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.
PI 3-kinase Inhibitors |
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Cat. No. | Product Name / Activity |
5595 | A66 |
Potent and selective PI 3-kinase p110α 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 | |
1699 | CGS 15943 |
Selective inhibitor of PI 3-kinase p110γ | |
7631 | Idelalisib |
Potent PI 3-Kinase δ isoform inhibitor | |
4840 | KU 0060648 |
Dual DNA-PK and PI 3-K inhibitor | |
1130 | LY 294002 hydrochloride |
Prototypical PI 3-kinase inhibitor; also inhibits other kinases | |
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 | |
2930 | PI 103 hydrochloride |
Inhibitor of PI 3-kinase, mTOR and DNA-PK | |
2814 | PI 828 |
PI 3-kinase inhibitor, more potent than LY 294002 (Cat. No. 1130) | |
7902 | PIK 90 |
Potent PI3K inhibitor, also used in hPSCs mesendoderm differentiation | |
3894 | PP 121 |
Dual kinase inhibitor; inhibits PI 3-K family kinases | |
1125 | Quercetin |
Non-selective 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 | |
PI 3-kinase Activators |
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Cat. No. | Product Name / Activity |
1983 | 740 Y-P |
Cell-permeable PI 3-kinase activator | |
Other |
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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 :
PI 3-Kinase Gene Data
Gene | Species | Gene Symbol | Gene Accession No. | Protein Accession No. |
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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 |