1. PI3K/Akt/mTOR
  2. PDK-1

GSK2334470 

Cat. No.: HY-14981 Purity: 99.87%
Data Sheet SDS Handling Instructions

GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.

For research use only. We do not sell to patients.
GSK2334470 Chemical Structure

GSK2334470 Chemical Structure

CAS No. : 1227911-45-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $132 In-stock
10 mg $120 In-stock
50 mg $350 In-stock
100 mg $650 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Featured Recommendations

Related Screening Libraries:

Related Small Molecules:

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC50 of 10 nM.

IC50 & Target

IC50: 10 nM(PDK1)[1]

In Vitro

Small molecule GSK2334470 inhibits PDK1 with an IC50 of ~10 nM, but does not suppress the activity of 93 other protein kinases including 13 AGC-kinases most related to PDK1 at 500-fold higher concentrations. Addition of GSK2334470 ablates T-loop residue phosphorylation and activation of SGK isoforms and S6K1 induced by serum or IGF-1 (insulin-like growth factor 1). GSK2334470 and AZD8055 effectively inhibite phosphorylation of PDK1 and mTOR, respectively, and induce higher G0–G1 ratio in LAN-1-MK than that in LAN-1 as well. PDK1 and mTOR inhibitors effecte on phosphorylation of GSK3β in some of resistant sublines[2].

In Vivo

The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn BrafV600E::Pten−/−mice subjected to systemic administration of 4-HT. Twice weekly administration of PDK1 results in marked inhibition of pigmented lesions and concomitant melanomagenesis, as well as significant inhibition of lung metastases, seen by H&E staining-based quantification (~80%), and lymph node metastases as by S100 immunostaining, similar to the phenotype seen upon genetic ablation of Pdk1[3].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 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
Cell Assay
[2]

GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use. To study the inhibitory effect of GSK2334470 on mTOR-S6K pathway, non-resistant cells and the resistant sublines are treated with GSK2334470 at 5 μM for 1.5 and 12 h in 10 % FBS medium with/without MK-2206 (5 μM)[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice is dissolved in DMSO and then diluted with PBS or saline. BrafV600E::Pten−/− are generated as previously described. Cohorts of six animals per group are used in each experimental group. GSK2334470 is administered through IP injection (100 mg/kg) 3 times per week starting the same day of topical administration of 4-hydroxytamoxifen and ending at the time of mouse collection, based on earlier studies[3]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

462.59

Formula

C₂₅H₃₄N₈O

CAS No.

1227911-45-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.87%

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GSK2334470
Cat. No.:
HY-14981
Quantity: