SB216763

For research use only. Not for use in humans.

Catalog No.S1075

30 publications

SB216763 Chemical Structure

Molecular Weight(MW): 371.22

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.

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Selleck's SB216763 has been cited by 30 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.
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 M1zVcGZ2dmO2aX;uJIF{e2G7 NFLLSYtIdHmlb3flckB{gW62aHHz[UBi[3Srdnn0fUBw\iCKRVuyPVMh[2WubIOsJIlvcGmkaYTpc44hd2ZiR2PLN{1j\XSjLDDFR|UxRTBwMjFOwG0> MVWxNlk1OTN|MR?=
human HDLM-2 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGTzPI9KdmirYnn0bY9vKG:oIHj1cYFvKEiGTF2tNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjB7OESg{txO MWHTRW5ITVJ?
human NCI-H1770 cell NUfYdoR2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVfJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUe3NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVAvOjl|OUKg{txO M{Xyd3NCVkeHUh?=
human HOP-62 cell M4TFNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmnvTY5pcWKrdHnvckBw\iCqdX3hckBJV1BvNkKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlg2OjV4IN88US=> NGWxUHpUSU6JRWK=
human JAR cell NInGPHlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M3HJNWlvcGmkaYTpc44hd2ZiaIXtZY4hUkGUIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MT6yNVA1PCEQvF2= MXTTRW5ITVJ?
human K5 cell MkXrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYfFe3ZGUW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6NCCLQ{WwQVEvPTN4OUig{txO MUjTRW5ITVJ?
human MV-4-11 cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MkHtTY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk43QTZ6NTFOwG0> NHLpWZNUSU6JRWK=
human BT-549 cell NH7r[JJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NES0fItKdmirYnn0bY9vKG:oIHj1cYFvKEKWLUW0PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOjl|N{[g{txO MomwV2FPT0WU
human LB2241-RCC cell NUTEWIZQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUTBSIExUW6qaXLpeIlwdiCxZjDoeY1idiCOQkKyOFEuWkOFIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj60Nlg4PCEQvF2= MlHiV2FPT0WU
human GAMG cell NUfpPYhRT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2flR2lvcGmkaYTpc44hd2ZiaIXtZY4hT0GPRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uOlU1ODlizszN NInJc3VUSU6JRWK=
human HMV-II cell MVnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NITpOWpKdmirYnn0bY9vKG:oIHj1cYFvKEiPVj3JTUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVcvPjd4MEeg{txO MY\TRW5ITVJ?
human RS4-11 cell NYLQelZMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYSyRldiUW6qaXLpeIlwdiCxZjDoeY1idiCUU{StNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjJ2MUSxJO69VQ>? M1[yXXNCVkeHUh?=
human NCI-H1993 cell MmfES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUm5N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvOzZ3M{Sg{txO NGHCNJVUSU6JRWK=
human IST-SL1 cell MkHnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2HlNGlvcGmkaYTpc44hd2ZiaIXtZY4hUVOWLWPMNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvODJyNDFOwG0> M2jYNnNCVkeHUh?=
human SK-OV-3 cell M3LBdmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NV\NVIZHUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3PWk0{KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS5zMECyJO69VQ>? M1Kye3NCVkeHUh?=
human ESS-1 cell NEHxd3lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NVT6PJBKUW6qaXLpeIlwdiCxZjDoeY1idiCHU2OtNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvPTl6N{Kg{txO MkTTV2FPT0WU
human G-361 cell NYm4OGR7T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYTJcohq[mm2aX;uJI9nKGi3bXHuJGcuOzZzIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUCuNVc6QCEQvF2= NFrYV5dUSU6JRWK=
human ALL-PO cell Mof0S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MkOyTY5pcWKrdHnvckBw\iCqdX3hckBCVExvUF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE4{PDd5IN88US=> M1nrenNCVkeHUh?=
human NB5 cell NYDxVnJ1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MV\Jcohq[mm2aX;uJI9nKGi3bXHuJG5DPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFzLkKxOVch|ryP M3z0e3NCVkeHUh?=
human DU-145 cell NYLkT3E{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVLjRlROUW6qaXLpeIlwdiCxZjDoeY1idiCGVT2xOFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS54NUO1JO69VQ>? Ml61V2FPT0WU
human NMC-G1 cell MUXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWnqU21TUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS55Mk[0JO69VQ>? M3\Hb3NCVkeHUh?=
human RPMI-7951 cell NYnXe4ZqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHW4fnJKdmirYnn0bY9vKG:oIHj1cYFvKFKSTVmtO|k2OSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LjDJR|UxRTFzLke4OlQh|ryP NFLq[pNUSU6JRWK=
human NCI-H2009 cell NXPWOYpXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{nyR2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwMkSyO{DPxE1? MV3TRW5ITVJ?
human LoVo cell NETBd|hIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYDJcohq[mm2aX;uJI9nKGi3bXHuJGxwXm9iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6zO|cyKM7:TR?= M3TZfXNCVkeHUh?=
human A2058 cell MlHHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MULJcohq[mm2aX;uJI9nKGi3bXHuJGEzODV6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOFY6KM7:TR?= MYPTRW5ITVJ?
human D-566MG cell NH;PVHVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmfrTY5pcWKrdHnvckBw\iCqdX3hckBFNTV4Nl3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVMvQTR6MTFOwG0> M2HwZ3NCVkeHUh?=
human QIMR-WIL cell NGTDTVZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4fTeGlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS54M{m0JO69VQ>? MlnxV2FPT0WU
human S-117 cell M4fFNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3L5TWlvcGmkaYTpc44hd2ZiaIXtZY4hWy1zMUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk41ODJ{IN88US=> NIflWYFUSU6JRWK=
human YH-13 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NH;a[WRKdmirYnn0bY9vKG:oIHj1cYFvKFmKLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvPjh4NTFOwG0> MYHTRW5ITVJ?
human IGROV-1 cell Mn;VS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MofaTY5pcWKrdHnvckBw\iCqdX3hckBKT1KRVj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVcvOjByMTFOwG0> MXXTRW5ITVJ?
human BHT-101 cell M3Oye2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M37jSWlvcGmkaYTpc44hd2ZiaIXtZY4hSkiWLUGwNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE4NjZyOUmg{txO MX\TRW5ITVJ?
human MKN45 cell MWLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmnBTY5pcWKrdHnvckBw\iCqdX3hckBOU052NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG4MlQyOjhizszN NHL5eFNUSU6JRWK=
human A498 cell NW\nbm1NT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH;hfmZKdmirYnn0bY9vKG:oIHj1cYFvKEF2OUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xPU41PTR7IN88US=> M4SyXHNCVkeHUh?=
human U-266 cell NGO2TlNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NIXuZ5hKdmirYnn0bY9vKG:oIHj1cYFvKFVvMk[2JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlAvQDd7NzFOwG0> NHzsZYVUSU6JRWK=
human BFTC-905 cell NU\FRphnT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnPxTY5pcWKrdHnvckBw\iCqdX3hckBDTlSFLUmwOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjF6N{mg{txO NX;YdolLW0GQR1XS
human BxPC-3 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2e5OWlvcGmkaYTpc44hd2ZiaIXtZY4hSniSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvOzV3NDFOwG0> NUfRUVhpW0GQR1XS
human NCI-SNU-1 cell NUTLTohkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MmH3TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvU17VMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS53NUW4JO69VQ>? M{nhNnNCVkeHUh?=
human SF539 cell Mnq1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYnvUVVOUW6qaXLpeIlwdiCxZjDoeY1idiCVRkWzPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIzNjBzOUig{txO NEnVZ4hUSU6JRWK=
human VA-ES-BJ cell NFu1S4FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVrJcohq[mm2aX;uJI9nKGi3bXHuJHZCNUWVLVLKJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvPTd4MzFOwG0> NHfsWXFUSU6JRWK=
human HuO-3N1 cell NV;GT3Q6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3fYe2lvcGmkaYTpc44hd2ZiaIXtZY4hUHWRLUPONUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIzNjZzNUGg{txO NFuyb29USU6JRWK=
human EM-2 cell NUe1fHBkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYCwW5hRUW6qaXLpeIlwdiCxZjDoeY1idiCHTT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvPjZ6OTFOwG0> NG\ocmhUSU6JRWK=
human T98G cell NW[wSVlXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NYjHSWRxUW6qaXLpeIlwdiCxZjDoeY1idiCWOUjHJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlMvOzByOTFOwG0> MXPTRW5ITVJ?
