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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

GSK 650394

HY-15192

(GSK650394; GSK-650394)

GSK 650394

GSK 650394 Chemical Structure

GSK650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $109 In-stock
5 mg $99 In-stock
10 mg $140 In-stock
50 mg $478 In-stock
100 mg Get quote
200 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €107 In-stock
5 mg €97 In-stock
10 mg €137 In-stock
50 mg €468 In-stock
100 mg Get quote
200 mg Get quote

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Product name: GSK 650394
Cat. No.: HY-15192

GSK 650394 Data Sheet

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    Purity: 99.62%

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Related Compound Libraries

Biological Activity of GSK 650394

GSK650394 is a novel SGK inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2 in the SPA assay respectively.
IC50 Value: 62 nM (SGK1); 103 nM (SGK2) [1]
Target: SGK
in vitro: GSK650394 inhibited the enzymatic activity of SGK1 and SGK2 in the SPA assay with IC50 values of 62 nM and 103 nM, respectively. GSK650394 is relatively non-toxic, with LC50 values of 41 μM in M1 cells (68 times its activity IC50) and a LC50 greater than 100 μM in HeLa cells in XTT assays, which measure mitochondrial enzymatic activity. GSK650394 inhibited SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. The selectivity of GSK650394 for SGK1 over that of Akt and other related kinases proved to be greater than 30-fold, while GSK650394 was more than 60-fold selective for SGK1 over the upstream AGC kinase PDK1 [1]. GSK650394 had no effect on cell survival or growth in the absence of androgens, the compound dramatically inhibited the androgen-stimulated growth of LNCaP cells. In the LNCaP growth assay, the IC50 of GSK650394 was approximately 1 μM (which is similar to the previously measured IC50 in other cell-based assays). Furthermore, 10 μM of GSK650394 completely abrogated androgen-mediated growth [1]. GSK650394A, on the other hand, selectively inhibits SGK1 and the finding that GSK650394A suppressed insulin-induced Na(+) absorption suggests that this response is dependent upon signalling via PI3K/SGK1 [2].
in vivo: GSK-650394 (an SGK1 activation antagonist, 1, 10, and 30 μM, 10 μL/rat, intrathecally) dose-dependently prevented CFA-induced pain behavior and the associated SGK1 phosphorylation, GluR1 trafficking, and protein-protein interactions at 1 day after CFA administration in rats [3]. Daily administration of GSK-650394 (an SGK1 antagonist; 100 nm, 10 μl, i.t.) not only exhibited effects similar to the kalirin mRNA-targeting siRNA but also attenuated pSGK1-kalirin costaining and SGK1-kalirin coupling [4].
 

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 382.45 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C25H22N2O2
CAS No 890842-28-1
Solvent & Solubility

DMSO: ≥ 40.7 mg/mL

Preparing Stock Solutions

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

References on GSK 650394

Inhibitor Kit