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220485 Sigma-AldrichChk2 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.

SDS
CoA
References
Data Sheet

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

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Overview

Replacement Information

Key Spec Table

CAS #	Empirical Formula
724708-21-8	C₁₅H₁₃N₅O₂

Pricing & Availability

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Description
Overview	A 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 Number	220485
Brand Family	Calbiochem®
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

References
References	Sharma, 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 number	724708-21-8
ATP Competitive	Y
Declaration	Sold under license from Michigan State University.
Form	Pale yellow solid
Hill Formula	C₁₅H₁₃N₅O₂
Chemical formula	C₁₅H₁₃N₅O₂
Hygroscopic	Hygroscopic
Reversible	Y
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Primary Target	Chk2
Primary Target IC<sub>50</sub>	8 nM against Chk2
Purity	≥95% by HPLC

Physicochemical Information
Cell permeable	Y

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 Instructions	Following 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

Title	Lot Number
220485	Enter Lot Number

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.

Revision	16-December-2009 RFH
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
Description	A 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).
Form	Pale yellow solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	724708-21-8
Chemical formula	C₁₅H₁₃N₅O₂
Structure formula
Purity	≥95% by HPLC
Solubility	DMSO (100 mg/ml)
Storage	Protect from light -20°C Hygroscopic
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Carcinogenic / Teratogenic
References	Sharma, V., and Tepe, J.J. 2004. Bioorg. Med. Chem. Lett. 14, 4319. Sharma, V., et al. 2004. J. Med. Chem. 47, 3700.

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