Bisindolylmaleimide I (GF 109203X)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.
  • y_2019, m_9, d_23, h_9
  • bvseo_bulk, prod_bvrr, vn_bulk_2.0.13
  • cp_1, bvpage1
  • co_hasreviews, tv_0, tr_1
  • loc_en_US, sid_24003, prod, sort_[SortEntry(order=SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getAggregateRating, 81ms
  • REVIEWS, PRODUCT
Synonym: 3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
Application: 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
* Refer to Certificate of Analysis for lot specific data (including water content).
Submit a review for this product and receive 15 CruzCredits

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 :
2396
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

Adobe Acrobat Reader is required to reliably view,
print and comment on PDF documents

Bisindolylmaleimide I (GF 109203X)  Product Citations

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

Citations 1 to 10 of 23 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: # 27590359  Sakamoto, K. et al. 2016. Eur. J. Pharmacol. 791: 213-220.

PMID: # 25851441  2015. Respiratory research. 16: 30.

PMID: # 25797437  Ma, XF. et al. 2015. Arch. Biochem. Biophys. 573: 52-8.

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

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

PMID: # 26546817  Liu, QF. et al. 2015. Biochem. Biophys. Res. Commun. 468: 617-21.

PMID: # 26084307  Matsuoka, H. et al. 2015. American journal of physiology. Cell physiology. 309: C251-63.

Citations 1 to 10 of 23 total
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getContent, 67ms
  • QUESTIONS, PRODUCT
  • bvseo-msg: The resource to the URL or file is currently unavailable.;
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
  • y_2019, m_9, d_23, h_9
  • bvseo_bulk, prod_bvrr, vn_bulk_2.0.13
  • cp_1, bvpage1
  • co_hasreviews, tv_0, tr_1
  • loc_en_US, sid_24003, prod, sort_[SortEntry(order=SUBMISSION_TIME, direction=DESCENDING)]
  • clientName_scbt
  • bvseo_sdk, java_sdk, bvseo-3.2.0
  • CLOUD, getReviews, 43ms
  • REVIEWS, PRODUCT

Santa Cruz Biotechnology, Inc. is a world leader in the development of products for the biomedical research market. Call us Toll Free at 1-800-457-3801.
Copyright © 2007-2019 Santa Cruz Biotechnology, Inc. All Rights Reserved. "Santa Cruz Biotechnology", and the Santa Cruz Biotechnology, Inc. logo, "Santa Cruz Animal Health", "San Juan Ranch", "Supplement of Champions", the San Juan Ranch logo, "Ultracruz", "Chemcruz", "Immunocruz", "Exactacruz", and "EZ Touch" are registered trademarks of Santa Cruz Biotechnology, Inc.
All trademarks are the property of their respective owners.