BIO

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

For research use only.

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.

BIO Chemical Structure

CAS No. 667463-62-9

Selleck's BIO has been cited by 27 publications

Purity & Quality Control

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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)
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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 MoTuSpVv[3Srb36gZZN{[Xl? MoS5VJJwfGWldHnvckBi\2GrboP0JINqe3CuYYTpck1qdmS3Y3XkJINmdGxiZHXheIghcW5ibnXvcoF1[WxibX;1d4UhUEWLLV;DNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3HzdIF{\S1|L{egZYN1cX[rdImsJGVEPTBiPTCwMlE6OiEQvF2u NFnR[lc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC5NVkyPSd-M{CwPVE6OTV:L3G+
SH-SY5Y MYXGeY5kfGmxbjDhd5NigQ>? NF7oOpFKdmirYnn0bY9vKG:oIFfTT|MudWWmaXH0[YQh[mW2YT3jZZNmcW5icHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFOKLWPZOXkh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiTVexN|Ih[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nzMEBKSzVyIE2gNE4zQSEQvF2u MmP0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh6MU[xNVAoRjF6OEG2NVExRC:jPh?=
K562 MnrNRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NVSxb3dwPzJiaILz Ml\rRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkOg{txONg>? MoXDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5OEOxOFkoRjF7N{izNVQ6RC:jPh?=
IMR90 MWPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MVu3NkBpenN? NWHH[|Y6SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDJUXI6OCClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyIE2gNU46KM7:TT6= NWDCeZhsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3PFMyPDlpPkG5O|g{OTR7PD;hQi=>
HCT116 M4f6OWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NEfMbGU4OiCqcoO= NUK3bYt4SW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[W[2ZYKgO|IhcHK|IHL5JG1VXCCjc4PhfUwhUUN3MDC9JFUvOiEQvF2u NFLrSIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe4N|E1QSd-MUm3PFMyPDl:L3G+
HepG2 NXjVOIZSS3m2b4TvfIlkcXS7IHHzd4F6 NFTwZW0zPCCqcoO= MYfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDI[ZBIOiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJIdzd3e2aDDpcohq[mm2aX;uJIFnfGW{IEK0JIhzeyCkeTDhcIFu[XJiYnz1[UBie3OjeTygTWM2OCB;IEWuN{DPxE1w NVLsbllMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3OFM1QTJpPkK4O|Q{PDl{PD;hQi=>
HL60 MXTBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? M4PHeVUh\GG7cx?= MVvBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiONkCgZ4VtdHNiYX\0[ZIhPSCmYYnzJIJ6KE2WVDDhd5NigSxiSVO1NEA:KDVwNDFOwG0v NIPSSoE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUe4N|E1QSd-MUm3PFMyPDl:L3G+
HuH7 M4nKSGFvfGmycn;sbYZmemG2aY\lJIF{e2G7 M1Xpc|czKGi{cx?= M1nkcGFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSIXIO{Bk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxKD1iNj6yJO69VS5? M4DKPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{izNVQ6Lz5zOUe4N|E1QTxxYU6=
SH-SY5Y NUXp[4NOS3m2b4TvfIlkcXS7IHHzd4F6 MYi0PEBpenN? Mn\JR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSVIILl[JVkfGmxbjDhd5NigSxiSVO1NEA:KDlizszNMi=> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDhzNkGxNEc,OTh6MU[xNVA9N2F-
SH-SY5Y MXLGeY5kfGmxbjDhd5NigQ>? MlHLOFghcHK| NIK5[GRUfXK4aY\hcEBw\iCqdX3hckBUUC2VWUXZJINmdGy|IHHmeIVzKDR6IHjyd{BjgSCPVGOgdoVlfWO2aX;uJIF{e2G7LDDJR|UxKD1iOT61JO69VS5? NX\SXVR6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4OVQxPjlpPkG2PFU1ODZ7PD;hQi=>
SH-SY5Y NFTNcm9HfW6ldHnvckBie3OjeR?= MYPE[YF1cCCxZjDoeY1idiCVSD3TXVV[KGOnbHzzJIlvKGGkc3XuZ4Uhd2ZiMkCgeW0hWS2YRD3PVIgh[nliTWTTJJJm\HWldHnvckBie3OjeTygTWM2OCB;IEGwJO69VS5? NYDCSZVXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4OVQxPjlpPkG2PFU1ODZ7PD;hQi=>
SH-SY5Y MmS4SpVv[3Srb36gZZN{[Xl? M2PkVWRm[XSqIH;mJIh2dWGwIGPIMXN[PVliY3XscJMhcW5icILld4Vv[2Vib3[gNlAhfU1iUT3WSE1QWGhiYomgUXRUKHKnZIXjeIlwdiCjc4PhfUwhUUN3MDC9JFE{KM7:TT6= M2T6NVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEW0NFY6Lz5zNki1OFA3QTxxYU6=
SH-SY5Y MWTGeY5kfGmxbjDhd5NigQ>? M2LITlI1KGi{cx?= MkLQV5Vzfmm4YXygc4YhcHWvYX6gV2guW1l3WTDj[YxteyCjZoTldkAzPCCqcoOgZpkhVVSVIILl[JVkfGmxbjDhd5NigSxiSVO1NEA:KDF6IN88UU4> MkHZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTZ6NUSwOlkoRjF4OEW0NFY6RC:jPh?=
IMR32 M3\6bGN6fG:2b4jpZ4l1gSCjc4PhfS=> MWm0PEBpenN? NXfPXoxsS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUU2UM{KgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigQ>? NHm4UmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUiwNlk1Pyd-MkG4NFI6PDd:L3G+
SK-N-SH MmT2R5l1d3SxeHnjbZR6KGG|c3H5 NEXwOm01QCCqcoO= NHTteIREgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUy2QLWPIJINmdGy|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[Xl? MXe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOThyMkm0O{c,OjF6MEK5OFc9N2F-
NB39 NWfEOYYyS3m2b4TvfIlkcXS7IHHzd4F6 MXK0PEBpenN? MUXDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDORlM6KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYm= M2jn[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzOECyPVQ4Lz5{MUiwNlk1PzxxYU6=
A673 MknNdWhVWyCjc4PhfS=> MYDxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? NYf2NIFDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
DAOY MnfhdWhVWyCjc4PhfS=> NWHmNYgxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 M4XPSJFJXFNiYYPzZZk> NF\TeZJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz MlfSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-37 NIX5fGpyUFSVIHHzd4F6 M2rZ[ZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2zO{Bk\Wyucx?= NVz5SXlbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD NH3jPVdyUFSVIHHzd4F6 MmDadWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NYTtVnA6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NHK2elRyUFSVIHHzd4F6 M4raeZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-12 NHXqRpFyUFSVIHHzd4F6 NXi4ZoR{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) M1rTSJFJXFNiYYPzZZk> NUKwNYJ{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz MkjoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB1643 Mn\SdWhVWyCjc4PhfS=> MlzwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 MUDxTHRUKGG|c3H5 M4jr[pFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCRSGOtOVAh[2WubIO= NXPQUG5bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 MmHKdWhVWyCjc4PhfS=> NH;tO|dyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 MlzUdWhVWyCjc4PhfS=> MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh|MDDj[Yxtew>? MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 MV;xTHRUKGG|c3H5 NGHwcHlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> NH7N[5I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC MUXxTHRUKGG|c3H5 NV[xcVg4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> MmjYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
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Assay
Methods Test Index PMID
Western blot p-AKT / AKT / p21 / p27 ; p-β-catenin / β-catenin ; FoxO3a / FoxO1 / p-FoxO3a / p-FoxO1 27510556 27211495
Immunofluorescence pAKT / p21 / p27 ; TNF-α ; E-cadherin / Nanog ; Oct3/4 27510556 24286133 25538040
Growth inhibition assay Cell proliferation 27510556
In vivo BIO suppresses melanoma tumor growth in a mouse xenograft model. [4]

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[4]
  • Animal Models: mouse
  • Dosages: 50 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 356.17
Formula

C16H10BrN3O2

CAS No. 667463-62-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04276857 Not yet recruiting Device: Irreversible electroporation (NanoKnife® ) Locally Advanced Pancreatic Cancer|Irreversible Electroporation University of Saskatchewan April 1 2022 Not Applicable
NCT04461301 Not yet recruiting Procedure: Multimodal Prehabilitation Frail Elderly Syndrome|Major Surgery University Hospital Inselspital Berne|University of Bern February 1 2022 Not Applicable
NCT05085730 Not yet recruiting Device: InMode Morpheus8 System Aging University of Texas Southwestern Medical Center February 1 2022 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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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