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Chemical Structure| 133052-90-1 Chemical Structure| 133052-90-1

Structure of Bisindolylmaleimide I
CAS No.: 133052-90-1

Chemical Structure| 133052-90-1

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GF109203X is a potent PKC inhibitor with IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ in cell-free assays, respectively, showing more than 3000-fold selectivity for PKC as compared to EGFR, PDGFR and insulin receptor.

Synonyms: Go 6850; GF109203X; GO6850. BIMI.

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Product Details of Bisindolylmaleimide I

CAS No. :133052-90-1
Formula : C25H24N4O2
M.W : 412.48
SMILES Code : O=C(N1)C(C2=CN(CCCN(C)C)C3=C2C=CC=C3)=C(C4=CNC5=C4C=CC=C5)C1=O
Synonyms :
Go 6850; GF109203X; GO6850. BIMI.
MDL No. :MFCD00236428
InChI Key :QMGUOJYZJKLOLH-UHFFFAOYSA-N
Pubchem ID :2396

Safety of Bisindolylmaleimide I

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H351
Precautionary Statements:P201-P202-P280-P308+P313-P405-P501

Related Pathways of Bisindolylmaleimide I

epigenetics
GPCR

Isoform Comparison

Biological Activity

Target
  • PKCβ

    PKCβ2, IC50:16 nM

    PKCβ1, IC50:17 nM

  • PKCγ

    PKCγ, IC50:20 nM

  • PKCα

    PKCα, IC50:20 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
KS483 cells 10 μmol/L 1 hour BIM significantly triggered cytosolic β-catenin accumulation PMC4875475
C2C12 cells 5 μmol/L 4 days BIM dose-dependently increased ALP activity and elevated osteogenic marker gene expression PMC4875475
rat distal colonic epithelium 25 nM 15 minutes Inhibited 17β-estradiol-induced PKA activity but did not affect cAMP-stimulated PKA activity PMC1571973

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.12mL

2.42mL

1.21mL

24.24mL

4.85mL

2.42mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

References

 

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