SB216763

For research use only.

Catalog No.S1075

44 publications

SB216763 Chemical Structure

CAS No. 280744-09-4

SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activates autophagy.

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10mM (1mL in DMSO) RMB 1351.27 In stock
RMB 1218.72 In stock
RMB 2208.01 In stock
RMB 7122.58 In stock
RMB 8763.30 In stock
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Selleck's SB216763 has been cited by 44 publications

Purity & Quality Control

Choose Selective GSK-3 Inhibitors

Biological Activity

Description SB216763 is a potent and selective GSK-3 inhibitor with IC50 of 34.3 nM for GSK-3α and equally effective at inhibiting human GSK-3β. SB216763 activates autophagy.
Targets
GSK-3α [1]
(Cell-free assay)
GSK-3β [1]
(Cell-free assay)
34.3 nM ~34.3 nM
In vitro

SB 216763 displays similar potency for GSK-3β with 96% inhibition at 10 μM while exhibiting minimal activity against 24 other protein kinases including PKBα and PDK1 with IC50 of >10 μM. SB 216763 stimulates glycogen synthesis in human liver cells with EC50 of 3.6 μM, and induces dose-dependent transcription of a β-catenin-LEF/TCF regulated reporter gene in HEK293 cells with a maximum 2.5-fold induction at 5 μM. [1] SB 216763 protects the cerebellar granule neurones from apoptotic cell death induced by LY-294002 or potassium-deprivation in a concentration-dependent manner, with a maximal neuroprotection at 3 μM in contrast with the effect of lithium chloride at which 10 mM is required. SB 216763 at 3 μM also completely prevents death of chicken dorsal root ganglion sensory neurones induced by LY-294002 regardless of NGF. SB 216763 treatment at 5 μM markedly inhibits the GSK-3-dependent phosphorylation of neuronal-specific microtubule-associated protein tau in cerebellar granule neurones or recombinant tau in HEK293 cells, and induces increased levels of cytoplasmic β-catenin in both cells mimicking the effect of Wnt-mediated inhibition of GSK-3. [2] In pancreatic cancer cell lines including BXPC-3, MIA-PaCa2, PANC1, ASPC1, and CFPAC, SB 216763 treatment at 25-50 μM reduces cell viability in a dose-dependent manner, and leads to significant increase in apoptosis by 50% at 72 hours due to the specific down regulation of GSK-3β, while has no effect in HMEC or WI38 cell lines. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEK293 cells M4PRdGZ2dmO2aX;uJIF{e2G7 M3jzU2dtgWOxZ3XuJJN6dnSqYYPlJIFkfGm4aYT5JI9nKEiHS{K5N{Bk\WyuczygbY5pcWKrdHnvckBw\iCJU1uzMYJmfGFuIFXDOVA:OC5{IN88US=> MVixNlk1OTN|MR?=
human HDLM-2 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\oTY5pcWKrdHnvckBw\iCqdX3hckBJTEyPLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxQTh2IN88US=> NVXyTFI4W0GQR1XS
human NCI-H1770 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFjRVZVKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVc4OCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LjDJR|UxRTBwMkmzPVIh|ryP M{f1VHNCVkeHUh?=
human HOP-62 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MofRTY5pcWKrdHnvckBw\iCqdX3hckBJV1BvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlg2OjV4IN88US=> NVu3eldnW0GQR1XS
human JAR cell NGLRUWtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NEL0bmFKdmirYnn0bY9vKG:oIHj1cYFvKEqDUjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlExPDRizszN MUDTRW5ITVJ?
human K5 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHzZZWNKdmirYnn0bY9vKG:oIHj1cYFvKEt3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJktKEmFNUC9NU42OzZ7ODFOwG0> NXTsdJRiW0GQR1XS
human MV-4-11 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4\5XWlvcGmkaYTpc44hd2ZiaIXtZY4hVVZvND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPjl4OEWg{txO MnPVV2FPT0WU
human BT-549 cell MoHaS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYHJcohq[mm2aX;uJI9nKGi3bXHuJGJVNTV2OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUWuNlk{PzZizszN MVHTRW5ITVJ?
human LB2241-RCC cell NHvCTXdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVPPZZRkUW6qaXLpeIlwdiCxZjDoeY1idiCOQkKyOFEuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj60Nlg4PCEQvF2= M1TpRXNCVkeHUh?=
human GAMG cell MnnUS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2K1WGlvcGmkaYTpc44hd2ZiaIXtZY4hT0GPRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uOlU1ODlizszN MkHjV2FPT0WU
human HMV-II cell MXjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVrJcohq[mm2aX;uJI9nKGi3bXHuJGhOXi2LSTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUeuOlc3ODdizszN MV7TRW5ITVJ?
human RS4-11 cell NV24UWRkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVHJcohq[mm2aX;uJI9nKGi3bXHuJHJUPC1zMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUiuNlQyPDFizszN MnjQV2FPT0WU
