| DC42548 |
AMPK activator 4 |
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect. |
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| DC42549 |
Parsaclisib hydrochloride
Featured
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Parsaclisib hydrochloride (INCB050465 hydrochloride) is a potent, selective and orally active inhibitor of PI3Kδ, with an IC50 of 1 nM at 1 mM ATP. Parsaclisib hydrochloride shows approximately 20000-fold selectivity over other PI3K class I isoforms. Parsaclisib hydrochloride can be used for the research of relapsed or refractory B-cell malignancies. |
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| DC44210 |
mTOR inhibitor-8 |
mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells. |
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| DC44211 |
(S)-PI3Kα-IN-4 |
(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer. |
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| DC44212 |
PI3Kα-IN-4 |
PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity. |
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| DC44213 |
PF-06843195
Featured
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PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy. |
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| DC44706 |
Metformin |
Metformin (1,1-Dimethylbiguanide), a widely used drug for treatment of type 2 diabetes, activates AMP-activated protein kinase (AMPK) in hepatocytes. Metformin promotes mitophagy in mononuclear cells. Metformin induces apoptosis of lung cancer cells throu |
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| DC44967 |
RMC-5552
Featured
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RMC-5552 is a potent and selective inhibitor of mTORC1. RMC-5552 inhibits phosphorylation of mTORC1 pS6K and p4EBP1 with IC50s of 0.14 nM and 0.48 nM, respectively. RMC-5552 has anti-cancer activity. |
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| DC45196 |
AS-041164 |
AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects. |
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| DC45312 |
(E)-Akt inhibitor-IV |
(E)-Akt inhibitor-IV ((E)-AKTIV) is a PI3K-Akt inhibitor, with potent cytotoxic. |
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| DC45325 |
Galegine hydrochloride |
Galegine hydrochloride, a guanidine derivative, contributes to weight loss in mice. Guanidine hydrochloride is the compound derived from G. officinalis, which gave rise to the biguanides, metformin and phenformin. Galegine hydrochloride activates AMPK in 3T3-L1 adipocytes and L6 myotubes, as well as in the H4IIE rat hepatoma and HEK293 human kidney cell lines. Galegine hydrochloride has antibacterial activity, with minimum inhibitory concentration of 4 mg/L against Staphylococcus aureus strains. |
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| DC45338 |
24-Methylenecycloartanyl ferulate |
24-Methylenecycloartanyl ferulate is a γ-oryzanol compound. 24-Methylenecycloartanyl ferulate promotes parvin-beta expression in human breast cancer cells. 24-Methylenecycloartanyl ferulate is a potential ATP-competitive Akt1 inhibitor (EC50= 33.3μM). |
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| DC45686 |
NVS-PI3-4 |
NVS-PI3-4 is a specific PI3Kγ inhibitor. NVS-PI3-4 can be used for the research of allergies, inflammatory and cancer diseases. |
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| DC45804 |
PKI-179 |
PKI-179 is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 shows anti-tumor activity in vivo. |
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| DC45808 |
FD223 |
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. |
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| DC45809 |
PKI-179 hydrochloride |
PKI-179 hydrochloride is a potent and orally active dual PI3K/mTOR inhibitor, with IC50s of 8 nM, 24 nM, 74 nM, 77 nM, and 0.42 nM for PI3K-α, PI3K-β, PI3K-γ, PI3K-δ and mTOR, respectively. PKI-179 hydrochloride also exhibits activity over E545K and H1047R, with IC50s of 14 nM and 11 nM, respectively. PKI-179 hydrochloride shows anti-tumor activity in vivo. |
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| DC45823 |
AZ2 |
AZ2 is a highly selective PI3Kγ inhibitor. AZ2 can be used for the research of inflammatory and immune diseases. |
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| DC45857 |
PP2A Cancerous-IN-1 |
PP2A Cancerous-IN-1 is a strong and potent CIP2A (Cancerous inhibitor of PP2A) and p-Akt inhibitor. PP2A Cancerous-IN-1 shows the most potent antiproliferative activities. |
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| DC45959 |
Malvidin-3-O-arabinoside chloride |
Malvidin-3-O-arabinoside chloride ameliorates ethyl carbamate-induced oxidative damage by stimulating AMPK-mediated autophagy. |
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| DC46266 |
PI3K-IN-20
Featured
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PI3K-IN-20 is a PI3k inhibitor extracted from WO2017101847 A1, compound 1. |
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| DC46273 |
740 Y-P TFA |
740 Y-P TFA is a potent and cell-permeable PI3K activator. 740 Y-P TFA readily binds GST fusion proteins containing both the N- and C- terminal SH2 domains of p85 but fails to bind GST alone. |
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| DC46384 |
PI3K-IN-19 hydrochloride |
PI3K-IN-19 hydrochloride is a phosphotidylinositol-3-kinase (PI3K) inhibitor extracted from patent WO2017153220, step 5. |
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| DC46457 |
PI3Kγ inhibitor 4 |
PI3Kγ inhibitor 4 is a potent, selective and orally active inhibitor of PI3Kγ, with an IC50 of 40 nM. PI3Kγ inhibitor 4 shows ∼7, 43, and 18-fold selectivity for PI3Kγ over the α, β, and δ isoforms, respectively. PI3Kγ inhibitor 4 can be used for the research of airway inflammation. |
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| DC46468 |
Hu7691 free base |
Hu7691 free base is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 free base inhibits tumor growth and enables decrease of cutaneous toxicity in mice. |
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| DC46469 |
Hu7691 |
Hu7691 is an orally active, selective Akt inhibitor with IC50s of 4.0 nM, 97.5 nM, 28 nM for Akt1, Akt2 and Akt3, respectively. Hu7691 inhibits tumor growth and enables decrease of cutaneous toxicity in mice. |
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| DC46520 |
iMDK quarterhydrate |
iMDK quarterhydrate, a MDK-positive H441 and H520 lung adenocarcinoma cells inhibitor, suppresses the growth of H441 cells by inhibiting the PI3 kinase (PI3K) pathway and inducing apoptosis. iMDK quarterhydrate decreases MDK-induced migration, angiogenesis of endothelial cells and abrogats the progression and metastasis of NSCLC cells. |
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| DC46918 |
Vevorisertib |
Vevorisertib (ARQ 751) is an orally active, potent and selective pan-AKT serine/threonine kinase inhibitor against AKT1 (IC50=0.55 nM), AKT2 (IC50=0.81 nM), and AKT3 (IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA / AKT / PTEN mutations. |
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| DC46919 |
AKT-IN-6 |
AKT-IN-6 (Example 13) is a potent Akt inhibitor. AKT-IN-6 inhibits Akt1, Akt2 and Akt3 with IC50s < 500nM, respectively. (patent WO2013056015A1). |
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| DC47088 |
Amdizalisib |
Amdizalisib is a PI3K inhibitor and used for the research of inflammatory disease, autoimmune disease or cancer. |
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| DC47100 |
MARK-IN-4 |
MARK-IN-4 is a potent microtubule affinity regulating kinase (MARK) inhibitor with an IC50 of 1 nM. Inhibition of microtubule affinity regulating kinase (MARK) represents a potentially attractive means of arresting neurofibrillary tangle pathology in Alzheimer's disease. |
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