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SB216763

For research use only.

Catalog No.S1075

56 publications

SB216763 Chemical Structure

CAS No. 280744-09-4

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

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Selleck's SB216763 has been cited by 56 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 MnzJSpVv[3Srb36gZZN{[Xl? NFfhUWNIdHmlb3flckB{gW62aHHz[UBi[3Srdnn0fUBw\iCKRVuyPVMh[2WubIOsJIlvcGmkaYTpc44hd2ZiR2PLN{1j\XSjLDDFR|UxRTBwMjFOwG0> MYOxNlk1OTN|MR?=
human HDLM-2 cell M1nPVmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MX3Jcohq[mm2aX;uJI9nKGi3bXHuJGhFVE1vMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUCuNlA6QDRizszN NH7kW5pUSU6JRWK=
human NCI-H1770 cell M4O2TGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MnjGTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvSEG3O|Ah[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigS5iSVO1NF0xNjJ7M{myJO69VQ>? M3HDO3NCVkeHUh?=
human HOP-62 cell NIOzcYlIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NFztOI1KdmirYnn0bY9vKG:oIHj1cYFvKEiRUD22NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVAvQDV{NU[g{txO MV;TRW5ITVJ?
human JAR cell Mmi5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MoXMTY5pcWKrdHnvckBw\iCqdX3hckBLSVJiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1zLkKxNFQ1KM7:TR?= NVnpTHJbW0GQR1XS
human K5 cell NWn1coZKT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVnNVVl2UW6qaXLpeIlwdiCxZjDoeY1idiCNNTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6NCCLQ{WwQVEvPTN4OUig{txO MWnTRW5ITVJ?
human MV-4-11 cell MnrOS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Ml\LTY5pcWKrdHnvckBw\iCqdX3hckBOXi12LUGxJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9Nk43QTZ6NTFOwG0> NGXzflJUSU6JRWK=
human BT-549 cell NEHRemtIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoDlTY5pcWKrdHnvckBw\iCqdX3hckBDXC13NEmgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME21MlI6Ozd4IN88US=> MWDTRW5ITVJ?
human LB2241-RCC cell M3r4c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MXXJcohq[mm2aX;uJI9nKGi3bXHuJGxDOjJ2MT3SR2Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF03NjR{OEe0JO69VQ>? NVvSWoRnW0GQR1XS
human GAMG cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2f1ZmlvcGmkaYTpc44hd2ZiaIXtZY4hT0GPRzDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPU[uOlU1ODlizszN NHTZSldUSU6JRWK=
human HMV-II cell MlrDS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NVPpVVY4UW6qaXLpeIlwdiCxZjDoeY1idiCKTW[tTWkh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF04NjZ5NkC3JO69VQ>? M3SxTnNCVkeHUh?=
human RS4-11 cell M2HM[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NF;aUoFKdmirYnn0bY9vKG:oIHj1cYFvKFKVND2xNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVgvOjRzNEGg{txO MnTRV2FPT0WU
human NCI-H1993 cell M2foSGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NVXVN5A3UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE6QTNiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD16LkO2OVM1KM7:TR?= NWW0XIpWW0GQR1XS
human IST-SL1 cell M3fuOmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NXL5WndpUW6qaXLpeIlwdiCxZjDoeY1idiCLU2StV2wyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:QS5yMkC0JO69VQ>? M2\kTXNCVkeHUh?=
human SK-OV-3 cell M1LHbGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4fOZmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvT2[tN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVkvOTByMjFOwG0> MlH0V2FPT0WU
human ESS-1 cell M3zk[Gdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MWrJcohq[mm2aX;uJI9nKGi3bXHuJGVUWy1zIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;OT61PVg4OiEQvF2= M3zhNHNCVkeHUh?=
human G-361 cell NGnVWGxIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NY[5O5BuUW6qaXLpeIlwdiCxZjDoeY1idiCJLUO2NUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVExNjF5OUig{txO NH3pXW1USU6JRWK=
