SB216763

For research use only.

Catalog No.S1075

41 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. SB216763 activates autophagy.

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Selleck's SB216763 has been cited by 41 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 NYHPNG9mTnWwY4Tpc44h[XO|YYm= M2rCZ2dtgWOxZ3XuJJN6dnSqYYPlJIFkfGm4aYT5JI9nKEiHS{K5N{Bk\WyuczygbY5pcWKrdHnvckBw\iCJU1uzMYJmfGFuIFXDOVA:OC5{IN88US=> MXWxNlk1OTN|MR?=
human HDLM-2 cell M4\n[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF\1dJlKdmirYnn0bY9vKG:oIHj1cYFvKEiGTF2tNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjB7OESg{txO MVLTRW5ITVJ?
human NCI-H1770 cell NVPScGpQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYfJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUe3NEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NiCLQ{WwQVAvOjl|OUKg{txO NV3IclhGW0GQR1XS
human HOP-62 cell NFTkZ4ZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXi4fVRjUW6qaXLpeIlwdiCxZjDoeY1idiCKT2CtOlIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0xNjh3MkW2JO69VQ>? M2L2bXNCVkeHUh?=
human JAR cell NVzlb2RxT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnX1TY5pcWKrdHnvckBw\iCqdX3hckBLSVJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkKxNFQ1KM7:TR?= NUj0e217W0GQR1XS
human K5 cell NWfP[pF4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUDJcohq[mm2aX;uJI9nKGi3bXHuJGs2KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImsJGlEPTB;MT61N|Y6QCEQvF2= M2f0ZXNCVkeHUh?=
human MV-4-11 cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUfNO2RXUW6qaXLpeIlwdiCxZjDoeY1idiCPVj20MVEyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Oi54OU[4OUDPxE1? MVHTRW5ITVJ?
human BT-549 cell M1rDNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2TuSmlvcGmkaYTpc44hd2ZiaIXtZY4hSlRvNUS5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OU4zQTN5NjFOwG0> MmL2V2FPT0WU
human LB2241-RCC cell NYDMVoFwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkjwTY5pcWKrdHnvckBw\iCqdX3hckBNSjJ{NEGtVmNEKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:Pi52Mki3OEDPxE1? M2nZPHNCVkeHUh?=
human GAMG cell NVrvUHhyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVrhTYFpUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok43PTRyOTFOwG0> NYW2N|NTW0GQR1XS
human HMV-II cell MYfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXKwV5BbUW6qaXLpeIlwdiCxZjDoeY1idiCKTW[tTWkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjZ5NkC3JO69VQ>? MlnhV2FPT0WU
human RS4-11 cell MXPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mn\pTY5pcWKrdHnvckBw\iCqdX3hckBTWzRvMUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME24MlI1OTRzIN88US=> MkDYV2FPT0WU
human NCI-H1993 cell M{HvSWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUPp[oNrUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE6QTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD16LkO2OVM1KM7:TR?= MXLTRW5ITVJ?
human IST-SL1 cell M2TnNGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIjHVYRKdmirYnn0bY9vKG:oIHj1cYFvKEmVVD3TUFEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF06NjB{MESg{txO MnrzV2FPT0WU
human SK-OV-3 cell MUHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MlziTY5pcWKrdHnvckBw\iCqdX3hckBUUy2RVj2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU4yODB{IN88US=> M13CNXNCVkeHUh?=
human ESS-1 cell NYW4PIVmT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{nOeWlvcGmkaYTpc44hd2ZiaIXtZY4hTVOVLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlU6QDd{IN88US=> NIPW[2lUSU6JRWK=
human G-361 cell NFHkcXFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGexU2RKdmirYnn0bY9vKG:oIHj1cYFvKEdvM{[xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVAvOTd7ODFOwG0> NY[0VnRDW0GQR1XS
human ALL-PO cell M2TNdGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH23fYZKdmirYnn0bY9vKG:oIHj1cYFvKEGOTD3QU{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjN2N{eg{txO NGXh[W1USU6JRWK=
human NB5 cell NWfLeYR1T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4fJc2lvcGmkaYTpc44hd2ZiaIXtZY4hVkJ3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUGuNlE2PyEQvF2= NWLTNGpYW0GQR1XS
human DU-145 cell NIm2fXZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{fBWGlvcGmkaYTpc44hd2ZiaIXtZY4hTFVvMUS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVEvPjV|NTFOwG0> NWrxS3FnW0GQR1XS
