| Identification | Back Directory | [Name]
IC86621 | [CAS]
404009-40-1 | [Synonyms]
IC 86621
(IC86621)
IC86621 CAS#: 404009-40-1
1-(2-hydroxy-4-Morpholinophenyl)ethanone
1-(2-Hydroxy-4-morpholinophenyl)ethan-1-one
Ethanone, 1-[2-hydroxy-4-(4-morpholinyl)phenyl]-
DNA-PK Inhibitor III - CAS 404009-40-1 - Calbiochem
ATP,Buchwald-Hartwig amination,Inhibitor,IC-86621,IC86621,IC 86621,DSB,antitumor,inhibit,Apoptosis,Fries rearrangement,DNA-dependent protein kinase,DNA-PK | [Molecular Formula]
C12H15NO3 | [MDL Number]
MFCD07370140 | [MOL File]
404009-40-1.mol | [Molecular Weight]
221.25 |
| Chemical Properties | Back Directory | [Melting point ]
98-100.3 °C | [Boiling point ]
425.5±45.0 °C(Predicted) | [density ]
1.210±0.06 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 15 mg/mL | [form ]
solid | [pka]
10.47±0.10(Predicted) | [color ]
off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [Definition]
ChEBI: 1-[2-hydroxy-4-(4-morpholinyl)phenyl]ethanone is an aromatic ketone. | [General Description]
A cell-permeable aryl-morpholino compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 120 nM) and PI 3-Kinase catalytic subunit p110β (IC50 = 135 nM). It inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC50 = 68 μM) and enhances DSB-induced antitumor activity both in vitro and in vivo, while exhibiting no cytotoxic effects (up to 50 μM) in the absence of DSBs. It inhibits PI 3-K p110α, p110γ, and p110δ only at much higher concentrations (IC50 = 1.4, 0.88, and 1.0 μM, respectively) and exhibits no effect against a panel of several other kinases, including, Cdk2, Src, PKA, PKC, Chk1, CK1, ATM, and FKBP12, even at concentrations as high as 100 μM. | [Biochem/physiol Actions]
Cell permeable: yes | [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. DOI:10.1007/s12272-012-0407-1
[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. DOI:10.1002/emmm.201000096 |
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Sigma-Aldrich
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021-61415566 800-8193336 |
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https://www.sigmaaldrich.cn |
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