human ALL-PO cell NHHDemJIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoLSTY5pcWKrdHnvckBw\iCqdX3hckBCVExvUF:gZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xNE4{PDd5IN88US=> M2fnZ3NCVkeHUh?=
human NB5 cell NWW3dY03T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M2f2dmlvcGmkaYTpc44hd2ZiaIXtZY4hVkJ3IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUGuNlE2PyEQvF2= NEfQOGNUSU6JRWK=
human DU-145 cell M4L4Umdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NH3lTZpKdmirYnn0bY9vKG:oIHj1cYFvKESXLUG0OUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVEyNjZ3M{Wg{txO MnW5V2FPT0WU
human NMC-G1 cell NGHrcIdIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NU\y[2h3UW6qaXLpeIlwdiCxZjDoeY1idiCQTVOtS|Eh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0yOS55Mk[0JO69VQ>? M3W1NXNCVkeHUh?=
human RPMI-7951 cell MmnRS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M2nvdWlvcGmkaYTpc44hd2ZiaIXtZY4hWlCPST23PVUyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XlwIFnDOVA:OTFwN{i2OEDPxE1? Mk\zV2FPT0WU
human NCI-H2009 cell MXHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M4C0NWlvcGmkaYTpc44hd2ZiaIXtZY4hVkOLLViyNFA6KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTNwMkSyO{DPxE1? MWHTRW5ITVJ?
human LoVo cell M174c2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MoXpTY5pcWKrdHnvckBw\iCqdX3hckBNd1[xIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuN|c4OSEQvF2= NF\nOWxUSU6JRWK=
human A2058 cell MkDPS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MVjJcohq[mm2aX;uJI9nKGi3bXHuJGEzODV6IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MUOuOFY6KM7:TR?= MkjXV2FPT0WU
human D-566MG cell NWHCXVM2T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MVzJcohq[mm2aX;uJI9nKGi3bXHuJGQuPTZ4TVegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xN{46PDhzIN88US=> MVHTRW5ITVJ?
human QIMR-WIL cell NH2wfppIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVPJcohq[mm2aX;uJI9nKGi3bXHuJHFKVVJvV1nMJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVUvPjN7NDFOwG0> MkLEV2FPT0WU
human S-117 cell NWTFR3hIT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M3XKXWlvcGmkaYTpc44hd2ZiaIXtZY4hWy1zMUegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2xOk41ODJ{IN88US=> NF3hXVZUSU6JRWK=
human YH-13 cell M1fwfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NFPqcHlKdmirYnn0bY9vKG:oIHj1cYFvKFmKLUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVYvPjh4NTFOwG0> M2O0SnNCVkeHUh?=
human IGROV-1 cell NF7VWFFIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MlL1TY5pcWKrdHnvckBw\iCqdX3hckBKT1KRVj2xJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVcvOjByMTFOwG0> NIHvU4lUSU6JRWK=
human BHT-101 cell MkXLS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NW\Dd3lnUW6qaXLpeIlwdiCxZjDoeY1idiCESGStNVAyKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OTdwNkC5PUDPxE1? MlvBV2FPT0WU
human MKN45 cell NEfodZVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MoT4TY5pcWKrdHnvckBw\iCqdX3hckBOU052NTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUG4MlQyOjhizszN NEPj[HhUSU6JRWK=
human A498 cell MVHHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NUG0UYFlUW6qaXLpeIlwdiCxZjDoeY1idiCDNEm4JINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NVkvPDV2OTFOwG0> MXvTRW5ITVJ?
human U-266 cell MXLHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MXXJcohq[mm2aX;uJI9nKGi3bXHuJHUuOjZ4IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;MkCuPFc6PyEQvF2= NE\zfZFUSU6JRWK=
human BFTC-905 cell MXfHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2DWXmlvcGmkaYTpc44hd2ZiaIXtZY4hSk[WQz25NFUh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS5zOEe5JO69VQ>? Mn;xV2FPT0WU
human BxPC-3 cell Mn;1S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NH;ybWVKdmirYnn0bY9vKG:oIHj1cYFvKEK6UFOtN{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVIyNjN3NUSg{txO NUDYdVQ2W0GQR1XS
human NCI-SNU-1 cell NUfGdFloT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= Ml\WTY5pcWKrdHnvckBw\iCqdX3hckBPS0lvU17VMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zOS53NUW4JO69VQ>? MUjTRW5ITVJ?
human SF539 cell M{Tz[2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M1TzZmlvcGmkaYTpc44hd2ZiaIXtZY4hW0Z3M{mgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNk4xOTl6IN88US=> M3nWcnNCVkeHUh?=
human VA-ES-BJ cell MoC5S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NXTzS5RyUW6qaXLpeIlwdiCxZjDoeY1idiCYQT3FV{1DUiClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTJ{LkW3OlMh|ryP MlfYV2FPT0WU
human HuO-3N1 cell MVPHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MWTJcohq[mm2aX;uJI9nKGi3bXHuJGh2Vy1|TkGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yNk43OTVzIN88US=> MXXTRW5ITVJ?
human EM-2 cell NWPwUWhUT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NVu0N25MUW6qaXLpeIlwdiCxZjDoeY1idiCHTT2yJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9NlIvPjZ6OTFOwG0> NWHNVJpKW0GQR1XS
human T98G cell NHnCclVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MUDJcohq[mm2aX;uJI9nKGi3bXHuJHQ6QEdiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{Mz6zNFA6KM7:TR?= MoCzV2FPT0WU
human SW1783 cell MkjMS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NHG4XWpKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUe4N{Bk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI{NjV{NEOg{txO Mlf2V2FPT0WU
human NKM-1 cell MlnmS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? M4\LUGlvcGmkaYTpc44hd2ZiaIXtZY4hVkuPLUGgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yN{45PTF{IN88US=> M3[yXnNCVkeHUh?=
human KOSC-2 cell NWPtN49zT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NY[xbHlwUW6qaXLpeIlwdiCxZjDoeY1idiCNT2PDMVIh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPC5zMkmyJO69VQ>? MX;TRW5ITVJ?
human SW48 cell MnfpS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MXLJcohq[mm2aX;uJI9nKGi3bXHuJHNYPDhiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{ND62NFY4KM7:TR?= MXLTRW5ITVJ?
human MIAPaCa2 cells NUnlWYlCT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MXW3NkBp MlrDS5Jwf3SqIHnubIljcXSrb36gc4YhcHWvYX6gUWlCWGGFYUKgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WUzDhd5NigSxiSVO1NF0zPSEQvF2= MVWxPVM{QDN3NR?=
human NCI-H28 cell NXTBU2Y6T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGPhOYNKdmirYnn0bY9vKG:oIHj1cYFvKE6FST3INlgh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPS5{MUC0JO69VQ>? NGf1W3BUSU6JRWK=
human 5637 cell M3zuV2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGPmbJpKdmirYnn0bY9vKG:oIHj1cYFvKDV4M{egZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2yOU45OTFzIN88US=> NWq4VXV7W0GQR1XS
human NB69 cell NWLodoxFT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M{jVZmlvcGmkaYTpc44hd2ZiaIXtZY4hVkJ4OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK2MlE4PjRizszN NYjPeWRiW0GQR1XS
human HT-29 cell MnOzS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MnTGTY5pcWKrdHnvckBw\iCqdX3hckBJXC1{OTDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK3MlE4PTJizszN NGS3NnFUSU6JRWK=
human PFSK-1 cell NE\NWHBIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NF\ZWWdKdmirYnn0bY9vKG:oIHj1cYFvKFCIU1utNUBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVI4NjV7MzFOwG0> NX3rW|JZW0GQR1XS
human UACC-257 cell M2TaNmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M2jQd2lvcGmkaYTpc44hd2ZiaIXtZY4hXUGFQz2yOVch[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0zPy55NEOg{txO NHvOVFlUSU6JRWK=
human D-423MG cell MnThS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NYPlV3V7UW6qaXLpeIlwdiCxZjDoeY1idiCGLUSyN21IKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OjdwOUGwOkDPxE1? NF3O[5hUSU6JRWK=