human NMC-G1 cell MnW5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmnDTY5pcWKrdHnvckBw\iCqdX3hckBPVUNvR{GgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU44OjZ2IN88US=> Mm\MV2FPT0WU
human RPMI-7951 cell MoKzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlrCTY5pcWKrdHnvckBw\iCqdX3hckBTWE2LLUe5OVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0yOS55OE[0JO69VQ>? NEXyUpdUSU6JRWK=
human NCI-H2009 cell NIW2OFFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4fWVGlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwMkSyO{DPxE1? MVzTRW5ITVJ?
human LoVo cell MU\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NFy1[XpKdmirYnn0bY9vKG:oIHj1cYFvKEyxVn:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{4{PzdzIN88US=> MmHhV2FPT0WU
human A2058 cell M{HTZmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{j1cWlvcGmkaYTpc44hd2ZiaIXtZY4hSTJyNUigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{41PjlizszN MVfTRW5ITVJ?
human D-566MG cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXLWeoZbUW6qaXLpeIlwdiCxZjDoeY1idiCGLUW2Om1IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwOUS4NUDPxE1? M4\5d3NCVkeHUh?=
human QIMR-WIL cell NUXZU3dVT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NH7TWHdKdmirYnn0bY9vKG:oIHj1cYFvKFGLTWKtW2lNKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTVwNkO5OEDPxE1? MUPTRW5ITVJ?
human S-117 cell NIHp[pNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1zMRWlvcGmkaYTpc44hd2ZiaIXtZY4hWy1zMUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk41ODJ{IN88US=> NGCwTpNUSU6JRWK=
human YH-13 cell MoH4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH72fo1KdmirYnn0bY9vKG:oIHj1cYFvKFmKLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvPjh4NTFOwG0> MXPTRW5ITVJ?
human IGROV-1 cell MkLDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHzSXFRKdmirYnn0bY9vKG:oIHj1cYFvKEmJUl;WMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yPy5{MECxJO69VQ>? M1rXcHNCVkeHUh?=
human BHT-101 cell MVLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWTTeY5zUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTdwNkC5PUDPxE1? MYDTRW5ITVJ?
human MKN45 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXvJcohq[mm2aX;uJI9nKGi3bXHuJG1MVjR3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUiuOFEzQCEQvF2= MmK1V2FPT0WU
human A498 cell MlHSS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M1zhTmlvcGmkaYTpc44hd2ZiaIXtZY4hSTR7ODDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG5MlQ2PDlizszN MXHTRW5ITVJ?
human U-266 cell NU\tbIVQT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1\mZWlvcGmkaYTpc44hd2ZiaIXtZY4hXS1{Nk[gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNE45Pzl5IN88US=> MWHTRW5ITVJ?
human BFTC-905 cell MWjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MojLTY5pcWKrdHnvckBw\iCqdX3hckBDTlSFLUmwOUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjF6N{mg{txO MV3TRW5ITVJ?
human BxPC-3 cell NXXYXYxpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M4fRXGlvcGmkaYTpc44hd2ZiaIXtZY4hSniSQz2zJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlEvOzV3NDFOwG0> MWfTRW5ITVJ?
human NCI-SNU-1 cell NEDuXI9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MmjUTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvU17VMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS53NUW4JO69VQ>? MWfTRW5ITVJ?
human SF539 cell MUTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Mlr3TY5pcWKrdHnvckBw\iCqdX3hckBUTjV|OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKyMlAyQThizszN NF;v[olUSU6JRWK=
human VA-ES-BJ cell M3zKfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUTOc3ZMUW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ{LkW3OlMh|ryP M1X4TnNCVkeHUh?=
human HuO-3N1 cell MWnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3nIdWlvcGmkaYTpc44hd2ZiaIXtZY4hUHWRLUPONUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIzNjZzNUGg{txO MV\TRW5ITVJ?
human EM-2 cell NVnDPJhbT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Mn\LTY5pcWKrdHnvckBw\iCqdX3hckBGVS1{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkKuOlY5QSEQvF2= NYq4OpkyW0GQR1XS
human T98G cell NGfySm5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MkjTTY5pcWKrdHnvckBw\iCqdX3hckBVQTiJIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkOuN|AxQSEQvF2= MYrTRW5ITVJ?
