Catalog No.
Product Name
Application
Product Information
Product Citation
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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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Akt inhibitor
Akt inhibitor GSK2141795 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. -
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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PI3K inhibitor
PQR309 is an orally bioavailable pan inhibitor of phosphoinositide-3-kinases (PI3K) and inhibitor of the mammalian target of rapamycin (mTOR), with potential antineoplastic activity. -
PI3K/mTOR Dual Inhibitor
LY3023414 is an oral ATP competitive inhibitor of the class I PI3K isoforms, mTOR and DNA-PK, extracted from patent WO/2012097039A1, compound example 1, has an IC50 of 64.9 nM, 42.1 nM, 10.6 nM, 19.1 nM for Akt1(pT308), Akt1 (pS473), P70S6(pT389), S6RP(pS240/242).- Zou Y, .et al. , Biochem Biophys Res Commun, 2017, Aug 19;490(2):385-392 PMID: 28623128
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PDK1 inhibitor
PDK1 inhibitor, potent, ATP-competitive and selective dual PI3K and PDPK1 inhibitor (IC50 values 34 nM and 94 nM for PDK1 and p-T308-PKB inhibition, respectively. -
ERK/Akt/NF-kB inhibitor
Tomatidine inhibits the phosphorylation of ERK, Akt, and the nuclear content of NF-kB. possess anti-inflammatory properties. -
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. -
PI3Kα inhibitor
PI3Kα inhibitor 1 is a PI3Kα inhibitor extracted from patent US/20120088764A1, compound 243, has an IC50 < 0.1 uM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 uM ??? IC50 ??? 1 uM) . -
PI3K/mTOR dual inhibitor
SAR245409 is a PI3K/mTOR dual kinase inhibitor XL765 is an orally bioavailable small molecule targeting the phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) kinases in the PI3K/mTOR signaling pathway, with potential antineoplastic activity. -
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. -
GSK-3β inhibitor
Indirubin-3'-monoxime is a powerful inhibitor of GSK-3β with IC50 of 22nM, also inhibits CDK1/5 (IC50 = 180/100 nM). -
NUAK1 inhibitor
HTH-01-015 is a potent and selective inhibitor of NUAK1 (IC50 = 100 nM) and does not affect the activity of a panel of 139 other kinases, including additional AMPK family members. -
AKT 1/2 inhibitor
Akt1 and Akt2-IN-1 is an allosteric inhibitor of Akt1 (IC50 = 3.5 nM) and Akt2 (IC50 = 42 nM), with potent and balanced activity. -
AKT inhibitor
ARQ 092 is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). -
PI3Kγ Inhibitor
IPI-549 is a potent and selective PI3Kγ Inhibitor with IC50 of 16 nM. -
PI3Kα/PI3Kδ inhibitor
AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50 of 5.7 nM and 6.2 nM, with selectivity against PI3Kβ (IC50 431 nM) and PI3Kγ (IC50 90 nM). -
Akt inhibitor
Afuresertib is a potent, orally bioavailable Akt inhibitor with Ki of 0.08 nM, 2 nM, and 2.6 nM for Akt1, Akt2, and Akt3, respectively. Phase 2. -
ATM inhibitor
AZD0156 is a potent and selective inhibitors of ATM kinase, with potential chemo-/radio-sensitizing and antineoplastic activities.- Yi-Ru Pan, .et al. , Biomolecules, 2020, Nov 9;10(11):1529 PMID: 33182492
- Chloroquine phosphate is a 4-aminoquinoline anti-malarial and anti-rheumatoid agent, also acting as an ATM activator.
- Vijaya Bharti, .et al. , Cell Rep, 2022, Dec 20;41(12):111826 PMID: 36543138
- Egawa Y, .et al. , PLoS One, 2018, Jun 7;13(6):e0198940 PMID: 29879220
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PI3Kδ inhibitor
GSK2292767 is a potent and selective inhibitor of phosphatidylinositol 3-kinase δ (PI3Kδ; Ki = 79 pM). GSK2292767 is >100-fold selective for PI3Kδ over a panel of 250 kinases. -
S6K inhibitor
Sodium Salicylate (Salicylic acid sodium salt) inhibits cyclo-oxygenase-2 (COX-2) activity independently of transcription factor (NF-κB) activation. Sodium Salicylate is also a S6K inhibitor.Sodium Salicylate is a NF-κB inhibitor that decreases inflammatory gene expression and improves repair in aged muscle. -
AMPK activator
EX229 (compound 991) is a potent AMPK activator that is 5-10-fold more potent than A769662 in activating AMPK.- CN Koyani, .et al. , Pharmacol Res, 2020, May 17;158:104870 PMID: 32434052
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PI3K inhibitor
Leniolisib(CDZ 173) is a potent PI3Kδ selective inhibitor with biochemical IC50 values of 0.244, 0.424, 2.23 and 0.011 μM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. -
PI3K inhibitor
Seletalisib is a novel small-molecule inhibitor of PI3Kδ with an IC50 value of 12 nM and shows significant selectivity to PI3Kδ with respect to the other class I PI3K isoforms (between 24- and 303-fold). -
dual PI3Kδ/γ inhibitor
Tenalisib, also known as RP6530, is a potent and selective dual PI3Kδ/γ inhibitor that inhibited growth of B-cell lymphoma cell lines with a concomitant reduction in the downstream biomarker, pAKT. -
AMPK activator
PF-06409577 is orally bioavailable AMPK activator with EC50 of 7 nM for α1β1γ1 in the TR-FRET assay and it shows no detectable inhibition of hERG in a patch-clamp assay (100 μM) and was not an inhibitor (IC50 > 100 μM) of the microsomal activities of major human cytochrome P450 isoforms.
