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GSK650394

Catalog No.S7209

For research use only.

GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.

CAS No. 890842-28-1

Selleck's GSK650394 has been cited by 19 publications

Purity & Quality Control

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Biological Activity

Description

GSK650394 is a serum- and glucocorticoid-regulated kinase-1 inhibitor with IC50 of 62 nM and 103 nM for SGK1 and SGK2, respectively.

Targets

SGK1 ^[1] (Cell-free assay)	SGK2 ^[1] (Cell-free assay)
62 nM	103 nM

In vitro

GSK650394 inhibits SGK1-mediated epithelial transport with an IC50 of 0.6 μM in the SCC assay. In LNCaP cells, GSK650394 inhibits the androgen-mediated enhancement of Nedd4-2 phosphorylation and androgen-mediated cell growth. ^[2] GSK650394 counteracts the Cortisol-induced decrease in neurogenesis, changes in Hedgehog signaling, and GR nuclear translocation. [2] GSK 650394 inhibits replication of influenza virus by impairing the export of influenza vRNPs into the cytoplasm of A549 cells. ^[3]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

human M-1 cells	MX;GeY5kfGmxbjDhd5NigQ>?	NGSzOFJKdmirYnn0bY9vKG:oIGPHT\|EudWWmaXH0[YQh\XCrdHjlcIlidCC\|b3TpeY0h[2ijbn7lcEBi[3Srdnn0fUBqdiCqdX3hckBONTFiY3XscJMh[XO\|ZYPz[YQh[XNic3jvdpQh[2m{Y4XpeEBkfXK{ZX70JIJ6KHeqb3zlJINmdGxiZXzlZ5Rzd3CqeYPpc4xw\2mlYXygeJJidnOncHn0bIVtcWGuIHX4dIVzcW2nboSsJGlEPTB;MD61PEDPxE1?	NUPSV4tFOTl2OUe3OFU>
human MV-4-11 cell	MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MknETY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NE4yPjR7IN88US=>	MYfTRW5ITVJ?
human Daoy cell	MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MXfJcohq[mm2aX;uJI9nKGi3bXHuJGRid3liY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLkWxOVMzKM7:TR?=	M4rVbHNCVkeHUh?=
human BFTC-905 cell	NEmyb\|JIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NYLTTXRRUW6qaXLpeIlwdiCxZjDoeY1idiCERmTDMVkxPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTBwN{i0OVUh\|ryP	NW\2WFY4W0GQR1XS
human KM12 cell	NVnPOFhjT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MXvJcohq[mm2aX;uJI9nKGi3bXHuJGtOOTJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1yLki1NFY6KM7:TR?=	NWjJR5d2W0GQR1XS
human GDM-1 cell	MkTUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MVrJcohq[mm2aX;uJI9nKGi3bXHuJGdFVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MD64O\|k{PyEQvF2=	MnP4V2FPT0WU
human RT-112 cell	NEGxfmdIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	Mme1TY5pcWKrdHnvckBw\iCqdX3hckBTXC1zMUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlAzPzh{IN88US=>	MYrTRW5ITVJ?
human MONO-MAC-6 cell	M{HucGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MXjJcohq[mm2aX;uJI9nKGi3bXHuJG1QVk9vTVHDMVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjF6MEm3JO69VQ>?	MUTTRW5ITVJ?
human HUTU-80 cell	NHLtb\|dIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MlvDTY5pcWKrdHnvckBw\iCqdX3hckBJXVSXLUiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU4{ODF5MjFOwG0>	NF7ld5VUSU6JRWK=
human HGC-27 cell	NYXrNIU3T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NFXzVWtKdmirYnn0bY9vKG:oIHj1cYFvKEiJQz2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvOzB6MkGg{txO	MWTTRW5ITVJ?
human LCLC-97TM1 cell	MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	Mkm4TY5pcWKrdHnvckBw\iCqdX3hckBNS0yFLUm3WG0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OS5\|Nke2PEDPxE1?	M2\M[XNCVkeHUh?=
human LXF-289 cell	NIn1OnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NF;nXmVKdmirYnn0bY9vKG:oIHj1cYFvKEy[Rj2yPFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yNjRyMUWyJO69VQ>?	NW\ERXVIW0GQR1XS
human HLE cell	NEPhN25Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MWPJcohq[mm2aX;uJI9nKGi3bXHuJGhNTSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTFwNEK2PFMh\|ryP	NX2xZldDW0GQR1XS
