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GSK-3 Inhibitor IX (BIO)

GSK-3α/GSK-3β inhibitor, cell-permeable, ATP-competitive and reversible CAS# 667463-62-9

GSK-3 Inhibitor IX (BIO)

Catalog No. BCC4510----Order now to get a substantial discount!

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Quality Control of GSK-3 Inhibitor IX (BIO)

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Chemical structure

GSK-3 Inhibitor IX (BIO)

3D structure

Chemical Properties of GSK-3 Inhibitor IX (BIO)

Cas No. 667463-62-9 SDF Download SDF
PubChem ID 5287844 Appearance Powder
Formula C16H10BrN3O2 M.Wt 356.17
Type of Compound N/A Storage Desiccate at -20°C
Synonyms 6BIO
Solubility DMSO : ≥ 23 mg/mL (64.58 mM)
H2O : < 0.1 mg/mL (insoluble)
*"≥" means soluble, but saturation unknown.
Chemical Name (3Z)-6-bromo-3-[3-(hydroxyamino)indol-2-ylidene]-1H-indol-2-one
SMILES C1=CC2=C(C(=C3C4=C(C=C(C=C4)Br)NC3=O)N=C2C=C1)NO
Standard InChIKey WNWSUJQVZJJGLF-SQFISAMPSA-N
Standard InChI InChI=1S/C16H10BrN3O2/c17-8-5-6-9-12(7-8)19-16(21)13(9)15-14(20-22)10-3-1-2-4-11(10)18-15/h1-7,20,22H,(H,19,21)/b15-13-
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of GSK-3 Inhibitor IX (BIO)

DescriptionPotent and selective, ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC50 values are 5, 83, 300, 320 and > 10 000 nM at GSK-3, CDK5/p25, CDK2/cyclin A, CDK1/cyclin B and other common kinases respectively). Maintains self-renewal and pluripotency in embryonic stem cells via activation of the Wnt signaling pathway in vitro; also promotes proliferation and dedifferentiation in cardiomyocytes. Negative control available.

GSK-3 Inhibitor IX (BIO) Dilution Calculator

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Preparing Stock Solutions of GSK-3 Inhibitor IX (BIO)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.8076 mL 14.0382 mL 28.0765 mL 56.153 mL 70.1912 mL
5 mM 0.5615 mL 2.8076 mL 5.6153 mL 11.2306 mL 14.0382 mL
10 mM 0.2808 mL 1.4038 mL 2.8076 mL 5.6153 mL 7.0191 mL
50 mM 0.0562 mL 0.2808 mL 0.5615 mL 1.1231 mL 1.4038 mL
100 mM 0.0281 mL 0.1404 mL 0.2808 mL 0.5615 mL 0.7019 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on GSK-3 Inhibitor IX (BIO)

GSK-3 inhibitor IX (BIO) is a potent, selective, cell-permeable, ATP-competitive and reversible inhibitor of GSK-3α (glycogen synthase kinase-3α) and GSK-3β (lycogen synthase kinase-3β) (IC50 = 5nM for GSK-3β). [1]

GSK3 (glycogen synthase kinase-3) is a serine/threonine protein kinase which contributes to cell survival, diabetes, insulin resistance and Alzheimer's diseases. It is contributed to β-catenin/Wnt signaling pathway.

BIO facilitated the proliferation in mammalian cardiomyocytes by increasing the proliferation potential of cardiomyocytes. It induced S phase entry and beta-catenin activity in neonatal cardiomyocyte. [3] BIO also activated Wnt signaling and involved in maintaining pluripotency in human and mouse ESCs (embryonic stem cells). [2] In Cos-1 cells treated with 5 μm BIO for 24 hours, phosphorylation of β-catenin was inhibited on GSK-3 specific sites. In cell line deficient for AhR or ARNT, 10 μm BIO treatment for 24 hours showed its effect is through a direct and AhR- independent pathway.[1]

In vivo study showed BIO activated maternal Wnt signaling pathway in Xenopus embryos. It caused a hyper dorso-anteriorization at the expense of trunk and tail in a dose-response manner. It also activated the dorsal genes (siamois and chordin) ectopically. [1]

References:
[1] Meijer L, Skaltsounis AL, Magiatis P, Polychronopoulos P, Knockaert M, Leost M, Ryan XP, Vonica CA, Brivanlou A, Dajani R, Crovace C, Tarricone C, Musacchio A, Roe SM, Pearl L, Greengard P.  GSK-3-selective inhibitors derived from Tyrian purple indirubins.  Chem Biol. 2003 Dec;10(12):1255-66.
[2] Sato N, Meijer L, Skaltsounis L, Greengard P, Brivanlou AH.  Maintenance of pluripotency in human and mouse embryonic stem cells through activation of Wnt signaling by a pharmacological GSK-3-specific inhibitor.  Nat Med. 2004 Jan;10(1):55-63. 
[3] Tseng AS, Engel FB, Keating MT.  The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes.  Chem Biol. 2006 Sep;13(9):957-63.

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References on GSK-3 Inhibitor IX (BIO)

The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes.[Pubmed:16984885]

Chem Biol. 2006 Sep;13(9):957-63.

The maintenance of self-renewal in stem cells appears to be distinct from the induction of proliferation of the terminally differentiated mammalian cardiomyocytes because it is believed that the latter are unable to divide. However, proliferation is a necessary step in both processes. Interestingly, the small molecule 6-bromoindirubin-3'-oxime (BIO) is the first pharmacological agent shown to maintain self-renewal in human and mouse embryonic stem cells. To determine whether a molecule that can maintain stem cell properties can also participate in controlling the proliferative capability of the highly differentiated cardiomyocytes, we examine the effect of BIO in postmitotic cardiac cells. Here, we show that BIO promotes proliferation in mammalian cardiomyocytes. Our demonstration of a second role for BIO suggests that the maintenance of stem cell self-renewal and the induction of proliferation in differentiated cardiomyocytes may share common molecular pathways.

Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases.[Pubmed:14761195]

J Med Chem. 2004 Feb 12;47(4):935-46.

Pharmacological inhibitors of glycogen synthase kinase-3 (GSK-3) and cyclin-dependent kinases have a promising potential for applications against several neurodegenerative diseases such as Alzheimer's disease. Indirubins, a family of bis-indoles isolated from various natural sources, are potent inhibitors of several kinases, including GSK-3. Using the cocrystal structures of various indirubins with GSK-3beta, CDK2 and CDK5/p25, we have modeled the binding of indirubins within the ATP-binding pocket of these kinases. This modeling approach provided some insight into the molecular basis of indirubins' action and selectivity and allowed us to forecast some improvements of this family of bis-indoles as kinase inhibitors. Predicted molecules, including 6-substituted and 5,6-disubstituted indirubins, were synthesized and evaluated as CDK and GSK-3 inhibitors. Control, kinase-inactive indirubins were obtained by introduction of a methyl substitution on N1.

GSK-3-selective inhibitors derived from Tyrian purple indirubins.[Pubmed:14700633]

Chem Biol. 2003 Dec;10(12):1255-66.

Gastropod mollusks have been used for over 2500 years to produce the "Tyrian purple" dye made famous by the Phoenicians. This dye is constituted of mixed bromine-substituted indigo and indirubin isomers. Among these, the new natural product 6-bromoindirubin and its synthetic, cell-permeable derivative, 6-bromoindirubin-3'-oxime (BIO), display remarkable selective inhibition of glycogen synthase kinase-3 (GSK-3). Cocrystal structure of GSK-3beta/BIO and CDK5/p25/indirubin-3'-oxime were resolved, providing a detailed view of indirubins' interactions within the ATP binding pocket of these kinases. BIO but not 1-methyl-BIO, its kinase inactive analog, also inhibited the phosphorylation on Tyr276/216, a GSK-3alpha/beta activation site. BIO but not 1-methyl-BIO reduced beta-catenin phosphorylation on a GSK-3-specific site in cellular models. BIO but not 1-methyl-BIO closely mimicked Wnt signaling in Xenopus embryos. 6-bromoindirubins thus provide a new scaffold for the development of selective and potent pharmacological inhibitors of GSK-3.

Description

GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.

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