| Identification | Back Directory | [Name]
Chk2 Inhibitor | [CAS]
724708-21-8 | [Synonyms]
SC203885
SC-203885
SC 203885
Chk2 Inhibitor
Chk2 Inhibitor - CAS 724708-21-8 - Calbiochem
Azepino[3,4-b]indol-1(2H)-one, 5-(2-amino-1,5-dihydro-5-oxo-4H-imidazol-4-ylidene)-3,4,5,10-tetrahydro-, (5Z)- | [Molecular Formula]
C15H13N5O2 | [MDL Number]
MFCD22380609 | [MOL File]
724708-21-8.mol | [Molecular Weight]
295.3 |
| Chemical Properties | Back Directory | [storage temp. ]
-20C | [solubility ]
DMSO: Soluble | [form ]
Pale yellow solid | [color ]
pale yellow | [InChIKey]
FRROPNANZGODOW-MKFZHGHUSA-N | [SMILES]
Cl.N1C(=N\C(=C2\CCNC(=O)c3[nH]c4c(c3\2)cccc4)\C1=O)N |
| Hazard Information | Back Directory | [Uses]
Chk2 Inhibitor is a checkpoint kinase inhibitor that mediates apoptosis and cell cycle arrest. | [General 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). | [Biochem/physiol Actions]
Primary TargetChk2 | [IC 50]
Chk2: 13.5 nM (IC50); Chk1: 220.4 nM (IC50) |
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