General Information of the Protein
Protein ID
PT03525
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform
Secondarily
Protein Name
Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit alpha
Phosphoinositide-3-kinase catalytic alpha polypeptide
Serine/threonine protein kinase PIK3CA
Gene Name
PIK3CA
Sequence
MPPRPSSGELWGIHLMPPRILVECLLPNGMIVTLECLREATLVTIKHELFREARKYPLHQLLQDETSYIFVSVTQEAEREEFFDETRRLCDLRLFQPFLKVIEPVGNREEKILNREIGFVIGMPVCEFDMVKDPEVQDFRRNILNVCKEAVDLRDLNSPHSRAMYVYPPNVESSPELPKHIYNKLDKGQIIVVIWVIVSPNNDKQKYTLKINHDCVPEQVIAEAIRKKTRSMLLSSEQLKLCVLEYQGKYILKVCGCDEYFLEKYPLSQYKYIRSCIMLGRMPNLMLMAKESLYSQLPIDSFTMPSYSRRISTATPYMNGETSTKSLWVINSALRIKILCATYVNVNIRDIDKIYVRTGIYHGGEPLCDNVNTQRVPCSNPRWNEWLNYDIYIPDLPRAARLCLSICSVKGRKGAKEEHCPLAWGNINLFDYTDTLVSGKMALNLWPVPHGLEDLLNPIGVTGSNPNKETPCLELEFDWFSSVVKFPDMSVIEEHANWSVSREAGFSYSHTGLSNRLARDNELRENDKEQLRALCTRDPLSEITEQEKDFLWSHRHYCVTIPEILPKLLLSVKWNSRDEVAQMYCLVKDWPPIKPEQAMELLDCNYPDPMVRSFAVRCLEKYLTDDKLSQYLIQLVQVLKYEQYLDNLLVRFLLKKALTNQRIGHFFFWHLKSEMHNKTVSQRFGLLLESYCRACGMYLKHLNRQVEAMEKLINLTDILKQEKKDETQKVQMKFLVEQMRQPDFMDALQGFLSPLNPAHQLGNLRLEECRIMSSAKRPLWLNWENPDIMSELLFQNNEIIFKNGDDLRQDMLTLQIIRIMENIWQNQGLDLRMLPYGCLSIGDCVGLIEVVRNSHTIMQIQCKGGLKGALQFNSHTLHQWLKDKNKGEIYDAAIDLFTRSCAGYCVATFILGIGDRHNSNIMVKDDGQLFHIDFGHFLDHKKKKFGYKRERVPFVLTQDFLIVISKGAQEYTKTREFERFQEMCYKAYLAIRQHANLFINLFSMMLGSGMPELQSFDDIAYIRKTLALDKTEQEALEYFTKQMNDAHHGGWTTKMDWIFHTIKQHALN
    Show/Hide
Organism
Mus musculus, Mouse
Protein Classification
Enzyme
>
Transferase
Function
Phosphoinositide-3-kinase (PI3K) phosphorylates phosphatidylinositol (PI) and its phosphorylated derivatives at position 3 of the inositol ring to produce 3-phosphoinositides. Uses ATP and PtdIns(4,5)P2 (phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Participates in cellular signaling in response to various growth factors. Involved in the activation of AKT1 upon stimulation by receptor tyrosine kinases ligands such as EGF, insulin, IGF1, VEGFA and PDGF. Involved in signaling via insulin-receptor substrate (IRS) proteins. Essential in endothelial cell migration during vascular development through VEGFA signaling, possibly by regulating RhoA activity. Required for lymphatic vasculature development, possibly by binding to RAS and by activation by EGF and FGF2, but not by PDGF. Regulates invadopodia formation through the PDPK1-AKT1 pathway. Participates in cardiomyogenesis in embryonic stem cells through a AKT1 pathway. Participates in vasculogenesis in embryonic stem cells through PDK1 and protein kinase C pathway. Also has serine-protein kinase activity: phosphorylates PIK3R1 (p85alpha regulatory subunit), EIF4EBP1 and HRAS. Plays a role in the positive regulation of phagocytosis and pinocytosis (PubMed:19604150).
    Show/Hide
Uniprot ID
Primary ID:
P42337

Secondarily ID:
Q0VGQ5
    Show/Hide
Ensembl ID
ENSG00000121879
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000218 , BT-474
Compound ID Compound Name Compound Formula
CP0561456
US9156831, 10
   Show/Hide
C22H31N9O4
 1
1
IC50 = 85 nM
   TI
   LI
   LO
   TS
CP0143273
US9156831, 3
   Show/Hide
C22H31N9O3
 1
1
IC50 = 90 nM
   TI
   LI
   LO
   TS
CP0503594
US9156831, 11
   Show/Hide
C22H31N9O4
 1
1
IC50 = 110 nM
   TI
   LI
   LO
   TS
CP0117467
US9156831, 9
   Show/Hide
C22H29N9O4
 1
1
IC50 = 330 nM
   TI
   LI
   LO
   TS
CP0093702
US9156831, 1
   Show/Hide
C21H29N9O3
 1
1
IC50 = 360 nM
   TI
   LI
   LO
   TS
CP0093703
US9156831, 7
   Show/Hide
C22H31N9O3
 1
1
IC50 = 420 nM
   TI
   LI
   LO
   TS
CP0173540
US9156831, 6
   Show/Hide
C22H31N9O3
 1
1
IC50 = 530 nM
   TI
   LI
   LO
   TS
CP0283502
US9156831, 8
   Show/Hide
C21H27N9O4
 1
1
IC50 = 590 nM
   TI
   LI
   LO
   TS
Similar Protein(s) and Bioactivity Statistics
90% Identity
Protein ID Protein Name Protein Organism
PT01045 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Homo sapiens, Human
PT01368 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Bos taurus, Bovine
PT07498 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform Rattus norvegicus, Rat