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Pathways Recommended: PI3K/Akt/mTOR
Results for "

AKT protein kinase inhibitor

" in MedChemExpress (MCE) Product Catalog:

42

Inhibitors & Agonists

4

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1

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2

Peptides

1

Inhibitory Antibodies

11

Natural
Products

2

Isotope-Labeled Compounds

1

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-10230
    Midostaurin
    Maximum Cited Publications
    37 Publications Verification

    PKC412; CGP 41251

    PKC VEGFR c-Kit NO Synthase Apoptosis Cancer
    Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
    Midostaurin
  • HY-122913

    Akt Cancer
    Borussertib, a chemical probe, is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Akt wt .
    Borussertib
  • HY-16558
    Butein
    5+ Cited Publications

    2’,3,4,4’-tetrahydroxy Chalcone

    EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
    Butein
  • HY-A0183
    Phosphatidylserine
    1 Publications Verification

    Phospholipids, phosphatidylserines; Serine glycerophosphatides

    Akt TGF-β Receptor Inflammation/Immunology
    Phosphatidylserine (Phospholipids) is a well-conserved anti-inflammatory and immunosuppressive signal. Phosphatidylserine is involved in membrane translocation and the activation of protein kinase C, participating in Akt signaling through its interaction with PIP3. The local exposure of Phosphatidylserine can interact with complement and other proteins, promoting microglial phagocytosis during critical periods of synaptic refinement. Phosphatidylserine can promote blood coagulation in the extracellular environment and acts as a "eat me" signal to clear out apoptotic cells. Phosphatidylserine can suppress inflammation in tissues by inducing TGF-β secretion and inhibiting immune responses .
    Phosphatidylserine
  • HY-N0281
    Daphnetin
    Maximum Cited Publications
    7 Publications Verification

    7,8-Dihydroxycoumarin

    EGFR PKA PKC Autophagy Apoptosis AMPK Akt mTOR Reactive Oxygen Species (ROS) Caspase Bcl-2 Family PARP Parasite Cardiovascular Disease Inflammation/Immunology Cancer
    Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1β, ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
    Daphnetin
  • HY-13326
    ASP3026
    5+ Cited Publications

    Anaplastic lymphoma kinase (ALK) Apoptosis ROS Kinase Caspase PARP IGF-1R STAT Akt JNK Cancer
    ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research .
    ASP3026
  • HY-N2081
    Skimmianine
    3 Publications Verification

    Cholinesterase (ChE) PI3K Akt NF-κB Neurological Disease Inflammation/Immunology Cancer
    Skimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC50 = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca 2+ signaling and protein kinase C signaling .
    Skimmianine
  • HY-N0699
    Daphnoretin
    3 Publications Verification

    Dephnoretin; Thymelol

    PKC Influenza Virus NOD-like Receptor (NLR) Apoptosis HBV JNK PI3K Akt CDK Caspase Bcl-2 Family Infection Inflammation/Immunology Cancer
    Daphnoretin (Dephnoretin; Thymelol) is a protein kinase C (PKC) activator that inhibits the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and exhibits antiviral activity. Daphnoretin exerts its antitumor effects by inhibiting the activation of the PI3K/AKT signaling pathway and triggers the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and activation of the NLRP3 inflammasome. Daphnoretin regulates the differentiation and maturation of dendritic cells, inhibits their immunostimulatory function by downregulating the phosphorylation level of JNK, and thus exerts a protective effect in skin graft rejection .
    Daphnoretin
  • HY-107597
    Halicin
    2 Publications Verification

    SU3327

    JNK Metabolic Disease Inflammation/Immunology
    Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase .
    Halicin
  • HY-121629

    PDK-1 Cancer
    PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K .
    PS210
  • HY-10721

    AKT protein kinase inhibitor

    Akt Cancer
    PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
    PF-AKT400
  • HY-160469

    Akt PROTACs Cancer
    INY-05-040 is an AKT degrader that can selectively and quickly degrade all three AKT isoforms. INY-05-040 exhibits anti-cancer activity. INY-05-040 can inhibit downstream signaling and cell proliferation in 288 cancer cell lines. INY-05-040 can suppress AKT signaling and induces the stress mitogen-activated protein kinase (MAPK) c-Jun N-terminal kinase (JNK). INY-05-040 is effective for breast cancer lines with a low-baseline activation of stress MAPK pathway. INY-05-040 can be studied for anti-cancer research .
    INY-05-040
  • HY-101246

