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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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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. -
mTOR inhibitor
Torin 2 is a potent and selective mTOR inhibitor (IC50 = 2.1 nM). Displays 800-fold cellular selectivity for mTOR over PI3K (cellular EC50 values are 0.25 and 200 nM for mTOR and PI3K respectively).- Diane Yang, .et al. , Diabetes, 2021, Oct;70(10):2419-2429 PMID: 34344789
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mTOR inhibitor
Torin1 is a potent inhibitor of mTOR with IC50 of 2-10 nM.- Andromachi Lambrianidou, .et al. , Cell Signal, 2021, Apr;80:109912 PMID: 33388443
- Kowalsky AH, .et al. , J Biol Chem, 2020, Feb 14;295(7):1769-1780 PMID: 31915252
- Ashyad Rayhan, .et al. , Biol Open, 2018, Jan 15; 7(1): bio031302 PMID: 29343513
- Jin H. Song, .et al. , Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
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GSK-3 Inhibitor
Tideglusib is a GSK-3 inhibitor currently in phase II clinical trials for the treatment of Alzheimer disease and progressive supranuclear palsy- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
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ATM/ATR inhibitor
VE-821 is a potent and selective inhibitor of protein kinase ATR.- Atsushi Saito, .et al. , Cell Rep, 2023, May 30;42(5):112479 PMID: 37178686
- Mitsuru Sasaki-Honda, .et al. , Hum Mol Genet, 2018, Dec 1; 27(23): 4024-4035 PMID: 30107443
- Kim J, .et al. , Mol Cell, 2018, Jan 4;69(1):36-47.e7 PMID: 29249653
- Antonio Postigo, .et al. , Cell Rep, 2017, May 2; 19(5): 1022-1032 PMID: 28467896
- Nnennaya Kanu, .et al. , Genome Biol, 2016, 17: 185 PMID: 27634334
- Carolyn Botting, .et al. , Virol J, 2016, 13: 15 PMID: 26817608
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S6 kinase inhibitor
PF 4708671 is a highly specific inhibitor of p70 ribosomal S6 kinase (S6K1) that inhibits S6K1-mediated phosphorylation of S6 protein in response to IGF-1 , while having no effect on highly related RSK and MSK kinases.- Nogami A, .et al. , Transl Oncol, 2018, Nov 22;12(2):336-349 PMID: 30472492