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220485 Chk2 Inhibitor - CAS 724708-21-8 - Calbiochem

The Chk2 Inhibitor, also referenced under CAS 724708-21-8, controls the biological activity of Chk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

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

Synonyms: 5-(2-Amino-5-oxo-1,5-dihydroimidazol-4-ylidine)-3,4,5,10-2H-azepino[3,4-b]indol-1-one, Chk1 Inhibitor II, Chk2 Inhibitor I

Primary Target: Chk2
220485
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
724708-21-8C₁₅H₁₃N₅O₂

Products

Catalogue NumberPackaging Qty/Pack
220485-500UG Plastic ampoule 500 μg
Description
OverviewA cell-permeable, ATP competitive, and reversible indoloazepine compound that displays anti-proliferative and anti-inflammatory properties. Acts as a potent inhibitor of Chk2 (IC50 = 8 nM) that targets the ATP binding pocket. Exhibits selectivity for Chk2 over MEK1, Chk1, CK1δ, PKCα, PKCβII and CK2 (IC50 = 89 nM, 237 nM, 1.352 µM, 2.539 µM, 3.381 µM, and > 10.0 µM, respectively). Blocks the production of IL-2 and TNF-α by preventing the transcriptional activation of NF-κB (IC50 = 3.55 µM for IL-2 production in PMA-stimulated Jurkat T cells; 8.16 µM for TNF-α production in LPS-stimulated THP-1 cells). Also reported to suppress the growth of leukemic T cells (GI50 = 1.73 µM).
Catalogue Number220485
Brand Family Calbiochem®
Synonyms5-(2-Amino-5-oxo-1,5-dihydroimidazol-4-ylidine)-3,4,5,10-2H-azepino[3,4-b]indol-1-one, Chk1 Inhibitor II, Chk2 Inhibitor I
References
ReferencesSharma, V., and Tepe, J.J. 2004. Bioorg. Med. Chem. Lett. 14, 4319.
Sharma, V., et al. 2004. J. Med. Chem. 47, 3700.
Product Information
CAS number724708-21-8
ATP CompetitiveY
DeclarationSold under license from Michigan State University.
FormPale yellow solid
Hill FormulaC₁₅H₁₃N₅O₂
Chemical formulaC₁₅H₁₃N₅O₂
Hygroscopic Hygroscopic
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetChk2
Primary Target IC<sub>50</sub>8 nM against Chk2
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 Carcinogenic / Teratogenic
Storage -20°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 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
220485-500UG 04055977201130

Documentation

Chk2 Inhibitor - CAS 724708-21-8 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Chk2 Inhibitor - CAS 724708-21-8 - Calbiochem Certificates of Analysis

TitleLot Number
220485

References

Reference overview
Sharma, V., and Tepe, J.J. 2004. Bioorg. Med. Chem. Lett. 14, 4319.
Sharma, V., et al. 2004. J. Med. Chem. 47, 3700.
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.

Revision16-December-2009 RFH
Synonyms5-(2-Amino-5-oxo-1,5-dihydroimidazol-4-ylidine)-3,4,5,10-2H-azepino[3,4-b]indol-1-one, Chk1 Inhibitor II, Chk2 Inhibitor I
DescriptionA cell-permeable, ATP competitive, and reversible indoloazepine compound that displays anti-proliferative and anti-inflammatory properties. Acts as a potent inhibitor of Chk2 (IC50 = 8 nM) that targets the ATP binding pocket. Exhibits selectivity for Chk2 over MEK1, Chk1, CK1δ, PKCα, PKCβII and CK2 (IC50 = 89 nM, 237 nM, 1.352 µM, 2.539 µM, 3.381 µM, and > 10.0 µM, respectively). Blocks the production of IL-2 and TNF-α by preventing the transcriptional activation of NF-κB (IC50 = 3.55 µM for IL-2 production in PMA-stimulated Jurkat T cells; 8.16 µM for TNF-α production in LPS-stimulated THP-1 cells). Also reported to suppress the growth of leukemic T cells (GI50 = 1.73 µM).
FormPale yellow solid
Intert gas (Yes/No) Packaged under inert gas
CAS number724708-21-8
Chemical formulaC₁₅H₁₃N₅O₂
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (100 mg/ml)
Storage Protect from light
-20°C
Hygroscopic
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity Carcinogenic / Teratogenic
ReferencesSharma, V., and Tepe, J.J. 2004. Bioorg. Med. Chem. Lett. 14, 4319.
Sharma, V., et al. 2004. J. Med. Chem. 47, 3700.