human SW1783 cell NFH5RVNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mo\hTY5pcWKrdHnvckBw\iCqdX3hckBUXzF5OEOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yN{42OjR|IN88US=> NX62S4tsW0GQR1XS
human NKM-1 cell NWnyeIxET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUPJcohq[mm2aX;uJI9nKGi3bXHuJG5MVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkOuPFUyOiEQvF2= NYXBZ4lYW0GQR1XS
human KOSC-2 cell M4LKOWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHuyenZKdmirYnn0bY9vKG:oIHj1cYFvKEuRU1OtNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI1NjF{OUKg{txO MkL3V2FPT0WU
human SW48 cell M3rZV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFvaUldKdmirYnn0bY9vKG:oIHj1cYFvKFOZNEigZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOE43ODZ5IN88US=> MVrTRW5ITVJ?
human MIAPaCa2 cells MmTtS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MlXsO|IhcA>? NVHrdmRIT3Kxd4ToJIlvcGmkaYTpc44hd2ZiaIXtZY4hVUmDUHHDZVIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UV{Bie3OjeTygTWM2OD1{NTFOwG0> M2i2OFE6OzN6M{W1
human NCI-H28 cell M4K1emdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH;FXHFKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPS5{MUC0JO69VQ>? NXv1U4dNW0GQR1XS
human 5637 cell NFfjNo5Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnHpTY5pcWKrdHnvckBw\iCqdX3hckA2PjN5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkWuPFEyOSEQvF2= MWDTRW5ITVJ?
human NB69 cell MYLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXjRRndYUW6qaXLpeIlwdiCxZjDoeY1idiCQQk[5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlYvOTd4NDFOwG0> Mn7OV2FPT0WU
human HT-29 cell NIP0dVRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NWnoeWw6UW6qaXLpeIlwdiCxZjDoeY1idiCKVD2yPUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4NjF5NUKg{txO NUPifVh1W0GQR1XS
human PFSK-1 cell NEnndGRIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWjJcohq[mm2aX;uJI9nKGi3bXHuJHBHW0tvMTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK3MlU6OyEQvF2= NIjWS3NUSU6JRWK=
human UACC-257 cell NU\0UZRCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1LFS2lvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPy55NEOg{txO MkTvV2FPT0WU
human D-423MG cell M4GyNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4rNfmlvcGmkaYTpc44hd2ZiaIXtZY4hTC12MkPNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4NjlzME[g{txO Mnn6V2FPT0WU
human NH-12 cell NW[2[YtDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFTmS25KdmirYnn0bY9vKG:oIHj1cYFvKE6KLUGyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlgvPDB3OTFOwG0> M1m0cXNCVkeHUh?=
human DEL cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4DobGlvcGmkaYTpc44hd2ZiaIXtZY4hTEWOIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkmuNFQ4PCEQvF2= MVPTRW5ITVJ?
human LS-513 cell M3PKZ2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHrBd4JKdmirYnn0bY9vKG:oIHj1cYFvKEyVLUWxN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjF|M{Sg{txO NVPOWJd2W0GQR1XS
human NBsusSR cell M3zNVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3zrZmlvcGmkaYTpc44hd2ZiaIXtZY4hVkK|dYPTVkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjV4N{ig{txO NHzXc3FUSU6JRWK=
human BV-173 cell NUjIUZFKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2TUd2lvcGmkaYTpc44hd2ZiaIXtZY4hSlZvMUezJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AvPzZ2OTFOwG0> MWrTRW5ITVJ?
human A101D cell NHPrUlhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFr2N4lKdmirYnn0bY9vKG:oIHj1cYFvKEFzMEHEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AvQTd6NDFOwG0> MVTTRW5ITVJ?
human LU-134-A cell NIfocWtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnLkTY5pcWKrdHnvckBw\iCqdX3hckBNXS1zM{StRUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMyNjB{M{ig{txO MY\TRW5ITVJ?
human ES3 cell MnfoS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGVUOyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTNzLkOzO|Yh|ryP NUKxR5ZPW0GQR1XS
human NY cell MVTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NYm3R2QzUW6qaXLpeIlwdiCxZjDoeY1idiCQWTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUOyMlI6PjVizszN MVrTRW5ITVJ?
human NCI-H1975 cell MmfxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGrVd45KdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVk4PSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN{LkO1PFIh|ryP MYDTRW5ITVJ?
human A704 cell M13jRmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV3Jcohq[mm2aX;uJI9nKGi3bXHuJGE4ODRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ND6yNFU6KM7:TR?= MkXzV2FPT0WU
human SK-MEL-24 cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NXvWenRxUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOjRiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|ND6yOVI{KM7:TR?= NWn5OnRkW0GQR1XS
human SW1088 cell MojES5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHLudnBKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUC4PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1NjN2NUKg{txO MlS4V2FPT0WU
human HepG2 cells NV3nV2xLTnWwY4Tpc44h[XO|YYm= MWmzOEDPxE1? MV2xNkBp M3K2RWlvcGmkaYTpc44hd2ZiR2PLN4JmfGFiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5icnH0bY8hd2ZicHjvd5Bpd3K7bHH0[YQhT1NxR2OgZZQhOzRidV2gZYZ1\XJiMUKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NWD0SVZuOjV2NkexOVA>
mouse 3T3L1 cells NY\yUnZSTnWwY4Tpc44h[XO|YYm= MkL5N|Qh|ryP NXvQfIZCOTJiaB?= NHyzdIpKdmO{ZXHz[UBqdiCpbIXjc5NmKGmwY3;ydI9z[XSrb36gbY4hdW:3c3WgN3Q{VDFiY3XscJMh[XRiM{SgeW0h[W[2ZYKgNVIhcHK|IHL5JIdtfWOxc3WgZZN{[Xl? M2rjTlI2PDZ5MUWw
human ST14A cells MV\GeY5kfGmxbjDhd5NigQ>? NXK4UZN2PiCq MkTNTY5pcWKrdHnvckBw\iCJU1utN{1j\XSjLX3l[IlifGWmIGfueEB{cWewYXzpcochcW5iaIXtZY4hW1RzNFGgZ4VtdHNiYYPz[ZN{\WRiYYOgbY5kemWjc3WgbY4h[WOldX31cIF1cW:wIH;mJIJmfGFvY3Hz[YlvKGG{b4Xu[EBvfWOuZYXzJIFnfGW{IE[gbJJ{KGK7IH3pZ5Jwe2OxcHnjJIFv[Wy7c3nz NYT3OmJGOjB5MEi5N|c>
human ReNcell VM cells Ml75VJJwdGmoZYLheIlwdiCjc4PhfS=> MYWzJO69VQ>? MlG5O|IhcA>? M4fpd2FvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iUnXOZ4VtdCCYTTDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4Yh[2WubDDwdo9tcW[ncnH0bY9vKGG2IEOgeW0h[W[2ZYKgO|IhcHK| NVvjVYNtOjB5MEi5N|c>
human SK-MEL-1 cell MYDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M3vjOmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTygTWM2OD1|ND63NVQh|ryP MWXTRW5ITVJ?
human MOLT-4 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MVfJcohq[mm2aX;uJI9nKGi3bXHuJG1QVFRvNDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO2MlE1PjdizszN MVLTRW5ITVJ?
human T47D cell NVu2T2k2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGrzPVBKdmirYnn0bY9vKG:oIHj1cYFvKFR2N1SgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zO{4yPjR5IN88US=> MkjSV2FPT0WU
human SW1710 cell M{SwUGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MVTJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO3MlM3ODhizszN NHzKbZRUSU6JRWK=
human MKN7 cell MXzHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHHsN5BKdmirYnn0bY9vKG:oIHj1cYFvKE2NTkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPE4xQTB7IN88US=> Mof3V2FPT0WU
human CAL-72 cell M33VPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M{XzOGlvcGmkaYTpc44hd2ZiaIXtZY4hS0GOLUeyJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|gvOTF5ODFOwG0> MXjTRW5ITVJ?
human AGS cell M2rp[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGTaPZJKdmirYnn0bY9vKG:oIHj1cYFvKEGJUzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlIxOzlizszN MkPWV2FPT0WU
human BE-13 cell M2LIXmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MV\Jcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{iuO|c5OyEQvF2= MkLDV2FPT0WU
human Calu-6 cell M2LuPGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3:4R2lvcGmkaYTpc44hd2ZiaIXtZY4hS2GudT22JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|kvPjl4NDFOwG0> NV3DTGlIW0GQR1XS
human CAL-27 cell NVT6NpYzT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NEPEdmhKdmirYnn0bY9vKG:oIHj1cYFvKEODTD2yO{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVQ1NjByNUSg{txO MoTrV2FPT0WU
human BB49-HNC cell MX7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NV\0WpVpUW6qaXLpeIlwdiCxZjDoeY1idiCEQkS5MWhPSyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTR2LkCyO|gh|ryP MV\TRW5ITVJ?

... 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 C[N]1C=C(C2=C1C=CC=C2)C3=C(C(=O)NC3=O)C4=CC=C(Cl)C=C4Cl

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 (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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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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

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