    RET Cancer
    RPI-1 is a specific, orally available 2-indolinone Ret tyrosine kinase inhibitor. RPI-1 inhibits proliferation, Ret tyrosine phosphorylation, Ret protein expression, and the activation of PLCgamma, ERKs and AKT in human medullary thyroid carcinoma TT cells. Antitumor activity .
    RPI-1
  • HY-P10323

    Tumstatin (74-98), human

    Integrin FAK mTOR Apoptosis Cancer
    T7 Peptide is a protein synthesis inhibitor and anti-angiogenic agent, with a Kd of 10 nM for human transferrin receptor. T7 Peptide inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma .
    T7 Peptide
  • HY-P10323A

    Tumstatin (74-98), human TFA

    Integrin FAK mTOR Apoptosis Cancer
    T7 Peptide TFA is a protein synthesis inhibitor and anti-angiogenic agent, with a Kd of 10 nM for human transferrin receptor. T7 Peptide TFA inhibits the phosphorylation of focal adhesion kinase, the activation of phosphatidylinositol 3-kinase and Akt, the kinase activity of mTOR, as well as the phosphorylation of 4E-BP1 in endothelial cells. T7 Peptide TFA induces G0/G1 cell cycle arrest, apoptosis and protective autophagy in hepatocellular carcinoma cells, and suppresses tumor growth in mouse models. T7 Peptide TFA is applicable to research related to cancer, glioblastoma, hepatocellular carcinoma and glioma .
    T7 Peptide TFA
  • HY-P991664

    Src Akt ERK TAM Receptor c-Met/HGFR MMP HIF/HIF Prolyl-Hydroxylase VEGFR Cancer
    AG01 is a monoclonal antibody against progranulin (GP88). AG01 inhibits triple-negative breast cancer (TNBC) cell proliferation and migration, reduces the expression of phosphorylated protein kinases p-Src, p-AKT, and p-ERK, and reduces the expression of oncogenic proteins such as Axl, c-MET, HIF-1α, and VEGF. AG01 inhibits tumor growth and Ki67 expression in a TNBC xenograft mouse model. AG01 can be used in the research of TNBC and other cancers .
    AG01
  • HY-10230S

    PKC412-d5; CGP 41251-d5

    Isotope-Labeled Compounds PKC Syk Akt PKA c-Kit Cancer
    Midostaurin-d5 (PKC412-d5) is a deuterium labeled Midostaurin. Midostaurin is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM .
    Midostaurin-d5
  • HY-147125

    HSP Akt CDK Raf Apoptosis Cancer
    DDO-6600 is a covalent Hsp90 inhibitor. DDO-6600 disrupts the interaction between Hsp90 and its co-chaperone protein Cdc37, thereby inducing the degradation of kinase client proteins (such as AKT, CDK4, c-Raf). DDO-6600 has inhibitory activity against various cancer cells. DDO-6600 inhibits the migration and invasion of HCT-116 cells, and induces cell cycle arrest and apoptosis. DDO-6600 significantly inhibits tumor growth in the HCT-116 xenograft tumor model. DDO-6600 can be used for research on colorectal cancer .
    DDO-6600
  • HY-174829

    Protease Activated Receptor (PAR) NF-κB Reactive Oxygen Species (ROS) Calcium Channel Akt ERK p38 MAPK PKC Cardiovascular Disease Metabolic Disease
    7,4'-Dimethoxy-3-hydroxyflavone is an orally active PAR4 antagonist. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation with an IC50 of 1.4 μM. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation and PAR4 signaling pathways, including NF-κB, Ca 2+/protein kinase C, Akt, ERK and p38. 7,4'-Dimethoxy-3-hydroxyflavone prevents vascular PAR4 expression, endothelial dysfunction and ameliorates oxidative stress in Streptozotocin (STZ) (HY-13753)-induced diabetic mice. 7,4'-Dimethoxy-3-hydroxyflavone prevents thrombosis in mice without affecting bleeding time [1][2].
    7,4'-Dimethoxy-3-hydroxyflavone
  • HY-150026

    VEGFR PDGFR FGFR c-Kit Akt Src Apoptosis Cancer
    Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .
    Multi-kinase-IN-2
  • HY-N2081R

    Reference Standards Cholinesterase (ChE) PI3K Akt NF-κB Neurological Disease Inflammation/Immunology Cancer
    Skimmianine (Standard) is the analytical standard of Skimmianine. This product is intended for research and analytical applications. Skimmianine is an orally active furoquiniline alkaloid present mainly in the Rutaceae family. Skimmianine has analgesic, antispastic, sedative, and anti-inflammatory properties. Skimmianine inhibits acetylcholinesterase (AChE) (IC50 = 8.6 μg/mL). Skimmianine exhibits cytotoxicity against a variety of cancer cell lines and genotoxicity. Skimmianine has antioxidant and anti-inflammatory effects on ischemia-reperfusion (IR) injury. Skimmianine exerts anti-inflammatory effects through activation of the phosphatidylinositol-3-kinase (PI3K)-protein kinase B (AKT) pathway. Skimmianine is neuroprotective by targeting the NF-κB activation pathway to prevent neuroinflammation. Skimmianine inhibits the release of histamine, intracellular Ca 2+ signaling and protein kinase C signaling .
    Skimmianine (Standard)
  • HY-16558R

    2’,3,4,4’-tetrahydroxy Chalcone (Standard)

    Reference Standards EGFR Autophagy Apoptosis Phosphodiesterase (PDE) Cancer
    Butein (Standard) is the analytical standard of Butein. This product is intended for research and analytical applications. Butein is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4 . Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60c-src in HepG2 cells . Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a . Butein is a SIRT1 activator (STAC).
    Butein (Standard)
  • HY-10230R

    PKC412 (Standard); CGP 41251 (Standard)

    Reference Standards PKC VEGFR c-Kit NO Synthase Apoptosis Cancer
    Midostaurin (Standard) is the analytical standard of Midostaurin. This product is intended for research and analytical applications. Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
    Midostaurin (Standard)
  • HY-W744699

    (+)-Larixol

    Src ERK Akt Inflammation/Immunology
    Larixol is an fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Larixol can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Larixol inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM), cathepsin G release (IC50: 2.76 μM), and chemotaxis. Larixol improves neutrophil hyperactivation and reduces inflammation or tissue damage. A series of Larixol derivatives were found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
    Larixol
  • HY-N0281R

    7,8-Dihydroxycoumarin (Standard)

    Reference Standards EGFR PKA PKC Autophagy Apoptosis AMPK Akt mTOR Reactive Oxygen Species (ROS) Caspase Bcl-2 Family PARP Parasite Inflammation/Immunology Cancer
    Daphnetin (Standard) is the analytical standard of Daphnetin. This product is intended for research and analytical applications. Daphnetin (7,8-dihydroxycoumarin), one coumarin derivative can be found in plants of the Genus Daphne, is a potent, oral active protein kinase inhibitor, with IC50s of 7.67 μM, 9.33 μM and 25.01 μM for EGFR, PKA and PKC in vitro, respectively. Daphnetin triggers ROS-induced cell apoptosis and induces cytoprotective autophagy by modulating the AMPK/Akt/mTOR pathway. Daphnetin has anti-inflammation activitity and inhibits TNF-α, IL-1 , ROS, and MDA production. Daphnetin has schizontocidal activity against malaria parasites. Daphnetin can be used for rheumatoid arthritis , cancer and anti-malarian research .
    Daphnetin (Standard)
  • HY-144060

    Akt Cancer
    AKT-IN-10 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-10 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 4) .
    AKT-IN-10
  • HY-144059

    Akt Cancer
    AKT-IN-9 is a potent inhibitor of AKT. Protein kinase B (PKB, also known as AKT) is central to PI3K/AKT/mTOR signaling in cells, and its function is important for cell growth, survival, differentiation and metabolism. AKT-IN-9 has the potential for the research of breast and prostate cancer (extracted from patent WO2021185238A1, compound 1) .
    AKT-IN-9
  • HY-161351

    Akt STAT Apoptosis Cancer
    STAT3/AKT-IN-1 is a dual inhibitor for the signal transducer and activator of transcription 3 (STAT3) and protein kinase B (AKT) signalling pathway, exhibits antitumor activity against gastric cancer and induces cell apoptosis in SGC-7901 cells .
    STAT3/AKT-IN-1
  • HY-101798

    PI3K Cancer
    MDVN1003 is a Bruton's tyrosine kinase (BTK) and phosphatidylinositol-3-kinase delta (PI3Kδ) dual inhibitor which prevents the activation of B cells and inhibits the phosphorylation of protein kinase B (AKT) and extracellular signal-regulated kinase 1/2 (ERK 1/2). MDVN1003 can be used for non-Hodgkin’s lymphoma (NHL) research .
    MDVN1003
  • HY-13326R

    Anaplastic lymphoma kinase (ALK) Apoptosis ROS Kinase Caspase PARP IGF-1R STAT Akt JNK Cancer
    ASP3026 (Standard) is the analytical standard of ASP3026. This product is intended for research and analytical applications. ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC50 value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research .
    ASP3026 (Standard)
  • HY-162499

    Phosphatase Metabolic Disease
    MY17 is an inhibitor of protein tyrosine phosphatase 1B (PTP1B) (IC50=0.41±0.05 μM). MY17 alleviates palmitic acid (PA) -induced insulin resistance by up-regulating the expression of phosphorylated insulin receptor substrate (IRS1) and protein kinase B (AKT). By binding with PTP1B, MY17 can inhibit the activity of PTP1B, thereby improving insulin signaling and having anti-diabetic activity. MY17 can be used in the study of type 2 diabetes .
    MY17
  • HY-W745090

    Formyl Peptide Receptor (FPR) Src ERK Akt p38 MAPK Others
    Isomaltulose monohydrate is a fMLP inhibitor and also inhibits Src kinase, ERK1/2, p38 and AKT phosphorylation signals in immune regulation. Isomaltulose monohydrate can interfere with the interaction between the βγ subunit of the fMLP receptor Gi protein and its downstream molecules, thereby inhibiting fMLP-induced respiratory burst. Isomaltulose monohydrate inhibits fMLP (0.1 μM)-induced superoxide anion production (IC50: 1.98 μM) , cathepsin G release (IC< sub>50: 2.76 μM) and chemotaxis. Isomaltulose monohydrate can improve excessive activation of neutrophils and reduce inflammation or tissue damage. A series of derivatives of Isomaltulose monohydrate are found to have inhibitory effects on FSGS-related TRPC6 functional mutants .
    Isomaltulose monohydrate
  • HY-W751179

    PKC412-13C6; CGP 41251-13C6

    Isotope-Labeled Compounds Apoptosis VEGFR PKC c-Kit NO Synthase Cancer
    Midostaurin- 13C6 (PKC412- 13C6) is the 13C-labeled Midostaurin (HY-10230). Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
    Midostaurin-13C6
  • HY-136765

    PI3K Cancer
    PI3K-IN-11 (compound 13) is a PI3K inhibitor, which selectively inhibits PI3Kα, PI3Kβ, PI3K, and PI3Kδ (IC50s=6.4, 13, 8, and 11 nM, respectively) over mTOR (IC50=2.9 μM). PX-13-17OH is greater than 420-fold selective for PI3K in a panel of 20 lipid and protein kinases. PX-13-17OH inhibits phosphorylation of Akt and S6 kinase (S6K) in PTEN-negative U87MG cells when used at concentrations ranging from 0.03 to 1 μg/mL. It inhibits tumor growth in a U87MG mouse xenograft model when administered at doses ranging from 2.5 to 10 mg/kg.
    PI3K-IN-11
  • HY-N0699R

    Dephnoretin (Standard); Thymelol (Standard)

    Reference Standards PKC NOD-like Receptor (NLR) Apoptosis HBV Caspase Akt JNK PI3K CDK Influenza Virus Bcl-2 Family Infection Inflammation/Immunology Cancer
    Daphnoretin (Dephnoretin; Thymelol) (Standard) is the analytical standard of Daphnoretin (HY-N0699). This product is used for research and analytical applications. Daphnoretin is a protein kinase C (PKC) activator that can inhibit the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and has antiviral activity. Daphnoretin exerts its anti-tumor effect by inhibiting the activation of the PI3K/AKT signaling pathway, triggering the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and the activation of the NLRP3 inflammasome. Daphnoretin can regulate the differentiation and maturation of dendritic cells, by down-regulating the phosphorylation level of JNK, inhibiting its immune stimulating function, thereby playing a protective role in skin transplant rejection reactions.
    Daphnoretin (Standard)
  • HY-116504

    EGFR Akt ERK Apoptosis Cancer
    WB-308 is a novel small molecule that was identified as an inhibitor of EGFR by an in vitro EGFR kinase activity system. WB-308 was able to reduce the proliferation and clonogenicity of NSCLC cells, causing G2/M phase arrest and apoptosis. In addition, WB-308 inhibited tumor growth in two in vivo animal models (lung orthotopic transplantation model and patient-derived clonal mouse model). WB-308 impaired the phosphorylation of EGFR, AKT, and ERK1/2 proteins. Compared with Gefitinib, WB-308 had lower cytotoxicity. This study showed that WB-308 is a new EGFR-TKI that may be considered as an alternative to Gefitinib in the clinical treatment of NSCLC.
    WB-308
  • HY-174324

    VEGFR P-glycoprotein Apoptosis Cancer
    VEGFR-2/P-gp-IN-1, a Licochalcone A (HY-N0372) derivative, is an orally active VEGFR-2 (IC50 = 0.885 μM) and P-gp inhibitor. VEGFR-2/P-gp-IN-1 achieves anti-tumor proliferation and overcomes chemotherapy resistance by synchronously inhibiting VEGFR-2 kinase activity and P-gp drug efflux pump function. VEGFR-2/P-gp-IN-1 inhibits phosphorylation of VEGFR-2 and downstream PI3K/AKT signaling pathway proteins, induces apoptosis, blocks cells in the S phase, and inhibits invasive migration. VEGFR-2/P-gp-IN-1 exerts potent in vivo anti-tumor effects in the HeLa/DDP cell xenograft tumor model. VEGFR-2/P-gp-IN-1 is used in cervical cancer research.
    VEGFR-2/P-gp-IN-1
  • HY-107597R

    SU3327 (Standard)

    Reference Standards JNK Metabolic Disease Inflammation/Immunology
    Halicin (Standard) is the analytical standard of Halicin (HY-107597). This product is intended for research and analytical applications. Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt Kinase .
    Halicin (Standard)
  • HY-N17632

    Estrogen Receptor/ERR Akt MELK COX Apoptosis Inflammation/Immunology Cancer
    Moracin G is a plant-derived kinase modulator and receptor ligand that forms stable bindings with multiple key proteins (AKT1, COX2 and Estrogen receptor 1) and competitively inhibits the activity of specific kinases. By binding to MELK to disrupt cell cycle regulation, Moracin G impairs the survival and proliferation of cancer cells, induces cancer cell apoptosis, and thereby exerts anti-tumor potential. Moracin G can be used in research related to periodontitis and breast cancer .
    Moracin G
  • HY-174645

    mRNA Metabolic Disease
    Human IL10RA mRNA encodes the human interleukin 10 receptor subunit alpha (IL10RA) protein, a receptor for interleukin 10. IL10RA been shown to mediate the immunosuppressive signal of interleukin 10, and thus inhibits the synthesis of proinflammatory cytokines. It is also reported to promote survival of progenitor myeloid cells through the insulin receptor substrate-2/PI 3-kinase/AKT pathway.
    Human IL10RA mRNA
  • HY-183327

    PI3K mTOR Akt Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism Bcl-2 Family Caspase Cancer
    PI3K/mTOR-IN-22 is an orally active PI3K/mTOR kinase dual inhibitor with IC50 values of 400.5 nM and 8.2 nM. PI3K/mTOR-IN-22 downregulates phosphorylation of the AKT and mTOR, upregulates pro-apoptotic proteins Bax and caspase-3 and downregulates anti-apoptotic protein Bcl-2. PI3K/mTOR-IN-22 exhibits antiproliferative activity against cancer cells, induces apoptosis and ROS production, and reduces mitochondrial membrane potential. PI3K/mTOR-IN-22 exhibits antitumor activity in breast cancer mice models .
    PI3K/mTOR-IN-22
  • HY-179623

    PI3K mTOR Akt CDK Cadherin Cancer
    PI3Kα-IN-29 is a potent, orally active and selective PI3Kα with an IC50 of 2.5 nM. PI3Kα-IN-29 exhibits >400-fold selectivity over PI3Kβ/δ/γ/mTOR. PI3Kα-IN-29 selectively degrades the H1047R mutant p110α protein and inhibits PI3Kα kinase activity. PI3Kα-IN-29 suppresses PI3K/AKT/mTOR signaling, induces G1 arrest, and inhibits migration. PI3Kα-IN-29 inhibits tumor growth in a T47 mouse model. PI3Kα-IN-29 can be used for the research of breast cancer .
    PI3Kα-IN-29

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