yingweiwo

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
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.
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.
Penetratin-PI3Kγ(126-150) V81077 Penetratin-PI3Kγ(126-150) Penetratin-PI3Kγ(126-150) is a PI3Kγ peptide inhibitor that plays important roles in respiratory diseases.
PF-04979064 V4430 PF-04979064 1220699-06-8 PF-04979064 is a novel, potent and selectivePI3K/mTORdual kinase inhibitor withKis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
PF-4989216 V0151 PF-4989216 1276553-09-3 PF-4989216 is a novel, potent, orally bioactive and selective small molecule inhibitor of PI3K (phosphatidylinositol 3-kinase) with potential anticancer activity.
Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate) V69236 Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate) 245126-95-8 Phosphatidylinositol 4,5-bisphosphate (L-alpha-Phosphatidylinositol-4,5-bisphosphate) is a phospholipid component of cell membranes.
PI-103 V0107 PI-103 371935-74-9 PI-103 is a novel and potent multi-targeted PI3K inhibitor for p110α/β/δ/γ with IC50 of 2 nM/3 nM/3 nM/15 nM in cell-free assays, and has anticancer activity.
PI-103 Hydrochloride V30716 PI-103 Hydrochloride 371935-79-4 PI-103 Hydrochloride (PI 103; PI103),the hydrochloride salt of PI-103, is a multi-targetedPI3K and mTOR inhibitorwith potential antineoplastic activity.
PI-3065 V0149 PI-3065 955977-50-1 PI-3065 is a novel, potent and selective inhibitor of PI3K (phosphatidylinositol 3-kinase) p110δ inhibitor with potential anticancer activity.
PI3K-IN-11 V102103 PI3K-IN-11 884539-95-1 PI3K-IN-11 (Compound 13) is a PI3K inhibitor that selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50 of 6.4, 13, 8, and 11 nM, respectively), but does not inhibit mTOR (IC50=2.9 μM).
PI3K-IN-18 dihydrochloride V101842 PI3K-IN-18 dihydrochloride 1188890-32-5 PI3K-IN-18 (Compound 1) dihydrochloride is a 4-morpholine-2-phenylquinazoline derivative and an inhibitor of PI3K p110α.
PI3K-IN-19 hydrochloride V69224 PI3K-IN-19 hydrochloride 2132943-80-5 PI3K-IN-19 HCl is a phosphatidylinositol-3-kinase (PI3K) inhibitor disclosed in patent WO2017153220, step 5.
Contact Us