220488

Chk2 Inhibitor, PV1019

The Chk2 Inhibitor, PV1019 controls the biological activity of Chk2. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

• 동의어(들): Chk2 Inhibitor, PV1019, NSC 744039
• 실험식(Hill 표기법): C₁₈H₁₇N₇O₃
• Molecular Weight: 379.37
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• Quality Level: 100
• 분석: ≥95% (HPLC)
• 형태: solid
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; desiccated (hygroscopic); protect from light
• 색상: orange
• solubility: DMSO: 5 mg/mL
• 배송 상태: ambient
• 저장 온도: −20°C

설명

일반 설명

A cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC₅₀ = 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 µM and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC₅₀ = 15.73 and 55 µM against substrate phosphorylation and Chk1 autophosphorylation with 10 µM ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser516) and its downstream substrate Cdc25c (on Ser216) in MCF7 cultures (IC₅₀<10 µM) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2^-/- cultures.

A cell-permeable nitroindolo-guanidinohydrazone compound that acts as a potent, ATP-competitive, and highly selective Chk2 inhibitor (IC₅₀ = 138 and 570 nM against the phosphorylation of histone H1 by Chk2 in the presence of 10 µM and 1 mM of ATP, respectively), while exhibiting much reduced or no activity against a panel of 52 other cellular kinases, including Chk1 (IC₅₀ = 15.73 and 55 µM against substrate phosphorylation and Chk1 autophosphorylation with 10 µM ATP). Shown to effectively suppress radiation-induced phosphorylation of Chk2 (on Ser⁵¹⁶) and its downstream substrate Cdc25c (on Ser²¹⁶) in MCF7 cultures (IC₅₀<10 µM) and reduce the sensitivity of wild-type murine thymocytes to radiation-induced apoptosis to the level seen in Chk2^-/- cultures.

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

Jobson, A.G., et al. 2009. J. Pharmacol. Exp. Ther.331, 816.

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable