Chk2 InhibitorA checkpoint kinase inhibitor that mediates apoptosis and cell cycle arrest

Chk2 Inhibitor (CAS 724708-21-8)

Chk2 Inhibitor | CAS 724708-21-8 is rated 5.0 out of 5 by 1.
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Synonym: 5-(2-Amino-5-oxo-1,5-dihydroimidazol-4-ylidine)-3,4,5,10-2H-azepino[3,4-b]indol-1-one
Application: A checkpoint kinase inhibitor that mediates apoptosis and cell cycle arrest
CAS Number: 724708-21-8
Purity: ≥95%
Molecular Weight: 295.3
Molecular Formula: C15H13N5O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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Chk2 Inhibitor is an indoloazepine checkpoint kinase inhibitor that mediates apoptosis and cell cycle arrest. Checkpoint kinase 2 is activated upon DNA damage or genomic instability which eventually causes apoptosis. Mechanistic studies show that Chk2 inhibitor causes autophosphorylation of Chk2 at Thr68 and targets ATP binding pockets of Chk2. Further studies demonstrate that Chk2 inhibitors also inhibit Chk1 and MEK-1 and affect interleukin-2 (IL-2), TNF-α, MEK-1, and GSK-3β.


References

1. Sharma, V. and Tepe, J.J. 2004. Bioorg. Med. Chem. Lett. 14: 4319-4321. PMID: 15261294
2. Sharma, V., et al. 2004. J. Med. Chem. 47: 3700-3703. PMID: 15214798
3. Jobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther. 331: 816-826. PMID: 19741151
4. Yeh, Y.H., et al. 2009. Oncogene. 28: 1366-1378. PMID: 19151762

Physical State :
Solid
Solubility :
Soluble in DMSO.
Storage :
Store at -20° C
IC50 :
Chk2: IC50 = 8 nM; MEK1: IC50 = 89 nM; Chk1: IC50 = 237 nM; CK1δ: IC50 = 1.35 µM; PKCα: IC50 = 2.54 µM; PKCβII: IC50 = 3.38 µM; CK2: IC50 = > 10.0 µM; IL-2 production: IC50 = 3.55 µM (PMA-stimulated Jurkat T cells); TNF-α production: IC50 = 8.16 µM ( LPS-stimulated THP-1 cells)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
PubChem CID :
9882612
SMILES :
C\\1CNC(=O)C2=C(/C1=C\\3/C(=O)N=C(N3)N)C4=CC=CC=C4N2

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Rated 5 out of 5 by from Yeh Yeh, YH. et al. (PubMed 19151762) used the Chk2 Inhibitor to present a regulatory loop between TTK/hMps1 and Chk2 whereby DNA damage-activated Chk2 may facilitate the stabilization of TTK/hMps1, therefore maintaining the checkpoint control. -SCBT Publication Review
Date published: 2015-04-01
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