GSK2334470

Name: GSK2334470
Brand: MedChemExpress
SKU: HY-14981
Rating: 5.0 (14 reviews)

製品番号: HY-14981 純度: 99.79%: Data Sheet SDS COA 取扱説明書
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GSK2334470 is a highly specific and potent inhibitor of PDK1 with an IC₅₀ of 10 nM.

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CAS 番号 : 1227911-45-6

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 64	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 64	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$63	在庫あり	Estimated Time of Arrival: December 31
10 mg	$99	在庫あり	Estimated Time of Arrival: December 31
50 mg	$330	在庫あり	Estimated Time of Arrival: December 31
100 mg	$550	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 14 publication(s) in Google Scholar

顧客検証

Flow Cytometry

Histological Imaging/Staining

Cell Proliferation/Viability Assay

: GSK2334470 purchased from MedChemExpress. Usage Cited in: Chin Med. 2024 May 15;19(1):70. [Abstract]; GPE promoted the phosphorylation of PDK1, PI3K, and Akt; however, those effect were abrogated by GSK2334470 (1 μM) treatment.

: GSK2334470 purchased from MedChemExpress. Usage Cited in: iScience. 2024 Apr 26;27(6):109798. [Abstract]; CD4 T cells from RA patients were isolated and treated with HS and/or GSK2334470 (GSK) (2.5 μM) for 3 days, and the proportion of Th17 cells was detected by flow cytometry.

: GSK2334470 purchased from MedChemExpress. Usage Cited in: iScience. 2024 Apr 26;27(6):109798. [Abstract]; GSK2334470 (GSK) (25 mg/kg, i.p.) treatment alleviated these arthritic symptoms and counteracted the adverse effects of HS diet on RA progression.

: GSK2334470 purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2020 Aug;123(4):542-555. [Abstract]; The combination of the PDK1 inhibitor GSK2334470 with AKT inhibitors of either class potentiated cell death in MDA-MB-361 cells

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製品説明

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

IC₅₀ & Target

IC50: 10 nM(PDK1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEL	IC₅₀	> 30 μM Compound: (3S,6R)-28d, GSK-2334470	Antiproliferative activity against human HEL 92.1.7 cells Antiproliferative activity against human HEL 92.1.7 cells	[PMID: 21341675]
K562	IC₅₀	18 μM Compound: (3S,6R)-28d, GSK-2334470	Antiproliferative activity against human K562 cells Antiproliferative activity against human K562 cells	[PMID: 21341675]
OCI-AML-3	IC₅₀	0.52 μM Compound: (3S,6R)-28d, GSK-2334470	Antiproliferative activity against human OCI-AML3 cells Antiproliferative activity against human OCI-AML3 cells	[PMID: 21341675]
OCI-AML2	IC₅₀	0.35 μM Compound: (3S,6R)-28d, GSK-2334470	Antiproliferative activity against human OCI-AML2 cells Antiproliferative activity against human OCI-AML2 cells	[PMID: 21341675]
PC-3	IC₅₀	113 nM Compound: (3S,6R)-28d, GSK-2334470	Inhibition of PDK1-mediated AKT phosphorylation at Thr308 residue in human PC3 cells by ELISA Inhibition of PDK1-mediated AKT phosphorylation at Thr308 residue in human PC3 cells by ELISA	[PMID: 21341675]
PC-3	IC₅₀	293 nM Compound: (3S,6R)-28d, GSK-2334470	Inhibition of PDK1-mediated RSK phosphorylation at Ser221 residue in human PC3 cells by ELISA Inhibition of PDK1-mediated RSK phosphorylation at Ser221 residue in human PC3 cells by ELISA	[PMID: 21341675]

体外実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 is tested in newborn Braf^V600E::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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

462.59

分子式

C₂₅H₃₄N₈O

CAS 番号

1227911-45-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C([C@@H]1CN(C2=NC(NC)=NC(C3=CC4=C(C=C3)C(N)=NN4)=C2)[C@H](C)CC1)NC5CCCCC5

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

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

溶剤 & 溶解度

体外:

DMSO : ≥ 50 mg/mL (108.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.40 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 99.79%

Select Batch:

データシート (278 KB) SDS (393 KB)

COA (247 KB) RP-HPLC (248 KB) LCMS (94 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Najafov A, et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem J.?2011 Jan 15;433(2):357-69. [Content Brief]

[2]. Qi L, et al. PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells. Cancer Cell Int.?2015 Sep 29;15:91. [Content Brief]

[3]. Scortegagna M, et al. Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf(V600E)::Pten(-/-) melanoma. Oncogene. 2014 Aug 21;33(34):4330-9. [Content Brief]

細胞実験 ^[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]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[3]	Mice is dissolved in DMSO and then diluted with PBS or saline. Braf^V600E::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]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Najafov A, et al. Characterization of GSK2334470, a novel and highly specific inhibitor of PDK1. Biochem J.?2011 Jan 15;433(2):357-69. [Content Brief] [2]. Qi L, et al. PDK1-mTOR signaling pathway inhibitors reduce cell proliferation in MK2206 resistant neuroblastoma cells. Cancer Cell Int.?2015 Sep 29;15:91. [Content Brief] [3]. Scortegagna M, et al. Genetic inactivation or pharmacological inhibition of Pdk1 delays development and inhibits metastasis of Braf(V600E)::Pten(-/-) melanoma. Oncogene. 2014 Aug 21;33(34):4330-9. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1617 mL	10.8087 mL	21.6174 mL	54.0435 mL
	5 mM	0.4323 mL	2.1617 mL	4.3235 mL	10.8087 mL
	10 mM	0.2162 mL	1.0809 mL	2.1617 mL	5.4044 mL
	15 mM	0.1441 mL	0.7206 mL	1.4412 mL	3.6029 mL
	20 mM	0.1081 mL	0.5404 mL	1.0809 mL	2.7022 mL
	25 mM	0.0865 mL	0.4323 mL	0.8647 mL	2.1617 mL
	30 mM	0.0721 mL	0.3603 mL	0.7206 mL	1.8015 mL
	40 mM	0.0540 mL	0.2702 mL	0.5404 mL	1.3511 mL
	50 mM	0.0432 mL	0.2162 mL	0.4323 mL	1.0809 mL
	60 mM	0.0360 mL	0.1801 mL	0.3603 mL	0.9007 mL
	80 mM	0.0270 mL	0.1351 mL	0.2702 mL	0.6755 mL
	100 mM	0.0216 mL	0.1081 mL	0.2162 mL	0.5404 mL

GSK2334470 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK23344701227911-45-6GSK 2334470GSK-2334470PDK-13-Phosphoinositide-dependent protein kinase 1Inhibitorinhibitorinhibit

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GSK2334470 関連抗体

Molarity Calculator

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Complete Stock Solution Preparation Table

GSK2334470 Related Classifications

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Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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