BIO

Catalog No.S7198 Synonyms: GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime

BIO Chemical Structure

Molecular Weight(MW): 356.17

BIO 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.

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1 Customer Review

  • 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.

Purity & Quality Control

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Biological Activity

Description BIO 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.
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
human SH-SY5Y cells Mn\qSpVv[3Srb36gZZN{[Xl? NGT2c2VKdmirYnn0bY9vKG:oIFfTT|MudWWmaXH0[YQh[mW2YT3jZZNmcW5icHjvd5Bpd3K7bHH0bY9vKGmwIHj1cYFvKFOKLWPZOXkh[2WubIOgbY4heHKnc3XuZ4Uhd2ZiTVexN|Ih[nliV3XzeIVzdiCkbH;0JIFv[Wy7c3nzMEBKSzVyPUCuNlkh|ryP MUmxPFgyPjFzMB?=
human K562 cells MlHSVJJwdGmoZYLheIlwdiCjc4PhfS=> MVi3NkBp MoXwRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS5|IN88US=> MXSxPVc5OzF2OR?=
human IMR90 cells MYDQdo9tcW[ncnH0bY9vKGG|c3H5 NH[wRZQ4OiCq MofORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCLTWK5NEBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTFwOTFOwG0> MW[xPVc5OzF2OR?=
human HCT116 cells NUmzPWVyWHKxbHnm[ZJifGmxbjDhd5NigQ>? NVnQRWdtPzJiaB?= MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEiFVEGxOkBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTVwMjFOwG0> NVTtN3J1OTl5OEOxOFk>
human HL60 cells NEP0V5pRem:uaX\ldoF1cW:wIHHzd4F6 NEjIUGE2KGSjeYO= NGPtTlZCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjMOlAh[2WubIOgZYZ1\XJiNTDkZZl{KGK7IF3UWEBie3OjeR?= MXyxPVc5OzF2OR?=
human HuH7 cells M4W3[HBzd2yrZnXyZZRqd25iYYPzZZk> NH3yWok4OiCq MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEi3SEegZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigQ>? NUXYVGs4OTl5OEOxOFk>
human SH-SY5Y cells Mom3R5l1d3SxeHnjxsBie3OjeR?= MoftOFghcA>? MWfDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDTTE1UYTW\IHPlcIx{KGGodHXyJFQ5KGi{czDifUBOXFNicnXkeYN1cW:wIHHzd4F6NCCLQ{WwQVkh|ryP NGfXTosyQDhzNkGxNC=>
human NB39 cells MV;DfZRwfG:6aXRCpIF{e2G7 MmrVOFghcA>? MVrDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDORlM6KGOnbHzzJIF{e2W|c3XkJIF{KGOnbHygeoli[mmuaYT5JIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYm= MnHaNlE5ODJ7NEe=
human SK-N-SH cells NFTyZ4pEgXSxdH;4bYPDqGG|c3H5 MVm0PEBp M4rQOmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHNMNU5vU1igZ4VtdHNiYYPz[ZN{\WRiYYOgZ4VtdCC4aXHibYxqfHliYX\0[ZIhPDhiaILzJIJ6KE2WVDDhd5NigQ>? MnHqNlE5ODJ7NEe=
mouse HT22 cells NYTmT2ZSTnWwY4Tpc44h[XO|YYm= M124eFExKM7:TR?= M{\QcVI1KGh? M13kOWlvcGmkaYTpc44hd2ZiR2PLN{1u\WSrYYTl[EBj\XSjIHPhd4VqdiCyaH;zdIhwenmuYYTpc44hcW5ibX;1d4UhUFR{MjDj[YxteyCjdDCxNEB2VSCjZoTldkAzPCCqcoOgZpkhX2W|dHXyckBjdG:2IHHuZYx6e2m|IHnuJJBz\XOnbnPlJI9nKE2JMUOy MWOyNlk6QDR2Mx?=
HEK293 cells NX;IfotoTnWwY4Tpc44h[XO|YYm= M2\qZVAvPS1zIN88US=> MmTNTY5pcWKrdHnvckBw\iCqdX3hckBIW0t|IHHjeIl3cXS7IHnuJGhGUzJ7MzDj[YxteyClb370ZYlvcW6pIITo[UBYdnRxYnX0ZU1k[XSnbnnuJIFkfGm4YYTl[EBz\XCxcoTldkBxW3WyZYLUU3BHVEGVSDCoV3RHOjl|IHPlcIx{MSCjdDCwMlUhfG9iMTD1UUBjgSCZboSgdoVxd3K2ZYKg[4Vv\SCjc4PhfS=> MmDENlQ3QTd{NES=

... Click to View More Cell Line Experimental Data

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

Protocol

Kinase Assay:[1]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: mouse
  • Formulation: freshly prepared in 30% Solutol (Basf) at a concentration of 10 mg/mL.
  • Dosages: 50 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 71 mg/mL (199.34 mM)
Ethanol 6 mg/mL (16.84 mM)
Water Insoluble
In vivo Add solvents individually and in order:
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.

Chemical Information

Molecular Weight 356.17
Formula

C16H10BrN3O2

CAS No. 667463-62-9
Storage powder
Synonyms GSK-3 Inhibitor IX, 6-bromoindirubin-3-oxime

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 (g) = Concentration (mol/L) × Volume (L) × 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).

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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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Molecular Weight Calculator

Molecular Weight Calculator

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Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02991495 Not yet recruiting Yellow Fever Epicentre April 2017 Phase 4
NCT03022708 Not yet recruiting Heart Defect, Congenital Xeltis March 2017 --
NCT03025516 Not yet recruiting Pulmonary TB|Diagnoses Diseases Find|Universidad Peruana Cayetano Heredia|University of Cape Town March 2017 --
NCT03044002 Not yet recruiting Peripheral Artery Disease|Access Site Complication|Outpatient Treatment Biotronik AG February 2017 --
NCT02753439 Not yet recruiting Impacted Third Molar Tooth The Baruch Padeh Medical Center, Poriya|Geistlich Pharma AG February 2017 --
NCT03008616 Not yet recruiting Severe Preeclampsia Velo Bio, LLC February 2017 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