Catalog No.
Product Name
Application
Product Information
Product Citation
-
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
-
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
-
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
-
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
-
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
-
AKT inhibitor
AZD5363 is a potent inhibitor of AKT with pharmacodynamic activity in vivo, has potential to treat a range of solid and hematologic tumors as monotherapy or a combinatorial agent.- Hiroyuki Tsuchiya, .et al. , Curr Issues Mol Biol, 2023, Jan 29;45(2):1073-1085 PMID: 36826016
- Giri R. Gnawali, .et al. , Medicinal Chemistry Research, 2022, 31: 1154-1175
- Jeremiah J Bearss, .et al. , EMBO Rep, 2021, Apr 7;22(4):e50835 PMID: 33586867
- Jin H. Song, .et al. , Mol Cancer Ther, 2018, Dec;17(12):2710-2721 PMID: 30190422
-
PI3K inhibitor
BAY 80-6946 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity.- Shin SM, .et al. , Sci Adv, 2020, Jan 15;6(3):eaay2174 PMID: 31998840
-
DNA-PK inhibitor
Compound 401 is a cell-permeable pyrimido-isoquinolinone compound that acts as a potent, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 280 nM) with ~19-fold selectivity over mTOR (IC50 = 5.3 μM). -
PI3K Inhibitor
GSK2636771 is a potent, orally bioavailable, PI3K beta-selective inhibitor.- Pridham KJ, .et al. , Neuro Oncol, 2018, Mar 27;20(4):494-505 PMID: 29016844
-
mTOR inhibitor
Zotarolimus is an immunosuppressant. It is a semi-synthetic derivative of rapamycin. It was designed for use in stents with phosphorylcholine as a carrier. -
AMPK inhibitor
BML-275 is a cell-permeable pyrazolopyrimidine compound shown to be an AMP-activated protein kinase (AMPK) and fatty acid synthase inhibitor.- Yang PM, .et al. , Am J Cancer Res, 2019, Oct 1;9(10):2120-2139 PMID: 31720078
- Schisandrin B is the most abundant dibenzocyclooctadiene isolated from the fruit of Schisandra chinensis (Turcz) Baillon or Wu-Wei-Zi (transliterally meaning "the fruit of five tastes" in Chinese), which is a commonly used tonic herb in Chinese medicine, particularly for the treatment of liver ailments.
-
PTEN Inhibitor
Shikonin, a component of chinese herbal medicine, inhibits chemokine receptor function and suppresses human immunodeficiency virus type 1.- Yang J, .et al. , Biomed Pharmacother, 2017, Sep;93:1343-1357 PMID: 28753907
-
PI3K-δ/PI3K-γ inhibitor
IPI-145, also known as INK-1197, 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. -
S6 Kinase inhibitor
BI-D1870 is a potent and specific inhibitor of the p90 ribosomal S6 kinase (RSK) isoforms in vitro and in vivo, which inhibits RSK1, RSK2, RSK3 and RSK4 in vitro with an IC50 of 10?€?30 nM. -
AKT inhibitor?€?
TIC10 inactivates Akt and ERK to induce TRAIL through Foxo3a, possesses superior drug properties: delivery across the blood-brain barrier, superior stability and improved pharmacokinetics. -
GSK-3 inhibitor
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) which plays an important role in many pathways, including initiation of protein synthesis, cell proliferation, cell differentiation, and apoptosis.- Yuki Shimizu, .et al. , NPJ Precis Oncol, 2022, Mar 17;6(1):16 PMID: 35301419
-
DNA-PK inhibitor
NU7026 is a novel DNA-dependent protein kinase inhibitor that potentiates the cytotoxicity of topoisomerase II poisons used in the treatment of leukemia.- Velichko AK, .et al. , Nucleic Acids Res, 2019, May 22. pii: gkz436 PMID: 31114877
-
PDK1 Inhibitor
GSK 2334470 is a potent 3-phosphoinositide-dependent protein kinase (PDK1) inhibitor (IC50 ~ 10 nM). -
GSK3 inhibitor
AZD1080 is a novel GSK3 inhibitor, rescues synaptic plasticity deficits in rodent brain and exhibits peripheral target engagement in humans.- Shengzhong Liu, .et al. , J Cell Biochem, 2019, 2019 PMID: 30887575
-
PI3K inhibitor
GDC-0032 is a potent, next-generation PI3 inhibitor targeting PI3 alpha. -
MELK inhibitor
OTSSP167 is a highly potent MELK (maternal embryonic leucine zipper kinase) inhibitor with IC50 of 0.41 nM. -
PI3K inhibitor
PF-4989216 is a potent and selective PI3K inhibitor with IC50 of 2 nM, 142 nM, 65 nM, 1 nM, and 110 nM for p110α, p110β, p110γ, p110δ, and VPS34, respectively. -
PI3K/mTOR Dual Inhibitor
PF-04979064 is a highly potent and orally bioavailable PI3K/mTOR dual inhibitor. -
PI3K Inhibitor
HS-173, a novel phosphatidylinositol 3-kinase (PI3K) inhibitor, has anti-tumor activity through promoting apoptosis and inhibiting angiogenesis.- Mostafa Khater, .et al. , J Biol Chem, 2021, Jan-Jun, 296:100805 PMID: 34022220
- Mostafa Khater, .et al. , J Biol Chem, 2021, Jan 22;296:100325 PMID: 33493514
-
AKT inhibitor?€?
Afuresertib, also known as GSK2110183, is an orally bioavailable inhibitor of the serine/threonine protein kinase Akt (protein kinase B) with potential antineoplastic activity. It binds to and inhibits the activity of Akt, which may result in inhibition of the PI3K/Akt signaling pathway and tumor cell proliferation and the induction of tumor cell apoptosis. Activation of the PI3K/Akt signaling pathway is frequently associated with tumorigenesis and dysregulated PI3K/Akt signaling may contribute to tumor resistance to a variety of antineoplastic agents. -
mTOR inhibitor
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates. -
AKT Inhibitor
Triciribine, also known as API-2, suppresses the phosphorylation level and kinase activity of Akt. -
DNA-PK inhibitor
KU0060648 is a potent and selective inhibitor of DNA-dependent protein kinase (DNA-PK), (IC50 = 8.6 nM); with 20-1000 fold selectivity for DNA-PK over other PIKKs and a panel of 60 kinases. KU-0060648 enhances HDR efficiency and attenuates NHEJ frequency. -
ATR inhibitor
ETP-46464 is a potent and selective inhibitor of ATR with IC50 of 25 nM.- Fu-Xing Gong, .et al. , Nucleic Acids Res, 2021, Sep 20;49(16):9342-9352 PMID: 34403458
-
Akt inhibitor
Borussertib is a covalent-allosteric and first-in-class inhibitor of protein kinase Akt, with an IC50 of 0.8 nM and a Ki of 2.2 nM for Aktwt.