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AKT Inhibitor
Triciribine phosphate inhibits the phosphorylation, activation, and signalling of Akt-1, -2, and -3, which may result in the inhibition of Akt-expressing tumor cell proliferation. -
Akt inhibitor
A-674563 is a B/Akt inhibitor with an IC50 of 14 nM and also shows inhibitory activity against PKA and CDK2 with IC50 of 16 and 46 nM, respectively.- Kobayashi T, .et al. , Biochem Biophys Res Commun, 2018, Jan 1;495(1):1468-1475 PMID: 29196261
- Lin Xu, .et al. , Biochem Biophys Res Commun, 2016, Apr 15;472(4):662-8 PMID: 26920060
- Zou Y, .et al. , Biochem Biophys Res Commun, 2016, Aug 12;477(1):1-8 PMID: 26970307
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mTOR/PI3K Inhibitor,
GSK2126458 is a highly potent, orally bioavailable inhibitor of PI3Kα and mTOR with in vivo activity in both pharmacodynamic and tumor growth efficacy models. -
mTOR Inhibitor
WYE-125132 is an ATP-competitive and specific inhibitor of mTORC1 and mTORC2 (IC50 = 0.19 nM; >5,000-fold selective versus PI3Ks). -
PI3K Inhibitor
YM201636 is a cell-permeable and selective inhibitor of PIKfyve (IC50 = 33 nM).- Krishna Chintaluri, .et al. , PLoS One, 2018, 13(6): e0198454 PMID: 29870544
- Dayam RM, .et al. , J Immunol, 2017, Sep 15;199(6):2096-2105 PMID: 28779020
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AMPK activator
A-769662 is a new activator of AMP-activated protein kinase (AMPK).- Daniel Missailidis, .et al. , Int J Mol Sci., 2021, Feb; 22(4): 2046 PMID: 33669532
- Lieberthal W, .et al. , Am J Physiol Renal Physiol, 2019, 2019 PMID: 30995114
- Kikuchi H, .et al. , Kidney Int, 2018, Nov 13. pii: S0085-2538(18)30635-5 PMID: 30455054
- Schneider H, .et al. , Hypertension, 2015, Jul;66(1):108-16 PMID: 26034200
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PI3K/mTOR inhibitor
PKI-587 is a highly potent PI3K/mTOR kinase inhibitor that inhibits PI3K-α,β,γ, δ isoforms and mTOR with IC50 of 0.4, 6.0, 5.4, 6.0 and 1.6 nM respectively.- Yusuke Murase, .et al. , Oncol Rep, 2022, Apr;47(4):61 PMID: 35088890
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GSK-3 inhibitor
CHIR-98014 is a very potent, selective, cell-permeable reversible inhibitor of GSK-3. -
DNA-PK inhibitor
NU-7441 (KU-57788) is a potent and selective DNA-dependent protein kinase (DNA-PK) inhibitor. The IC50 values are 14, 1700, 5000, >100000 and >100000 nM for DNA-PK, mTOR, PI 3-K, ATM and ATR respectively.- Ryo Sakasai, .et al. , Biochem Biophys Res Commun, 2023, Aug 6;668:42-48 PMID: 37244033
- Shahar Biechonski, .et al. , Sci Rep, 2018, Apr 17 PMID: 29666389
- Ihara M, .et al. , J Radiat Res, 2018, Nov 23 PMID: 30476230
- Chwastek J, .et al. , Int J Biochem Cell Biol, 2017, Jun;87:38-53 PMID: 28341201
- Masaaki Yanai, .et al. , Yonago Acta Med, 2017, Mar; 60(1): 9-15 PMID: 28331416
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PDK-1 inhibitor
BX-795 is a potent PDK1 inhibitor that blocks PDK1/Akt signaling in tumor cells and inhibits the anchorage-dependent growth of a variety of tumor cell lines in culture or induced apoptosis.- Hirosumi Tamura, .et al. , Oncol Rep, 2018, Aug; 40(2): 635-646 PMID: 29917168
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Autophagy/PI3K Inhibitor
3-Methyladenine is an inhibitor of class III phosphatidylinositol 3-kinase (PI 3-kinase).- Yu-Chih Hsu, .et al. , Int J Med Sci, 2023, 20(4): 444-454 PMID: 37057216
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PI3K/HDAC inhibitor
CUDC-907 (Fimepinostat) is a single small molecule inhibitor that targets both PI3K and HDAC. CUDC-907 is more efficacious than either a single PI3K or HDAC inhibitor reference compound or a combination of the two single agents at maximally tolerated doses.- Caner Gunaydın, .et al. , Immunopharmacol Immunotoxicol, 2022, Jun;44(3):447-455 PMID: 35291899
- Chie Ishikawa, .et al. , Eur J Haematol, 2020, Eur J Haematol PMID: 32780889
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RSK Inhibitor
SL 0101-1 is a selective inhibitor of p90 ribosomal S6 kinase (RSK) (IC50 = 89 nM for RSK2). It also inhibits the growth of MCF-7 human breast cancer cells with no effect on the normal breast cell line.
- Pirbhoy PS, .et al. , Learn Mem, 2017, Aug; 24(8): 341-357 PMID: 28716954
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PI3K inhibitor
Wortmannin is a potent, selective, cell-permeable and irreversible inhibitor of phosphatidylinositol 3-kinase (PI 3-kinase) (IC50 = 2 - 4 nM) which also potently inhibits polo-like kinase 1 (PLK1) (IC50 = 5.8 nM).
- Hirotake Ishida, .et al. , J Neurosci, 2021, Oct 13;41(41):8494-8507 PMID: 34452938
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PI3K inhibitor
NVP-BGT226, novel phosphoinositide 3-kinase/mTOR dual inhibitor, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo.
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Akt Inhibitor
GDC-0068 is a selective, ATP-competitive, pan-Akt inhibitor that targets Akt1, 2, and 3 with IC50 values of 5, 18, and 8 nM, respectively in cell-free assays -
PI3K inhibitor
PX-866 is a small-molecule wortmannin analogue inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. -
multi-kinase inhibitor
Cenisertib (AS-703569) is a multi-kinase inhibitor that blocks the activity of Aurora-kinase-A/B, ABL1, AKT, STAT5 and FLT3. -
Akt kinase inhibitor
AKT Kinase Inhibitor is an Akt kinase inhibitor with anti-tumor activity. -
AKT inhibitor
AKT inhibitor VIII is a cell-permeable and reversible quinoxaline compound that potently and selectively inhibits Akt1/Akt2 activity (IC50 = 58 nM, 210 nM, and 2.12 μM for Akt1, Akt2, and Akt3, respectively, in in vitro kinase assays).- Bjune K, .et al. , PLoS One, 2019, Jun 19;14(6):e0218537 PMID: 31216345
- Hoshiba T, .et al. , Biochim Biophys Acta, 2016, Nov;1863(11):2749-2757 PMID: 27558478
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mTORC1/2 inhibitor
AZD2014 is an orally bioavailable inhibitor of the mammalian target of rapamycin (mTOR) with potential antineoplastic activity. mTOR kinase inhibitor.- Shuhang Dai, .et al. , Biochim Biophys Acta Mol Cell Res, 2022, Jul;1869(7):119252 PMID: 35271909
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dual PI3K and mTOR kinase inhibitor
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2. -
PI3K Inhibitor
BLY719 is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.- Elaheh S Abutorabi, .et al. , Mol Biol Rep, 2023, May;50(5):4073-4082 PMID: 36877344
- Lisann Pelzl, .et al. , J Thromb Haemost, 2022, Feb;20(2):387-398 PMID: 34752677
- J Wei, .et al. , bioRxiv, 2018, 2018
- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
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PI3K inhibitor
CZC24832 is a selective inhibitor of PI 3-Kinase γ (IC50 = 1.0 μM in a PI 3-Kγ-dependent fMLP-induced neutrophil migration assay).- Yoshihiro Umezawa, .et al. , J Biol Chem, 2017, Dec 1; 292(48): 19639-19655 PMID: 28974577
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RSK inhibitor
FMK is potent, highly specific and irreversible inhibitor of p90 ribosomal protein S6 kinase RSK1 and RSK2; Fmk binds in the CTKD ATP-binding site and inhibits RSK autophosphorylation at Ser386. Fmk induces significant apoptosis in human FGFR3-expressing, t(4;14)-positive multiple myeloma cells.- Huang-Ming Chang, .et al. , Cell Death Dis, 2021, Apr 17;12(5):409 PMID: 33866326
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PI3Kα/δ inhibitor
Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold). -
Akt inhibitor
Isobavachalcone (Corylifolinin) is derived from Psoralea corylifolia Linn. and is a potent inhibitor of Akt signaling pathway, which induces apoptosis in human cancer cells (Inhibits OVCAR-8 cell growth with an IC50 value of 7.92 μM). -
mTOR inhibitor
INK 128 is a TORC1/2 inhibitor, is also an orally bioavailable inhibitor of raptor-mTOR (TOR complex 1 or TORC1) and rictor-mTOR (TOR complex 2 or TORC2) with potential antineoplastic activity.- Ashlyn Parkhurst, .et al. , Cell Death Dis, 2022, Apr 28;13(4):410 PMID: 35484114
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PI3K/PDK-1 Inhibitor
NVP-BAG956 acts as a potent, reversible, and ATP-competitive PI 3-K/PDK1 dual kinase inhibitor, displaying much reduced potency against VEGFR1 (IC50 = 2.56 uM) and little or no activity toward a panel of 15 other kinases (IC50 >10 uM). -
PDK1 inhibitor
PDK1 inhibitor is a potent and selective inhibitor of PDK1 with potential as anticancer agent.