human NCI-H1993 cell M1niXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIjHRWxKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVk6OyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRThwM{[1N|Qh|ryP M4XqWHNCVkeHUh?=
human IST-SL1 cell NVTPR5BwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2m3PGlvcGmkaYTpc44hd2ZiaIXtZY4hUVOWLWPMNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvODJyNDFOwG0> MoDsV2FPT0WU
human SK-OV-3 cell NVqzNXBIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWXJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlExODJizszN NWPSXXcyW0GQR1XS
human ESS-1 cell NIe1WYNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlKxTY5pcWKrdHnvckBw\iCqdX3hckBGW1NvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUmuOVk5PzJizszN M2noZnNCVkeHUh?=
human G-361 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH3nVZdKdmirYnn0bY9vKG:oIHj1cYFvKEdvM{[xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvOTd7ODFOwG0> NE\FcnZUSU6JRWK=
human ALL-PO cell Mnn6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MU\Jcohq[mm2aX;uJI9nKGi3bXHuJGFNVC2STzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlM1PzdizszN NHLrVGhUSU6JRWK=
human NB5 cell MkXxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NE\nVmVKdmirYnn0bY9vKG:oIHj1cYFvKE6ENTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlIyPTdizszN NWjrU4NEW0GQR1XS
human DU-145 cell NY\CNIZrT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkX6TY5pcWKrdHnvckBw\iCqdX3hckBFXS1zNEWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU43PTN3IN88US=> NYfTRo1wW0GQR1XS
human NMC-G1 cell Mlr6S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn7XTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU44OjZ2IN88US=> M3m4bnNCVkeHUh?=
human RPMI-7951 cell Mn;HS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFPTbmZKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LjDJR|UxRTFzLke4OlQh|ryP M{HFZXNCVkeHUh?=
human NCI-H2009 cell M1TRdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4jLTmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwMkSyO{DPxE1? MVHTRW5ITVJ?
human LoVo cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnnxTY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuN|c4OSEQvF2= NHTJfpdUSU6JRWK=
human A2058 cell M4jSSmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmHUTY5pcWKrdHnvckBw\iCqdX3hckBCOjB3ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlQ3QSEQvF2= M1\zenNCVkeHUh?=
human D-566MG cell MnTHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYWxbYY6UW6qaXLpeIlwdiCxZjDoeY1idiCGLUW2Om1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwOUS4NUDPxE1? MljWV2FPT0WU
human QIMR-WIL cell NI\CPVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH\0eZVKdmirYnn0bY9vKG:oIHj1cYFvKFGLTWKtW2lNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTVwNkO5OEDPxE1? MW\TRW5ITVJ?
human S-117 cell NYe3TVZoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3zoSGlvcGmkaYTpc44hd2ZiaIXtZY4hWy1zMUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk41ODJ{IN88US=> MYjTRW5ITVJ?
human YH-13 cell MoD2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnjQTY5pcWKrdHnvckBw\iCqdX3hckB[UC1zMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG2MlY5PjVizszN NILyOG1USU6JRWK=
human IGROV-1 cell M3TGcWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEe5VnJKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPy5{MECxJO69VQ>? NFS3SpdUSU6JRWK=
human BHT-101 cell M4nrbWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIHRUGNKdmirYnn0bY9vKG:oIHj1cYFvKEKKVD2xNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPy54MEm5JO69VQ>? M3fnNHNCVkeHUh?=
human MKN45 cell NEH2[WRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGnjeIVKdmirYnn0bY9vKG:oIHj1cYFvKE2NTkS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVgvPDF{ODFOwG0> NVj4S|Q3W0GQR1XS
human A498 cell NXX2W5RtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlGxTY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuOFU1QSEQvF2= NVf6Z2ZyW0GQR1XS
human U-266 cell NH3ae49Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKGi3bXHuJHUuOjZ4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkCuPFc6PyEQvF2= NYj4OXBmW0GQR1XS
human BFTC-905 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWHJcohq[mm2aX;uJI9nKGi3bXHuJGJHXENvOUC1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvOTh5OTFOwG0> NHHFS|lUSU6JRWK=
human BxPC-3 cell Ml3hS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3\k[WlvcGmkaYTpc44hd2ZiaIXtZY4hSniSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvOzV3NDFOwG0> NWP2VVRqW0GQR1XS