human SW1783 cell NEDLe4RIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NITVUGhKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUe4N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjV{NEOg{txO NXrYWnR2W0GQR1XS
human NKM-1 cell MlzJS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXjqdm5YUW6qaXLpeIlwdiCxZjDoeY1idiCQS12tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{Njh3MUKg{txO NFGxXpBUSU6JRWK=
human KOSC-2 cell NHXy[JpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1exeGlvcGmkaYTpc44hd2ZiaIXtZY4hU0:VQz2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvOTJ7MjFOwG0> MlrVV2FPT0WU
human SW48 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHNYPDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{ND62NFY4KM7:TR?= NVu2N4VLW0GQR1XS
human MIAPaCa2 cells M3LsdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmPxO|IhcA>? MX7Hdo94fGhiaX7obYJqfGmxbjDv[kBpfW2jbjDNTWFR[UOjMjDj[YxteyCjZoTldkA4OiCqcoOgZpkhVVSVIHHzd4F6NCCLQ{WwQVI2KM7:TR?= M{XmRVE6OzN6M{W1
human NCI-H28 cell MnXCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml7WTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlUvOjFyNDFOwG0> MnHxV2FPT0WU
human 5637 cell M4XHdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1HlW2lvcGmkaYTpc44hd2ZiaIXtZY4hPTZ|NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK1MlgyOTFizszN NYTD[mc3W0GQR1XS
human NB69 cell Ml36S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml7BTY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mk[uNVc3PCEQvF2= M33C[nNCVkeHUh?=
human HT-29 cell NIrJOHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVTJcohq[mm2aX;uJI9nKGi3bXHuJGhVNTJ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkeuNVc2OiEQvF2= NXzFO214W0GQR1XS
human PFSK-1 cell M2TCbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MUPJcohq[mm2aX;uJI9nKGi3bXHuJHBHW0tvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK3MlU6OyEQvF2= NUfFcYY{W0GQR1XS
human UACC-257 cell NFvoenNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4DsZWlvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPy55NEOg{txO MV;TRW5ITVJ?
human D-423MG cell NIfTO2lIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUXJcohq[mm2aX;uJI9nKGi3bXHuJGQuPDJ|TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO{46OTB4IN88US=> NHOxSIlUSU6JRWK=
human NH-12 cell NIXNOYtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXnJcohq[mm2aX;uJI9nKGi3bXHuJG5JNTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkiuOFA2QSEQvF2= NG[3bXZUSU6JRWK=
human DEL cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGnSdohKdmirYnn0bY9vKG:oIHj1cYFvKESHTDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK5MlA1PzRizszN M1X2enNCVkeHUh?=
human LS-513 cell M1rPb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX7nVpd2UW6qaXLpeIlwdiCxZjDoeY1idiCOUz21NVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OC5zM{O0JO69VQ>? NVfrcoVbW0GQR1XS
human NBsusSR cell NVjG[mhMT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NX;PN|c4UW6qaXLpeIlwdiCxZjDoeY1idiCQQoP1d3NTKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzBwNU[3PEDPxE1? MmeyV2FPT0WU
human BV-173 cell M3:3ZWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXPhUHBYUW6qaXLpeIlwdiCxZjDoeY1idiCEVj2xO|Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OC55NkS5JO69VQ>? MY\TRW5ITVJ?
human A101D cell M3HqS2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvRNJJKdmirYnn0bY9vKG:oIHj1cYFvKEFzMEHEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AvQTd6NDFOwG0> NFrYeFNUSU6JRWK=
human LU-134-A cell MnzIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIn3ZXFKdmirYnn0bY9vKG:oIHj1cYFvKEyXLUGzOE1CKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzFwMEKzPEDPxE1? M1XSc3NCVkeHUh?=
human ES3 cell NVv5RWZpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1T1XmlvcGmkaYTpc44hd2ZiaIXtZY4hTVN|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{GuN|M4PiEQvF2= MX7TRW5ITVJ?
human NY cell NGrvPXlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYjGUZUzUW6qaXLpeIlwdiCxZjDoeY1idiCQWTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOyMlI6PjVizszN NGq2RpBUSU6JRWK=
human NCI-H1975 cell M{nuTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVHJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUm3OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMzNjN3OEKg{txO MkXIV2FPT0WU
human A704 cell MlPIS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVu1bGdlUW6qaXLpeIlwdiCxZjDoeY1idiCDN{C0JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QvOjB3OTFOwG0> NWXscm8{W0GQR1XS
human SK-MEL-24 cell Ml;1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3vjR2lvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVI1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzRwMkWyN{DPxE1? MYXTRW5ITVJ?
human SW1088 cell M4i1NGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXe1ZYg3UW6qaXLpeIlwdiCxZjDoeY1idiCVV{GwPFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PC5|NEWyJO69VQ>? MoHVV2FPT0WU
human HepG2 cells NFHlPGlHfW6ldHnvckBie3OjeR?= M1u2UVM1KM7:TR?= NVv3TW9pOTJiaB?= Mn:xTY5pcWKrdHnvckBw\iCJU1uzZoV1[SCrbjDoeY1idiCKZYDHNkBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiC{YYTpc{Bw\iCyaH;zdIhwenmuYYTl[EBIWy:JUzDheEA{PCC3TTDh[pRmeiBzMjDodpMh[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nz NFPFRnEzPTR4N{G1NC=>
mouse 3T3L1 cells Mn\TSpVv[3Srb36gZZN{[Xl? M3j2OFM1KM7:TR?= MXKxNkBp NYKweHYyUW6lcnXhd4UhcW5iZ3z1Z49{\SCrbnPvdpBwemG2aX;uJIlvKG2xdYPlJFNVO0xzIHPlcIx{KGG2IEO0JJVOKGGodHXyJFEzKGi{czDifUBodHWlb4PlJIF{e2G7 M3HNRVI2PDZ5MUWw
human ST14A cells NYrNe2d{TnWwY4Tpc44h[XO|YYm= NWXMXm5qPiCq NYjHWIJuUW6qaXLpeIlwdiCxZjDHV2suOy2kZYThMY1m\GmjdHXkJHdvfCC|aXfuZYxqdmdiaX6gbJVu[W5iU2SxOGEh[2WubIOgZZN{\XO|ZXSgZZMhcW6lcnXhd4UhcW5iYXPjeY12dGG2aX;uJI9nKGKndHGtZ4F{\WmwIHHyc5Vv\CCwdXPs[ZV{KGGodHXyJFYhcHK|IHL5JI1q[3Kxc3PvdIlkKGGwYXz5d4l{ M3rwOVIxPzB6OUO3
human ReNcell VM cells NVvoeZlTWHKxbHnm[ZJifGmxbjDhd5NigQ>? NF\sNXk{KM7:TR?= MnrlO|IhcA>? MWXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFKnTnPlcIwhXk1iY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJINmdGxicILvcIln\XKjdHnvckBifCB|IIXNJIFnfGW{IEeyJIhzew>? Mn;ZNlA4ODh7M{e=
human SK-MEL-1 cell MofrS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M{nWNmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTygTWM2OD1|ND63NVQh|ryP MX;TRW5ITVJ?
human MOLT-4 cell MkiwS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mn61TY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOk4yPDZ5IN88US=> Mo[xV2FPT0WU
human T47D cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUHJcohq[mm2aX;uJI9nKGi3bXHuJHQ1P0RiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Nz6xOlQ4KM7:TR?= MU\TRW5ITVJ?
human SW1710 cell NHv0WIpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{f5cmlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzN{GwJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|cvOzZyODFOwG0> MkGzV2FPT0WU
human MKN7 cell NV7id5d6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M17CdWlvcGmkaYTpc44hd2ZiaIXtZY4hVUuQNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlA6ODlizszN NHPQfHRUSU6JRWK=
human CAL-72 cell NXS0cm0{T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVTJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC15MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlEyPzhizszN NIjwZldUSU6JRWK=
human AGS cell M1XkR2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYGwSJdXUW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPE4zODN7IN88US=> M3HMTnNCVkeHUh?=
human BE-13 cell MojPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NG[3VGxKdmirYnn0bY9vKG:oIHj1cYFvKEKHLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|gvPzd6MzFOwG0> NF\6VY1USU6JRWK=
human Calu-6 cell NFTjbIRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NV;hNol2UW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{QS54OU[0JO69VQ>? MmXIV2FPT0WU
human CAL-27 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MUjJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS0MlAxPTRizszN NY\WO3BoW0GQR1XS
human BB49-HNC cell Ml3FS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXvJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFQvODJ5ODFOwG0> NI\y[m1USU6JRWK=

... 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)
  • Formulation: Dissolved in DMSO, and diluted in saline
  • 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 C[N]1C=C(C2=C1C=CC=C2)C3=C(C(=O)NC3=O)C4=CC=C(Cl)C=C4Cl

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).

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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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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

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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

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID