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GSK 650394 Sale

(Synonyms: 2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸) 目录号 : GC15441

A SGK1 inhibitor

GSK 650394 Chemical Structure

Cas No.:890842-28-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥798.00
现货
5mg
¥672.00
现货
10mg
¥956.00
现货
25mg
¥2,268.00
现货
50mg
¥3,339.00
现货
500mg
¥8,400.00
现货
1g
¥12,600.00
现货

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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Kinase experiment [1]:

Scintillation proximity assay (SPA)

SGK1 S422D (60-431 aa; 0.275 μg/mL final concentration) or SGK2 (0.875 μg/mL final concentration) were activated by PDK1 (1.1 μg/mL final concentration) in a buffer consisting of 50 mM Tris (pH 7.5), 0.1 mM EGTA, 0.1 mM EDTA, 10 mM MgCl2, 0.1% β-mercaptoethanol, 1 mg/mL BSA, and ATP (final concentration of 0.15 mM) and incubated for 30 mins at 30 °C. SGK2 was prepared exactly as described for SGK1, except it corresponded to the full-length protein. A solution containing biotinylated CROSStide peptide at a final concentration of 75 μM and γ32P-ATP corresponding to 2 × 106 cpm was prepared in the reaction buffer. In a 96-well plate, 5 μL of GSK 650394 was added to 25 μL of the activated enzyme mixture. To this, 20 μL of the CROSStide mixture was added and incubated for 1 hr at room temperature. Next, 50 μL of a 25 mg/mL slurry of streptavidin-coated SPA beads in PBS with 0.1 M EDTA, pH 8.0 was added. The plate was then sealed and centrifuged for 8 mins at 2000 rpm, and the signal was detected by measuring for 30 sec/well in a Packard TopCount NXT Scintillation Counter. The IC50 values of the inhibition of SGK1 and SGK2 activities by GSK 650394 were calculated from these data using GraphPad Prism 3 Software.

Cell experiment [1]:

Cell lines

LNCaP cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

~ 10 μM; 7 days

Applications

In LNCaP cells, GSK 650394 inhibited androgen-mediated enhancement of Nedd4-2 phosphorylation. In addition, GSK 650394 also significantly inhibited androgen-stimulated growth of LNCaP cells, with an IC50 value of ~ 1 μM.

References:

[1]. Sherk A B, Frigo D E, Schnackenberg C G, et al. Development of a small-molecule serum-and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer research, 2008, 68(18): 7475-7483.

产品描述

GSK 650394 is a small molecule inhibitor of serum and glucocorticoid-regulated kinase 1 (SGK1) with IC50 value of 13nM [1].

Sgk1 gene is a target gene of androgen. Knockdown of SGK1 expression attenuates androgen-mediated growth of the prostate cancer cell line. Thus, the inhibition of SGK1 is a novel mechanism for the treatment of prostate cancer. GSK 650394 is a competitive inhibitor of SGK1. It shows potent inhibitory activity against the purified SGK1 with IC50 value of 13nM in a fluorescence polarization assay. In the activity-based scintillation proximity assay, GSK 650394 prevents the phosphorylation activity of SGK1 and SGK2 with IC50 values of 62nM and 103nM, respectively. Moreover, GSK 650394 suppresses the androgen-mediated increase of Nedd4-2 phosphorylation in LNCaP cells. It also significantly inhibits cell growth stimulated by androgen with IC50 value of about 1μM [1].

References:
[1] Sherk A B, Frigo D E, Schnackenberg C G, et al. Development of a small-molecule serum-and glucocorticoid-regulated kinase-1 antagonist and its evaluation as a prostate cancer therapeutic. Cancer research, 2008, 68(18): 7475-7483.

Chemical Properties

Cas No. 890842-28-1 SDF
别名 2-环戊基-4-(5-苯基-1H-吡咯并[2,3-B]吡啶-3-基)苯甲酸
化学名 2-cyclopentyl-4-(5-phenyl-1H-pyrrolo[2,3-b]pyridin-3-yl)benzoic acid
Canonical SMILES C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=NC=C(C=C34)C5=CC=CC=C5)C(=O)O
分子式 C25H22N2O2 分子量 382.45
溶解度 ≥ 19.1mg/mL in DMSO 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.6147 mL 13.0736 mL 26.1472 mL
5 mM 0.5229 mL 2.6147 mL 5.2294 mL
10 mM 0.2615 mL 1.3074 mL 2.6147 mL
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