PI 3-kinase

PI 3-Kinases (phosphoinositide 3-kinases, PI 3-Ks) are a family of lipid kinases capable of phosphorylating the 3'OH of the inositol ring of phosphoinositides. They are responsible for coordinating a diverse range of cell functions including proliferation and survival.

Products
Background
Literature
Gene Data

Inhibitors

Cat No Product Name / Activity
5595 A66
Potent and selective PI 3-kinase p110α inhibitor
3671 AS 252424
Selective inhibitor of PI 3-kinase γ
3578 AS 605240
Potent and selective PI 3-kinase γ (PI 3-Kγ) inhibitor
4839 AZD 6482
Potent and selective PI 3-Kβ inhibitor
3606 BAG 956
Dual PI 3-kinase and PDPK1 (PDK1) inhibitor
4674 CZC 24832
Selective inhibitor of PI 3-kinase γ
4702 ETP 45658
Potent PI 3-kinase inhibitor; also inhibits DNA-PK and mTOR
4026 GSK 1059615
Potent PI 3-kinase inhibitor
4840 KU 0060648
Dual DNA-PK and PI 3-K inhibitor
5835 LTURM 36
PI 3-kinase δ inhibitor
1130 LY 294002 hydrochloride
Prototypical PI 3-kinase inhibitor; also inhibits other kinases
2418 LY 303511
Negative control of LY 294002 (Cat. No. 1130)
3977 3-Methyladenine
Class III PI 3-kinase inhibitor; also inhibits autophagy
4820 PF 04691502
Potent and selective dual PI 3-K/mTOR inhibitor
4823 PF 05212384
Potent and selective dual PI 3-K/mTOR inhibitor
2930 PI 103 hydrochloride
Inhibitor of PI 3-kinase, mTOR and DNA-PK
5919 PI 3065
Potent and selective PI 3-kinase p110δ inhibitor
2814 PI 828
PI 3-kinase inhibitor, more potent than LY 294002 (Cat. No. 1130)
3894 PP 121
Dual kinase inhibitor; inhibits PI 3-K family kinases
1125 Quercetin
Non-selective PI 3-kinase inhibitor
6036 STK16-IN-1
PI 3Kδ and PI 3Kγ kinase inhibitor; also inhibits mTOR and STK16 kinases
4264 TG 100713
PI 3-kinase inhibitor
5832 TGX 221
Potent and selective PI 3-kinase β inhibitor
1232 Wortmannin
Potent, irreversible inhibitor of PI 3-kinase. Also inhibitor of PLK1

Activators

Cat No Product Name / Activity
1983 740 Y-P
Cell-permeable PI 3-kinase activator

Other

Cat No Product Name / Activity
5126 iMDK
Suppressor of MDK expression; inhibits PI 3-K signaling

PI 3-Kinases (phosphoinositide 3-kinases, PI 3-Ks) are a family of lipid kinases capable of phosphorylating the 3'OH of the inositol ring of phosphoinositides. They are responsible for coordinating a diverse range of cell functions including proliferation, cell survival, degranulation, vesicular trafficking and cell migration.

The PI 3-kinases are grouped into three distinct classes. Class I PI 3-kinases are heteromeric consisting of a regulatory subunit and a 110 kDa catalytic subunit (3 forms in class 1A : α-, β- and δ- and one in class 1B : γ-). PI 3-kinases p110 α- and β- are ubiquitously expressed whilst p110 δ- expression is associated with leukocytes. Activating mutations in the p110α- subunit have recently been discovered in certain types of cancer cell. Class II PI 3-kinases are large homomeric enzymes (C2α-, β- and γ-) that are sensitive to wortmannin (although less sensitive than Class I PI 3-kinases) but are resistant to LY 294002. Class III contains just one member, hVps34p, which is thought to play an important role in both protein sorting and nutrient sensing in concert with the mTOR pathway.

Literature for PI 3-kinase

Cancer

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
Cardiovascular

Cardiovascular Research Product Guide

A collection of over 250 products for cardiovascular research, the guide includes research tools for the study of:

  • Hypertension
  • Thrombosis and Hemostasis
  • Atherosclerosis
  • Myocardial Infarction
  • Ischemia/Reperfusion Injury
  • Arrhythmias
  • Heart Failure
Kinases

Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

  • Receptor Tyrosine Kinases
  • Protein Kinases A, C, D and G
  • PI-3 Kinase, Akt and mTOR
  • MAPK Signaling
  • Receptor Serine/Threonine Kinases
Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling

PI 3-Kinase Gene Data

Gene Species Gene Symbol Gene Accession No. Protein Accession No.
Class IA
p85α, p50α, p55α
Human PIK3R1 NM_181504 P27986
Mouse Pik3r1 NM_001077495 P26450
Rat Pik3r1 NM_013005 O55168
Class IA
p85β
Human PIK3R2 NM_005027 O00459
Mouse Pik3r2 NM_008841 O08908
Rat Pik3r2 NM_022185 Q63788
Class IA
p55γ
Human PIK3R3 NM_003629 Q92569
Mouse Pik3r3 NM_181585 Q64143
Rat Pik3r3 NM_022213 Q63789
Class IA
p110α
Human PIK3CA NM_006218 P42336
Mouse Pik3ca NM_008839 P42337
Rat Pik3ca BC099154 Q4KLK3
Class IA
p110β
Human PIK3CB NM_006219 P42338
Mouse Pik3cb NM_029094 Q8BTI9
Rat Pik3cb NM_053481 Q9Z1L0
Class IA
p110δ
Human PIK3CD NM_005026 O00329
Mouse Pik3cd NM_008840 O35904
Class IB
p101
Human PIK3R5 NM_014308 Q8WYR1
Mouse Pik3r5 NM_177320 Q5SW28
Class IB
p101γ
Human PIK3CG NM_002649 P48736
Mouse Pik3cg NM_020272 Q9JHG7
Class II
C2α
Human PIK3C2A NM_002645 O00443
Mouse Pik3c2a NM_011083 Q61194
Class II
C2β
Human PIK3C2B NM_002646 O00750
Mouse Pik3c2b AK049181 A2RSK1
Class II
C2γ
Human PIK3C2G NM_004570 O75747
Mouse Pik3c2g NM_207683 O70167
Rat Pik3c2g NM_053923 O70173
Class III
p150
Human PIK3R4 NM_014602 Q99570
Mouse Pik3r4 NM_001081309 Q8VD65
Class III
Vps34
Human PIK3C3 NM_002647 Q8NEB9
Mouse Pik3c3 NM_181414 Q6PF93
Rat Pik3c3 NM_022958 O88763