human NCI-SNU-1 cell NWXYW403T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWDOZ5V{UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{MT61OVU5KM7:TR?= MkjRV2FPT0WU
human SF539 cell M3HrS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYXJcohq[mm2aX;uJI9nKGi3bXHuJHNHPTN7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkKuNFE6QCEQvF2= NFjOOlhUSU6JRWK=
human VA-ES-BJ cell NGfqeWxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M16zemlvcGmkaYTpc44hd2ZiaIXtZY4hXkFvRWOtRmoh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOi53N{[zJO69VQ>? NWDUb4ZTW0GQR1XS
human HuO-3N1 cell M{LVeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVTOb2ZyUW6qaXLpeIlwdiCxZjDoeY1idiCKdV:tN24yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjJwNkG1NUDPxE1? NYLzXGs{W0GQR1XS
human EM-2 cell MmC4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2L3NWlvcGmkaYTpc44hd2ZiaIXtZY4hTU1vMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlY3QDlizszN NIXQTZNUSU6JRWK=
human T98G cell M4S3Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYnDVmdwUW6qaXLpeIlwdiCxZjDoeY1idiCWOUjHJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlMvOzByOTFOwG0> MVzTRW5ITVJ?
human SW1783 cell MnO4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWPJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTd6MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKzMlUzPDNizszN NYnxRZVxW0GQR1XS
human NKM-1 cell MX3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIrHXopKdmirYnn0bY9vKG:oIHj1cYFvKE6NTT2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlMvQDVzMjFOwG0> M1jNTnNCVkeHUh?=
human KOSC-2 cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVvJcohq[mm2aX;uJI9nKGi3bXHuJGtQW0NvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlEzQTJizszN NFe4dlBUSU6JRWK=
human SW48 cell MXnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NETqeZJKdmirYnn0bY9vKG:oIHj1cYFvKFOZNEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE43ODZ5IN88US=> MWrTRW5ITVJ?
human MIAPaCa2 cells NH:5VXBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NI\GV244OiCq MoTWS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWlCWGGFYUKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NF0zPSEQvF2= NYnQSZljOTl|M{izOVU>
human NCI-H28 cell M2LkV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NETINIxKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPS5{MUC0JO69VQ>? M3nzTHNCVkeHUh?=
human 5637 cell MoP1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NUPlTZdWUW6qaXLpeIlwdiCxZjDoeY1idiB3NkO3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlUvQDFzMTFOwG0> MVHTRW5ITVJ?
human NB69 cell M13ybWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUPJcohq[mm2aX;uJI9nKGi3bXHuJG5DPjliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Nj6xO|Y1KM7:TR?= NHrqWm5USU6JRWK=
human HT-29 cell M4WycGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIDObnFKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvOTd3MjFOwG0> MoHGV2FPT0WU
human PFSK-1 cell M3SyTWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHTGcXFKdmirYnn0bY9vKG:oIHj1cYFvKFCIU1utNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4NjV7MzFOwG0> MWfTRW5ITVJ?
human UACC-257 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUHqT4x2UW6qaXLpeIlwdiCxZjDoeY1idiCXQVPDMVI2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ5Lke0N{DPxE1? NYTkfo1EW0GQR1XS
human D-423MG cell NFW5R2NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MX;Jcohq[mm2aX;uJI9nKGi3bXHuJGQuPDJ|TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO{46OTB4IN88US=> M{TrVXNCVkeHUh?=
human NH-12 cell NInrZpBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlPOTY5pcWKrdHnvckBw\iCqdX3hckBPUC1zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlQxPTlizszN MnnXV2FPT0WU
human DEL cell NXK4c|VPT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGnuXZJKdmirYnn0bY9vKG:oIHj1cYFvKESHTDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5MlA1PzRizszN M2PuZ3NCVkeHUh?=
human LS-513 cell NIXkT|lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlHWTY5pcWKrdHnvckBw\iCqdX3hckBNWy13MUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNE4yOzN2IN88US=> NXyzUW45W0GQR1XS
human NBsusSR cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mo\2TY5pcWKrdHnvckBw\iCqdX3hckBPSnO3c2PSJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AvPTZ5ODFOwG0> MlXsV2FPT0WU
human BV-173 cell M3XJW2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmfrTY5pcWKrdHnvckBw\iCqdX3hckBDXi1zN{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNE44PjR7IN88US=> M1TuenNCVkeHUh?=
human A101D cell M1PPV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MYjJcohq[mm2aX;uJI9nKGi3bXHuJGEyODGGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{CuPVc5PCEQvF2= MWfTRW5ITVJ?
human LU-134-A cell M{\zdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGxWNTF|ND3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|EvODJ|ODFOwG0> NGTwUlFUSU6JRWK=
human ES3 cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEjUbJRKdmirYnn0bY9vKG:oIHj1cYFvKEWVMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOxMlM{PzZizszN NHjKPJFUSU6JRWK=
human NY cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXjJcohq[mm2aX;uJI9nKGi3bXHuJG5[KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzJwMkm2OUDPxE1? MVHTRW5ITVJ?
human NCI-H1975 cell Mln4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWLJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUm3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMzNjN3OEKg{txO MlXYV2FPT0WU
human A704 cell Mn2yS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXzJcohq[mm2aX;uJI9nKGi3bXHuJGE4ODRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ND6yNFU6KM7:TR?= MVzTRW5ITVJ?
human SK-MEL-24 cell MYPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnKyTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNlQh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PC5{NUKzJO69VQ>? Moi3V2FPT0WU
human SW1088 cell MlPMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2DmZ2lvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMEi4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QvOzR3MjFOwG0> MnnMV2FPT0WU
human HepG2 cells MULGeY5kfGmxbjDhd5NigQ>? M3nsblM1KM7:TR?= MWKxNkBp MorXTY5pcWKrdHnvckBw\iCJU1uzZoV1[SCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC{YYTpc{Bw\iCyaH;zdIhwenmuYYTl[EBIWy:JUzDheEA{PCC3TTDh[pRmeiBzMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NVT2RYF{OjV2NkexOVA>
mouse 3T3L1 cells Mn\sSpVv[3Srb36gZZN{[Xl? NXrGToZmOzRizszN M36ydlEzKGh? MUTJcoNz\WG|ZTDpckBodHWlb4PlJIlv[2:{cH;yZZRqd25iaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOzRidV2gZYZ1\XJiMUKgbJJ{KGK7IHfseYNwe2ViYYPzZZk> NWHYdWxOOjV2NkexOVA>
human ST14A cells MmHzSpVv[3Srb36gZZN{[Xl? MVm2JIg> NH2z[GtKdmirYnn0bY9vKG:oIFfTT{0{NWKndHGtcYVlcWG2ZXSgW451KHOrZ37hcIlv\yCrbjDoeY1idiCVVEG0RUBk\WyuczDhd5Nme3OnZDDhd{BqdmO{ZXHz[UBqdiCjY3P1cZVt[XSrb36gc4Yh[mW2YT3jZZNmcW5iYYLveY5lKG63Y3zleZMh[W[2ZYKgOkBpenNiYomgcYlkem:|Y3;wbYMh[W6jbInzbZM> NGnwOW8zODdyOEmzOy=>
human ReNcell VM cells MVHQdo9tcW[ncnH0bY9vKGG|c3H5 NHHtcYM{KM7:TR?= MkL3O|IhcA>? M{LrbWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUnXOZ4VtdCCYTTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGG2IEOgeW0h[W[2ZYKgO|IhcHK| M2fxVVIxPzB6OUO3
human SK-MEL-1 cell NG\XbHZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml\QTY5pcWKrdHnvckBw\iCqdX3hckBUUy2PRVytNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7LDDJR|UxRTN2LkexOEDPxE1? MlnmV2FPT0WU
human MOLT-4 cell MoLiS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1W3NmlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|YvOTR4NzFOwG0> MWTTRW5ITVJ?
human T47D cell Mkn1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mmn1TY5pcWKrdHnvckBw\iCqdX3hckBVPDeGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{euNVY1PyEQvF2= MVzTRW5ITVJ?
human SW1710 cell NF\tb2FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHfLem9KdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM4NjN4MEig{txO NUj6OZg3W0GQR1XS
human MKN7 cell M2Tr[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYHwUoNHUW6qaXLpeIlwdiCxZjDoeY1idiCPS163JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|gvODlyOTFOwG0> MoK0V2FPT0WU
human CAL-72 cell MomzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVnJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC15MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlEyPzhizszN MoW4V2FPT0WU
human AGS cell M4fzc2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF3sV5ZKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlIxOzlizszN MWXTRW5ITVJ?
human BE-13 cell NFnmd5RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2TxWGlvcGmkaYTpc44hd2ZiaIXtZY4hSkVvMUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPE44Pzh|IN88US=> NH3wbYRUSU6JRWK=
human Calu-6 cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2jU[mlvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|kvPjl4NDFOwG0> NF3mOnFUSU6JRWK=
human CAL-27 cell MorHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHjDbHZKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ1NjByNUSg{txO NWT6OWR3W0GQR1XS
human BB49-HNC cell NI\2T21Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2q1[mlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ2OT3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01PC5yMke4JO69VQ>? MljlV2FPT0WU

