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GSK2334470
GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases.
CAS No. 1227911-45-6
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GSK2334470関連製品
PDPK1阻害剤の選択性比較
Cell Data
| Cell Lines | Assay Type | Concentration | Incubation Time | 活性情報 | PMID |
|---|---|---|---|---|---|
| OCI-AML3 cells | Proliferation assay | Antiproliferative activity against human OCI-AML3 cells, IC50=0.52 μM | 21341675 | ||
| OCI-AML2 cells | Proliferation assay | Antiproliferative activity against human OCI-AML2 cells, IC50=0.35 μM | 21341675 | ||
| K562 cells | Proliferation assay | Antiproliferative activity against human K562 cells, IC50=18 μM | 21341675 | ||
| PC3 cells | Function assay | Inhibition of PDK1-mediated RSK phosphorylation at Ser221 residue in human PC3 cells by ELISA, IC50=0.293 μM | 21341675 | ||
| PC3 cells | Function assay | Inhibition of PDK1-mediated AKT phosphorylation at Thr308 residue in human PC3 cells by ELISA, IC50=0.113 μM | 21341675 | ||
| F-36P cells | Proliferation assay | Antiproliferative activity against human F-36P cells, IC50=0.28 μM | 21341675 | ||
| insect cells | Function assay | Inhibition of recombinant full length PDK1 (unknown origin) expressed in insect cells assessed as inhibition of Akt activation measured for 30 mins in presence of [gamma32P-ATP], IC50=0.01 μM | 23448267 | ||
| 他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい | |||||
生物活性
| 製品説明 | GSK2334470 is a novel PDK1 inhibitor with IC50 of ~10 nM in a cell-free assay, with no activity at other close related AGC-kinases. | ||
|---|---|---|---|
| Targets |
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| In Vitro | ||||
| In vitro |
GSK2334470 inhibits PDK1 from activating full-length Akt1 in the presence of PtdIns(3,4,5)P3-containing lipid vesicles or a mutant of Akt1 lacking the PH domain (ΔPH-Akt1) with IC50 of ~10 nM. GSK2334470 also similarly inhibits PDK1 from phosphorylating the PDKtide peptide substrate with IC50 of ~10 nM. GSK2334470 (0.1 μM–0.3 μM) induces significant dose-dependent inhibition of endogenous NDRG1 with over 50% reduction in phosphorylation in HEK-293 cells. GSK2334470 (30 nM) induces a significant dose-dependent inhibition of the T-loop phosphorylation of each SGK isoform in HEK-293 cells. GSK2334470 (1 μM) inhibits hydrophobic motif phosphorylation of S6K1 to a similar extent as T-loop phosphorylation in HEK-293 cells. GSK2334470 (3 μM) also suppresses S6K1 activity and phosphorylation induced by IGF1 stimulation of serum-starved HEK-293 cells. GSK2334470 (3 μM) markedly inhibits the phosphorylation of several Akt substrates [FoxO (forkhead box O), GSK3 and PRAS40]. GSK2334470 (3 μM) also induces near maximal inhibition of Akt1 activity and phosphorylation within 5 min, and Akt substrate phosphorylation (FoxO, GSK3 and PRAS40) is inhibited at a slightly later time point (10 min). GSK2334470 (0.3 μM) significantly inhibits phosphorylation of Akt or PRAS40/GSK3 in PDK1K465E/K465E knock-in but not wild-type ES cells. GSK2334470 (1 μM) effectively suppresses SGK1 activity as judged by the inhibition of NDRG1 phosphorylation in U87 glioblastoma cells. GSK2334470 (1 μM) also potently suppresses activation of S6K1 (Figure 7B) as well as SGK1 in MEF (mouse embryonic fibroblast) cells. GSK2334470 (0.1 μM) induces ~50% inhibition of RSK2 activity in HEK-293 cells. [1] GSK2334470 (30 µM) suppresses U46619 induced Ca2+-sensitized force in α-toxin permeabilized rabbit pulmonary artery SM. GSK2334470 (30 µM) results in a significant decrease in the contractile force in response to [Ca2+]. [2] GSK2334470 (1 μM) results in total abrogation of the EGF-induced intracellular calcium increase and inositol phosphates accumulation in MDA-MB-231 cells. GSK2334470 (1 μM) inhibits PLCγ1 Tyr783 phosphorylation in MDA-MB-231 cells. [3] |
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|---|---|---|---|---|
| Kinase Assay | Kinase activity assays | |||
| Endogenous Akt, S6K and RSK are immunoprecipitated from 0.1 mg to 1 mg of cell lysate for 2 hours at 4℃ on a vibrating platform using 3 μg–5 μg of the indicated antibodies. For the SGK activity assays, 150 μg of transfected lysate is incubated with 5 μg of glutathione–Sepharose for 3 hours at 4℃. The immunoprecipitates are washed twice with lysis buffer containing 0.5 mM NaCl, followed by two washes with kinase buffer. Kinase reactions are initiated by a reaction mixture to bring the final concentrations of the reaction components to 0.1 mM [γ-32P]ATP (~200 c.p.m./pmol), 5 mM magnesium acetate, 0.1% 2-mercaptoethanol and 30 mM Crosstide peptide (GRPRTSSFAEGKK). Reactions are carried out for 20 min at 30℃ on a vibrating platform and stopped by spotting the reactions on to P81 phosphocellulose paper. Cerenkov counting is done after washing the papers in phosphoric acid, rinsing in acetone and air-drying. One unit of activity is defined as that which catalysed the incorporation of 1 nmol of [32P]phosphate into the substrate over 1 hour. | ||||
| 細胞実験 | 細胞株 | MDA-MB-231 cells | ||
| 濃度 | 1 µM | |||
| 反応時間 | 30 minutes | |||
| 実験の流れ | Cells were incubated with 1 µM of GSK2334470 for 30 minutes. Cells treated with DMSO were used as control. |
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| 実験結果図 | Methods | Biomarkers | 結果図 | PMID |
| Western blot | pRb / pPDK1 / pAKT / pRSK2 / p70S6K / pPRAS40 / pS6 p-Myc / Myc / p-p70 / p70 |
|
28249908 | |
| Immunofluorescence | KDM4A / Pol-I |
|
26729372 | |
| In Vivo | ||
| In Vivo |
GSK2334470 is a highly specific and potent inhibitor of PDK1. |
|
|---|---|---|
| 動物実験 | 動物モデル | Nude mice |
| 投与量 | 100 mg/kg | |
| 投与経路 | i.p. | |
化学情報
| 分子量 | 462.59 | 化学式 | C25H34N8O |
| CAS No. | 1227911-45-6 | SDF | Download GSK2334470 SDFをダウンロードする |
| Smiles | CC1CCC(CN1C2=NC(=NC(=C2)C3=CC4=C(C=C3)C(=NN4)N)NC)C(=O)NC5CCCCC5 | ||
| 保管 | |||
|
In vitro |
DMSO : 93 mg/mL ( (201.04 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。) Ethanol : 93 mg/mL Water : Insoluble |
モル濃度計算器 |
|
in vivo Add solvents to the product individually and in order. |
投与溶液組成計算機 | ||||
実験計算
投与溶液組成計算機(クリア溶液)
ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）
mg/kg
g
μL
匹
ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結果：
投与溶媒濃度： mg/ml;
DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )
投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。
投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。
注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。
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