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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USD 270 In stock
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Cited by 24 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 MUDGeY5kfGmxbjDhd5NigQ>? MWLHcJlkd2enbjDzfY51cGG|ZTDhZ5Rqfmm2eTDv[kBJTUt{OUOgZ4VtdHNuIHnubIljcXSrb36gc4YhT1ONMz3i[ZRiNCCHQ{WwQVAvOiEQvF2= M1XNXVEzQTRzM{Ox
human HDLM-2 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NIjuZVNKdmirYnn0bY9vKG:oIHj1cYFvKEiGTF2tNkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvOjB7OESg{txO MlrUV2FPT0WU
human NCI-H1770 cell NYP0UoxpT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MkLlTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG3O|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0xNjJ7M{myJO69VQ>? MVjTRW5ITVJ?
human HOP-62 cell MnfmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF7Wd4VKdmirYnn0bY9vKG:oIHj1cYFvKEiRUD22NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDV{NU[g{txO NUH2cZZqW0GQR1XS
human JAR cell M4XkV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFTZclZKdmirYnn0bY9vKG:oIHj1cYFvKEqDUjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGuNlExPDRizszN Mm\nV2FPT0WU
human K5 cell MnH1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF\1fIpKdmirYnn0bY9vKG:oIHj1cYFvKEt3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJktKEmFNUC9NU42OzZ7ODFOwG0> MXvTRW5ITVJ?
human MV-4-11 cell M3X4Smdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NEGwblFKdmirYnn0bY9vKG:oIHj1cYFvKE2YLUStNVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zNjZ7Nki1JO69VQ>? M1POXnNCVkeHUh?=
human BT-549 cell MljpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NV\qcW5HUW6qaXLpeIlwdiCxZjDoeY1idiCEVD21OFkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF02NjJ7M{e2JO69VQ>? MUDTRW5ITVJ?
human LB2241-RCC cell NEHMPWdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1nRcmlvcGmkaYTpc44hd2ZiaIXtZY4hVEJ{MkSxMXJESyClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTZwNEK4O|Qh|ryP MUfTRW5ITVJ?
human GAMG cell MmXvS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXPibmdqUW6qaXLpeIlwdiCxZjDoeY1idiCJQV3HJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Ok43PTRyOTFOwG0> M2LQV3NCVkeHUh?=
human HMV-II cell MVvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M{TZZ2lvcGmkaYTpc44hd2ZiaIXtZY4hUE2YLVnJJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9O{43PzZyNzFOwG0> NHHoWFdUSU6JRWK=
human RS4-11 cell M1LGXGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1XjNGlvcGmkaYTpc44hd2ZiaIXtZY4hWlN2LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PE4zPDF2MTFOwG0> NGToWGhUSU6JRWK=
human NCI-H1993 cell MnPCS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJG5EUS2KMUm5N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvOzZ3M{Sg{txO NIruWoNUSU6JRWK=
human IST-SL1 cell M2T5S2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1rUbWlvcGmkaYTpc44hd2ZiaIXtZY4hUVOWLWPMNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvODJyNDFOwG0> NFmy[YNUSU6JRWK=
human SK-OV-3 cell NEfyeVNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWnJcohq[mm2aX;uJI9nKGi3bXHuJHNMNU:YLUOgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME25MlExODJizszN NVfmPXlvW0GQR1XS
human ESS-1 cell MXvHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NHy5WXJKdmirYnn0bY9vKG:oIHj1cYFvKEWVUz2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9PU42QTh5MjFOwG0> M{\QZnNCVkeHUh?=
human G-361 cell NFXZOFVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoLvTY5pcWKrdHnvckBw\iCqdX3hckBINTN4MTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUGwMlE4QThizszN NWL2eYw{W0GQR1XS
human ALL-PO cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoPZTY5pcWKrdHnvckBw\iCqdX3hckBCVExvUF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE4{PDd5IN88US=> NYTwZ2FwW0GQR1XS
human NB5 cell NIrtbWtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVLJcohq[mm2aX;uJI9nKGi3bXHuJG5DPSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTFzLkKxOVch|ryP Ml3HV2FPT0WU
human DU-145 cell M1S1dmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnrwTY5pcWKrdHnvckBw\iCqdX3hckBFXS1zNEWgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNU43PTN3IN88US=> MlXTV2FPT0WU
human NMC-G1 cell M4H1cmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYLu[oxHUW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS55Mk[0JO69VQ>? MmTIV2FPT0WU
human RPMI-7951 cell M2W5NGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M3vH[2lvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST23PVUyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XlwIFnDOVA:OTFwN{i2OEDPxE1? NF71U3VUSU6JRWK=
human NCI-H2009 cell NHjI[m9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXX4RndZUW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFIxODliY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6yOFI4KM7:TR?= M1fMenNCVkeHUh?=
human LoVo cell NF3PbnJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKGi3bXHuJGxwXm9iY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zMz6zO|cyKM7:TR?= NGq1UItUSU6JRWK=
human A2058 cell NYDxeXM2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXPJcohq[mm2aX;uJI9nKGi3bXHuJGEzODV6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOFY6KM7:TR?= NGfSNGVUSU6JRWK=
human D-566MG cell NFfpfmVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MWXJcohq[mm2aX;uJI9nKGi3bXHuJGQuPTZ4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{46PDhzIN88US=> Ml60V2FPT0WU
human QIMR-WIL cell M3H1W2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYjlb5JzUW6qaXLpeIlwdiCxZjDoeY1idiCTSV3SMXdKVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTF3Lk[zPVQh|ryP MXjTRW5ITVJ?
human S-117 cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml;oTY5pcWKrdHnvckBw\iCqdX3hckBUNTFzNzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG2MlQxOjJizszN Ml[yV2FPT0WU
human YH-13 cell MoX1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF;Zd5pKdmirYnn0bY9vKG:oIHj1cYFvKFmKLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvPjh4NTFOwG0> M3rpXXNCVkeHUh?=
human IGROV-1 cell MnW4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MYLJcohq[mm2aX;uJI9nKGi3bXHuJGlIWk:YLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xO{4zODBzIN88US=> NWTYdolnW0GQR1XS
human BHT-101 cell NV\3[JFlT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVXFeIhzUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTdwNkC5PUDPxE1? MV\TRW5ITVJ?
human MKN45 cell M3uyXWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGTV[ZJKdmirYnn0bY9vKG:oIHj1cYFvKE2NTkS1JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVgvPDF{ODFOwG0> MXnTRW5ITVJ?
human A498 cell MoLnS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYPod|dMUW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPDV2OTFOwG0> MnH3V2FPT0WU
human U-266 cell M2DCVWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 Mm\VTY5pcWKrdHnvckBw\iCqdX3hckBWNTJ4NjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKwMlg4QTdizszN MXLTRW5ITVJ?
human BFTC-905 cell Mki2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M3S1dGlvcGmkaYTpc44hd2ZiaIXtZY4hSk[WQz25NFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS5zOEe5JO69VQ>? NVLUOHNxW0GQR1XS
human BxPC-3 cell MkTQS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MWjJcohq[mm2aX;uJI9nKGi3bXHuJGJ5WENvMzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKxMlM2PTRizszN MYXTRW5ITVJ?
human NCI-SNU-1 cell MVjHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4XPb2lvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLWPOWU0yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjFwNUW1PEDPxE1? MkTJV2FPT0WU
human SF539 cell NET1TodIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NHLNeoRKdmirYnn0bY9vKG:oIHj1cYFvKFOINUO5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvODF7ODFOwG0> M3TQ[nNCVkeHUh?=
human VA-ES-BJ cell NVP1PGdET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1rZeWlvcGmkaYTpc44hd2ZiaIXtZY4hXkFvRWOtRmoh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOi53N{[zJO69VQ>? M{DaVXNCVkeHUh?=
human HuO-3N1 cell NXTFdYlYT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVvmZ|d4UW6qaXLpeIlwdiCxZjDoeY1idiCKdV:tN24yKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjJwNkG1NUDPxE1? M{THXnNCVkeHUh?=
human EM-2 cell M1LMVGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVL6SGlYUW6qaXLpeIlwdiCxZjDoeY1idiCHTT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvPjZ6OTFOwG0> M4XzOXNCVkeHUh?=
human T98G cell M4nVfGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MlrPTY5pcWKrdHnvckBw\iCqdX3hckBVQTiJIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkOuN|AxQSEQvF2= NUDDSW8yW0GQR1XS
human SW1783 cell NGjORZFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVXJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTd6MzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUKzMlUzPDNizszN NYLoNlFKW0GQR1XS
human NKM-1 cell MY\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MULJcohq[mm2aX;uJI9nKGi3bXHuJG5MVS1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkOuPFUyOiEQvF2= M{XzWXNCVkeHUh?=
human KOSC-2 cell NUXCOo15T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MY\Jcohq[mm2aX;uJI9nKGi3bXHuJGtQW0NvMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK0MlEzQTJizszN Mo[wV2FPT0WU
human SW48 cell NWDDdVRKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NWnVV3dvUW6qaXLpeIlwdiCxZjDoeY1idiCVV{S4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlQvPjB4NzFOwG0> MVjTRW5ITVJ?
human MIAPaCa2 cells Ml;mS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnztO|IhcA>? NFvYZlhIem:5dHigbY5pcWKrdHnvckBw\iCqdX3hckBOUUGSYVPhNkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTTJIF{e2G7LDDJR|UxRTJ3IN88US=> MVqxPVM{QDN3NR?=
human NCI-H28 cell MW\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MnH4TY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEK4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlUvOjFyNDFOwG0> NIfpfmJUSU6JRWK=
human 5637 cell NFfaUZpIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MnvCTY5pcWKrdHnvckBw\iCqdX3hckA2PjN5IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkWuPFEyOSEQvF2= M1\nb3NCVkeHUh?=
human NB69 cell MVfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? Ml\uTY5pcWKrdHnvckBw\iCqdX3hckBPSjZ7IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;Mk[uNVc3PCEQvF2= NXnXc45{W0GQR1XS
human HT-29 cell M1zoeGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NI\LeGxKdmirYnn0bY9vKG:oIHj1cYFvKEiWLUK5JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvOTd3MjFOwG0> MofIV2FPT0WU
human PFSK-1 cell M2PsT2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH[2OodKdmirYnn0bY9vKG:oIHj1cYFvKFCIU1utNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4NjV7MzFOwG0> M3TFXnNCVkeHUh?=
human UACC-257 cell MmqzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXHJcohq[mm2aX;uJI9nKGi3bXHuJHVCS0NvMkW3JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlcvPzR|IN88US=> MUnTRW5ITVJ?
human D-423MG cell NIr4[4FIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M4PN[WlvcGmkaYTpc44hd2ZiaIXtZY4hTC12MkPNS{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4NjlzME[g{txO MYjTRW5ITVJ?
human NH-12 cell NIHmSYhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MXTJcohq[mm2aX;uJI9nKGi3bXHuJG5JNTF{IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkiuOFA2QSEQvF2= M4i3XnNCVkeHUh?=
human DEL cell NVPJd2NTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MYnJcohq[mm2aX;uJI9nKGi3bXHuJGRGVCClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ7LkC0O|Qh|ryP NHX2T25USU6JRWK=
human LS-513 cell M2PL[mdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NHHYXWhKdmirYnn0bY9vKG:oIHj1cYFvKEyVLUWxN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjF|M{Sg{txO MXHTRW5ITVJ?
human NBsusSR cell NWfCe5pET3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MWTJcohq[mm2aX;uJI9nKGi3bXHuJG5De3W|U2KgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNE42Pjd6IN88US=> NX70[3ZPW0GQR1XS
human BV-173 cell NYXFblBDT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NHy5WYtKdmirYnn0bY9vKG:oIHj1cYFvKEKYLUG3N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjd4NEmg{txO NF3HcVNUSU6JRWK=
human A101D cell M2W2NWdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NIHkT5RKdmirYnn0bY9vKG:oIHj1cYFvKEFzMEHEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AvQTd6NDFOwG0> M2Cx[HNCVkeHUh?=
human LU-134-A cell NWfOd4pTT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1rNNmlvcGmkaYTpc44hd2ZiaIXtZY4hVFVvMUO0MWEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OS5yMkO4JO69VQ>? MVLTRW5ITVJ?
human ES3 cell NH;hXW9Iem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mn;zTY5pcWKrdHnvckBw\iCqdX3hckBGWzNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|MT6zN|c3KM7:TR?= MVPTRW5ITVJ?
human NY cell NXfXWpNJT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NFPyNldKdmirYnn0bY9vKG:oIHj1cYFvKE6\IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{KuNlk3PSEQvF2= M3ewPXNCVkeHUh?=
human NCI-H1975 cell Mo[1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NFHL[mxKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INVk4PSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN{LkO1PFIh|ryP NH35RY1USU6JRWK=
human A704 cell NEDmRndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF:4cXBKdmirYnn0bY9vKG:oIHj1cYFvKEF5MESgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOE4zODV7IN88US=> NX3Fe|huW0GQR1XS
human SK-MEL-24 cell NGTucZZIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M1jP[WlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVI1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzRwMkWyN{DPxE1? M3myfXNCVkeHUh?=
human SW1088 cell NULzPYdwT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M135fGlvcGmkaYTpc44hd2ZiaIXtZY4hW1dzMEi4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|QvOzR3MjFOwG0> NVrodGRnW0GQR1XS
human HepG2 cells MofZSpVv[3Srb36gZZN{[Xl? MXKzOEDPxE1? NVvNOnJOOTJiaB?= MYLJcohq[mm2aX;uJI9nKEeVS{Pi[ZRiKGmwIHj1cYFvKEincFeyJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKHKjdHnvJI9nKHCqb4PwbI9zgWyjdHXkJGdUN0eVIHH0JFM1KHWPIHHmeIVzKDF{IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYO= MVqyOVQ3PzF3MB?=
mouse 3T3L1 cells MofLSpVv[3Srb36gZZN{[Xl? M2XWTVM1KM7:TR?= NH\N[3AyOiCq M176V2lv[3KnYYPlJIlvKGeudXPvd4UhcW6lb4Lwc5JifGmxbjDpckBud3W|ZTCzWFNNOSClZXzsd{BifCB|NDD1UUBi\nSncjCxNkBpenNiYomg[4x2[2:|ZTDhd5NigQ>? MWCyOVQ3PzF3MB?=
human ST14A cells M37vUGZ2dmO2aX;uJIF{e2G7 M1S5bVYhcA>? MYDJcohq[mm2aX;uJI9nKEeVSz2zMYJmfGFvbXXkbYF1\WRiV370JJNq\26jbHnu[{BqdiCqdX3hckBUXDF2QTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBi[2O3bYXsZZRqd25ib3[gZoV1[S2lYYPlbY4h[XKxdX7kJI52[2yndYOgZYZ1\XJiNjDodpMh[nlibXnjdo9{[2:yaXOgZY5idHm|aYO= NHmybpczODdyOEmzOy=>
human ReNcell VM cells MUHQdo9tcW[ncnH0bY9vKGG|c3H5 NXHkR4lqOyEQvF2= MkW1O|IhcA>? NGm2cpZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGLlUoNmdGxiVl2gZ4VtdHNiYYPz[ZN{\WRiYYOgdoVlfWO2aX;uJI9nKGOnbHygdJJwdGmoZYLheIlwdiCjdDCzJJVOKGGodHXyJFczKGi{cx?= MWeyNFcxQDl|Nx?=
human SK-MEL-1 cell MVrHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUXpNXVOUW6qaXLpeIlwdiCxZjDoeY1idiCVSz3NSWwuOSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5MEBKSzVyPUO0MlcyPCEQvF2= NUjRZ3BWW0GQR1XS
human MOLT-4 cell NHXWSnBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M2\uXGlvcGmkaYTpc44hd2ZiaIXtZY4hVU:OVD20JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|YvOTR4NzFOwG0> NGLTSZRUSU6JRWK=
human T47D cell M{TQU2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUHCdVlNUW6qaXLpeIlwdiCxZjDoeY1idiCWNEfEJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|cvOTZ2NzFOwG0> MnTqV2FPT0WU
human SW1710 cell MWDHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWTJcohq[mm2aX;uJI9nKGi3bXHuJHNYOTdzMDDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO3MlM3ODhizszN M2jD[HNCVkeHUh?=
human MKN7 cell NXjkNGMyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MlHUTY5pcWKrdHnvckBw\iCqdX3hckBOU055IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{iuNFkxQSEQvF2= NYj0NJA3W0GQR1XS
human CAL-72 cell NFXBd2pIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MYTJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC15MjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUO4MlEyPzhizszN MX;TRW5ITVJ?
human AGS cell MYnHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NY\FVJI5UW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPE4zODN7IN88US=> MYnTRW5ITVJ?
human BE-13 cell MnXPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MUTJcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{iuO|c5OyEQvF2= MUXTRW5ITVJ?
human Calu-6 cell NHHwTZNIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NXXsNVB1UW6qaXLpeIlwdiCxZjDoeY1idiCFYXz1MVYh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{QS54OU[0JO69VQ>? MmW5V2FPT0WU
human CAL-27 cell NHvoXndIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVvJcohq[mm2aX;uJI9nKGi3bXHuJGNCVC1{NzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUS0MlAxPTRizszN MkHwV2FPT0WU
human BB49-HNC cell MV7Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXXJcohq[mm2aX;uJI9nKGi3bXHuJGJDPDlvSF7DJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9OFQvODJ5ODFOwG0> M2rFNHNCVkeHUh?=

... 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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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

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

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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:

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Molecular Weight Calculator

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

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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)
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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