SB216763

Catalog No.S1075

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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In DMSO USD 165 In stock
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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 MlTESpVv[3Srb36gZZN{[Xl? NUL6[XRJT2y7Y3;n[Y4he3mwdHjhd4Uh[WO2aY\peJkhd2ZiSFXLNlk{KGOnbHzzMEBqdmirYnn0bY9vKG:oIFfTT|Mu[mW2YTygSWM2OD1yLkKg{txO MlLqNVI6PDF|M{G=
human HDLM-2 cell NFT6V3FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnLTTY5pcWKrdHnvckBw\iCqdX3hckBJTEyPLUKgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2wMlIxQTh2IN88US=> Mke1V2FPT0WU
human NCI-H1770 cell NYjuRW5MT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWXqT3FLUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE4PzBiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeT6gTWM2OD1yLkK5N|kzKM7:TR?= NYnKR5lIW0GQR1XS
human HOP-62 cell NHTseZdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXntSXRKUW6qaXLpeIlwdiCxZjDoeY1idiCKT2CtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjh3MkW2JO69VQ>? NIKycVlUSU6JRWK=
human JAR cell MnPLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mnq0TY5pcWKrdHnvckBw\iCqdX3hckBLSVJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkKxNFQ1KM7:TR?= NEPPfmVUSU6JRWK=
human K5 cell NX;p[FZoT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{XoOWlvcGmkaYTpc44hd2ZiaIXtZY4hUzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUwhUUN3ME2xMlU{Pjl6IN88US=> M{ezUnNCVkeHUh?=
human MV-4-11 cell NXPIO3I6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2S3WmlvcGmkaYTpc44hd2ZiaIXtZY4hVVZvND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIvPjl4OEWg{txO NXO4Z3d2W0GQR1XS
human BT-549 cell NWXUcnNjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFjiN2NKdmirYnn0bY9vKG:oIHj1cYFvKEKWLUW0PUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVUvOjl|N{[g{txO M1jneXNCVkeHUh?=
human LB2241-RCC cell M3Xze2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MknjTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi52Mki3OEDPxE1? NU\BVoo1W0GQR1XS
human GAMG cell M4f6WGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnfBTY5pcWKrdHnvckBw\iCqdX3hckBISU2JIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Nj62OVQxQSEQvF2= NYfOWoRJW0GQR1XS
human HMV-II cell MlTDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYfv[VNOUW6qaXLpeIlwdiCxZjDoeY1idiCKTW[tTWkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjZ5NkC3JO69VQ>? NXTk[VR1W0GQR1XS
human RS4-11 cell M{TpcGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MkTvTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlI1OTRzIN88US=> MkjrV2FPT0WU
human NCI-H1993 cell NES4R|JIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mlu5TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG5PVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF05NjN4NUO0JO69VQ>? MWDTRW5ITVJ?
human IST-SL1 cell NFTZSFdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYnJcohq[mm2aX;uJI9nKGi3bXHuJGlUXC2VTEGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlAzODRizszN NH\pS3hUSU6JRWK=
human SK-OV-3 cell NULnb|ZOT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYLJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlExODJizszN NHjvcm5USU6JRWK=
human ESS-1 cell NGLsU5BIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1nXOmlvcGmkaYTpc44hd2ZiaIXtZY4hTVOVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlU6QDd{IN88US=> MnK5V2FPT0WU
human G-361 cell MWTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGrjTHNKdmirYnn0bY9vKG:oIHj1cYFvKEdvM{[xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvOTd7ODFOwG0> M1:zb3NCVkeHUh?=
human ALL-PO cell NIruUG5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NH;XXIdKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjN2N{eg{txO NIG0R3JUSU6JRWK=
human NB5 cell MWfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NGnWd3lKdmirYnn0bY9vKG:oIHj1cYFvKE6ENTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlIyPTdizszN M3XwSXNCVkeHUh?=
human DU-145 cell NWHVRoNwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkXzTY5pcWKrdHnvckBw\iCqdX3hckBFXS1zNEWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU43PTN3IN88US=> NHnUTo9USU6JRWK=
human NMC-G1 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXPJcohq[mm2aX;uJI9nKGi3bXHuJG5OSy2JMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGxMlczPjRizszN M2G2NXNCVkeHUh?=
human RPMI-7951 cell M3PFb2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NX[2Uo9HUW6qaXLpeIlwdiCxZjDoeY1idiCUUF3JMVc6PTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeT6gTWM2OD1zMT63PFY1KM7:TR?= M2rvS3NCVkeHUh?=
human NCI-H2009 cell M3LDO2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mn7DTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEKwNFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOy5{NEK3JO69VQ>? M2jFUXNCVkeHUh?=
human LoVo cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M1TueGlvcGmkaYTpc44hd2ZiaIXtZY4hVG:YbzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGzMlM4PzFizszN Mn;IV2FPT0WU
human A2058 cell MkDNS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2m3XmlvcGmkaYTpc44hd2ZiaIXtZY4hSTJyNUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{41PjlizszN M2HJRXNCVkeHUh?=
human D-566MG cell NGW3WINIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NX\CbpJ6UW6qaXLpeIlwdiCxZjDoeY1idiCGLUW2Om1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwOUS4NUDPxE1? MoTOV2FPT0WU
human QIMR-WIL cell MkLVS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4rxUGlvcGmkaYTpc44hd2ZiaIXtZY4hWUmPUj3XTWwh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPS54M{m0JO69VQ>? M3PPenNCVkeHUh?=
human S-117 cell MUjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NEDUOWpKdmirYnn0bY9vKG:oIHj1cYFvKFNvMUG3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvPDB{MjFOwG0> NX3QNYdvW0GQR1XS
human YH-13 cell NUmyU4ZjT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NF[0WJhKdmirYnn0bY9vKG:oIHj1cYFvKFmKLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvPjh4NTFOwG0> Mo\yV2FPT0WU
human IGROV-1 cell NGnPO4ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{\HOWlvcGmkaYTpc44hd2ZiaIXtZY4hUUeUT2[tNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVE4NjJyMEGg{txO NFzCWZBUSU6JRWK=
human BHT-101 cell M4[wOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHnxe5RKdmirYnn0bY9vKG:oIHj1cYFvKEKKVD2xNFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPy54MEm5JO69VQ>? MkTIV2FPT0WU
human MKN45 cell M33iemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXLJcohq[mm2aX;uJI9nKGi3bXHuJG1MVjR3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUiuOFEzQCEQvF2= NYjmSXFZW0GQR1XS
human A498 cell NHLJbnVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmHoTY5pcWKrdHnvckBw\iCqdX3hckBCPDl6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUmuOFU1QSEQvF2= MluzV2FPT0WU
human U-266 cell NGXoS|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MorMTY5pcWKrdHnvckBw\iCqdX3hckBWNTJ4NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKwMlg4QTdizszN NWraR|h{W0GQR1XS
human BFTC-905 cell NV\BUXI6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHvte|hKdmirYnn0bY9vKG:oIHj1cYFvKEKIVFOtPVA2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwMUi3PUDPxE1? Mk\HV2FPT0WU
human BxPC-3 cell NVr6[YNtT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlvpTY5pcWKrdHnvckBw\iCqdX3hckBDgFCFLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNU4{PTV2IN88US=> NI\XcXNUSU6JRWK=
human NCI-SNU-1 cell MXTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NVnpZlBDUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtV25WNTFiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{MT61OVU5KM7:TR?= NESzTppUSU6JRWK=
human SF539 cell NV3VRmlxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{S3V2lvcGmkaYTpc44hd2ZiaIXtZY4hW0Z3M{mgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNk4xOTl6IN88US=> NFvhR21USU6JRWK=
human VA-ES-BJ cell M4\O[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{nUZWlvcGmkaYTpc44hd2ZiaIXtZY4hXkFvRWOtRmoh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOi53N{[zJO69VQ>? NGHGU5BUSU6JRWK=
human HuO-3N1 cell NXrtd5FXT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEe5V4pKdmirYnn0bY9vKG:oIHj1cYFvKEi3Tz2zUlEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOi54MUWxJO69VQ>? MX;TRW5ITVJ?
human EM-2 cell M4C1Vmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXHEN5o3UW6qaXLpeIlwdiCxZjDoeY1idiCHTT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvPjZ6OTFOwG0> M2XPTHNCVkeHUh?=
human T98G cell Mkn2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MX3Jcohq[mm2aX;uJI9nKGi3bXHuJHQ6QEdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Mz6zNFA6KM7:TR?= NVjWfYdUW0GQR1XS
human SW1783 cell M2XYTmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXTKRlQ{UW6qaXLpeIlwdiCxZjDoeY1idiCVV{G3PFMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOy53MkSzJO69VQ>? MkK4V2FPT0WU
human NKM-1 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3fXV2lvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yN{45PTF{IN88US=> NHvJPIdUSU6JRWK=
human KOSC-2 cell MX\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MYHJcohq[mm2aX;uJI9nKGi3bXHuJGtQW0NvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlEzQTJizszN NGHMVINUSU6JRWK=
human SW48 cell NEPaZVlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NYraTnNIUW6qaXLpeIlwdiCxZjDoeY1idiCVV{S4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPjB4NzFOwG0> NXjDZlRYW0GQR1XS
human MIAPaCa2 cells NGq2RVVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoXGO|IhcA>? NVj6W3FbT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUmDUHHDZVIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD1{NTFOwG0> NYLBR2NqOTl|M{izOVU>
human NCI-H28 cell NVr1WYQ2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnfjTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlUvOjFyNDFOwG0> NF70bGdUSU6JRWK=
human 5637 cell MmLPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoXuTY5pcWKrdHnvckBw\iCqdX3hckA2PjN5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkWuPFEyOSEQvF2= NYTSeIZkW0GQR1XS
human NB69 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUXrZYJxUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlYvOTd4NDFOwG0> NVLoUHJxW0GQR1XS
human HT-29 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NI[wfFNKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvOTd3MjFOwG0> M{S4WXNCVkeHUh?=
human PFSK-1 cell MV3Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mo\4TY5pcWKrdHnvckBw\iCqdX3hckBRTlONLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yO{42QTNizszN M{PU[XNCVkeHUh?=
human UACC-257 cell NX\ac4RsT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NUG3e2R2UW6qaXLpeIlwdiCxZjDoeY1idiCXQVPDMVI2PyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ5Lke0N{DPxE1? NYPpPJJtW0GQR1XS
human D-423MG cell NHTycGVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlizTY5pcWKrdHnvckBw\iCqdX3hckBFNTR{M13HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvQTFyNjFOwG0> NXTNUpRnW0GQR1XS
human NH-12 cell NHTiRopIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MojmTY5pcWKrdHnvckBw\iCqdX3hckBPUC1zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlQxPTlizszN Mm[2V2FPT0WU
human DEL cell MnqyS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVHJcohq[mm2aX;uJI9nKGi3bXHuJGRGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ7LkC0O|Qh|ryP M3;mR3NCVkeHUh?=
human LS-513 cell MlPkS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVW4PJRwUW6qaXLpeIlwdiCxZjDoeY1idiCOUz21NVMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OC5zM{O0JO69VQ>? M3zXV3NCVkeHUh?=
human NBsusSR cell NUXGTY46T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3L0SmlvcGmkaYTpc44hd2ZiaIXtZY4hVkK|dYPTVkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjV4N{ig{txO M33GenNCVkeHUh?=
human BV-173 cell MmXsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGJXNTF5MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOwMlc3PDlizszN NHLoVllUSU6JRWK=
human A101D cell M{Hucmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV7Jcohq[mm2aX;uJI9nKGi3bXHuJGEyODGGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{CuPVc5PCEQvF2= NEfyPG5USU6JRWK=
human LU-134-A cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXy0SlA3UW6qaXLpeIlwdiCxZjDoeY1idiCOVT2xN|QuSSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNzLkCyN|gh|ryP M4HubXNCVkeHUh?=
human ES3 cell Mne1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NW\pV4RSUW6qaXLpeIlwdiCxZjDoeY1idiCHU{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNU4{Ozd4IN88US=> NG\3PHJUSU6JRWK=
human NY cell MlzSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NWfpPIpWUW6qaXLpeIlwdiCxZjDoeY1idiCQWTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOyMlI6PjVizszN MoftV2FPT0WU
human NCI-H1975 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{XlWmlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLVixPVc2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzJwM{W4NkDPxE1? M4DzTnNCVkeHUh?=
human A704 cell NYfHfI0yT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1;icGlvcGmkaYTpc44hd2ZiaIXtZY4hSTdyNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO0MlIxPTlizszN NWDYcmltW0GQR1XS
human SK-MEL-24 cell NIXQNo5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWXDXY1OUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ND6yOVI{KM7:TR?= MX;TRW5ITVJ?
human SW1088 cell MWXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYnOPJB6UW6qaXLpeIlwdiCxZjDoeY1idiCVV{GwPFgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{PC5|NEWyJO69VQ>? MWHTRW5ITVJ?
human HepG2 cells MWLGeY5kfGmxbjDhd5NigQ>? NF3ZdYs{PCEQvF2= MXixNkBp NXHZOmtvUW6qaXLpeIlwdiCxZjDHV2s{[mW2YTDpckBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDyZZRqdyCxZjDwbI9{eGixconsZZRm\CCJUz;HV{BifCB|NDD1UUBi\nSncjCxNkBpenNiYomgW4V{fGW{bjDicI91KGGwYXz5d4l{ M{L4WFI2PDZ5MUWw
mouse 3T3L1 cells M{S3NWZ2dmO2aX;uJIF{e2G7 NYX2PZFqOzRizszN NIOy[XoyOiCq MVzJcoNz\WG|ZTDpckBodHWlb4PlJIlv[2:{cH;yZZRqd25iaX6gcY92e2ViM2SzUFEh[2WubIOgZZQhOzRidV2gZYZ1\XJiMUKgbJJ{KGK7IHfseYNwe2ViYYPzZZk> MmDUNlU1PjdzNUC=
human ST14A cells MlLJSpVv[3Srb36gZZN{[Xl? NV;HdnRXPiCq M332VGlvcGmkaYTpc44hd2ZiR2PLMVMu[mW2YT3t[YRq[XSnZDDXcpQhe2mpbnHsbY5oKGmwIHj1cYFvKFOWMUTBJINmdGy|IHHzd4V{e2WmIHHzJIlv[3KnYYPlJIlvKGGlY4XteYxifGmxbjDv[kBj\XSjLXPhd4VqdiCjcn;1coQhdnWlbHX1d{Bi\nSncjC2JIhzeyCkeTDtbYNzd3Olb4DpZ{BidmGueYPpdy=> MknWNlA4ODh7M{e=
human ReNcell VM cells MW\Qdo9tcW[ncnH0bY9vKGG|c3H5 MmrRN{DPxE1? MVe3NkBp NYDSW|J{SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDS[W5k\WyuIG\NJINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBw\iClZXzsJJBzd2yrZnXyZZRqd25iYYSgN{B2VSCjZoTldkA4OiCqcoO= M2PxO|IxPzB6OUO3
human SK-MEL-1 cell MlvHS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUjJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU2HTD2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHluIFnDOVA:OzRwN{G0JO69VQ>? M4L3WHNCVkeHUh?=
human MOLT-4 cell M{HrZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4LHUWlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|YvOTR4NzFOwG0> MWXTRW5ITVJ?
human T47D cell MWrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MmXCTY5pcWKrdHnvckBw\iCqdX3hckBVPDeGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{euNVY1PyEQvF2= NIf5UoFUSU6JRWK=
human SW1710 cell M1z5WGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NE\yeIRKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM4NjN4MEig{txO NH;4RYxUSU6JRWK=
human MKN7 cell NGDMbIxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{DwNWlvcGmkaYTpc44hd2ZiaIXtZY4hVUuQNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlA6ODlizszN NIXDVmZUSU6JRWK=
human CAL-72 cell M1;HdWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWHJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC15MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlEyPzhizszN NFW5WYdUSU6JRWK=
human AGS cell MmHsS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NIj3Z4ZKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlIxOzlizszN NHX4bZRUSU6JRWK=
human BE-13 cell NH\3fItIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXfiW486UW6qaXLpeIlwdiCxZjDoeY1idiCERT2xN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM5Njd5OEOg{txO NF\VSZVUSU6JRWK=
human Calu-6 cell NWDaVY9FT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MofYTY5pcWKrdHnvckBw\iCqdX3hckBE[Wy3LU[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPU43QTZ2IN88US=> MUTTRW5ITVJ?
human CAL-27 cell NWXnfVJkT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3[0WmlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUK3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFQvODB3NDFOwG0> MYDTRW5ITVJ?
human BB49-HNC cell NYTkZVVKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3:1ZWlvcGmkaYTpc44hd2ZiaIXtZY4hSkJ2OT3IUmMh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF01PC5yMke4JO69VQ>? Mn\OV2FPT0WU

... 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

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).

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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

If you have any other enquiries, please leave a message.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID