GSK-3 Inhibitor IX CAS: 667463-62-9
MF: C16H10BrN3O2
MW: 356.17

GSK-3 Inhibitor IX (CAS 667463-62-9)

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Noms alternatifs: GSK-3 Inhibitor IX is also known as BIO.
Application: GSK-3 Inhibitor IX is a cell-permeable, highly potent, selective, reversible, and ATP-competitive inhibitor of GSK-3α and GSK-3β.
Numéro CAS: 667463-62-9
Pureté: >97%
Masse Moléculaire: 356.17
Formule Moléculaire: C16H10BrN3O2
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
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GSK-3 Inhibitor IX (BIO) is a cell-permeable, highly potent, selective, reversible, and ATP-competitive inhibitor of GSK-3α and GSK-3β (IC50 = 5 nM). GSK-3 (Glycogen synthase kinase-3) plays important roles in numerous signaling pathways that regulate a variety of cellular processes including cell proliferation, differentiation, apoptosis and embryonic development. GSK-3 Inhibitor IX also inhibits PKB Kinase (phosphoinositide-dependent kinase 1; PDK1 or PDPK1), a master kinase responsible for the activation of AKT/PKB, PKC, p70 S6 kinase (S6K) and SGK (serum/glucocorticoid regulated kinase). Research shows that PKB Kinase inhibition halts endothelial cell migration. GSK-3 Inhibitor IX has been been widely-used in embryonic stem cell studies to maintain human embryonic stem cells in their undifferentiated state, and to sustain expression of the pluripotent state-specific transcription factors Oct-3/4, Rex-1 and Nanog. GSK-3 Inhibitor IX has been shown to induce the differentiation of neonatal cardiomyocytes and maintain self-renewal in both human and mouse embryonic stem cells through wnt signaling activation.


Références

1. Meijer, Laurent., et al., 2003. GSK-3-selective inhibitors derived from Tyrian purple indirubins. Chemistry & biology. 10(12): 1255-66. PMID: 14700633

2. Polychronopoulos, Panagiotis., et al., 2004. Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. Journal of medicinal chemistry. 47(4): 935-46. PMID: 14761195

3. Tseng, Ai-Sun., et al., 2006. The GSK-3 inhibitor BIO promotes proliferation in mammalian cardiomyocytes. Chemistry & biology. 13(9): 957-63. PMID: 16984885

4. Zahler, Stefan., et al., 2007. Inverse in silico screening for identification of kinase inhibitor targets. Chemistry & biology. 14(11): 1207-14. PMID: 18022559

5. Xu, Chong., et al., 2009. Regulation of protein stability by GSK3 mediated phosphorylation. Cell cycle (Georgetown, Tex.). 8(24): 4032-9. PMID: 19923896

6. Rasola, Andrea., et al., 2010. Signal transduction to the permeability transition pore. FEBS letters. 584(10): 1989-96. PMID: 20153328

7. Spokoini, Rachel., et al., 2010. Glycogen synthase kinase-3 plays a central role in mediating glucocorticoid-induced apoptosis. Molecular endocrinology (Baltimore, Md.). 24(6): 1136-50. PMID: 20371704

8. Fairbairn, E.A. et al. 2012. Aquat. Toxicol. 124-125 : 188-196. PMID: 22975441

État Physique :
Solid
Solubilité :
Soluble in DMSO ( >5 mg/ml), ethanol (10 mM), DMF (10 mg/ml), and 1:2 DMSO:PBS (pH 7.2) (~0.3 mg/ml).
STOCKAGE :
Store at 4° C
Point d'Ébullition :
~554.26° C at 760 mmHg (Predicted)
Densité :
~1.80 g/cm3 (Predicted)
Indice de Réfraction :
n20D 1.80 (Predicted)
IC50 :
GSK-3α/β: IC50 = 5 nM; Cdk5/p25: IC50 = 83 nM; Cdk2/A: IC50 = 300 nM; Cdk1/B: IC50 = 320 nM; Cdk4/D1: IC50 = 10 µM
Valeurs pK :
pKa: 9.56 (Predicted)
Pour la Recherche Uniquement. Non conforme pour le Diagnostic ou pour une Utilisation Thérapeutique.
WGK Allemagne :
3
PubChem CID :
Numéro MDL :
MFCD08705318
SMILES :
C1=CC2=C(/C(=C/3\\C4=C(C=C(C=C4)Br)NC3=O)/N=C2C=C1)NO

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GSK-3 Inhibitor IX (CAS 667463-62-9)  Références bibliographiques

Consultez les publications faisant référence à l' utilisation de GSK-3 Inhibitor IX (CAS 667463-62-9). Cliquez sur le lien pour afficher lentrée PubMed .

Citations 1 à 9 sur un total de 9

PMID: # 30388586  2019. Spectrochim Acta A Mol Biomol Spectrosc. 209: 150-164.

PMID: # 30984989  2019. Turk Neurosurg. 29: 513-521.

PMID: # 30412805  2019. J Pharm Biomed Anal. 164: 317-325.

PMID: # 26831110  Iovino, S.|Burkart, AM.|Warren, L.|Patti, ME.|Kahn, CR.| et al. 2016. Proc. Natl. Acad. Sci. U.S.A. 113: 1889-94.

PMID: # 27997540  Li, Y. et al. 2016. PLoS Med. 13: e1002200.

PMID: # 26264578  Zhang, Y. et al. 2015. Human molecular genetics. 24: 6029-40.

PMID: # 22574208  Shao, M. et al. 2012. PLoS ONE. 7: e36655.

PMID: # 32430065  Biol. Res. 53: 22.

PMID: # 31088549  BMC Complement Altern Med. 104.

Citations 1 à 9 sur un total de 9
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