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HomeProduct name listIC86621

IC86621

Synonym(s):DNA-PK Inhibitor III - CAS 404009-40-1 - Calbiochem;IC86621, 1-(2-Hydroxy-4-morpholin-4-yl-phenyl)ethanone

IC86621 Structural

What is IC86621?

What are the applications of Application

DNA-PK Inhibitor III is a potent, selective, & an ATP-competitive inhibitor of DNA-PK & PI 3-Kinase catalytic subunit p110β

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

Properties of IC86621

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
pka 10.47±0.10(Predicted)
form  solid
color  off-white

Safety information for IC86621

Computed Descriptors for IC86621

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