] Koga,F., Xu,W., Karpova,T.S., McNally,J.G., Baron,R. and Neckers,L., et al.
Hsp90 inhibition transiently activates Src kinase and promotes Src-dependent Akt and Erk activation
[6] Jones P.F., Jakubowicz T., Pitossi F.J., Maurer F., Hemmings B.A.
Molecular cloning and identification of a serine/threonine protein kinase of the second-messenger subfamily.
[7] Matsubara A., Wasson J.C., Donelan S.S., Welling C.M., Glaser B., Permutt M.A.
Isolation and characterization of the human AKT1 gene, identification of 13 single nucleotide polymorphisms (SNPs), and their lack of association with Type II diabetes.
[8] Coffer P.J., Woodgett J.R.
Molecular cloning and characterisation of a novel putative protein-serine kinase related to the cAMP-dependent and protein kinase C families.
[9] Coffer P.J., Woodgett J.R.
Eur. J. Biochem. 205:1217-1218(1992).
[10] Delcommenne M., Tan C., Gray V., Rue L., Woodgett J.R., Dedhar S.
Phosphoinositide-3-OH kinase-dependent regulation of glycogen synthase kinase 3 and protein kinase B/AKT by the integrin-linked kinase.

Additional Information

Name AKT1, Unactive (GWB-885085)
Availability Discontinued
Related Product Names EC; RAC-PK-alpha; Protein kinase B; PKB; C-AKT PKB; RACRAC-alpha serine/threonine-protein kinaseAKT1
Swissprot ID P31749
NCBI Acc Number NP_001014431.1
Molecular Weight 0.5
Source Sf9 Insect Cells
GI Number 62241013
Stability 1 year at -20 degree C.
Sequence Length 480
Storage Store product at -70 degree C. For optimal storage, aliquot target into smaller quantities after centrifugation and store at recommended temperature.
Datasheets/Manuals Printable datasheet for GWB-885085
Intended Use Research Use Only