human RKO cell	NHTibHpIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NWf0[lAxUW6qaXLpeIlwdiCxZjDoeY1idiCUS1:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlU4QDZ7IN88US=>	NVLCOlBwW0GQR1XS
human SNG-M cell	MUPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M1vnTWlvcGmkaYTpc44hd2ZiaIXtZY4hW06JLV2gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlc6QDV\|IN88US=>	NXTDVGhVW0GQR1XS
human MCF7 cell	MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NWfD[mpkUW6qaXLpeIlwdiCxZjDoeY1idiCPQ1[3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU45OTd6IN88US=>	NUH0T5luW0GQR1XS
human A431 cell	NHfzbVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NFvNOWJKdmirYnn0bY9vKG:oIHj1cYFvKEF2M{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlg2QTB{IN88US=>	MoPZV2FPT0WU
human BC-3 cell	NFfRR\|RIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NHvCbIxKdmirYnn0bY9vKG:oIHj1cYFvKEKFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xMlg4ODl2IN88US=>	NGXsOGtUSU6JRWK=
human A427 cell	MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M4Lid2lvcGmkaYTpc44hd2ZiaIXtZY4hSTR{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUGuPFc3OTFizszN	M{TtO3NCVkeHUh?=
human SW620 cell	MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NHfkRZJKdmirYnn0bY9vKG:oIHj1cYFvKFOZNkKwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46OjhzNjFOwG0>	M17KTHNCVkeHUh?=
human HOS cell	NUm0blVHT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NE\QOndKdmirYnn0bY9vKG:oIHj1cYFvKEiRUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUGuPVc{OTJizszN	M3K1W3NCVkeHUh?=
human MFH-ino cell	MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MnHETY5pcWKrdHnvckBw\iCqdX3hckBOTkhvaX7vJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NU46QDZ3ODFOwG0>	MkLoV2FPT0WU
human TE-12 cell	NHPNVYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NWDJbmozUW6qaXLpeIlwdiCxZjDoeY1idiCWRT2xNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEvQTlzMkig{txO	NUC2NVkzW0GQR1XS
human KU812 cell	NWPrbG5uT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M{LaWWlvcGmkaYTpc44hd2ZiaIXtZY4hU1V6MUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlE5PzFizszN	NIXYOXdUSU6JRWK=
human NCI-H2342 cell	MoDwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MlnRTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKzOFIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjF7MEWzJO69VQ>?	NYDaboF4W0GQR1XS
human BC-1 cell	NFrJ[VBIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M4jXcmlvcGmkaYTpc44hd2ZiaIXtZY4hSkNvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUKuOVE3PTFizszN	MmnwV2FPT0WU
human TE-15 cell	NXHSdJA5T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M37xXmlvcGmkaYTpc44hd2ZiaIXtZY4hXEVvMUWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yMlU6OThzIN88US=>	MoraV2FPT0WU
human T84 cell	NHTzPZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NE\BS2NKdmirYnn0bY9vKG:oIHj1cYFvKFR6NDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUKuOlA1PDZizszN	NX3sSINFW0GQR1XS
human SW1710 cell	NXTEPHNtT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NFTHdJlKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPzByOEKg{txO	M3v0enNCVkeHUh?=
human CAL-12T cell	M1S5[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NECzc2FKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2xNnQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjdzMUW4JO69VQ>?	NVexempCW0GQR1XS
human NKM-1 cell	NGnD[YpIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NX;qdFMxUW6qaXLpeIlwdiCxZjDoeY1idiCQS12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPzZ5M{Gg{txO	NHr5ToZUSU6JRWK=
