Bisindolylmaleimide I (GF 109203X) CAS: 133052-90-1
MF: C25H24N4O2
MW: 412.48
A highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3.

Bisindolylmaleimide I (GF 109203X) (CAS 133052-90-1)

Bisindolylmaleimide I (GF 109203X) | CAS 133052-90-1 is rated 5.0 out of 5 by 1.
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Alternate Names: 3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
Application: Bisindolylmaleimide I (GF 109203X) is a highly selective inhibitor of all PKC isoforms and slight inhibitor of GSK-3
CAS Number: 133052-90-1
Purity: ≥98%
Molecular Weight: 412.48
Molecular Formula: C25H24N4O2
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data (including water content).
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Bisindolylmaleimide I (GF 109203X) is a staurosporine (sc-3510) inspired molecule, which has been shown to display equally potent inhibition, but with vastly superior selectivity, for all of the known isoforms of PKC (IC50 = 8-20 nM). Inhibition is competitive with respect to ATP, which suggests that Bisindolylmaleimide I occupies the ATP binding domain of the PKC isoforms. Bisindolylmaleimide I (GF 109203X) has been used to selectively probe for PKC-mediated pathways for transduction of hormone, cytokine, and growth factor signals. It inhibits PKC within intact platelets and T cells, Fas-mediated apoptosis, and T cell-mediated autoimmune diseases, as well as GSK-3. See sc-24004 for water soluble form of Bisindolylmaleimide I. Bisindolylmaleimide I (GF 109203X) is an inhibitor of PHK/CaM, PKC α, PKC β, PKC δ, PKC ε, PKC γ and SR/HTR3.


References

1. Toullec, D., et al. 1991. J. Biol. Chem. 266: 15771-15781. PMID: 1874734
2. Martiny-Baron, G., et al. 1993. J. Biol. Chem. 268: 9194-9197. PMID: 8486620
3. Kiss, Z., et al. 1995. Biochim. Biophys. Acta. 1265: 93-95. PMID: 7857990
4. Zhou, T., et al. 1999. Nat. Med. 5: 42-48. PMID: 9883838

Physical State :
Solid
Solubility :
Soluble in DMSO (~1 mg/ml), DMF (10 mg/ml; warm to 40°C & vortex well), and 1:10 DMSO:PBS (pH 7.2) (~0.1 mg/ml). Insoluble in water.
Storage :
Store at -20° C
Melting Point :
328.06° C (Predicted)
Boiling Point :
~685.64° C at 760 mmHg (Predicted)
Density :
~1.31 g/cm3 (Predicted)
Refractive Index :
n20D 1.69 (Predicted)
IC50 :
GSK-3: IC50 = 360 nM; GSK-3β: IC50 = 170 nM; Phosphorylase Kinase: IC50 = 700 nM; cAMP-Dependent Protein Kinase: IC50 = 2000 nM; Protein kinase C α isoforms: IC50 = 8.4 nM; Protein kinase C β1 isoforms: IC50 = 18 nM; Protein kinase C δ isoforms: IC50 = 210 nM; Protein kinase C ε isoforms: IC50 = 132 nM; Protein kinase C ζ isoforms: IC50 = 5.8 µM; MLCK: IC50 = 0.6 µM; PKG: IC50 = 4.6 µM; PKA: IC50 = 33 µM
Ki Data :
PKA: Ki= 2 mM; 5-HT3 receptor: Ki= 29.5 nM; PKC: Ki= 14 nM
pK Values :
pKa: 8.13 (Predicted), pKb: 9.61 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
MDL Number :
MFCD00236428
SMILES :
CN(C)CCCN1C=C(C2=CC=CC=C21)C3=C(C(=O)NC3=O)C4=CNC5=CC=CC=C54

Download SDS (MSDS)

Certificate of Analysis

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Bisindolylmaleimide I (GF 109203X) (CAS 133052-90-1)  Product Citations

See how others have used Bisindolylmaleimide I (GF 109203X) (CAS 133052-90-1). Click on the entry to view the PubMed entry .

Citations 1 to 10 of 32 total

PMID: # 30783129  Klarström Engström, K. et al. 2019. Sci Rep. 9: 2296.

PMID: # 29626608  Gao, K.|Wang, P.|Peng, J.|Xue, J.|Chen, K.|Song, Y.|Wang, J.|Li, G.|An, X.|Cao, B.| et al. 2018. J. Steroid Biochem. Mol. Biol. 181: 98-108.

PMID: # 28120492  Palm, E. et al. 2017. APMIS. 125: 157-169.

PMID: # 27630226  Wu, S. et al. 2016. J. Virol. 90: 10414-10422.

PMID: # 27338016  Shen, J. et al. 2016. J. Pathol. 240: 149-60.

PMID: # 27590359  Sakamoto, K. et al. 2016. Eur. J. Pharmacol. 791: 213-220.

PMID: # 26054746  Peng, J. et al. 2015. Mol. Cell. Endocrinol. 412: 104-15.

PMID: # 25529920  2015. Journal of lipid research. 56: 546-61.

PMID: # 26890419  Tabeling, C.|Noe, E.|Naujoks, J.|Doehn, JM.|Hippenstiel, S.|Opitz, B.|Suttorp, N.|Klopfleisch, R.|Witzenrath, M.| et al. 2015. J Vasc Res. 52: 279-88.

PMID: # 25700266  Peng, JY. et al. 2015. Domest. Anim. Endocrinol. 52: 1-10.

Citations 1 to 10 of 32 total
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Rated 5 out of 5 by from Denning Denning, et. al. (PubMed ID 9624138) used GF109203X, an inhibitor of PKC, was used to study how PKC is involved in the activation of ERKs. -SCBT Publication Review
Date published: 2015-02-17
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