human NH-12 cell NFLtNodIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Ml;4TY5pcWKrdHnvckBw\iCqdX3hckBPUC1zMjDj[YxtKGe{b4f0bEBqdiCjIHPlcIwhfmmjYnnsbZR6KGG|c3H5MEBKSzVyPUK4MlQxPTlizszN MXzTRW5ITVJ?
human DEL cell M3W0fmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 MmW0TY5pcWKrdHnvckBw\iCqdX3hckBFTUxiY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1{OT6wOFc1KM7:TR?= NILUN|NUSU6JRWK=
human LS-513 cell MXXHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2GwWWlvcGmkaYTpc44hd2ZiaIXtZY4hVFNvNUGzJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|AvOTN|NDFOwG0> MWfTRW5ITVJ?
human NBsusSR cell M2Pnbmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4rmU2lvcGmkaYTpc44hd2ZiaIXtZY4hVkK|dYPTVkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVMxNjV4N{ig{txO NU\Ic3B7W0GQR1XS
human BV-173 cell NVPyVoNyT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NU\lXoo5UW6qaXLpeIlwdiCxZjDoeY1idiCEVj2xO|Mh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTDhd5NigSxiSVO1NF0{OC55NkS5JO69VQ>? MoL1V2FPT0WU
human A101D cell NUjyXpJHT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= M1;mOmlvcGmkaYTpc44hd2ZiaIXtZY4hSTFyMVSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNE46Pzh2IN88US=> NUnl[VJwW0GQR1XS
human LU-134-A cell NUHPXlNqT3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MUjJcohq[mm2aX;uJI9nKGi3bXHuJGxWNTF|ND3BJINmdGxiZ4Lve5RpKGmwIHGgZ4VtdCC4aXHibYxqfHliYYPzZZktKEmFNUC9N|EvODJ|ODFOwG0> MlTlV2FPT0WU
human ES3 cell M{[5SGdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NYrjdVJDUW6qaXLpeIlwdiCxZjDoeY1idiCHU{OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zNU4{Ozd4IN88US=> Mnq4V2FPT0WU
human NY cell MorxS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? MmjBTY5pcWKrdHnvckBw\iCqdX3hckBPYSClZXzsJIdzd3e2aDDpckBiKGOnbHygeoli[mmuaYT5JIF{e2G7LDDJR|UxRTN{LkK5OlUh|ryP MVnTRW5ITVJ?
human NCI-H1975 cell MV;Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? NWHP[lE3UW6qaXLpeIlwdiCxZjDoeY1idiCQQ1mtTFE6PzViY3XscEBoem:5dHigbY4h[SClZXzsJJZq[WKrbHn0fUBie3OjeTygTWM2OD1|Mj6zOVgzKM7:TR?= M4rKXHNCVkeHUh?=
human A704 cell NULTXYE4T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= MnPFTY5pcWKrdHnvckBw\iCqdX3hckBCPzB2IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{SuNlA2QSEQvF2= MWnTRW5ITVJ?
human SK-MEL-24 cell MV\Hdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? M2fKXGlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVI1KGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:OzRwMkWyN{DPxE1? NIf4[GFUSU6JRWK=
human SW1088 cell M1zxe2dzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NGDVdHBKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUC4PEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM1NjN2NUKg{txO MoLLV2FPT0WU
human HepG2 cells NInxTGdHfW6ldHnvckBie3OjeR?= MoHGN|Qh|ryP NXLFcHQ4OTJiaB?= M4KxV2lvcGmkaYTpc44hd2ZiR2PLN4JmfGFiaX6gbJVu[W5iSHXwS|Ih[2WubIOgZZN{\XO|ZXSgZZMh\GWlcnXhd4UhcW5icnH0bY8hd2ZicHjvd5Bpd3K7bHH0[YQhT1NxR2OgZZQhOzRidV2gZYZ1\XJiMUKgbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> M4TaXFI2PDZ5MUWw
mouse 3T3L1 cells M{\sOmZ2dmO2aX;uJIF{e2G7 NGTNS3g{PCEQvF2= NYrtTpRZOTJiaB?= NGmw[VBKdmO{ZXHz[UBqdiCpbIXjc5NmKGmwY3;ydI9z[XSrb36gbY4hdW:3c3WgN3Q{VDFiY3XscJMh[XRiM{SgeW0h[W[2ZYKgNVIhcHK|IHL5JIdtfWOxc3WgZZN{[Xl? MUGyOVQ3PzF3MB?=
human ST14A cells MVPGeY5kfGmxbjDhd5NigQ>? MnHCOkBp MWHJcohq[mm2aX;uJI9nKEeVSz2zMYJmfGFvbXXkbYF1\WRiV370JJNq\26jbHnu[{BqdiCqdX3hckBUXDF2QTDj[YxteyCjc4Pld5Nm\CCjczDpcoNz\WG|ZTDpckBi[2O3bYXsZZRqd25ib3[gZoV1[S2lYYPlbY4h[XKxdX7kJI52[2yndYOgZYZ1\XJiNjDodpMh[nlibXnjdo9{[2:yaXOgZY5idHm|aYO= M2\E[FIxPzB6OUO3
human ReNcell VM cells M4LqUnBzd2yrZnXyZZRqd25iYYPzZZk> NFvKN|k{KM7:TR?= MoC0O|IhcA>? MmryRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCUZV7j[YxtKF[PIHPlcIx{KGG|c3Xzd4VlKGG|IILl[JVkfGmxbjDv[kBk\WyuIIDyc4xq\mW{YYTpc44h[XRiMzD1UUBi\nSncjC3NkBpenN? MoHGNlA4ODh7M{e=
human SK-MEL-1 cell M13Vemdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 M4jiOmlvcGmkaYTpc44hd2ZiaIXtZY4hW0tvTVXMMVEh[2WubDDndo94fGhiaX6gZUBk\WyuII\pZYJqdGm2eTygTWM2OD1|ND63NVQh|ryP M{e1TXNCVkeHUh?=
human MOLT-4 cell MkC4S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mnv0TY5pcWKrdHnvckBw\iCqdX3hckBOV0yWLUSgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zOk4yPDZ5IN88US=> NWG1NGlVW0GQR1XS
human T47D cell NGTQO|dIem:5dHigbY5pcWKrdHnvckBie3OjeR?= Mo\OTY5pcWKrdHnvckBw\iCqdX3hckBVPDeGIHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{euNVY1PyEQvF2= MW\TRW5ITVJ?
human SW1710 cell NYLr[214T3Kxd4ToJIlvcGmkaYTpc44h[XO|YYm= NGTYNopKdmirYnn0bY9vKG:oIHj1cYFvKFOZMUexNEBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM4NjN4MEig{txO NX;EOJZJW0GQR1XS
human MKN7 cell MofTS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? Mk\4TY5pcWKrdHnvckBw\iCqdX3hckBOU055IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{iuNFkxQSEQvF2= MXvTRW5ITVJ?
human CAL-72 cell Mlm2S5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NF[1Z5NKdmirYnn0bY9vKG:oIHj1cYFvKEODTD23NkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM5NjFzN{ig{txO MYnTRW5ITVJ?
human AGS cell M4jYfmdzd3e2aDDpcohq[mm2aX;uJIF{e2G7 NUCxbI1HUW6qaXLpeIlwdiCxZjDoeY1idiCDR2OgZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME2zPE4zODN7IN88US=> MUPTRW5ITVJ?
human BE-13 cell NF\lR|NIem:5dHigbY5pcWKrdHnvckBie3OjeR?= MVTJcohq[mm2aX;uJI9nKGi3bXHuJGJGNTF|IHPlcIwh\3Kxd4ToJIlvKGFiY3XscEB3cWGkaXzpeJkh[XO|YYmsJGlEPTB;M{iuO|c5OyEQvF2= M{HVdXNCVkeHUh?=
human Calu-6 cell MonhS5Jwf3SqIHnubIljcXSrb36gZZN{[Xl? NGq5b2dKdmirYnn0bY9vKG:oIHj1cYFvKEOjbIWtOkBk\WyuIHfyc5d1cCCrbjDhJINmdGxidnnhZoltcXS7IHHzd4F6NCCLQ{WwQVM6NjZ7NkSg{txO NEn4eVRUSU6JRWK=
human CAL-27 cell MYTHdo94fGhiaX7obYJqfGmxbjDhd5NigQ>? MoPxTY5pcWKrdHnvckBw\iCqdX3hckBESUxvMkegZ4VtdCCpcn;3eIghcW5iYTDj[YxtKH[rYXLpcIl1gSCjc4PhfUwhUUN3ME20OE4xODV2IN88US=> MlvtV2FPT0WU
human BB49-HNC cell NHvIbVhIem:5dHigbY5pcWKrdHnvckBie3OjeR?= NGTSWZlKdmirYnn0bY9vKG:oIHj1cYFvKEKENEmtTG5EKGOnbHyg[5Jwf3SqIHnuJIEh[2WubDD2bYFjcWyrdImgZZN{[XluIFnDOVA:PDRwMEK3PEDPxE1? NYW5bllLW0GQR1XS

... Click to View More Cell Line Experimental Data

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

PubMed: 28042322     


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

c-Myb; 

PubMed: 21795403     


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

28042322 21795403
Growth inhibition assay
Cell viability; 

PubMed: 24779365     


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

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

Protocol

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

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

Solubility (25°C)

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

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

Chemical Information

Molecular Weight 371.22
Formula

C19H12N2O2Cl2

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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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Bio Calculators

Molarity Calculator

Molarity Calculator

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

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

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

Dilution Calculator

Dilution Calculator

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

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

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

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

The Serial Dilution Calculator Equation

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  • Computed Result

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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.

Molarity Calculator

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Tech Support

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

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID