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 (4)
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
6324 Autophinib
Potent VPS34 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
6792 Omipalisib
Highly potent PI 3-kinase inhibitor; also potent inhibitor of mTOR and DNA-PK
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)
6440 PIK 93
Potent PI 3-Kγ, PI 3-Kα and PI 4-KIIIβ inhibitor
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
6079 TC KHNS 11
Potent and selective PI 3-kinase δ inhibitor; orally bioavailable
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
6856 α-Mangostin
Downregulates the PI3K/Akt pathway; anticarcinogenic
6762 Urolithin A
PI 3-K/Akt/mTOR signaling inhibitor; blocks phosphorylation of Akt and p70S6K in vitro

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.

External sources of pharmacological information for PI 3-kinase :

    Literature for PI 3-kinase

    Tocris offers the following scientific literature for PI 3-kinase to showcase our products. We invite you to request* or download your copy today!

    *Please note that Tocris will only send literature to established scientific business / institute addresses.


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    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