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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
ETP-46321 V2910 ETP-46321 1252594-99-2 ETP-46321 is a novel, potent and orally bioavailable inhibitor of PI3Kα and PI3Kδ with Kiappvalues of 2.3 nM and 14.2 nM, respectively inbiochemical assays.
ETP-47037 V69223 ETP-47037 1316760-76-5 ETP-47037 is a potent inhibitor of PI3Kα isoforms with IC50 of 0.99 nM.
FAP-PI3KI1 V69233 FAP-PI3KI1 2415941-98-7 FAP-PI3KI1 is a fibroblast activation protein (FAP)-targeted PI3K inhibitor that can selectively target human idiopathic pulmonary fibrosis (IPF) cells expressing FAP and effectively inhibit collagen synthesis and reduce collagen deposition.
FD2056 V69226 FD2056 2685870-87-3 FD2056 is a potent orally bioactive PI3K inhibitor.
FD274 V69197 FD274 2641899-38-7 FD274 is a potent dual (bifunctional) inhibitor of PI3K/mTOR, with IC50s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM and 2.03 nM for PI3Kα/β/γ/δ and mTOR respectively.
Gallein (alizarin violet; Pyrogallol phthalein) V69202 Gallein (alizarin violet; Pyrogallol phthalein) 2103-64-2 Gallein is an inhibitor (blocker/antagonist) of G protein βγ (Gβγ) subunit signaling.
GDC-0326 V4526 GDC-0326 1282514-88-8 GDC-0326 is a novel, potent and selectivePI3Kα (α-Isoform of Phosphoinositide 3-Kinase)inhibitor with aKiof 0.2 nM.
Gilmelisib V70264 Gilmelisib 1845777-61-8 This product is discontinued due to commercial reason. Gilmelisib is an antitumor active molecule.
GNE-317 V0146 GNE-317 1394076-92-6 GNE-317, an oxetane analog of GDC-0980, is a novel, potent, and selective PI3K/mTOR dual inhibitor with excellent BBB (blood-brain barrier) penetrating ability.
GNE-477 V4333 GNE-477 1032754-81-6 GNE-477 is a novel, potent and efficacious dual inhibitor ofPI3K(IC50=4 nM)/mTOR(Ki=21 nM).
GSK1059615 V0126 GSK1059615 958852-01-2 GSK1059615 is a novel, potent and reversible inhibitor of P13K (phosphatidylinositol-3-kinases) with potential anticancer activity.
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).
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