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Pathways Recommended:	PI3K/Akt/mTOR

Results for "

PI3K inhibition

" in MedChemExpress (MCE) Product Catalog:

By Targets:	PI3K (20) Akt (4) Apoptosis (5) ATM/ATR (2) Autophagy (2) Cytochrome P450 (1) DNA-PK (1) Endogenous Metabolite (2) G Protein-coupled Receptor Kinase (GRK) (1) HSP (1) Lipase (1) MEK (2) mTOR (5) P2X Receptor (1) PI4K (1) Polo-like Kinase (PLK) (1) VEGFR (1)
By Research Areas:	Cancer (17) Cardiovascular Disease (2) Infection (2) Inflammation/Immunology (9) Neurological Disease (1)

Inhibitors & Agonists

Screening Libraries

Natural
Products

Targets Recommended: PI3K

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-131502

Taspine	P2X Receptor	Inflammation/Immunology
Taspine is a natural product with anti-inflammatory activity. Taspine suppresses P2X4 receptor activity via PI3K inhibition. Taspine inhibits pro-inflammatory signalling via inhibition of P2X4 receptors in macrophage .

HY-128333

PI3K/mTOR Inhibitor-4	PI3K mTOR	Cancer
PI3K/mTOR Inhibitor-4 is an orally active pan-class I *PI3K/mTOR* inhibitor. PI3K/mTOR Inhibitor-4 has enzymatic inhibition activity for PI3Kα, PI3Kγ, PI3Kδ and mTOR with IC₅₀ values of 0.63 nM, 22 nM, 9.2 nM and 13.85 nM, respectively. PI3K/mTOR Inhibitor-4 can be used for the research of cancer .

HY-156406

PITCOIN4	PI3K	Inflammation/Immunology
PITCOIN4 is a highly selective Class II Alpha *PI3K-C2α* inhibitor. PITCOIN4 shows nanomolar inhibition of PI3K-C2α and >100-fold selectivity in a general kinase panel .

HY-N0776

Isorhamnetin 5+ Cited Publications 3'-Methylquercetin	MEK PI3K Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology Cancer
Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and *PI3K*.

HY-155066

FD274	PI3K mTOR	Cancer
FD274 is a highly potent *PI3K/mTOR* dual inhibitor with IC₅₀s of 0.65 nM, 1.57 nM, 0.65 nM, 0.42 nM, and 2.03 nM against PI3Kα/β/γ/δ and mTOR, respectively. FD274 exhibits significant anti-proliferation of AML cell lines (HL-60 and MOLM-16). FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .

HY-144450

PI3K-IN-29	PI3K Akt	Cancer
PI3K-IN-29 is a potent *PI3K* inhibitor. PI3K-IN-29 displays good inhibition potencies against U87MG, HeLa and HL60 cells with IC₅₀ values of 0.264, 2.04 and 1.14 µM, respectively. PI3K-IN-29 inhibits *PI3K/Akt* pathway by inhibiting phosphorylation of Akt that is catalyzed by *PI3K* .

HY-106006

RV-1729	PI3K	Others Inflammation/Immunology
RV-1729 is an inhibitor of the phosphatidylinositol 3-kinase-δ (PI3Kδ). RV-1729 identifies inhibition of the PI3K isotype by quantifying the release of phosphatidylinositol 3,4, 5-triphosphate (PIP3) (IC₅₀=12 nM), showing twice the selectivity for PI3Kδ relative to PI3Kγ. RV-1729 is also 16 times more selective to PI3Kα. RV-1729 regulates immune and inflammatory responses by inhibiting PI3Kδ. RV-1729 can be used in studies of asthma and chronic obstructive pulmonary disease (COPD) .

HY-100603A

(S)-GSK-F1	PI3K PI4K	Infection
(S)-GSK-F1 (Compound 28) is an inhibitor for type III phosphatidylinositol 4-kinase α (PI4KIIIα). (S)-GSK-F1 inhibits PI4Kα, PI4Kβ, PI4Kγ, PI3Kα, PI3Kβ and PI3Kδ with pIC₅₀ of 8.3, 6.0, 5.6, 5.6, 5.1 and 5.6, respectively. (S)-GSK-F1 exhibits anti-hepatitis C virus (HCV) activity through inhibition of HCV replication. (S)-GSK-F1 exhibits moderate pharmacokinetic characters in rat model .

HY-N0776R

Isorhamnetin (Standard) 3'-Methylquercetin (Standard)	MEK PI3K Endogenous Metabolite	Cardiovascular Disease Inflammation/Immunology Cancer
Isorhamnetin (Standard) is the analytical standard of Isorhamnetin. This product is intended for research and analytical applications. Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and *PI3K*.

HY-144686

ATM Inhibitor-3	ATM/ATR PI3K mTOR	Cancer
ATM Inhibitor-3 (compound 34) is a potent and selective ATM inhibitor, with an IC₅₀ of 0.71 nM. ATM Inhibitor-3 shows inhibition of *PI3K* kinases family. ATM Inhibitor-3 exhibits favorable metabolic stability .

HY-144687

ATM Inhibitor-4	ATM/ATR PI3K mTOR	Cancer
ATM Inhibitor-4 (compound 39) is a potent and selective ATM inhibitor, with an IC₅₀ of 0.32 nM. ATM Inhibitor-4 shows stronger inhibition of *PI3K* kinases family. ATM Inhibitor-4 shows a full inhibition of mTOR at 1 μM. ATM Inhibitor-4 exhibits favorable metabolic stability .

HY-163533

CPD-002	VEGFR	Inflammation/Immunology
CPD-002 is an inhibitor for vascular endothelial growth factor receptor 2 (VEGFR 2), that inhibits angiogenesis through inhibition of VEGFR2/PI3K/AKT signaling pathway. CPD-002 exhibits anti-inflammatory activity and attenuates rheumatoid arthritis .

HY-103224

PIT-1	PI3K	Cancer
PIT-1 is a selective PIP3 (phosphatidylinositol 3,4,5-trisphosphate) antagonist. PIT-1 inhibits cancer cell survival and induces apoptosis by inhibition of PIP3 dependent PI3K / Akt signaling. PIT-1 exhibits antitumor activity in vivo .

HY-12481

SAR405 Maximum Cited Publications 20 Publications Verification	PI3K Autophagy	Cancer
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC₅₀=1.2 nM; K_d=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity .

HY-N0284

Esculetin 4 Publications Verification	PI3K Akt	Inflammation/Immunology Cancer
Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of *PI3K/Akt* pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .

HY-123862

LAS195319	PI3K Lipase G Protein-coupled Receptor Kinase (GRK)	Inflammation/Immunology
LAS195319 is an orally active and potent inhibitor against PI3Kδ with an IC₅₀ value of 0.5 nM. LAS195319 is also a highly selective inhibitor against an extensive panel of proteins, lipid kinases and GPCRs. LAS195319 causes an inhibition of neutrophil and eosinophil infiltration. LAS195319 is promising for research of respiratory diseases such as asthma and chronic obstructive pulmonary disease (COPD) .

HY-121222

alpha-Bisabolol	PI3K Apoptosis	Cancer
alpha-Bisabolol, an orally active sesquiterpene alcohol, induces cell cycle arrest, mitochondrial apoptosis and inhibition of *PI3K/Akt* signalling pathways. alpha-Bisabolol exerts a protective action against Cisplatin (HY-17394)-induced nephrotoxicity by mitigating inflammation and oxidative stress through the inhibition of NFκB activation. alpha-Bisabolol exhibits anti-inflammatory, analgesic, antibiotic and anticancer activities .

HY-12037

Rigosertib sodium 5 Publications Verification ON-01910 sodium	Polo-like Kinase (PLK) PI3K Apoptosis	Cancer
Rigosertib sodium (ON-01910 sodium) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the *PI3K/Akt* pathway, promotes the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib sodium is a selective and non-ATP-competitive inhibitor of PLK1 with an IC₅₀ of 9 nM .

HY-114923

SU-11752	DNA-PK PI3K	Cancer
SU-11752 is an inhibitor for DNA-dependent protein kinase (DNA-PK) with an IC₅₀ of 0.13 μM. SU-11752 inhibits PI3K p110γ kinase with IC₅₀ of 1.1 μM. SU-11752 binds competitively for ATP-site in DNA-PK, results in inhibition of intracellular DNA double-strand break repair and increases the sensitivity of cells to radiotherapy .

HY-N0284R

Esculetin (Standard)	PI3K Akt	Inflammation/Immunology Cancer
Esculetin (Standard) is the analytical standard of Esculetin. This product is intended for research and analytical applications. Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .

HY-N2045

Musk ketone 1 Publications Verification	PI3K Akt Apoptosis Cytochrome P450	Neurological Disease
Musk ketone is a widely used artificial fragrance. Musk ketone is also a cytochrome P450 enzyme inducer. Musk ketone shows mutagenic and comutagenic effects in Hep G2 cells and induces neural stem cell proliferation and differentiation in cerebral ischemia via activation of the *PI3K/Akt* signaling pathway. In the brain, musk ketone is neuroprotective against stroke injury through inhibition of cell apoptosis .

HY-132231

FD223	PI3K Apoptosis	Cancer
FD223 is a potent and selective phosphoinositide 3-kinase delta *(PI3Kδ)* inhibitor. FD223 displays high potency (IC₅₀=1 nM) and good selectivity over other isoforms (IC₅₀s of 51 nM, 29 nM and 37 nM, respectively for α, β and γ). FD223 exhibits efficient inhibition of the proliferation of acute myeloid leukemia (AML) cell lines by suppressing p-AKT Ser473 thus causing G1 phase arrest during the cell cycle. FD223 has potential for the research of leukemia such as AML .

HY-151137

HSP90/mTOR-IN-1	mTOR HSP Apoptosis Autophagy	Cancer
HSP90/mTOR-IN-1 is a potent and orally active Hsp90 and mTOR inhibitor with IC₅₀ values of 69 nM and 29 nM, respectively. HSP90/mTOR-IN-1 suppresses the proliferation of SW780 cells through the over-activation of the *PI3K/AKT/mTOR* pathway. HSP90/mTOR-IN-1 induces apoptosis and autophagy via selective Hsp90 and mTOR inhibition. HSP90/mTOR-IN-1 also has considerable in vivo anti-tumor activity. HSP90/mTOR-IN-1 can be used for researching bladder cancer .

HY-W130965

1-Formyl-beta-carboline	Others	Infection
1-Formyl-beta-carboline is an alkaloid with inhibitory activity against Newcastle disease virus (NDV). 1-Formyl-beta-carboline can effectively inhibit different genotypes of NDV with IC50 values within 10 μM, and its inhibition rate is more than 90% at a concentration of 20 μM. 1-Formyl-beta-carboline mainly exerts its effects by inhibiting the adsorption and entry processes in the NDV life cycle. 1-Formyl-beta-carboline has been identified as a novel HN inhibitor that can directly interact with the NDV HN protein and affect the adsorption of NDV. 1-Formyl-beta-carboline also inhibits the entry of NDV by inhibiting the PI3K/Akt signaling pathway rather than the ERK pathway .

HY-116497

PH11	Others	Cancer
PH11 is a novel focal adhesion kinase (FAK) inhibitor that rapidly induces apoptosis in TRAIL-resistant PANC-1 cells when combined with TRAIL, but has no effect on normal human fibroblasts. The study found that PH11 downregulates c-FLIP through inhibition of FAK and phosphatidylinositol-3-kinase (PI3K)/AKT pathways, thereby restoring the TRAIL apoptotic pathway, suggesting that this combination therapy may provide an attractive therapeutic strategy for the safe and effective treatment of pancreatic cancer. PH11 selectively inhibits c-FLIP expression by modulating upstream signaling pathways and may represent an innovative therapeutic strategy. Although further work is needed to fully elucidate the mechanism of PH11-induced TRAIL sensitization, we believe that our results will provide a new approach to target c-FLIP without the risk of interfering with caspase-8 processing, which could potentially lead to TRAIL resistance. This study also suggests a role for the FAK/AKT signaling pathway in regulating c-FLIP expression in TRAIL-induced apoptosis, and this understanding will provide important clues to control the resistance mechanism to optimize the potential of TRAIL-based pancreatic cancer treatment.

Cat. No.	Product Name

HY-L015

PI3K/Akt/mTOR Compound Library	600 compounds
The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials. MCE owns a unique collection of 600 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

PI3K/Akt/mTOR Compound Library

600 compounds

The PI3K/Akt/mTOR pathway controls many cellular processes that are important for the formation and progression of cancer, including apoptosis, transcription, translation, metabolism, angiogenesis, and cell cycle progression. Every major node of this signaling network is activated in a wide range of human tumors. Mechanisms for the pathway activation include activation of receptor tyrosine kinases (RTKs) upstream of PI3K, mutation or amplification of PIK3CA encoding p110α catalytic subunit of PI3K, mutation or loss of PTEN tumor suppressor gene, and mutation or amplification of Akt1. Once the pathway is activated, signaling through Akt can stimulate a series of substrates including mTOR which is involved in protein synthesis. Thus, inhibition of this pathway is an attractive concept for cancer prevention and/or therapy. Currently some mTOR inhibitors are approved for several indications, and there are several novel PI3K/Akt/mTOR inhibitors in clinical trials.

MCE owns a unique collection of 600 compounds that can be used for PI3K/Akt/mTOR pathway research. PI3K/Akt/mTOR Compound Library also acts as a useful tool for anti-cancer drug discovery.

Isorhamnetin Maximum Cited Publications 10 Publications Verification 3'-Methylquercetin	Cardiovascular Disease Flavonols Structural Classification Classification of Application Fields Source classification Hippophaë rhamnoides Plants Endogenous metabolite Flavonoids Microorganisms Leguminosae Elaeagnaceae Phenols Polyphenols Glycyrrhiza uralensis Fisch. Inflammation/Immunology Disease Research Fields	MEK PI3K Endogenous Metabolite
Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and *PI3K*.

Esculetin 4 Publications Verification	Structural Classification Oleaceae Classification of Application Fields Fraxinus rhynchophylla Hance Source classification Coumarins Phenols Polyphenols Phenylpropanoids Plants Inflammation/Immunology Disease Research Fields	PI3K Akt
Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of *PI3K/Akt* pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .

alpha-Bisabolol	Structural Classification other families Classification of Application Fields Terpenoids Sesquiterpenes Source classification Plants Disease Research Fields Cancer	PI3K Apoptosis
alpha-Bisabolol, an orally active sesquiterpene alcohol, induces cell cycle arrest, mitochondrial apoptosis and inhibition of *PI3K/Akt* signalling pathways. alpha-Bisabolol exerts a protective action against Cisplatin (HY-17394)-induced nephrotoxicity by mitigating inflammation and oxidative stress through the inhibition of NFκB activation. alpha-Bisabolol exhibits anti-inflammatory, analgesic, antibiotic and anticancer activities .

1-Formyl-beta-carboline	Structural Classification Alkaloids Simaroubaceae Source classification Pyridine Alkaloids Plants Picrasma quassioides(D．Don)Benn．	Others
1-Formyl-beta-carboline is an alkaloid with inhibitory activity against Newcastle disease virus (NDV). 1-Formyl-beta-carboline can effectively inhibit different genotypes of NDV with IC50 values within 10 μM, and its inhibition rate is more than 90% at a concentration of 20 μM. 1-Formyl-beta-carboline mainly exerts its effects by inhibiting the adsorption and entry processes in the NDV life cycle. 1-Formyl-beta-carboline has been identified as a novel HN inhibitor that can directly interact with the NDV HN protein and affect the adsorption of NDV. 1-Formyl-beta-carboline also inhibits the entry of NDV by inhibiting the PI3K/Akt signaling pathway rather than the ERK pathway .

Isorhamnetin (Standard) 3'-Methylquercetin (Standard)	Cardiovascular Disease Structural Classification Classification of Application Fields Source classification Hippophaë rhamnoides Plants Endogenous metabolite Flavonoids Leguminosae Elaeagnaceae Phenols Inflammation/Immunology Disease Research Fields Glycyrrhiza uralensis Fisch.	MEK PI3K Endogenous Metabolite
Isorhamnetin (Standard) is the analytical standard of Isorhamnetin. This product is intended for research and analytical applications. Isorhamnetin is a flavonoid compound extracted from the Chinese herb Hippophae rhamnoides L.. Isorhamnetin suppresses skin cancer through direct inhibition of MEK1 and *PI3K*.

Esculetin (Standard)	Structural Classification Oleaceae Fraxinus rhynchophylla Hance Source classification Coumarins Phenols Polyphenols Phenylpropanoids Plants	PI3K Akt
Esculetin (Standard) is the analytical standard of Esculetin. This product is intended for research and analytical applications. Esculetin is an active ingredient extracted mainly from the bark of Fraxinus rhynchophylla. Esculetin inhibits platelet-derived growth factor (PDGF)-induced airway smooth muscle cells (ASMCs) phenotype switching through inhibition of PI3K/Akt pathway. Esculetin has antioxidant, antiinflammatory, and antitumor activities .

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