260961
DNA-PK Inhibitor II
The DNA-PK Inhibitor II, also referenced under CAS 154447-35-5, controls the biological activity of DNA-PK. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonim(y):
DNA-PK Inhibitor II, NU7026, DNA-Dependent Protein Kinase Inhibitor II, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, LY293646
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About This Item
Wzór empiryczny (zapis Hilla):
C17H15NO3
Numer CAS:
Masa cząsteczkowa:
281.31
Numer MDL:
Kod UNSPSC:
12352200
Polecane produkty
Poziom jakości
Próba
≥95% (HPLC)
Postać
crystalline solid
producent / nazwa handlowa
Calbiochem®
warunki przechowywania
OK to freeze
protect from light
rozpuszczalność
DMSO: 2 mg/mL
methanol: 700 μg/mL
Warunki transportu
ambient
temp. przechowywania
2-8°C
InChI
1S/C17H15NO3/c19-15-11-16(18-7-9-20-10-8-18)21-17-13-4-2-1-3-12(13)5-6-14(15)17/h1-6,11H,7-10H2
Klucz InChI
KKTZALUTXUZPSN-UHFFFAOYSA-N
Opis ogólny
A cell-permeable benzochromenone compound that acts as a potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK with an IC50 of 0.23 µM. It is highly selective towards DNA-PK over PI3K-related kinases (IC50 = 13 µM for PI 3-K and >100 µM for ATM and ATR) and has no effect on PARP-1. Inhibits DNA-PK-mediated, but not PARP-1-mediated, cellular DNA DSB (double strand break) repair and PLDR (potentially lethal damage recovery) following IR (ionizing radiation). Shown to sensitize both proliferating and quiescent cells to IR.
A cell-permeable, potent, specific, reversible, and ATP-competitive inhibitor of DNA-PK (IC50 = 230 nM). Reported to be highly selective for DNA-PK compared to PI3 K-related kinases (IC50 = 13 µM for PI 3-K and >100 µM for ATM and ATR). Exhibits no inhibitory effect on PARP-1. Shown to inhibit DNA-PK-mediated, but not PARP-1-mediated, cellular DNA double strand break (DSB) repair and potentially lethal damage recovery (PLDR) following ionizing radiation (IR). Also shown to sensitize both proliferating and quiescent cells to IR.
Działania biochem./fizjol.
Cell permeable: yes
Primary Target
DNA-PK
DNA-PK
Product competes with ATP.
Reversible: yes
Target IC50: 0.23 µM against DNA-PK
Opakowanie
Packaged under inert gas
Ostrzeżenie
Toxicity: Carcinogenic / Teratogenic (D)
Rekonstytucja
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Inne uwagi
Willmore, E., et al. 2004. Blood,103, 4659.
Hollick, J.J., et al. 2003. Bioorg. Med. Chem. Lett.13, 3083.
Veuger, S.J., et al. 2003. Cancer Res.63, 6008.
Vlahos, C.J., et al. 1994. J. Biol. Chem.269, 5241.
Hollick, J.J., et al. 2003. Bioorg. Med. Chem. Lett.13, 3083.
Veuger, S.J., et al. 2003. Cancer Res.63, 6008.
Vlahos, C.J., et al. 1994. J. Biol. Chem.269, 5241.
Informacje prawne
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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Kod klasy składowania
11 - Combustible Solids
Klasa zagrożenia wodnego (WGK)
WGK 3
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