BIO 667463-62-9

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Molecular Weight: 356.17 BIO (6-bromoindirubin-3'-oxime) is a specific inhibitor of GSK-3 with IC50 of 5 nM for GSK-3α/β, shows >16-fold selectivity over CDK5, also a pan-JAK Inhibitor.


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. 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. BIO promotes proliferation in mammalian cardiomyocytes. 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.


BIO suppresses melanoma tumor growth in a mouse xenograft model.


The first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells.

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 Assay: [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 Study: [4]

Animal Models	mouse
Formulation	freshly prepared in 30% Solutol (Basf) at a concentration of 10 mg/mL.
Dosages	50 mg/kg
Administration	Oral gavage
Solubility	30% PEG400/0.5% Tween80/5% propylene glycol, 30 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	356.17
Formula	C16H10BrN3O2
CAS No.	667463-62-9

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime

Solubility (25°C) *	In vitro	DMSO	71 mg/mL (199.34 mM)
		Water	<1 mg/mL (
		Ethanol	21 mg/mL (58.96 mM)
	In vivo	30% PEG400/0.5% Tween80/5% propylene glycol	30 mg/mL
* <1 mg/ml means slightly soluble or insoluble. * 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 Name	2H-Indol-2-one, 6-bromo-3-[(3E)-1,3-dihydro-3-(hydroxyimino)-2H-indol-2-ylidene]-1,3-dihydro-, (3Z)-

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