1-(2-hydroxy-4-morpholin-4-ylphenyl)ethanone

Names

[ Name ]:
1-(2-hydroxy-4-morpholin-4-ylphenyl)ethanone

[Synonym ]:
1-[2-Hydroxy-4-(4-morpholinyl)phenyl]ethanone
AR2783
1-(2-Hydroxy-4-morpholin-4-yl-phenyl)ethanone
DNA-PK Inhibitor III
HMS3229C13
1-(2-hydroxy-4-morpholin-4-ylphenyl)ethanone
Ethanone, 1-[2-hydroxy-4-(4-morpholinyl)phenyl]-

Biological Activity

[Description]:

IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> DNA-PK

Research Areas >> Inflammation/Immunology

Signaling Pathways >> PI3K/Akt/mTOR >> DNA-PK

[Target]

IC50: 120 nM (DNA-PK)[1]

[In Vitro]

IC 86621 exhibits high selectivity against other kinases such as PI3K, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12[1]. IC 86621 (0-100 nM, 24 h) protects RA (rheumatoid arthritis) T cells from apoptosis[2]. Apoptosis Analysis[2] Cell Line: CD4+CD45RO- T cells (from six control donors and seven RA patients) Concentration: 0 nM, 50 nM, 100 nM Incubation Time: 24 h Result: Protected RA (rheumatoid arthritis) T cells from apoptosis.

[References]

[1]. Chandra G, et al. Improved synthesis of a DNA-dependent protein kinase inhibitor IC86621. Arch Pharm Res. 2012 Mar;35(4):639-45.

[2]. Shao L, et al. DNA-dependent protein kinase catalytic subunit mediates T-cell loss in rheumatoid arthritis. EMBO Mol Med. 2010 Oct;2(10):415-27.

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
425.5±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₂H₁₅NO₃

[ Molecular Weight ]:
221.252

[ Flash Point ]:
211.1±28.7 °C

[ Exact Mass ]:
221.105194

[ PSA ]:
49.77000

[ LogP ]:
1.40

[ Vapour Pressure ]:
0.0±1.0 mmHg at 25°C

[ Index of Refraction ]:
1.570

[ Storage condition ]:
-20℃

MSDS

Click to get detail MSDS

Safety Information

[ HS Code ]:
2934999090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%