WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406413
Description: 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.
MedKoo Cat#: 406413
Chemical Formula: C12H9N5O
Exact Mass: 239.08071
Molecular Weight: 239.23276
Elemental Analysis: C, 60.25; H, 3.79; N, 29.27; O, 6.69
This product is not in stock, which may be available by custom synthesis.
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Synonym: OK1035; OK 1035; OK-1035.
IUPAC/Chemical Name: (E)-2-(hydrazonomethyl)-6-oxo-1,6-dihydro-[3,4'-bipyridine]-5-carbonitrile
InChi Key: KJRKRHGTENMKAI-FRKPEAEDSA-N
InChi Code: 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+
SMILES Code: N#CC1=CC(C2=CC=NC=C2)=C(/C=N/N)NC1=O
Appearance: white solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 239.23276 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Stockley M, Clegg W, Fontana G, Golding BT, Martin N, Rigoreau LJ, Smith GC, Griffin RJ. Synthesis, crystal structure determination, and biological properties of the DNA-dependent protein kinase (DNA-PK) inhibitor 3-cyano-6-hydrazonomethyl-5-(4-pyridyl)pyrid-[1H]-2-one (OK-1035). Bioorg Med Chem Lett. 2001 Nov 5;11(21):2837-41. PubMed PMID: 11597411.
2: Chakravarthy BR, Walker T, Rasquinha I, Hill IE, MacManus JP. Activation of DNA-dependent protein kinase may play a role in apoptosis of human neuroblastoma cells. J Neurochem. 1999 Mar;72(3):933-42. PubMed PMID: 10037464.
3: Kruszewski M, WojewÃ³dzka M, Iwaneńko T, Szumiel I, Okuyama A. Differential inhibitory effect of OK-1035 on DNA repair in L5178Y murine lymphoma sublines with functional or defective repair of double strand breaks. Mutat Res. 1998 Oct 21;409(1):31-6. PubMed PMID: 9806500.
4: Take Y, Kumano M, Teraoka H, Nishimura S, Okuyama A. DNA-dependent protein kinase inhibitor (OK-1035) suppresses p21 expression in HCT116 cells containing wild-type p53 induced by adriamycin. Biochem Biophys Res Commun. 1996 Apr 16;221(2):207-12. PubMed PMID: 8619835.
5: Take Y, Kumano M, Hamano Y, Fukatsu H, Teraoka H, Nishimura S, Okuyama A. OK-1035, a selective inhibitor of DNA-dependent protein kinase. Biochem Biophys Res Commun. 1995 Oct 4;215(1):41-7. PubMed PMID: 7575620.