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.

• 동의어(들): DNA-PK Inhibitor II, NU7026, DNA-Dependent Protein Kinase Inhibitor II, 2-(Morpholin-4-yl)-benzo[h]chromen-4-one, LY293646
• 실험식(Hill 표기법): C₁₇H₁₅NO₃
• CAS Number: 154447-35-5
• Molecular Weight: 281.31
• MDL number: MFCD06798345
• UNSPSC 코드: 12352200

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 형태: crystalline solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• solubility: DMSO: 2 mg/mL; methanol: 700 μg/mL
• 배송 상태: ambient
• 저장 온도: 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
• InChI key: KKTZALUTXUZPSN-UHFFFAOYSA-N

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
DNA-PK

Product competes with ATP.

Reversible: yes

Target IC₅₀: 0.23 µM against DNA-PK

포장

Packaged under inert gas

경고

Toxicity: Carcinogenic / Teratogenic (D)

재구성

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

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.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3