DNA-PK Inhibitor IIICAS: 404009-40-1
MF: C12H15NO3
MW: 221.26
A potent, selective, & an ATP-competitive inhibitor of DNA-PK & PI 3-Kinase catalytic subunit p110β.

DNA-PK Inhibitor III (CAS 404009-40-1)

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Application: A potent, selective, & an ATP-competitive inhibitor of DNA-PK & PI 3-Kinase catalytic subunit p110β
CAS Number: 404009-40-1
Purity: ≥95%
Molecular Weight: 221.26
Molecular Formula: C12H15NO3
* Refer to Certificate of Analysis for lot specific data (including water content).
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DNA-PK Inhibitor III is a cell-permeable aryl-morpholino compound that is potent, selective, and an ATP-competitive inhibitor of DNA-PK (IC50= 120 nM) and PI 3-Kinase catalytic subunit p110β (IC50= 135 nM). Inhibits DNA-PK-mediated cellular DNA DSB (double strand break) repair (EC50= 68 μM) and enhances DSB-induced antitumor activity in vitro, while exhibiting no cytotoxic effects (up to 50 μM) in the absence of DSBs. Also inhibits PI 3K p110α, p110γ, and p110δ only at much higher concentrations (IC50= 1.4 μM, 880 nM, 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.


References

Kashishian, A., et al. 2004. Mol. Cancer Ther. 2, 1257. Willmore, E., et al. 2004. Blood,103, 4659.

Physical State :
Solid
Solubility :
Soluble in DMSO (5 mg/ml).
Storage :
Store at 4° C
Melting Point :
98-100.3° C
Boiling Point :
425.49° C at 760 mmHg (Predicted)
Density :
1.21 g/cm3 (Predicted)
Refractive Index :
n20D 1.57 (Predicted)
IC50 :
DNA-PK: IC50 = 120 nM; PI 3-Kinase catalytic subunit p110β: IC50 = 135 nM; DNA-PK-mediated cellular DNA DSB repair: EC5050 = 68 µM; PI 3-K p110α: IC50 = 1.4 µM; p110γ: IC50 = 0.88 µM; p110δ: IC50 = 1.0 µM
pK Values :
pKa: 10.47 (Predicted), pKb: 1.95 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
9859309
MDL Number :
MFCD07370140
SMILES :
CC(=O)C1=C(C=C(C=C1)N2CCOCC2)O

Download SDS (MSDS)

Certificate of Analysis

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