DNA-PK Inhibitor III CAS: 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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Applicazione: DNA-PK Inhibitor III is a potent, selective, & an ATP-competitive inhibitor of DNA-PK & PI 3-Kinase catalytic subunit p110β
Numero CAS: 404009-40-1
Purezza: ≥95%
Peso molecolare: 221.26
Formula molecolare: C12H15NO3
Solo per uso in Ricerca. Non previsto per Uso Diagnostico o Terapeutico.
* Vedere Certificato di Analisi per informazioni sul lotto specifico (incluso il contenuto d'acqua).

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.


Referenze

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

Stato fisico :
Solid
Solubilità :
Soluble in DMSO (5 mg/ml).
CONSERVAZIONE :
Store at 4° C
Punto di scioglimento :
98-100.3° C
Punto di ebollizione :
425.49° C at 760 mmHg (Predicted)
Densità :
1.21 g/cm3 (Predicted)
Indice di rifrazione :
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
Valori pK :
pKa: 10.47 (Predicted), pKb: 1.95 (Predicted)
Solo per uso in Ricerca. Non previsto per Uso Diagnostico o Terapeutico.
WGK Germania :
3
PubChem CID :
9859309
Numero MDL :
MFCD07370140
SMILES :
CC(=O)C1=C(C=C(C=C1)N2CCOCC2)O

Download SDS (MSDS)

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