DC5081 |
Apitolisib
Featured
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GDC-0980 (RG7422) is a potent, class I PI3K inhibitor for PI3Kα/β/δ/γ with IC50 of 5 nM/27 nM/7 nM/14 nM, respectively. Also a mTOR inhibitor with Ki of 17 nM, and highly selective versus others PIKK family kinases. |
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DC8410 |
GNE-317
Featured
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GNE-317 is a potent, brain-penetrant PI3K inhibitor. |
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DC8257 |
GNE 477
Featured
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GNE-477 is a potent and efficacious dual PI3K/mTOR inhibitor with IC50 of 4 nM for PI3Kα, Kiapp is 21 nM for mTOR. |
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DC8502 |
GNE-490
Featured
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GNE-490 is a highly selective pan-PI3K inhibitor and demonstrates selectivity over mTOR. |
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DC7953 |
GNE-493
Featured
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GNE-493 is a potent, selective, and orally available dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/12/16/16/32 nM for PI3Kα/PI3Kβ/PI3Kγ/PI3Kδ/mTOR respectively. |
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DC9515 |
PI3K inhibitor GS1059615 |
GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
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DC7141 |
Omipalisib
Featured
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GSK2126458 is a highly selective and potent inhibitor of PI3K with Ki of 0.019 nM/0.13 nM/0.024 nM/0.06 nM and 0.18 nM/0.3 nM for p110α/β/δ/γ, mTORC1/2 , respectively. |
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DC9943 |
PI3Kδ inhibitor GS2269557 |
GSK-2269557 is a potent and selective PI3Kδ inhibitor over the closely related isoforms. |
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DC9944 |
PI3Kδ inhibitor GS2292767 |
GSK2292767 is a potent and selective PI3Kδ inhibitor. |
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DC2070 |
GSK690693
Featured
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GSK690693 is a pan-Akt inhibitor targeting Akt1, Akt2 and Akt3 with IC50 of 2 nM, 13 nM, and 9 nM, respectively. |
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DC10061 |
PI4KA inhibitor-A1
Featured
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GSK-A1 is a potent inhibitor of PI4KA. In vitro using HEK-AT1 cells, GSK-A1 had an IC50 of about 3 nM. |
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DC7705 |
HTH-01-015
Featured
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HTH-01-015 is a selective inhibitor of NUAK1 kinase with an IC50 value of 100 nM. |
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DC7156 |
IC-87114
Featured
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IC-87114 was the first isoform-selective PI3K inhibitor. p110δ(IC50 = 0.13 μM) vs. p110α(IC50 = 200 μM), p110β(IC50 = 16 μM) and p110γ(IC50 = 61 μM). |
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DC11151 |
ICSN3250 hydrochloride |
ICSN3250 (ICSN-3250) hydrochloride is a halitulin-analogue that acts as a new-class, specific mTOR inhibitor through a mechanism distinct from previous mTOR inhibitors. |
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DC11150 |
ICSN3250 |
ICSN3250 (ICSN-3250) is a halitulin-analogue that acts as a new-class, specific mTOR inhibitor through a mechanism distinct from previous mTOR inhibitors. |
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DC7171 |
INK-128(Sapanisertib)
Featured
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INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms. |
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DC7873 |
INK-055 (PI3Kγ inhibitor 1) |
INK055 is a dual PI3Kg/d inhibitor. |
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DC5072 |
Duvelisib (IPI-145, INK1197)
Featured
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IPI-145 is an orally bioavailable, highly selective and potent small molecule inhibitor of the delta and gamma isoforms of phosphoinositide-3 kinase (PI3K) with potential immunomodulating and antineoplastic activities. |
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DC9829 |
IPI-549
Featured
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IPI-549 is an orally administered immuno-oncology development candidate that selectively inhibits PI3K-gamma. |
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DC10746 |
KDU691
Featured
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KDU691 is a PI4K inhibitor. |
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DC3101 |
Ku-0063794 |
KU-0063794 is a potent and highly specific mTOR inhibitor for both mTORC1 and mTORC2 with IC50 ~10 nM. |
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DC12386 |
Leniolisib (CDZ173)
Featured
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Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders. |
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DC10754 |
LX2343
Featured
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LX-2343 is a novel non-ATP competitive PI3K inhibitor, negatively regulating AKT/mTOR signaling, thus promoting autophagy, and increasing A-beta clearance. |
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DC1058 |
LY294002
Featured
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LY294002 is a PI3K inhibitor for p110α, p110δ and p110β with IC50 of 0.5 μM, 0.57 μM and 0.97 μM, respectively. |
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DC10219 |
LY3023414
Featured
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LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK. |
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DC7210 |
LY-303511(Nv-128)
Featured
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LY303511, an inactive analogue of LY294002, is a mTOR inhibitor that did not inhibit PI3-K. |
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DC10015 |
MELK-8a
Featured
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MELK-8a is a novel MELK inhibitor. |
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DC11465 |
MELK-T1
Featured
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MELK-T1 is a potent and selective inhibitor of protein kinase MELK. |
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DC7465 |
MK-2206 2HCl
Featured
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MK-2206 2HCl is a highly selective inhibitor of Akt1/2/3 with IC50 of 8 nM/12 nM/65 nM, respectively; no inhibitory activities against 250 other protein kinases observed. Phase 2. |
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DC11405 |
MK-3903
Featured
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MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM.
generation of catalytically active enzyme. |
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