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Catalog No.
Product Name
Application
Product Information
Product Citation
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AKT Inhibitor
Palomid 529 is a dual TORC1/2 inhibitor of the PI3K/Akt/mTOR pathway having broad activity in angiogenesis and cellular proliferation. -
PI3K Inhibitor
XL147 is a potent, selective and orally bioavailable small molecule inhibitor of class I phosphatidylinositol 3 kinase (PI3K) with potential antineoplastic activity.- Yushi Hayashida, .et al. , Int J Cancer, 2016, Aug 1;139(3):700-11 PMID: 26989815
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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 Inhibitor
WYE-125132 is an ATP-competitive and specific inhibitor of mTORC1 and mTORC2 (IC50 = 0.19 nM; >5,000-fold selective versus PI3Ks). -
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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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
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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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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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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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). -
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. -
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. -
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
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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. -
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
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PTEN inhibitor
SF1670 is a selective PTEN inhibitor (IC50=2 uM). As PTEN-mTOR pathway is critical for controlling the regenerative capacity of corticospinal neurons, PTEN deletion or its inhibitor enhances the regenerative ability of adult corticospinal neurons. Pretreatment with SF1670 augments the efficacy of granulocyte transfusion in a clinically relevant mouse model. -
AKT/PKB inhibitor?€?
10-DEBC HCl is a selective inhibitor of Akt/PKB. It inhibits IGF-1-stimulated phosphorylation and activation of Akt (complete inhibition at 2.5 μM), suppressing downstream activation of mTOR, p70 S6 kinase and S6 ribosomal protein. -
GSK-3β inhibitor
1-Azakenpaullone is a potent and selective GSK-3β inhibitor with IC50 of 18 nM, >100-fold selectivity over CDK1/cyclin B and CDK5/p25. -
Akt inhibitor
AT7867 dihydrochloride is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively, little activity outside the AGC kinase family. -
mTOR inhibitor
mTOR inhibitor is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 1.5 nM. -
p70S6K inhibitor
LY-2584702 tosylate salt is an orally available inhibitor of p70S6K signaling; inhibits p70S6K and prevents phosphorylation of the S6 subunit of ribosomes. -
p110α inhibitor
MLN1117, also known as INK1117 and TAK-117, is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha isoform with potential antineoplastic activity. -
endothelial barrier enhancer
Ginsenoside Rk1, one of the main elements of Sung Ginseng, has been confirmed as a new endothelial barrier enhancer recently and has anti-cancer activity. -
ATR inhibitor
AZD6738 is a potent inhibitor of ATR kinase activity with an IC50 of 1 nM against the isolated enzyme and 74 nM against ATR kinase-dependent CHK1 phosphorylation in cells.- Brian F Kiesel, .et al. , Cancer Chemother Pharmacol, 2022, Feb;89(2):231-242 PMID: 35066692
- Albert Job, .et al. , Sci Rep, 2020, Nov 3;10(1):18924 PMID: 33144657
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AMPK activator
GSK621 is a potent and selective AMPK agonist.- Harvey W. Smith, .et al. , Nat Commun, 2019, 10, 2901(2019) PMID: 31263101
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PI4KIIIβ inhibitor
PI4KIIIbeta-IN-10 is the most potent PI4KIIIbeta inhibitor currently reported, with very minor off-target inhibition of PI4KIIIbeta related lipid kinases (IC50 = 3.6 nM). -
PI4KIIIβ inhibitor
PI4KIIIbeta-IN-9 is a potent PI4KIIIbeta inhibitor (IC50 of 7 nM) and is >140-fold selective over PI3Kgamma and >20-fold selective over PI3Kδ, and shows no inhibition of vps34 at concentrations up to 20 uM. -
PI3Kδ inhibitor
TGR-1202 is an orally available, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively. -
PI3Kδ inhibitor
TGR-1202 hydrochloride is an orally available, next generation PI3Kδ inhibitor, inhibits PI3Kδ activity in enzyme and cell based assays with IC50 and EC50 values of 22.2 and 24.3 nM respectively.
