Name: BIO
Brand: Selleck Chemicals
SKU: S7198
Rating: 5 (27 reviews)

CAS No. 667463-62-9

Selleck's BIO has been cited by 27 publications

Purity & Quality Control

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GSK-3 Signaling Pathway Map

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)	Click to View More Targets
5 nM	30 nM	0.08 μM	0.30 μM	0.32 μM	Click to View More Targets

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	MX\GeY5kfGmxbjDhd5NigQ>?			NWTzZphYWHKxdHXjeIlwdiCjZ3HpcpN1KGOrc4DsZZRqdi2rbnT1Z4VlKGOnbHyg[IVifGhiaX6gcoVwdmG2YXygcY92e2ViSFXJMW9EOSClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4F{eGG\|ZT2zM\|ch[WO2aY\peJktKEWFNUCgQUAxNjF7MjFOwG0v	MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODB7MUmxOUc,OzByOUG5NVU9N2F-
SH-SY5Y	MnnuSpVv[3Srb36gZZN{[Xl?			NGrLZ5FKdmirYnn0bY9vKG:oIFfTT\|MudWWmaXH0[YQh[mW2YT3jZZNmcW5icHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFOKLWPZOXkh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiTVexN\|Ih[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nzMEBKSzVyIE2gNE4zQSEQvF2u	NYDYN5BTRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi4NVYyOTBpPkG4PFE3OTFyPD;hQi=>
K562	NYrZPFM1SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MWe3NkBpenN?	MlvNRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCNNU[yJINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSBzLkOg{txONg>?	MkLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl5OEOxOFkoRjF7N{izNVQ6RC:jPh?=
IMR90	MVPBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>?		NIrUbFA4OiCqcoO=	M2q0bmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSV3SPVAh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OCB;IEGuPUDPxE1w	MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd6M{G0PUc,OTl5OEOxOFk9N2F-
HCT116	Mni4RY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl?		MVq3NkBpenN?	NFW0fFVCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG\|c3H5MEBKSzVyIE2gOU4zKM7:TT6=	NX[2SVJFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm3PFMyPDlpPkG5O\|g{OTR7PD;hQi=>
HepG2	M4\zc2N6fG:2b4jpZ4l1gSCjc4PhfS=>		M3fLflI1KGi{cx?=	NXHRVJc6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUGWyR{KgZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCCpcn;3eIghcW6qaXLpeIlwdiCjZoTldkAzPCCqcoOgZpkh[WyjbXHyJIJtfWViYYPzZZktKEmFNUCgQUA2NjNizszNMi=>	MkXRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5NEO0PVIoRjJ6N{SzOFkzRC:jPh?=
HL60	NU\mN3Q5SW62aYDyc4xq\mW{YYTpeoUh[XO\|YYm=		MVi1JIRigXN?	MnfhRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKTE[wJINmdGy\|IHHmeIVzKDViZHH5d{BjgSCPVGSgZZN{[XluIFnDOVAhRSB3LkSg{txONg>?	M1H1[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7N{izNVQ6Lz5zOUe4N\|E1QTxxYU6=
HuH7	M3;ieGFvfGmycn;sbYZmemG2aY\lJIF{e2G7		NGH2WHA4OiCqcoO=	Mlj5RY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6\|dDDoeY1idiCKdVi3JINmdGy\|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVAhRSB4LkKg{txONg>?	MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTd6M{G0PUc,OTl5OEOxOFk9N2F-
SH-SY5Y	MkjUR5l1d3SxeHnjbZR6KGG\|c3H5		M37sWFQ5KGi{cx?=	MlnWR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gV2guW1l3WTDj[YxteyCjZoTldkA1QCCqcoOgZpkhVVSVIILl[JVkfGmxbjDhd5NigSxiSVO1NEA:KDlizszNMi=>	MnqwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh6MU[xNVAoRjF6OEG2NVExRC:jPh?=
SH-SY5Y	MXzGeY5kfGmxbjDhd5NigQ>?		MUO0PEBpenN?	NXjad\|Z7W3W{dnn2ZYwhd2ZiaIXtZY4hW0hvU2m1XUBk\WyuczDh[pRmeiB2ODDodpMh[nliTWTTJJJm\HWldHnvckBie3OjeTygTWM2OCB;IEmuOUDPxE1w	M4HKelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEW0NFY6Lz5zNki1OFA3QTxxYU6=
SH-SY5Y	MVnGeY5kfGmxbjDhd5NigQ>?			NYPjXJdHTGWjdHigc4YhcHWvYX6gV2guW1l3WTDj[YxteyCrbjDhZpNmdmOnIH;mJFIxKHWPIGGtWmQuV1CqIHL5JG1VWyC{ZXT1Z5Rqd25iYYPzZZktKEmFNUCgQUAyOCEQvF2u	NYXBV3BJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4OVQxPjlpPkG2PFU1ODZ7PD;hQi=>
SH-SY5Y	MkPUSpVv[3Srb36gZZN{[Xl?			M2iyTGRm[XSqIH;mJIh2dWGwIGPIMXN[PVliY3XscJMhcW5icILld4Vv[2Vib3[gNlAhfU1iUT3WSE1QWGhiYomgUXRUKHKnZIXjeIlwdiCjc4PhfUwhUUN3MDC9JFE{KM7:TT6=	NXTm[5RyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[4OVQxPjlpPkG2PFU1ODZ7PD;hQi=>
SH-SY5Y	NXLWPGxqTnWwY4Tpc44h[XO\|YYm=		NETwbZMzPCCqcoO=	MXvTeZJ3cX[jbDDv[kBpfW2jbjDTTE1UYTW\IHPlcIx{KGGodHXyJFI1KGi{czDifUBOXFNicnXkeYN1cW:wIHHzd4F6NCCLQ{WwJF0hOThizszNMi=>	M2OyTlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF4OEW0NFY6Lz5zNki1OFA3QTxxYU6=
IMR32	Mnz6R5l1d3SxeHnjbZR6KGG\|c3H5		NIn0SY81QCCqcoO=	MWDDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDJUXI{OiClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC0PEBpenNiYomgUXRVKGG\|c3H5	NFe3Xoc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUiwNlk1Pyd-MkG4NFI6PDd:L3G+
SK-N-SH	MlvMR5l1d3SxeHnjbZR6KGG\|c3H5		MX60PEBpenN?	NH\1d29EgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBUUy2QLWPIJINmdGy\|IHHzd4V{e2WmIHHzJINmdGxidnnhZoltcXS7IHHmeIVzKDR6IHjyd{BjgSCPVGSgZZN{[Xl?	MoryQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF6MEK5OFcoRjJzOECyPVQ4RC:jPh?=
NB39	NWmwe2dXS3m2b4TvfIlkcXS7IHHzd4F6		NHrC[oc1QCCqcoO=	M37X[GN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJG5DOzliY3XscJMh[XO\|ZYPz[YQh[XNiY3XscEB3cWGkaXzpeJkh[W[2ZYKgOFghcHK\|IHL5JG1VXCCjc4PhfS=>	MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOThyMkm0O{c,OjF6MEK5OFc9N2F-
A673	M4fMOpFJXFNiYYPzZZk>			NW\zN\|VxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFG2O\|Mh[2WubIO=	MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
DAOY	MlLvdWhVWyCjc4PhfS=>			NYKyR\|hGeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO=	NWTWZYFXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2	M4XHSZFJXFNiYYPzZZk>			M3:y[JFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	MVe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
BT-37	MX\xTHRUKGG\|c3H5			NFKzXVRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN\|ch[2WubIO=	M1vrb\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD	MWDxTHRUKGG\|c3H5			M4L0NpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCURDDj[Yxtew>?	NY\HXXVHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH	M1vTbZFJXFNiYYPzZZk>			NVLzdlZleUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM>	M3rxXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12	NV;NOG9OeUiWUzDhd5NigQ>?			MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN?	M363blxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R)	MULxTHRUKGG\|c3H5			M1zoV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?=	MnfoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
NB1643	NIfkcJFyUFSVIHHzd4F6			M4DZPJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO=	M1HuS\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
OHS-50	MXTxTHRUKGG\|c3H5			NULxUGZNeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=>	MmDMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
Rh41	M4fzZZFJXFNiYYPzZZk>			MUfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>?	NIDuT4Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N\|UyOzl:L3G+
Rh30	NEHkS4RyUFSVIHHzd4F6			MYHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh\|MDDj[Yxtew>?	M1vB[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2	NHP1bldyUFSVIHHzd4F6			NH;iPFJyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=>	M3u0TlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC	NX3sXIlEeUiWUzDhd5NigQ>?			NUD6OWMyeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM>	MVW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
NB-EBc1	MWnxTHRUKGG\|c3H5			NWfjVZhieUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM>	MoP6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
LAN-5	MXTxTHRUKGG\|c3H5			MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN?	M13Ze\|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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Click to View More Cell Line Experimental Data

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

References

[4] Liu L, et al. Cancer Res. 2011 Jun 1;71(11):3972-3279.

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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. Click to purchase: PEG300 Tween 80	3 mg/mL

Chemical Information

Molecular Weight	356.17
Formula	C₁₆H₁₀BrN₃O₂
CAS No.	667463-62-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	C1=CC=C2C(=C1)C(=C(N2)C3=C(NC4=C3C=CC(=C4)Br)O)N=O

Download BIO SDF

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:μL Number of animals:

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

Dilution Calculator Molecular Weight Calculator

Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05447351	Not yet recruiting	--	Overweight and Obesity\|Cardiovascular Diseases\|Metabolic Syndrome\|Non-Alcoholic Fatty Liver Disease	University of Bari	January 2023	--
NCT05456997	Not yet recruiting	Procedure: Muscle biopsy	Cushing Syndrome\|Pheochromocytoma\|Conns Syndrome\|Metabolic Myopathy	Barts & The London NHS Trust\|Imperial College London\|Queen Mary University of London	October 2022	--
NCT05415358	Not yet recruiting	Other: Biomarkers and ctDNA	Lung	Wake Forest University Health Sciences	September 2022	Not Applicable
NCT05472532	Not yet recruiting	Procedure: Patient sampling.	Cancer Metastatic\|Prostate Cancer\|Breast Cancer\|Lung Cancer\|Ovarian Cancer\|Gastric Cancer	Hospices Civils de Lyon	September 1 2022	Not Applicable
NCT04276857	Not yet recruiting	Device: Irreversible electroporation (NanoKnife® )	Locally Advanced Pancreatic Cancer\|Irreversible Electroporation	University of Saskatchewan	September 1 2022	Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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