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402081 Indirubin Derivative E804 - CAS 854171-35-0 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: IDR E804

Primary Target: Src
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
854171-35-0C₂₀H₁₉N₃O₄
Description
Overview

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.
Catalogue Number402081
Brand Family Calbiochem®
SynonymsIDR E804
References
ReferencesNam, S., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 5998.
Product Information
CAS number854171-35-0
ATP CompetitiveY
FormDark red solid
Hill FormulaC₂₀H₁₉N₃O₄
Chemical formulaC₂₀H₁₉N₃O₄
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetSrc
Primary Target IC<sub>50</sub>430 nM, 210 nM, 540 nM, 1.65 µM, against Src, Cdk1/cyclin E, Cdk2/cyclin A, and Cdk1/cyclin B, respectively
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Shipped with Blue Ice or with Dry Ice
Toxicity Standard Handling
Storage -20°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
402081 0

Documentation

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

Title

Safety Data Sheet (SDS) 

Indirubin Derivative E804 - CAS 854171-35-0 - Calbiochem Certificates of Analysis

TitleLot Number
402081

References

Reference overview
Nam, S., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 5998.

Brochure

Title
An Introduction to Inhibitors and Their Biological Applications - 1st Edition

Technical Info

Title
JAK/STAT Signaling Research Focus
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision13-April-2011 RFH
SynonymsIDR E804
DescriptionA 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.
FormDark red solid
Intert gas (Yes/No) Packaged under inert gas
CAS number854171-35-0
Chemical formulaC₂₀H₁₉N₃O₄
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (200 mg/ml)
Storage Protect from light
-20°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesNam, S., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 5998.