OK-1035 is a potent and selective DNA-PK inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner.
CAS 98293-88-0 MFCD98293880
化学结构图
SMILES: N#Cc1cc(-c2ccncc2)c(/C=N/N)[nH]c1=O
化学属性
| Mol. Weight | 239.23276 |
|---|---|
| Appearance | white solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | OK-1035 is a potent and selective DNA-PK inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner. |
|---|---|
| Formula | C12H9N5O |
| Synonym | OK1035; OK 1035; OK-1035. |
| IUPAC Name | (E)-2-(hydrazonomethyl)-6-oxo-1,6-dihydro-[3,4'-bipyridine]-5-carbonitrile |
| InChIKey | KJRKRHGTENMKAI-FRKPEAEDSA-N |
| InChI | InChI=1S/C12H9N5O/c13-6-9-5-10(8-1-3-15-4-2-8)11(7-16-14)17-12(9)18/h1-5,7H,14H2,(H,17,18)/b16-7+ |
| Canonical SMILES | N#CC1=CC(C2=CC=NC=C2)=C(/C=N/N)NC1=O |
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- OK-1035 is a potent and selective DNA-PK inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner.