human OCUB-M cell	NHL5O45Iem:5dHigbY5pcWKrdHnvckBie3OjeR?=	M3\LbGlvcGmkaYTpc44hd2ZiaIXtZY4hV0OXQj3NJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk44QDh4MTFOwG0>	M3PJXnNCVkeHUh?=
human 786-0 cell	NIOyNnpIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MWjJcohq[mm2aX;uJI9nKGi3bXHuJFc5Pi1yIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;Mj65OFgzPSEQvF2=	M{Cwc3NCVkeHUh?=
human EW-13 cell	NV3ldIRnT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGVYNTF\|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;Mz6wNVU2QCEQvF2=	NIT1TpBUSU6JRWK=
human 5637 cell	MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MnzhTY5pcWKrdHnvckBw\iCqdX3hckA2PjN5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;Mz6yNFY3QSEQvF2=	NFLhTIpUSU6JRWK=
human PA-1 cell	MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M4LuO2lvcGmkaYTpc44hd2ZiaIXtZY4hWEFvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUOuN\|MxQDNizszN	NFfjfWJUSU6JRWK=
human NCI-H2122 cell	NXLOWGkyT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NXPlOWtPUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIyOjJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1\|LkOzN{DPxE1?	NGjr[JNUSU6JRWK=
human NCI-H460 cell	NWDPTZdKT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MVvJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KNE[wJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N{41ODRzIN88US=>	M4i1XXNCVkeHUh?=
human CHL-1 cell	MmP4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M4HyNWlvcGmkaYTpc44hd2ZiaIXtZY4hS0iOLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlQ6PjZ3IN88US=>	NYLYVXB2W0GQR1XS
human MOLT-16 cell	NHnGOWVIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NIr6S2NKdmirYnn0bY9vKG:oIHj1cYFvKE2RTGStNVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{NjVzNUW1JO69VQ>?	MYXTRW5ITVJ?
human HCT-15 cell	M1LRWWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	MYrJcohq[mm2aX;uJI9nKGi3bXHuJGhEXC1zNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUOuOlI5PDJizszN	MWXTRW5ITVJ?
human G-361 cell	NU\nS3hKT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M2\QfmlvcGmkaYTpc44hd2ZiaIXtZY4hTy1\|NkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlcyPzR3IN88US=>	NVHyWIRrW0GQR1XS
human SK-LU-1 cell	MoW4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	MWLJcohq[mm2aX;uJI9nKGi3bXHuJHNMNUyXLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zMlk4ODF2IN88US=>	MoLtV2FPT0WU
human ES4 cell	NGf3T\|ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NIXJdVVKdmirYnn0bY9vKG:oIHj1cYFvKEWVNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUSuNFYxPjlizszN	NVvmbYE6W0GQR1XS
human TE-8 cell	NWe1bmU4T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MnPKTY5pcWKrdHnvckBw\iCqdX3hckBVTS16IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;ND6xNVU5OiEQvF2=	MVXTRW5ITVJ?
human IGR-1 cell	MVzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MnzMTY5pcWKrdHnvckBw\iCqdX3hckBKT1JvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUSuNlM{KM7:TR?=	Mn3sV2FPT0WU
human SW954 cell	MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	NF7N[o1KdmirYnn0bY9vKG:oIHj1cYFvKFOZOUW0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OE41PjF{NDFOwG0>	NIO4bnFUSU6JRWK=
human A375 cell	MYXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	M4\XNmlvcGmkaYTpc44hd2ZiaIXtZY4hSTN5NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUWuNlU1QTJizszN	NEXUW4NUSU6JRWK=
human CAL-27 cell	MUnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MlfvTY5pcWKrdHnvckBw\iCqdX3hckBESUxvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlM{OjJzIN88US=>	MUTTRW5ITVJ?
human CAL-51 cell	NHPqR5RIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	MYPJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC13MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUWuN\|U2QDNizszN	MoLSV2FPT0WU
human SK-LMS-1 cell	M1y3cmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	NYnzW\|lpUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3MUXMuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRTVwM{iyOVUh\|ryP	M3nHdHNCVkeHUh?=
human HT-1080 cell	NUm1Tmh4T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MmLJTY5pcWKrdHnvckBw\iCqdX3hckBJXC1zMEiwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU41QTN2NzFOwG0>	Ml2zV2FPT0WU
human NCI-H1299 cell	NFrpPJVIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	Ml3TTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEGyPVkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02Njl6NUW3JO69VQ>?	NUPwd4loW0GQR1XS
human HT-29 cell	M{fYTGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7	M3Hwc2lvcGmkaYTpc44hd2ZiaIXtZY4hUFRvMkmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME23MlI3QDR\|IN88US=>	MV3TRW5ITVJ?
human A388 cell	MmXjS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NVfEVXdTUW6qaXLpeIlwdiCxZjDoeY1idiCDM{i4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{42QTl4NTFOwG0>	NYfibJF{W0GQR1XS
human SK-MEL-30 cell	NYC1dZpCT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NUGxZoFFUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD15Lkm3NlE2KM7:TR?=	MXjTRW5ITVJ?
human CMK cell	MULHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MVvJcohq[mm2aX;uJI9nKGi3bXHuJGNOUyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR\|UxRThwMkWzO\|ch\|ryP	MoT5V2FPT0WU
human HuP-T4 cell	NVvKPJdST3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MmrtTY5pcWKrdHnvckBw\iCqdX3hckBJfVBvVESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlUxOjN2IN88US=>	MmW4V2FPT0WU
human SF126 cell	NUe3cJFxT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MXnJcohq[mm2aX;uJI9nKGi3bXHuJHNHOTJ4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;OD64NFIxQCEQvF2=	NEm0d2FUSU6JRWK=
human MKN1 cell	NIHidWpIem:5dHigbY5pcWKrdHnvckBie3OjeR?=	NHTIZolKdmirYnn0bY9vKG:oIHj1cYFvKE2NTkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlE5PTZ3IN88US=>	NIf2RXBUSU6JRWK=
human LoVo cell	MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	MmXZTY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;OT65NVI6OiEQvF2=	M161PXNCVkeHUh?=
human HEL cell	NWXSfYg{T3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	M332UGlvcGmkaYTpc44hd2ZiaIXtZY4hUEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MUCuOlgh\|ryP	NYL1PXB3W0GQR1XS
human SW872 cell	NXHzdZcxT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	MmLyTY5pcWKrdHnvckBw\iCqdX3hckBUXzh5MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUGzMlY5QTZizszN	M{n6SnNCVkeHUh?=
human SW982 cell	MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	Mnr4TY5pcWKrdHnvckBw\iCqdX3hckBUXzl6MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG\|c3H5MEBKSzVyPUGzMlc6OTZizszN	M3j5UHNCVkeHUh?=
human HuH-7 cell	MofLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	M{DDbWlvcGmkaYTpc44hd2ZiaIXtZY4hUHWKLUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPE4zPzh\|IN88US=>	M3f3O3NCVkeHUh?=
human DU-145 cell	MojHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NHLxe4NKdmirYnn0bY9vKG:oIHj1cYFvKESXLUG0OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIxNjR7NUWg{txO	MmS5V2FPT0WU
human MC116 cell	NWn2PJJVT3Kxd4ToJIlvcGmkaYTpc44h[XO\|YYm=	NWrNb\|hTUW6qaXLpeIlwdiCxZjDoeY1idiCPQ{GxOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjJ4N{[g{txO	NYDrS2pDW0GQR1XS
human H4 cell	MmLqS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl?	NE[wWXBKdmirYnn0bY9vKG:oIHj1cYFvKEh2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO\|YYmsJGlEPTB;MkGuOFI1PCEQvF2=	M1fXfHNCVkeHUh?=
human SK-MEL-3 cell	MUfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>?	Mn\3TY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjB{Mkig{txO	NFjERVdUSU6JRWK=

Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID

Western blot	p21 / LC3 / p62 / PARP / Cleaved PARP ; c-Jun / NRF2 ; p-SGK1 / SGK1 ; p-SGK2 / SGK2	29017179 31136958 30873046 26392083
Immunofluorescence	LC3	29017179
Growth inhibition assay	Cell viability	29017179

Protocol (from reference)

Kinase Assay:^[1]	Scintillation proximity assay (SPA): SGK1 S422D (60–431 aa; 0.275 μg/mL final concentration) or SGK2 (0.875 μg/mL final concentration) are 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 min at 30°C. SGK2 is 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 is prepared in the reaction buffer. In a 96-well plate, 5 μL of GSK650394 is added to 25 μL of the activated enzyme mixture. To this, 20 μL of the CROSStide mixture is added and incubated for 1 h 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 is added. The plate is then sealed and centrifuged for 8 min at 2000 rpm, and the signal is 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 GSK650394 are calculated from these data using GraphPad Prism 3 Software.
Cell Research:^[1]	Cell lines: LNCaP cells Concentrations: ~10 μM Incubation Time: 7 days Method: LNCaP cells are plated at a density of 5,000 cells per well in 96-well plates in 100 μL PRF-RPMI 1640, supplemented with 8% CS-FBS, 0.1 mM NEAA, and 1 mM NaPyr. At day three, cells are treated with hormone with or without GSK650394 by removing 50 μL of the media and replacing this with 50 μL of PRF-RPMI 1640 with 8% CS-FBS, NEAA, NaPyr containing a 2X concentration of the appropriate hormone/inhibitor treatment. At days 5 and 7, the treatment is repeated. On the tenth day, the media is removed and the relative cell number is measured using the FluoReporter Blue assay according to the manufacturer’s instructions.

Kinase Assay:^[1]

Scintillation proximity assay (SPA):
SGK1 S422D (60–431 aa; 0.275 μg/mL final concentration) or SGK2 (0.875 μg/mL final concentration) are 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 min at 30°C. SGK2 is 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 is prepared in the reaction buffer. In a 96-well plate, 5 μL of GSK650394 is added to 25 μL of the activated enzyme mixture. To this, 20 μL of the CROSStide mixture is added and incubated for 1 h 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 is added. The plate is then sealed and centrifuged for 8 min at 2000 rpm, and the signal is 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 GSK650394 are calculated from these data using GraphPad Prism 3 Software.

Cell Research:^[1]

Cell lines: LNCaP cells
Concentrations: ~10 μM
Incubation Time: 7 days
Method: LNCaP cells are plated at a density of 5,000 cells per well in 96-well plates in 100 μL PRF-RPMI 1640, supplemented with 8% CS-FBS, 0.1 mM NEAA, and 1 mM NaPyr. At day three, cells are treated with hormone with or without GSK650394 by removing 50 μL of the media and replacing this with 50 μL of PRF-RPMI 1640 with 8% CS-FBS, NEAA, NaPyr containing a 2X concentration of the appropriate hormone/inhibitor treatment. At days 5 and 7, the treatment is repeated. On the tenth day, the media is removed and the relative cell number is measured using the FluoReporter Blue assay according to the manufacturer’s instructions.

References	[1] Sherk AB, et al. Cancer Res. 2008, 68(18), 7475-7483. [2] Anacker C, et al. Proc Natl Acad Sci U S A. 2013, 110(21), 8708-8713. [3] Alamares-Sapuay JG, et al. J Virol. 2013, 87(10), 6020-6066.

References

Solubility (25°C)

In vitro	DMSO	76 mg/mL (198.71 mM)
	Water	Insoluble
	Ethanol	Insoluble

Chemical Information

Molecular Weight	382.45
Formula	C₂₅H₂₂N₂O₂
CAS No.	890842-28-1
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1CCC(C1)C2=C(C=CC(=C2)C3=CNC4=C3C=C(C=N4)C5=CC=CC=C5)C(=O)O

Download GSK650394 SDF

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