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PI3K

PI3K

PI3K (Phosphoinositide 3-kinase), via phosphorylation of the inositol lipid phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2), forms the second messenger molecule phosphatidylinositol (3,4,5)-trisphosphate (PI(3,4,5)P3) which recruits and activates pleckstrin homology domain containing proteins, leading to downstream signalling events crucial for proliferation, survival and migration. The four distinct catalytic isoforms of class I PI3K enzymes are PI3K, PI3K, PI3K, and PI3K.
Three main classes of PI3K enzymes exist, with class IA being strongly linked to cancer. Catalytic subunits (p110α, p110β, or p110δ; encoded by PIK3CA, PIK3CB, and PIK3CD genes, respectively) and regulatory subunits (p85) make up heterodimeric lipid kinases known as class IA PI3K.

The PI3K pathway is crucial for the progression of the cell cycle, cell growth and survival, actin rearrangement and migration, and intracellular vesicular transport, among many other biological processes.

PI3K related products

Structure Cat No. Product Name CAS No. Product Description
GSK2292767 V2546 GSK2292767 1254036-66-2 GSK2292767 is a novel and selective PI3Kδ inhibitor being investigator for the treatment of respiratory diseases such as asthma and COPD.
GSK2636771 V0135 GSK2636771 1372540-25-4 GSK2636771 is a novel, potent, selective and orally bioavailable inhibitor of PI3Kβ (phosphatidylinositol 3-kinase β)with potential anticancer activity.
HS-173 V0148 HS-173 1276110-06-5 HS-173 is a novel and potent PI3Kα (phosphatidylinositol 3-kinase) inhibitor (IC50 = 0.8 nM) with a potential to be used asan effective therapeutic agent for ameliorating liver fibrosis.
Hydroxy celecoxib V103314 Hydroxy celecoxib 170571-00-3 Hydroxycelecoxib, a derivative of celecoxib, is a PI3K/Akt signaling pathway activator that promotes epithelial repair.
IC-87114 V0110 IC-87114 371242-69-2 IC-87114 is a novel, potent, selective andATP-competitive PI3Kδ inhibitor (p110delta-selective) with potential anticancer activity.
IHMT-PI3K-315 V97283 IHMT-PI3K-315 IHMT-PI3K-315 (20e) is a potent and selective PI3Kγ/δ inhibitor with IC50 values of 4.0 and 9.1 nM for PI3Kγ and PI3Kδ, respectively.
IHMT-PI3K-455 V80354 IHMT-PI3K-455 IHMT-PI3K-455 (Compound 15u) is a specific and orally bioactive dual PI3Kγ/δ inhibitor.
iMDK quarterhydrate V76896 iMDK quarterhydrate iMDK quarterhydrate is a potent PI3K inhibitor that suppresses the growth factor MDK (also known as midkine or MK).
IPI-3063 V3109 IPI-3063 1425043-73-7 IPI-3063 is a potent and selective PI3Kp110δinhibitor with IC50 of 2.5 ± 1.2 nM and IC50 values of >1000 nM for other classes of PI3K isoforms (p110α, p110β, p110γ).
KTC1101 V87885 KTC1101 2764833-47-6 KTC1101 is an orally active pan-PI3K inhibitor.
LY-294002 V0103 LY294002 154447-36-6 LY294002,a morpholine-containing compound designed based on the flavonoid quercetin,is apotent and cell-permeable PI3K inhibitor, inhibiting PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM in cell-free assays, respectively.
MCX 28 V69220 MCX 28 1414453-58-9 MCX 28 is a PI3K/mTOR/PIM inhibitor showing low nanomolar activity.
ME-401 (P110δ-IN-1 ) V25217 ME-401 (P110δ-IN-1 ) 1595129-71-7 PWT143, formerly known as ME-401, is an orally bioavailable inhibitor of the delta isoform of phosphatidylinositide 3-kinase (PI3K), with potential antineoplastic activity.
ML-220 V115557 ML-220 662151-10-2 ML-220 is a PI3K modulator that can be used in research on tumors and infectious diseases.
MLN-1117 V2898 MLN-1117 1268454-23-4 Serabelisib (formerly known as INK-1117, MLN-1117, and/or TAK-117) is a potent, selective, and oral bioavailable inhibitor of PI3Kα (phosphoinositide 3-kinase) isoform with IC50 of 21 nmol/L against PI3Kα.
Nemiralisib succinate V94330 Nemiralisib succinate 1364799-98-3 Nemiralisib Succinate is a potent and selective PI3Kδ inhibitor with a pKi of 9.9.
Nic-15 V98364 Nic-15 2896739-91-4 Nic-15 (compound 4n) is an anticontractile agent used to antagonize the hypovascular properties of pancreatic tumors.
NSC-781406 V5023 NSC-781406 1676893-24-5 NSC781406 is a novel and highly potent dual inhibitor of PI3K and mTOR with an IC50of 2 nM for PI3Kα.
NU7441 (KU57788) V0108 NU7441 (KU57788) 503468-95-9 NU7441 (also called KU-57788) is a highly potent, selective and ATP-competitive inhibitor of DNA-PK (DNA-dependent protein kinase) with IC50 of 14 nM, has anticancer activity.
OMS14 V103791 OMS14 OMS14 has inhibitory effects on phosphoinositide 3-kinase γ (PI3Kγ) and PIK3CD/PIK3R1, inhibiting 19% PI3Kγ and 65% PIK3CD/PIK3R1 activities at 100 μM.
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