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
pGSK-3β / GSK-3β / E2F1 / β-catenin ; 

PubMed: 28042322     


Inhibition of GSK3β increased LSH expression. U251 (A) and HS683 (B) with treatment of SB216763 with different concentration as indicated were examined for the expression of LSH, p-GSK3β, GSK3β, E2F1, β-catenin and GAPDH by Western analysis. U251 (C) and HS683 (D) with treatment of 10μM SB216763 with time as indicated were examined for the expression of LSH, p-GSK3β, GSK3β, E2F1, β-catenin and GAPDH by Western analysis.

c-Myb; 

PubMed: 21795403     


Jurkat, K562, and RPMI 8226 cells were treated with or without 5 or 10 μM SB216763 for 8 h, and cell lysates were analyzed by immunoblotting. 

28042322 21795403
Growth inhibition assay
Cell viability; 

PubMed: 24779365     


Cell viability of mouse embryonic stem cells after exposure to GSK3 inhibitors. (A) Cell viability of the mouse embryonic stem cell line ES-D3 after a three day treatment with different concentrations of BIO, SB-216763, CHIR-99021 and CHIR-98014. Cell viability was measured with the MTT assay. DMSO without inhibitors was used as vehicle control. Data are expressed as percentages normalized to the control condition without inhibitors. (B) Cell viability of the mouse embryonic stem cell line ES-CCE after a three day treatment with different concentrations of BIO, SB-216763, CHIR-99021 and CHIR-98014. Values are means ± SEM, n = 3-5. ANOVA plus Dunnett’s post hoc test. ** p ≤ 0.01, * p ≤ 0.05 compared to the control.

24779365
In vivo Administration of SB 216763 at 20 mg/kg significantly prevents lung inflammation and the subsequent fibrosis in bleomycin (BLM)-induced pulmonary inflammation and fibrosis model in mice by significantly blocking the production of inflammatory cytokines MCP-1 and TNF-α by macrophages, and significantly improves the survival of BLM-treated mice. SB 216763 treatment causes a significant reduction in BLM-induced alveolitis by inhibiting alveolar epithelial cell damage. [4]

Protocol

Kinase Assay:[1]
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GSK-3 activity assay:

GSK-3 kinase activity is measured, in the presence of various concentrations of SB 216763, in a reaction mixture containing final concentrations of 1 nM human GSK-3α, 50 mM MOPS pH 7.0, 0.2 mM EDTA, 10 mM Mg-acetate, 7.5 mM β-mercaptoethanol, 5% (w/v) glycerol, 0.01% (w/v) Tween-20, 10% (v/v) DMSO, and 28 μM GS-2 peptide substrate. The GS-2 peptide sequence corresponds to a region of glycogen synthase that is phosphorylated by GSK-3. The assay is initiated by the addition of 0.34 μCi [33P]γ-ATP. The total ATP concentration is 10 μM. Following 30 minutes incubation at room temperature the assay is stopped by the addition of one third assay volume of 2.5% (v/v) H3PO4 containing 21 mM ATP. Samples are spotted onto P30 phosphocellulose mats and washed six times in 0.5% (v/v) H3PO4. The filter mats are sealed into sample bags containing Wallac betaplate scintillation fluid. 33P incorporation into the substrate peptide is determined by counting the mats in a Wallac microbeta scintillation counter.
Cell Research:[3]
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  • Cell lines: BXPC-3, MIA-PaCa2, PANC1, ASPC1, and CFPAC cells
  • Concentrations: Dissolved in DMSO, final concentrations ~50 μM
  • Incubation Time: 24, 48, and 72 hours
  • Method: Cells are exposed to various concentrations of SB 216763 for 24, 48 and 72 hours. Relative cell viability is measured using the MTS assay. Apoptotic cells are determined by staining with Hoechst.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: C57BL/6N mice with lung inflammation and fibrosis induced by bleomycin (BLM)
  • Dosages: 20 mg/kg
  • Administration: Intravenously
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 23 mg/mL (61.95 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+corn oil
For best results, use promptly after mixing.
4mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 371.22
Formula

C19H12N2O2Cl2

CAS No. 280744-09-4
Storage powder
in solvent
Synonyms N/A
Smiles CN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=C(C=C(C=C4)Cl)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation ()
% DMSO % % Tween 80 % ddH2O
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Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

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  • Computed Result

  • C1=C0/X C1: LOG(C1):
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Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID