BIO

For research use only.

Catalog No.S7198 Synonyms: GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052

16 publications

BIO Chemical Structure

CAS No. 667463-62-9

BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.

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Selleck's BIO has been cited by 16 publications

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  • Lysates of HCT116p53KO cells were harvested 24 hs after treatment with different GSK3 inhibitors and GSK3A/B activation/inactivation checked by western blot: a mix of pSer21-GSK3A and pSer9-GSK3B antibodies and antibody cross-reacting with both pTyr279-GSK3A and pTyr216-GSK3B were used to assess the specificity of the inhibitor for GSK3A. BIO: 6-bromoindirubin-3'-oxime, TWS: TWS119, SB2: SB216763, SB4: SB415286.

    PLoS One 2014 9(7), e100947. BIO purchased from Selleck.

  • (e and f) Confocal immunofluorescence staining. U87 GSLCs and U251 GSLCs were seeded in suspension and treated with control, Tet, BIO or ICG-001 for 48 h. Blue fluorescence represents DAPI, red fluorescence represents β-catenin, and green fluorescence represents TUNEL. Scale bars, 40 μm

    Int J Oncol, 2017, 50(1):101-110. BIO purchased from Selleck.

Purity & Quality Control

Choose Selective GSK-3 Inhibitors

Biological Activity

Description BIO (GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β in a cell-free assay, shows >16-fold selectivity over CDK5, also a pan-JAK inhibitor with IC50 of 30 nM for Tyk2. BIO induces apoptosis in human melanoma cells.
Features The first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells.
Targets
GSK-3 [1]
(Cell-free assay)
TYK2 [4]
(Cell-free assay)
CDK5/p35 [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
CDK1/CyclinB [1]
(Cell-free assay)
5 nM 30 nM 0.08 μM 0.30 μM 0.32 μM
In vitro

BIO (6-bromoindirubin-3'-oxime) is a specific inhibitor of glycogen synthase kinase-3 (GSK-3), with IC50 of 5 nM for GSK-3α/β, shows >16-fold selectivity over CDK5. BIO interacts within the ATP binding pocket of these kinases, reduces β-catenin phosphorylation on a GSK-3-specific site in cellular models, closely mimicks Wnt signaling in Xenopus embryos. [1] In human and mouse embryonic stem cells, BIO maintains the undifferentiated phenotype and sustains expression of the pluripotent state-specific transcription factors Oct-3/4, Rex-1 and Nanog. BIO-mediated Wnt activation is functionally reversible, as withdrawal of the compound leads to normal multidifferentiation programs in both human and mouse embryonic stem cells. [2] BIO promotes proliferation in mammalian cardiomyocytes. [3]6BIO is also a pan-JAK inhibitor, with IC50 values of 0.03, 1.5, 8.0, 0.5 μM for TYK2, JAK1, JAK2 and JAK3. BIO selectively inhibits phosphorylation of STAT3 and induces apoptosis of human melanoma cells. [4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HEI-OC1 MlThSpVv[3Srb36gZZN{[Xl? NH7MfIZRem:2ZXP0bY9vKGGpYXnud5Qh[2m|cHzheIlvNWmwZIXj[YQh[2WubDDk[YF1cCCrbjDu[Y9v[XSjbDDtc5V{\SCKRVmtU2MyKGOnbHzzJIF{e2W|c3XkJIF{KHKnZIXjeIlwdiCrbjDjZZNx[XOnLUOvO{Bi[3Srdnn0fUwhTUN3MDC9JFAvOTl{IN88UU4> NEj4TVk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC5NVkyPSd-M{CwPVE6OTV:L3G+
SH-SY5Y Ml7RSpVv[3Srb36gZZN{[Xl? MXPJcohq[mm2aX;uJI9nKEeVS{OtcYVlcWG2ZXSgZoV1[S2lYYPlbY4heGixc4Doc5J6dGG2aX;uJIlvKGi3bXHuJHNJNVO\NWmgZ4VtdHNiaX6gdJJme2WwY3Wgc4YhVUdzM{KgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|LDDJR|UxKD1iMD6yPUDPxE1w MWW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhzNkGxNEc,OTh6MU[xNVA9N2F-
K562 NXLueYxXSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MkDaO|IhcHK| NFrIWGdCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFu1OlIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGuN{DPxE1w M3\4NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{izNVQ6Lz5zOUe4N|E1QTxxYU6=
IMR90 NHrkU5RCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= M3LRe|czKGi{cx?= MVLBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEmPUkmwJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkmg{txONg>? MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd6M{G0PUc,OTl5OEOxOFk9N2F-
HCT116 NV3veVM3SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NVfGWYpOPzJiaILz M4DRXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTBiPTC1MlIh|ryPLh?= NF;3VXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe4N|E1QSd-MUm3PFMyPDl:L3G+
HepG2 MVnDfZRwfG:6aXPpeJkh[XO|YYm= MVuyOEBpenN? NYfMRZc5S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkAzPCCqcoOgZpkh[WyjbXHyJIJtfWViYYPzZZktKEmFNUCgQUA2NjNizszNMi=> NYL6SIZVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3OFM1QTJpPkK4O|Q{PDl{PD;hQi=>
HL60 NVrVN2dQSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MmrROUBl[Xm| M1v5WGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFy2NEBk\WyuczDh[pRmeiB3IHThfZMh[nliTWTUJIF{e2G7LDDJR|UxKD1iNT60JO69VS5? MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd6M{G0PUc,OTl5OEOxOFk9N2F-
HuH7 MkHjRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MXu3NkBpenN? M4jTbGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSIXIO{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iNj6yJO69VS5? M3fSSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{izNVQ6Lz5zOUe4N|E1QTxxYU6=
SH-SY5Y MoLRR5l1d3SxeHnjbZR6KGG|c3H5 NWfYUZFEPDhiaILz MmC5R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSVIILl[JVkfGmxbjDhd5NigSxiSVO1NEA:KDlizszNMi=> NGnsZ|Q9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOEixOlEyOCd-MUi4NVYyOTB:L3G+
SH-SY5Y NXXHeZZzTnWwY4Tpc44h[XO|YYm= M1jaT|Q5KGi{cx?= NHX4SYdUfXK4aY\hcEBw\iCqdX3hckBUUC2VWUXZJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGOgdoVlfWO2aX;uJIF{e2G7LDDJR|UxKD1iOT61JO69VS5? NIDIRXE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zNki1OFA3QSd-MU[4OVQxPjl:L3G+
SH-SY5Y M2jvRmZ2dmO2aX;uJIF{e2G7 M{LEPGRm[XSqIH;mJIh2dWGwIGPIMXN[PVliY3XscJMhcW5iYXLz[Y5k\SCxZjCyNEB2VSCTLW\EMW9RcCCkeTDNWHMhemWmdXP0bY9vKGG|c3H5MEBKSzVyIE2gNVAh|ryPLh?= NXLvdGtoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4OVQxPjlpPkG2PFU1ODZ7PD;hQi=>
SH-SY5Y NFXMTFdHfW6ldHnvckBie3OjeR?= NX3ncW02TGWjdHigc4YhcHWvYX6gV2guW1l3WTDj[YxteyCrbjDwdoV{\W6lZTDv[kAzOCC3TTDRMXZFNU:SaDDifUBOXFNicnXkeYN1cW:wIHHzd4F6NCCLQ{WwJF0hOTNizszNMi=> MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yPjh3NEC2PUc,OTZ6NUSwOlk9N2F-
SH-SY5Y NW\lVWt3TnWwY4Tpc44h[XO|YYm= MYiyOEBpenN? NV:xW2VtW3W{dnn2ZYwhd2ZiaIXtZY4hW0hvU2m1XUBk\WyuczDh[pRmeiB{NDDodpMh[nliTWTTJJJm\HWldHnvckBie3OjeTygTWM2OCB;IEG4JO69VS5? NXPG[3dRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4OVQxPjlpPkG2PFU1ODZ7PD;hQi=>
IMR32 MX7DfZRwfG:6aXPpeJkh[XO|YYm= MYq0PEBpenN? NEHQO4ZEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBKVVJ|MjDj[YxteyCjc4Pld5Nm\CCjczDj[YxtKH[rYXLpcIl1gSCjZoTldkA1QCCqcoOgZpkhVVSWIHHzd4F6 M4TRd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOECyPVQ4Lz5{MUiwNlk1PzxxYU6=
SK-N-SH MVjDfZRwfG:6aXPpeJkh[XO|YYm= MVK0PEBpenN? NWS1OmZ2S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hW0tvTj3TTEBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDh[pRmeiB2ODDodpMh[nliTWTUJIF{e2G7 MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOThyMkm0O{c,OjF6MEK5OFc9N2F-
NB39 M1r5S2N6fG:2b4jpZ4l1gSCjc4PhfS=> MXO0PEBpenN? M3fkRmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5DOzliY3XscJMh[XO|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK|IHL5JG1VXCCjc4PhfS=> M4L5bVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOECyPVQ4Lz5{MUiwNlk1PzxxYU6=
A673 NVvWdnZseUiWUzDhd5NigQ>? NYDpN5c3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= NH3lfIo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
DAOY M3KxcJFJXFNiYYPzZZk> MVjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>? NIHCNWE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 MVzxTHRUKGG|c3H5 MX\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| M1GwfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 Mn[2dWhVWyCjc4PhfS=> NUL3coR2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz Mn3BQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD NEDsZpRyUFSVIHHzd4F6 NFLmcWFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? NWflcoRXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH MWHxTHRUKGG|c3H5 NXnRSHVReUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> MWK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-12 NXS0Z49reUiWUzDhd5NigQ>? NWPObWdveUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz NYfRUoVNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) NIDRU3NyUFSVIHHzd4F6 NX31Ool6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz M3HhclxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 NEjaTnZyUFSVIHHzd4F6 NFPKTYRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKxOlQ{KGOnbHzz Mny2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NHjlfmFyUFSVIHHzd4F6 M4TwepFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NUe3[21[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 NFXEbGZyUFSVIHHzd4F6 M17FfZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 NV:2Wld3eUiWUzDhd5NigQ>? M13DNJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEOwJINmdGy| MYm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 M1XUUZFJXFNiYYPzZZk> MX7xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MYPxTHRUKGG|c3H5 MWLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NXHnc|NWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB-EBc1 MUTxTHRUKGG|c3H5 MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= MknsQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 MmPmdWhVWyCjc4PhfS=> NV[4VWtbeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz MmDqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh18 MojTdWhVWyCjc4PhfS=> M4HEV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaEG4JINmdGy| Mkn6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
A549 NVz4eog2TnWwY4Tpc44h[XO|YYm= M3fJUVExKHWP M2nSSVE2KG2rboO= M1LZTmlvcGmkaYTpc44hd2ZiaIXtZY4hdVCJRWOxJIZzd21iaIXtZY4hSTV2OTDj[YxteyCjc4Pld5Nm\CCjczDQS2UzKGG2IEGwJJVOKGGodHXyJFE2KG2rboOgZpkhUFCOQx?= NVnrR2FoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2PVczPDRpPkK0Olk4OjR2PD;hQi=>
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sf9 NFWySYFHfW6ldHnvckBie3OjeR?= NUnQenFuOSC3TR?= M4D1U2lvcGmkaYTpc44hd2ZiaIXtZY4hVi22ZYLtbY5idCCJU2SvTIl{Pi22YXfn[YQhTkeIUkGgLGc1ODBidH:gVlgzOCC{ZYPp[JVmeyliZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKHOoOTDj[YxteyCjdDCxJJVOKHW|aX7nJHBwdHlqR3z1MHR6eil2OkGgZZMhe3Wkc4TyZZRmKGK7IH\pcJRmeiCkaX7kbY5oKGG|c3H5 NUDOcHE3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki1OVc1OzBpPkK4OVU4PDNyPD;hQi=>
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sf9 NYTz[VQ1TnWwY4Tpc44h[XO|YYm= M4DZU|EhfU1? M1zLNmlvcGmkaYTpc44hd2ZiaIXtZY4hVi22ZYLtbY5idCCJU2SteIFo\2WmIFH1do9z[SCEIDjNNUB1dyCVMkegdoV{cWS3ZYOpJIV5eHKnc4Pl[EBqdiC|ZkmgZ4VtdHNiYYSgNUB2VSC3c3nu[{BETEN{NVOt[IVzcX[nZDDw[ZB1cWSnIHHzJJN2[nO2cnH0[UBjgSCoaXz0[ZIh[mmwZHnu[{Bie3OjeR?= MmDMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh3NUe0N|AoRjJ6NUW3OFMxRC:jPh?=
HT22 MXXGeY5kfGmxbjDhd5NigQ>? MXexNEB2VQ>? M4jaW|I1KGi{cx?= NXu4WXdoUW6qaXLpeIlwdiCxZjDHV2s{NW2nZHnheIVlKGKndHGgZ4F{\WmwIIDoc5NxcG:{eXzheIlwdiCrbjDtc5V{\SCKVEKyJINmdGy|IHH0JFExKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4SgZY5idHm|aYOgbY4heHKnc3XuZ4Uhd2ZiTVexN|I> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl7OES0N{c,OjJ7OUi0OFM9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-AKT / AKT / p21 / p27 ; 

PubMed: 27510556     


In BIO treatment of cardiac fibroblasts for 1 day, the protein levels of phosphorylated Akt, p21, and p27 were assessed.

p-β-catenin / β-catenin ; 

PubMed: 27211495     


ERKi and GSK3i differently regulate PI3K/Akt and β-catenin pathways. U0126 increased while BIO decreased Akt phosphorylation after 24 hours of treatment. BIO prevented β-catenin phosphorylation leading to intact β-catenin accumulation, while U0126 only had a marginal effect.

FoxO3a / FoxO1 / p-FoxO3a / p-FoxO1 ; 

PubMed: 27211495     


U0126 markedly increased the phosphorylation of Akt downstream targets FOXO1 and FOXO3a, while BIO decreased it.

27510556 27211495
Immunofluorescence
pAKT / p21 / p27 ; 

PubMed: 27510556     


Protein expressions of pAkt, p21 and p27 were determined by immunofluorescence staining in cardiac fibroblasts treated with BIO for 1 day. *p < 0.05, t-test. Scale bar = 100 μm.

TNF-α; 

PubMed: 24286133     


Detection of TNF-α protein expression by immunofluorescence microscopy. Nucleus pulposus cells were cultured with or without 1.0 μM BIO for 24 h, fixed, and stained with an antibody against c-fos. Left: cells stained with an antibody to TNF-α; middle: cells stained with 4′,6-diamidino-2-phenylindole (DAPI), to identify healthy nuclei; right: cells stained with an antibody to TNF-α and with DAPI. Scale bar, 50 μm (original magnification, 20×).

E-cadherin / Nanog ; 

PubMed: 25538040     


hESCs were treated with either vehicle (Veh) or BIO for 6 hours. Twenty-four hours after removal of BIO, hESCs exhibit thick and compact colonies that express higher levels of E‐cadherin (E‐cad) and Nanog.

Oct3/4; 

PubMed: 25538040     


hESCs were treated with either vehicle (Veh) or BIO for 6 hours. Twenty‐four hours after removal of BIO, hESCs exhibit thick and compact colonies that express higher levels of E‐cadherin (E‐cad) and Oct3/4. In contrast, long-term BIO treatment leads to opposing results. Scale bar = 20 µm.

27510556 24286133 25538040
Growth inhibition assay
Cell proliferation ; 

PubMed: 27510556     


The increase in cardiomyocyte proliferation after treatment with BIO for 4 days was also confirmed by MTT assay.

27510556
In vivo BIO suppresses melanoma tumor growth in a mouse xenograft model. [4]

Protocol

Kinase Assay:[1]
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Kinase assay:

Kinase activities are assayed in Buffer A or C at 30°C, at a final ATP concentration of 15 μM. Blank values are subtracted and activities calculated as pmoles of phosphate incorporated during a 10 min incubation. Controls are performed with appropriate dilutions of dimethylsulfoxide. In a few cases phosphorylation of the substrate is assessed by autoradiography after SDS-PAGE. GSK-3α/β is purified from porcine brain by affinity chromatography on immobilized axin. It is assayed, following a 1/100 dilution in 1 mg BSA/ml 10 mM DTT, with 5 μl 40 μM GS-1 peptide, a specific GSK-3 substrate, (YRRAAVPPSPSLSRHSSPHQSpEDEEE), in buffer A, in the presence of 15 μM [γ-32P] ATP (3,000 Ci/mmol; 1 mCi/ml) in a final volume of 30 μl. After 30 min incubation at 30°C, 25 μl aliquots of supernatant are spotted onto 2.5 × 3 cm pieces of Whatman P81 phosphocellulose paper, and 20 seconds later, the filters are washed five times (for at least 5 min each time) in a solution of 10 ml phosphoric acid/liter of water. The wet filters are counted in the presence of 1 ml ACS scintillation fluid.
Cell Research:[1]
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  • Cell lines: COS1, Hepa or SH-SY5Y cells
  • Concentrations: ~10 μM
  • Incubation Time: 12 or 24 h
  • Method: COS1, Hepa (wild-type, CEM/LM AhR deficient and ELB1 ARNT deficient), or SH-SY5Y cells are grown in 6 cm culture dishes in Dulbecco's Modified Medium (DMEM) containing 10% fetal bovine serum. For treatment, IO (5 μM), BIO (5 or 10 μM), MeBIO (5 or 50 μM), LiCl (20 or 40 mM), or mock solution (DMSO, 0.5% final concentration) is added to medium when cell density reaches ∼70% confluence. After 12 (SH-SY5Y) or 24 hours, the cells, while still in plate, are lysed with lysis buffer (1% SDS, 1 mM sodium orthovanadate, 10 mM Tris [pH 7.4]). The lysate is passed several times through a 26G needle, centrifuged at 10,000 × g for 5 min, and adjusted to equal protein concentration. About 8 μg of each sample is loaded for immunoblotting. Enhanced chemiluminescence is used for detection. The following primary antibodies are used: mouse anti-β-catenin CT (Upstate Biotechnolgies, Clone 7D8, recognizes total β-catenin), mouse anti-phospho-β-catenin (Upstate Biotechnologies, Clone 8E7, recognizes dephosphorylated β-catenin), mouse anti-GSK-3 β, mouse anti-GSK-3 phosphoTyr216, rabbit anti-AhR (Aryl hydrocarbon receptor), and rabbit anti-actin.
    (Only for Reference)
Animal Research:[4]
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  • Animal Models: mouse
  • Dosages: 50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 71 mg/mL (199.34 mM)
Water Insoluble
Ethanol '6 mg/mL
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+40% PEG 300+5% Tween 80+50%ddH2O
For best results, use promptly after mixing.
3 mg/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 356.17
Formula

C16H10BrN3O2

CAS No. 667463-62-9
Storage powder
in solvent
Synonyms GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime, 6-Bromoindirubin-3'-oxime, MLS 2052
Smiles C1=CC=C2C(=C1)C(=C(N2)C3=C(NC4=C3C=CC(=C4)Br)O)N=O

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 ()
% DMSO % % Tween 80 % ddH2O
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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

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
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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

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04263519 Not yet recruiting Drug: Tacrolimus Alzheimer Disease|Mild Cognitive Impairment Massachusetts General Hospital December 1 2021 Phase 2

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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GSK-3 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID