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Pathways Recommended: PI3K/Akt/mTOR
Results for "

Akt inhibition

" in MedChemExpress (MCE) Product Catalog:

59

Inhibitors & Agonists

1

Screening Libraries

4

Peptides

1

Inhibitory Antibodies

22

Natural
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1

Isotope-Labeled Compounds

2

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1

Oligonucleotides

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-15186
    Ipatasertib
    Maximum Cited Publications
    45 Publications Verification

    GDC-0068; RG7440

    Organoid Akt Apoptosis Cancer
    Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
    Ipatasertib
  • HY-N4182
    Licochalcone E
    1 Publications Verification

    Akt p38 MAPK Autophagy Inflammation/Immunology
    Licochalcone E, a flavonoid compound isolated from Glycyrrhiza uralensis, inhibits NF-κB and AP-1 transcriptional activity through the inhibition of AKT and MAPK activation .
    Licochalcone E
  • HY-19934A

    TAS-117 hydrochloride

    Akt Apoptosis Autophagy Cancer
    Pifusertib (TAS-117) hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib hydrochloride induces apoptosis and autophagy .
    Pifusertib hydrochloride
  • HY-121222

    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-103224

    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-P10049

    Akt Cancer
    TAT-TCL1-Akt-in is an Akt inhibitor .
    TAT-TCL1-Akt-in
  • HY-15186C

    GDC-0068 tosylate; RG7440 tosylate

    Organoid Akt Apoptosis Cancer
    Ipatasertib (GDC-0068) tosylate is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib tosylate synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib tosylate also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models .
    Ipatasertib tosylate
  • HY-P1115

    Akt Others
    AKTide-2T is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
    AKTide-2T
  • HY-P1115A

    Akt Others
    AKTide-2T TFA is an excellent in vitro substrate for AKT and shows competitive inhibition of histone H2B phosphorylation with a Ki of 12 nM. AKTide-2T TFA mimics the optimal phosphorylation sequence of Akt and is an inhibitory peptide with the wildtype AKTide lacking Thr in the S22 position .
    AKTide-2T TFA
  • HY-19934

    TAS-117

    Akt Apoptosis Autophagy Cancer
    Pifusertib (TAS-117) is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). Pifusertib triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. Pifusertib induces apoptosis and autophagy .
    Pifusertib
  • HY-163533

    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-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 .
    Esculetin
  • HY-N0717
    L-Valine
    4 Publications Verification

    (S)-Valine

    Bacterial Arginase Akt Infection
    L-Valine (Valine) is a new 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-144450

    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-113427
    trans-Vaccenic acid
    1 Publications Verification

    Endogenous Metabolite Bcl-2 Family Apoptosis Cardiovascular Disease Cancer
    trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity .
    trans-Vaccenic acid
  • HY-12037A
    Rigosertib
    5+ Cited Publications

    ON-01910

    Polo-like Kinase (PLK) PI3K Apoptosis Cancer
    Rigosertib (ON-01910) is a multi-kinase inhibitor and a selective anti-cancer agent, which induces apoptosis by inhibition the PI3 kinase/Akt pathway, promots the phosphorylation of histone H2AX and induces G2/M arrest in cell cycle . Rigosertib is a selective and non-ATP-competitive inhibitor of PLK1 with an IC50 of 9 nM .
    Rigosertib
  • HY-N3584
    Paris saponin VII
    3 Publications Verification

    Chonglou Saponin VII

    Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis Cancer
    Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
    Paris saponin VII
  • HY-N1365

    6-Hydroxy-7-methoxycoumarin

    HBV p38 MAPK NF-κB STAT Akt ERK JNK Infection Inflammation/Immunology Cancer
    Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively . Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitory activity against HBV replication . Isoscopoletin exhibits anti-inflammatory activity through inhibition of MAPK/NF-κB/STAT/AKT signaling pathway .
    Isoscopoletin
  • HY-N3074R

    Bacterial Antibiotic Infection Inflammation/Immunology Cancer
    alpha-Bisabolol (Standard) is the analytical standard of alpha-Bisabolol. This product is intended for research and analytical applications. 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 .
    Hexahydrofarnesyl acetone (Standard)
  • HY-128741

    Endogenous Metabolite Reactive Oxygen Species 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-N0284R

    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-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-103224R

    PI3K Cancer
    PIT-1 (Standard) is the analytical standard of PIT-1. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N15474

    Na+/Ca2+ Exchanger Cancer
    12-O-Deacetyl-phomoxanthone A, a Na +/Ca 2+ exchanger 1 (NCX1) activator, causes an increase in cellular Ca 2+ signaling and subsequent inhibition of the downstream PI3K/AKT/β-catenin pathway. 12-O-Deacetyl-phomoxanthone A induces apoptosis and induces G1 phase arrest. 12-O-Deacetyl-phomoxanthone A can be used in the research for melanoma .
    12-O-Deacetyl-phomoxanthone A
  • HY-N1365R

    6-Hydroxy-7-methoxycoumarin (Standard)

    HBV p38 MAPK NF-κB STAT Akt ERK JNK Infection Inflammation/Immunology Cancer
    Isoscopoletin (Standard) is the analytical standard of Isoscopoletin. This product is intended for research and analytical applications. Isoscopoletin (6-Hydroxy-7-methoxycoumarin) is an active constituent in Artemisia argyi leaves. Isoscopoletin shows substantial inhibition against cell proliferation, with IC50s of 4.0 μM and 1.6 μM for human CCRF-CEM leukaemia cells and multidrug resistant subline CEM/ADR5000, respectively . Isoscopoletin (6-Hydroxy-7-methoxycoumarin) possesses inhibitory activity against HBV replication . Isoscopoletin exhibits anti-inflammatory activity through inhibition of MAPK/NF-κB/STAT/AKT signaling pathway .
    Isoscopoletin (Standard)
  • HY-113427R

    Endogenous Metabolite Bcl-2 Family Apoptosis Cardiovascular Disease Cancer
    trans-Vaccenic acid (Standard) is the analytical standard of trans-Vaccenic acid (HY-113427). This product is intended for research and analytical applications. trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity.
    trans-Vaccenic acid (Standard)
  • HY-N12124

    Monascinol

    Akt mTOR AMPK Androgen Receptor Apoptosis Autophagy Cancer
    Monascuspiloin (Monascinol) exhibits anti-androgenic activity with an IC50 of 7 μM. Monascuspiloin inhibits viability of PC-3 and LNCaP with IC50 of 45 and 47 μM. Monascuspiloin induces apoptosis in LNCaP through inhibition of Akt/mTOR signaling pathway, induces autophagy through activation AMPK signaling pathway and arrest cell cycle at G2/M phase in PC-3. Monascuspiloin exhibits antitumor efficacy in mice .
    Monascuspiloin
  • 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 .
    Musk ketone
  • HY-107661
    Arundic Acid
    1 Publications Verification

    ONO-2506; (R)-2-Propyloctanoic acid

    Others Neurological Disease
    Arundic acid (ONO-2506) is an astrocyte-modulating agent, which delays the expansion of cerebral infarcts by modulating the activation of astrocytes through inhibition of S-100β synthesis. Arundic acid also increases the expression level of EAAT1 by activating the Akt, ERK, and NF-κB signaling pathways, which has the potential to eliminate excess glutamate and inhibit excitotoxic brain damage or death. Arundic acid has the potential for stroke and Alzheimer’s disease research .
    Arundic Acid
  • HY-N0717R

    (S)-Valine (Standard)

    Arginase Akt Bacterial Others
    L-Valine (Standard) is the analytical standard of L-Valine. This product is intended for research and analytical applications. L-Valine (Valine) is a new nonlinear semiorganic material. L-Valine standrd causes lipid peroxidation and accumulation of malondialdehyde (MDA), exhibits inhibitory activity against cyanobacteria. L-Valine standrd inhibits multidrug-resistant bacteria through activation of PI3K/Akt signaling pathway and inhibition of arginase .
    L-Valine (Standard)
  • HY-N0721

    Neoandrographiside

    ERK p38 MAPK JNK NF-κB PI3K PPAR GSK-3 CaMK NO Synthase Reactive Oxygen Species 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-113427S

    Isotope-Labeled Compounds Endogenous Metabolite Bcl-2 Family Apoptosis Cardiovascular Disease Cancer
    trans-Vaccenic acid-d13 is deuterium labeled trans-Vaccenic acid (HY-113427). trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity .
    trans-Vaccenic acid-d13
  • HY-N3584R

    Akt p38 MAPK P-glycoprotein Bcl-2 Family Caspase PARP Autophagy Apoptosis Cancer
    Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
    Paris saponin VII (Standard)
  • HY-16958R

    Antibiotic Dimethylargininase (DDAH) Inflammation/Immunology
    Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
    PD 404182 (Standard)
  • HY-15113

    Prolyl Endopeptidase (PREP) Neurological Disease Cancer
    Y-29794 is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 penetrates the brain-blood barrier (BBB) .
    Y-29794
  • HY-15113A

    Prolyl Endopeptidase (PREP) Neurological Disease Cancer
    Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PREP), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB) .
    Y-29794 tosylate
  • HY-B0808A

    Oxaprozinum potassium; Wy21743 potassium

    COX NF-κB Akt IKK Apoptosis Inflammation/Immunology Cancer
    Oxaprozin potassium is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin potassium also inhibits the activation of NF-κB. Oxaprozin potassium induces cell apoptosis. Oxaprozin potassium shows anti-inflammatory activity. Oxaprozin potassium-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties .
    Oxaprozin potassium
  • HY-B0808

    Oxaprozinum; Wy21743

    COX NF-κB Akt IKK Apoptosis Inflammation/Immunology Cancer
    Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties .
    Oxaprozin
  • HY-145102

    HSP Apoptosis Cancer
    NCT-58 is a potent inhibitor of C-terminal HSP90. NCT-58 does not induce the heat shock response (HSR) due to its targeting of the C-terminal region and elicits anti-tumor activity via the simultaneous downregulation of HER family members as well as inhibition of Akt phosphorylation. NCT-58 kills Trastuzumab-resistant breast cancer stem-like cells. NCT-58 induces apoptosis in HER2-positive breast cancer cells .
    NCT-58
  • HY-N0721R

    Neoandrographiside (Standard)

    Reference Standards ERK p38 MAPK JNK NF-κB PI3K PPAR GSK-3 NO Synthase Reactive Oxygen Species 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-B0808R

    Oxaprozinum (Standard); Wy21743 (Standard)

    COX NF-κB Akt IKK Apoptosis Inflammation/Immunology Cancer
    Oxaprozin (Standard) is the analytical standard of Oxaprozin. This product is intended for research and analytical applications. Oxaprozin is an orally active and potent COX inhibitor, with IC50 values of 2.2 μM for human platelet COX-1 and and 36 μM for IL-1-stimulated human synovial cell COX-2, respectively. Oxaprozin also inhibits the activation of NF-κB. Oxaprozin induces cell apoptosis. Oxaprozin shows anti-inflammatory activity. Oxaprozin-mediated inhibition of the Akt/IKK/NF-κB pathway contributes to its anti-inflammatory properties .
    Oxaprozin (Standard)
  • HY-156002

    Paluratide

    Ras ERK Cancer
    LUNA18 is an orally-available cyclic peptide KRAS and ERK inhibitor. LUNA18 phosphorylates ERK and AKT and decreases cell proliferation in RAS-mutated cancer cells. LUNA18 exhibits RAS signal inhibition and potent anti-cancer activities through inhibiting interaction between RAS and guanine nucleotide exchange factors (GEFs) in a mouse xenograft model. LUNA18 shows significant cellular efficacy against cell lines with KRAS genetic alterations, such as colon cancer, stomach cancer, non-small cell lung cancer and pancreaticcancer .
    LUNA18
  • HY-146325

    HSP Cancer
    HSP90-IN-11 (Compound 12c) is a potent inhibitor of HSP90. HSP90-IN-11 displays potent HSP90α inhibition comparable to AUY-922 (Luminespib). HSP90-IN-11 shows significant antiproliferative activity in CRC and NSCLC cells in a double digit nM range. HSP90-IN-11 leads to rapid degradation of client proteins EGFR and Akt in NSCLC cells. HSP90-IN-11 induces significant accumulation of a sub-G1 phase population .
    HSP90-IN-11
  • HY-N6932

    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-13270

    E7010

    Microtubule/Tubulin Autophagy Apoptosis Cancer
    ABT-751 (E7010) is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
    ABT-751
  • HY-132231

    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-107738
    Guggulsterone
    10+ Cited Publications

    Z/E-Guggulsterone

    Apoptosis JNK Akt Caspase FXR Autophagy Cancer
    Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt . Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively .
    Guggulsterone
  • HY-13270A

    E7010 hydrochloride

    Microtubule/Tubulin Autophagy Apoptosis Cancer
    ABT-751 (E7010) hydrochloride is a novel, highly orally bioavailable sulfonamides antimitotic compound and tubulin binder. It prevents tubulin aggregation by binding to the colchicine site on β-tubulin, leading to cell cycle arrest in G2/M phase and inducing apoptosis, thus effectively preventing cell division. ABT-751 (E7010) hydrochloride induces autophagy by inhibiting the AKT/MTOR signaling pathway. ABT-751 (E7010) hydrochloride showed significant inhibition against various types of cancer cells, including lung, gastric, colon, and breast cancer .
    ABT-751 hydrochloride
  • HY-172620

    IKK Akt Apoptosis Cancer
    LIB3S0280 is a potent TBK1 inhibitor with an IC50 value of 493.9 nM. LIB3S0280 can inhibit TBK1 downstream signaling by decreasing the phosphorylation of IκBα and AKT. LIB3S0280 leads to G2/M arrest and induces apoptosis in pancreatic cancer cells. LIB3S0280 shows significant inhibition against pancreatic cancer cell lines that highly express TBK1 with IC50 values of 6.64-10.98 μM at 96 h. LIB3S0280 has the potential for pancreatic ductal adenocarcinoma (PDAC) research .
    LIB3S0280
  • HY-151137

    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

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