GSK2334470

Alias: GSK 2334470; GSK2334470; GSK-2334470
Cat No.:V0237 Purity: ≥98%
GSK2334470 (GSK-2334470) is a novel, highly specific and potent inhibitor of PDK1 (3-phosphoinositide-dependent protein kinase) with potential antitumor activity.
GSK2334470 Chemical Structure CAS No.: 1227911-45-6
Product category: PDK-1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

GSK2334470 (GSK-2334470) is a novel, highly specific and potent inhibitor of PDK1 (3-phosphoinositide-dependent protein kinase) with potential antitumor activity.In a cell-free assay, it inhibits PDK-1 with an IC50 of 10 nM and has no impact on closely related AGC-kinases. GSK2334470 inhibited PDK1 from activating full-length Akt1 or mutant Akt1 lacking the PH domain, which resulted in strong antiproliferative activity in vitro and high antitumor efficacy in vivo.

Biological Activity I Assay Protocols (From Reference)
Targets
PDK1 (IC50 = 10 nM)
ln 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. With an IC50 of less than 10 nM, GSK2334470 similarly prevents PDK1 from phosphorylating the PDKtide peptide substrate. In HEK-293 cells, GSK2334470 (0.1 M-0.3 M) causes a significant dose-dependent inhibition of endogenous NDRG1 with a phosphorylation reduction of over 50%. In HEK-293 cells, GSK2334470 (30 nM) causes a significant, dose-dependent inhibition of each SGK isoform's T-loop phosphorylation. 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]
ln Vivo
GSK2334470 is a highly specific and potent PDK1 inhibitor.
Enzyme Assay
Endogenous Akt, S6K, and RSK are immunoprecipitated using 3 g to 5 g of the designated antibodies from 0.1 mg to 1 mg of cell lysate for two hours at 4 °C on a vibrating platform. In order to measure the SGK activity, 150 g of transfected lysate is incubated with 5 g of glutathione-Sepharose at 4 °C for 3 hours. The immunoprecipitates are then washed twice with kinase buffer and twice with lysis buffer containing 0.5 mM NaCl. A reaction mixture is used to start kinase reactions, resulting in final concentrations of 0.1 mM [-32P]ATP (200 c.p.m./pmol), 5 mM magnesium acetate, 0.1% 2-mercaptoethanol, and 30 mM Crosstide peptide (GRPRTSSFAEGKK).
Cell Assay
GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use. GSK2334470 is administered to non-resistant cells and resistant sublines for 1.5 and 12 hours in 10% FBS medium with/without MK-2206 (5 M) to investigate its inhibitory effect on the mTOR-S6K pathway.
Animal Protocol
In order to dilute the mice, DMSO is first dissolved in PBS or saline. As previously mentioned, BrafV600E::Pten are generated. Each experimental group utilizes cohorts of six animals. Based on previous studies[3], GSK2334470 is administered by IP injection (100 mg/kg) three times per week beginning on the day that 4-hydroxytamoxifen is topically applied and ending at the time of mouse collection.
References

[1]. Biochem J. 2011 Jan 15;433(2):357-69.

[2]. Cancer Cell Int. 2015 Sep 29;15:91.

[3]. J Cell Sci. 2012 Jul 1;125(Pt 13):3153-63.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C25H34N8O
Molecular Weight
462.5905
Exact Mass
462.28556
Elemental Analysis
C, 64.91; H, 7.41; N, 24.22; O, 3.46
CAS #
1227911-45-6
Appearance
white solid powder
SMILES
O=C([C@@H]1CN(C2=NC(NC)=NC(C3=CC4=C(C=C3)C(N)=NN4)=C2)[C@H](C)CC1)NC5CCCCC5
InChi Key
QLPHOXTXAKOFMU-WBVHZDCISA-N
InChi Code
InChI=1S/C25H34N8O/c1-15-8-9-17(24(34)28-18-6-4-3-5-7-18)14-33(15)22-13-20(29-25(27-2)30-22)16-10-11-19-21(12-16)31-32-23(19)26/h10-13,15,17-18H,3-9,14H2,1-2H3,(H,28,34)(H3,26,31,32)(H,27,29,30)/t15-,17+/m1/s1
Chemical Name
(3S,6R)-1-(6-(3-amino-1H-indazol-6-yl)-2-(methylamino)pyrimidin-4-yl)-N-cyclohexyl-6-methylpiperidine-3-carboxamide
Synonyms
GSK 2334470; GSK2334470; GSK-2334470
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~90 mg/mL (194.6 mM)
Water: <1 mg/mL
Ethanol: 90 mg/mL (194.6 mM)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1617 mL 10.8087 mL 21.6174 mL
5 mM 0.4323 mL 2.1617 mL 4.3235 mL
10 mM 0.2162 mL 1.0809 mL 2.1617 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

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