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402081

Sigma-Aldrich

Indirubin Derivative E804 - CAS 854171-35-0 - Calbiochem

Synonym(s):

Indirubin Derivative E804 - CAS 854171-35-0 - Calbiochem, IDR E804

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About This Item

Empirical Formula (Hill Notation):
C20H19N3O4
CAS Number:
Molecular Weight:
365.38
UNSPSC Code:
12352200

Assay

≥95% (HPLC)

Quality Level

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

dark red

solubility

DMSO: 200 mg/mL

shipped in

wet ice

storage temp.

−20°C

General description

This product has been discontinued.



A cell-permeable indirubin derivative (IDR) that blocks the Src-Stat3 signaling pathway and displays anti-tumor properties. Shown to be a potent, reversible, and ATP-competitive inhibitor of the kinase activities of Src (IC50 = 430 nM), Cdk1/cyclin E (IC50 = 210 nM), Cdk2/cyclin A (IC50 = 540 nM), and Cdk1/cyclin B (IC50 = 1.65 µM). Reduces the tyrosine phosphorylation levels of Src, JAK1, and Stat3 in MDA-MB-468 cells in a time- and dose-dependent manner. Selectively induces apoptosis in cells expressing high levels of active Stat3, but not cells lacking activated Stat3. The apoptotic effect of E804 is shown to be due to the down-regulation of antiapoptotic proteins Mcl-1 and survivin.

A cell-permeable indirubin derivative (IDR) that blocks the Src-Stat3 signaling pathway and displays anti-tumor properties. Shown to be a potent, reversible, and ATP-competitive inhibitor of the kinase activities of Src (IC50 = 430 nM), Cdk1/cyclin E (IC50 = 210 nM), Cdk2/cyclin A (IC50 = 540 nM), and Cdk1/cyclin B (IC50 = 1.65 µM). Reduces the tyrosine phosphorylation levels of Src, JAK1, and Stat3 in MDA-MB-468 cells in a time- and dose-dependent manner. Selectively induces apoptosis in cells expressing high levels of active Stat3, but not cells lacking activated Stat3. The apoptotic effect of E804 is shown to be due to the down-regulation of antiapoptotic proteins Mcl-1 and survivin.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Src
Product competes with ATP.
Reversible: yes
Target IC50: 430 nM, 210 nM, 540 nM, 1.65 µM, against Src, Cdk1/cyclin E, Cdk2/cyclin A, and Cdk1/cyclin B, respectively

Packaging

Packaged under inert gas

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Nam, S., et al. 2005. Proc. Natl. Acad. Sci. USA102, 5998.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Storage Class Code

10-13 - German Storage Class 10 to 13


Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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