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Pathways Recommended: PI3K/Akt/mTOR
Results for "

PI3K inhibition

" in MedChemExpress (MCE) Product Catalog:

66

Inhibitors & Agonists

1

Screening Libraries

2

Inhibitory Antibodies

19

Natural
Products

16

Isotope-Labeled Compounds

1

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0776
    Isorhamnetin
    15+ 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.
    Isorhamnetin
  • HY-N0717
    L-Valine
    5 Publications Verification

    (S)-Valine

    		 Bacterial Arginase Akt Infection
    L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
    L-Valine
  • HY-N0484
    Liensinine
    Maximum Cited Publications
    20 Publications Verification

    		 Reactive Oxygen Species (ROS) Autophagy Apoptosis VEGFR JAK Amyloid-β p38 MAPK HIF/HIF Prolyl-Hydroxylase STAT PI3K JNK Akt Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Liensinine is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke .
    Liensinine
  • HY-12481
    SAR405
    Maximum Cited Publications
    35 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; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity .
    SAR405
  • HY-159852
    BBO-10203

    		PI3K Ras Akt Cancer
    BBO-10203 is a potent inhibitor of PI3Kα and KRAS G12C, selectively and covalently binding to Cys242 in the RAS-Binding Domain of PI3Kα, and inhibiting both the GTP-bound and GDP-bound states of KRAS G12C with an IC50 of 0.031 nM and an EC50 of 0.02 nM. BBO-10203 disrupts the interaction between RAS isoforms and PI3Kα, leading to the inhibition of RAS-mediated PI3Kα activation, and reduces pERK expression, cell growth, and induces G1 arrest and apoptosis. BBO-10203 can be used for the research of breast cancer, colorectal cancer, and non-small cell lung cancer .
    BBO-10203
  • HY-N0284
    Esculetin
    5+ Cited Publications

    		 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 .
    Esculetin
  • HY-I1124
    L-Valine-d8
    1 Publications Verification

    L-VALINE-2,3,4,4,4,5,5,5-d8

    		 Isotope-Labeled Compounds Arginase Akt Bacterial Infection
    L-Valine-d8 is a deuterated form of L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
    L-Valine-d8
  • HY-N0721
    Neoandrographolide
    1 Publications Verification

    Neoandrographiside

    		 ERK p38 MAPK JNK NF-κB PI3K PPAR GSK-3 CaMK NO Synthase Reactive Oxygen Species (ROS) Apoptosis Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Neoandrographolide is a diterpenoid compound isolated from Andrographis paniculata. Neoandrographolide inhibits osteoclasts differentiation and bone resorption through inhibition of MAPK/NF-κB/PI3K/AKT/GSK3β/PPAR/CAMK signaling pathway. Neoandrographolide inhibits apoptosis in rat embryonic ventricular cardiomyocytes. Neoandrographolide inhibits iNOS and the generation of ROS, activates eNOS, exhibiting anti-inflammatory and hypolipidemic activity .
    Neoandrographolide
  • HY-N0876
    Arenobufagin
    4 Publications Verification

    		 Apoptosis Autophagy PI3K Akt mTOR PARP Caspase Atg8/LC3 Cancer
    Arenobufagin is a natural bufadienolide that can be extracted from toad venom. Arenobufagin can induce apoptosis and autophagy in human hepatocellular carcinoma cells through inhibition of PI3K/Akt/mTOR pathway. Arenobufagin has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells. Arenobufagin can inhibit VEGF-mediated angiogenesis through suppression of VEGFR-2 signaling pathway .
    Arenobufagin
  • HY-128741
    D-Allose

    		Endogenous Metabolite Reactive Oxygen Species (ROS) Apoptosis Toll-like Receptor (TLR) PI3K Akt Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    D-Allose exhibits antitumor activity against various cancer cells. D-Allose scavenges reactive oxygen species (ROS) and reduces oxidative stress damage. D-Allose exhibits anti-inflammatory and neuroprotective through inhibition of TLR4/PI3K/AKT signaling pathway. D-Allose exhibits antihypertensive, cryoprotective, and anti-osteoporotic activities .
    D-Allose
  • 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 .
    alpha-Bisabolol
  • HY-N0717S6
    L-Valine-13C5

    (S)-Valine-13C5

    		 Isotope-Labeled Compounds Arginase Akt Bacterial Infection
    L-Valine- 13C5 ((S)-Valine- 13C5) is the 13C-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
    L-Valine-13C5
  • HY-12037
    Rigosertib sodium
    5+ Cited Publications

    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 .
    Rigosertib sodium
  • HY-N0717R
    L-Valine (Standard)

    (S)-Valine (Standard)

    		 Reference Standards Arginase Akt Bacterial Infection
    L-Valine (Standard) ((S)-Valine (Standard)) is the analytical standard of L-Valine (HY-N0717). This product is intended for research and analytical applications. L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
    L-Valine (Standard)
  • HY-N0717S4
    L-Valine-1-13C

    (S)-Valine-1-13C

    		 Isotope-Labeled Compounds Arginase Akt Bacterial Infection
    L-Valine-1- 13C ((S)-Valine-1- 13C) is the 13C-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
    L-Valine-1-13C
  • 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 .
    Taspine
  • HY-156406
    PITCOIN4
    1 Publications Verification

    		 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 .
    PITCOIN4
  • 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 .
    PIT-1
  • HY-N2045
    Musk ketone
    1 Publications Verification

    		 Environmental Pollutants Apoptosis Akt Cytochrome P450 PI3K 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 .
    Musk ketone
  • HY-N0717S
    L-Valine-15N

    (S)-Valine-15N

    		 Isotope-Labeled Compounds Arginase Akt Bacterial Infection
    L-Valine- 15N ((S)-Valine- 15N) is the 15N-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
    L-Valine-15N
  • HY-N0717S1
    L-Valine-13C5,15N

    (S)-Valine-13C5,15N

    		 Isotope-Labeled Compounds Arginase Akt Bacterial Infection
    L-Valine- 13C5, 15N ((S)-Valine- 13C5, 15) is the 13C- and 15N-labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
    L-Valine-13C5,15N
  • 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 .
    PI3K/mTOR Inhibitor-4
  • HY-N6932
    Voacamine

    		Cannabinoid Receptor P-glycoprotein PI3K Akt mTOR Apoptosis Autophagy EGFR Metabolic Disease Cancer
    Voacamine is an indole alkaloid with cannabinoid 1 (CB1) antagonistic activity. Voacamine can inhibit nuclear translocation. Voacamine is effective in enhancing the effect of Doxorubicin (HY-15142A) as it interferes with the P-glycoprotein (P-gp) function. Voacamine promotes apoptosis-independent autophagic cell death in human osteosarcoma cells. Voacamine activates mitochondrial-associated apoptosis signaling pathway and inhibition of PI3K/Akt/mTOR signaling pathway to suppress breast cancer progression. Voacamine inhibits EGFR to exert oncogenic activity against colorectal cancer .
    Voacamine
  • HY-W130965
    1-Formyl-beta-carboline

    		Influenza Virus Akt 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 .
    1-Formyl-beta-carboline
  • HY-176239
    PROTAC PI3Kδ degrader-1

    		PROTACs PI3K Akt Apoptosis Autophagy Cancer
    PROTAC PI3Kδ degrader-1 is a Lysine-targeted covalent PI3Kδ PROTAC degrader with a DC50 of 3.98 nM. PROTAC PI3Kδ degrader-1 has a potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). PROTAC PI3Kδ degrader-1 also significantly degrades p-AKT, induces cell cycle arrest in G1 phase and prompts cell apoptosis and autophagy. PROTAC PI3Kδ degrader-1 effectively inhibits the tumor growth in SU-DHL-6 xenograft mice model . Pink: PI3Kδ ligand (HY-169983); Blue: VHL ligase ligand (HY-112078); Black: linker (HY-W013381)
    PROTAC PI3Kδ degrader-1
  • 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 .
    (S)-GSK-F1
  • HY-155066
    FD274

    		PI3K mTOR Apoptosis 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 arrests HL-60 cell cycle at G1 phase and increases apoptosis. FD274 demonstrates dose-dependent inhibition of tumor growth in the HL-60 xenograft model. FD274 has the potential for acute myeloid leukemia research .
    FD274
  • HY-N0284R
    Esculetin (Standard)

    		Reference Standards 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 .
    Esculetin (Standard)
  • HY-146223
    AZD4625

    		Ras p38 MAPK PI3K Apoptosis Cancer
    AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
    AZD4625
  • HY-N5014
    Liensinine perchlorate
    Maximum Cited Publications
    20 Publications Verification

    		 Reactive Oxygen Species (ROS) Autophagy Apoptosis VEGFR JAK Amyloid-β p38 MAPK HIF/HIF Prolyl-Hydroxylase STAT PI3K JNK Akt Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
    Liensinine perchlorate is a bisbenzylisoquinoline alkaloid. By inhibiting the PI3K/AKT and JNK/p38-MAPK signaling pathways, Liensinine perchlorate suppresses autophagy and apoptosis, clears Aβ, and exerts anti-inflammatory, antioxidant and neuroprotective effects. Liensinine perchlorate activates AMPK and inhibits the expression of HIF-1α and VEGF, thereby suppressing angiogenesis. Liensinine perchlorate exerts anti-tumor effects through ROS-mediated inhibition of the JAK2/STAT3 signaling pathway. Liensinine perchlorate can be used for the research of diseases such as Alzheimer's disease, hepatocellular carcinoma, osteosarcoma, sepsis-induced organ injury and stroke .
    Liensinine perchlorate
  • HY-128633
    DHW-208

    		PI3K Akt Apoptosis Cancer
    PI3K-IN-4 is a potent Pan-PI3K inhibitor. PI3K-IN-4 has high activity for three PI3K isoforms with the IC50 values of picomole. PI3K-IN-4 shows superior inhibitory activity against PI3Kα (IC50 = 0.20 nM), PI3Kβ (IC50 = 2.99 nM), PI3Kδ (IC50 = 0.48 nM) and PI3Kγ (IC50 = 0.58 nM) and has no significant activity against EGFR. PI3K-IN-4 inhibits cancer cell growth though PI3K/Akt signaling pathway, leading to the inhibition of colony formation and the induction of apoptosis. PI3K-IN-4 can be used for lung, colon and breast cancer research .
    DHW-208
  • HY-115814
    AM-1430

    		PI3K Inflammation/Immunology
    AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC50 of 4.6 nM. AM-1430 exhibits IC50s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases .
    AM-1430
  • HY-N0776R
    Isorhamnetin (Standard)

    3'-Methylquercetin (Standard)

    		 Reference Standards 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.
    Isorhamnetin (Standard)
  • HY-128741S
    D-Allose-13C

    		Isotope-Labeled Compounds Endogenous Metabolite Akt Apoptosis Reactive Oxygen Species (ROS) PI3K Cancer
    D-Allose- 13C is the 13C labeled D-Allose (HY-128741). D-Allose exhibits antitumor activity against various cancer cells. D-Allose scavenges reactive oxygen species (ROS) and reduces oxidative stress damage. D-Allose exhibits anti-inflammatory and neuroprotective through inhibition of TLR4/PI3K/AKT signaling pathway. D-Allose exhibits antihypertensive, cryoprotective, and anti-osteoporotic activities .
    D-Allose-13C
  • HY-N0721R
    Neoandrographolide (Standard)

    Neoandrographiside (Standard)

    		 Reference Standards ERK p38 MAPK JNK NF-κB PI3K PPAR GSK-3 NO Synthase Reactive Oxygen Species (ROS) Apoptosis Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Neoandrographolide (Standard) is the analytical standard of Neoandrographolide. This product is intended for research and analytical applications. Neoandrographolide is a diterpenoid compound isolated from Andrographis paniculata. Neoandrographolide inhibits osteoclasts differentiation and bone resorption through inhibition of MAPK/NF-κB/PI3K/AKT/GSK3β/PPAR/CAMK signaling pathway. Neoandrographolide inhibits apoptosis in rat embryonic ventricular cardiomyocytes. Neoandrographolide inhibits iNOS and the generation of ROS, activates eNOS, exhibiting anti-inflammatory and hypolipidemic activity .
    Neoandrographolide (Standard)
  • 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 .
    FD223
  • 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 .
    HSP90/mTOR-IN-1
  • HY-P991524
    MM-111

    		EGFR Cancer
    MM-111 is a bispecific antibody fusion protein targeting the ErbB2/ErbB3 oncogenic unit. MM-111 blocks activation of the PI3K pro-survival pathway. MM-111 binds to the ErbB2 receptor, which localizes the bispecific molecule to ErbB2 over-expressing tumor cells and promotes binding of the anti-ErbB3 arm to the ErbB3 receptor. MM-111 binding to ErbB3 results in inhibition of ErbB3 signaling by blocking the binding of the ErbB3 physiological ligand heregulin. MM-111 can be used for the study of ErbB2 over-expressing breast tumors .
    MM-111
  • HY-146223A
    (3R,10R,14aS)-AZD4625

    		Ras PI3K p38 MAPK Apoptosis Cancer
    (3R,10R,14aS)-AZD4625 is the isomer of AZD4625 (HY-146223), and can be used as an experimental control. AZD4625 is an orally active, selective irreversible, covalent allosteric GTPase KRASG12C inhibitor with an IC50 of 3 nM. AZD4625 can inhibit the MAPK pathway (with decreased pCRAF, pMEK, and pERK) and the PI3K pathway (with decreased pAKT and pS6), and induce cell apoptosis. AZD4625 has no binding and inhibition of wild-type RAS or isoforms carrying non-KRASG12C mutations. AZD4625 can be used for the study of KRASG12C mutant non-small cell lung cancer .
    (3R,10R,14aS)-AZD4625
  • HY-178775
    PI4K-IN-3

    		PI4K Parasite MAP4K PI3K Infection
    PI4K-IN-3 (Compound 27) is an orally active PI4K inhibitor with an IC50 of 1.9  nM for Plasmodium vivax PI4K. PI4K-IN-3 has no hERG channel inhibition and mammalian cytotoxicity. PI4K-IN-3 has significant selectivity against the human MINK1 and MAP4K4 kinases but with low selectivity against human PI3Kα and PI4Kβ. PI4K-IN-3 has potent antimalarial activity and significantly reduces parasitaemia in NSG mice mouse models of Plasmodium falciparum malaria .
    PI4K-IN-3
  • HY-141876
    PRT543

    		Histone Methyltransferase Notch PI3K Akt Bcl-2 Family DNA/RNA Synthesis Cancer
    PRT543 is an orally active selective PRMT5 inhibitor. PRT543 reduces intracellular symmetric dimethylarginine (sDMA) levels, downregulates the expression of genes related to DNA damage repair and DNA replication pathways, and induces abnormal alternative splicing. PRT543 inhibits the MYB, NOTCH1 and PI3K/AKT signaling pathways, promotes nuclear translocation of FOXO1, upregulates the pro-apoptotic protein BAX, and enhances cellular sensitivity to BCL-2 inhibition. PRT543 disrupts the normal RNA splicing process and exerts a synthetic lethal effect on myeloid tumor cells carrying splicing factor mutations. PRT543 can be used in research related to various cancers including breast cancer, ovarian cancer and acute myeloid leukemia .
    PRT543
  • 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 .
    PI3K-IN-29
  • 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) .
    RV-1729
  • HY-116497
    PH11

    		FAK 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.
    PH11
  • 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 .
    ATM Inhibitor-3
  • 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 .
    ATM Inhibitor-4
  • 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 .
    CPD-002
  • 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) .
    LAS195319
  • 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 .
    SU-11752
  • HY-178305S
    L-Valine-d

    		Isotope-Labeled Compounds Bacterial Arginase Akt Infection
    L-Valine-d is the deuterium labeled L-Valine (HY-N0717). L-Valine ((S)-Valine) is a nonlinear semiorganic material. L-Valine causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
    L-Valine-d

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