PK11007 |
| Catalog No.GC32946 |
PK11007은 항암 활성이 있는 약한 티올 알킬화제입니다. PK11007은 DNA 결합 활성을 손상시키지 않으면서 두 개의 표면에 노출된 시스테인의 선택적 알킬화를 통해 p53을 안정화합니다. PK11007은 활성산소종(ROS) 수준을 증가시켜 돌연변이 p53 암세포 사멸을 유도합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 38275-34-2
Sample solution is provided at 25 µL, 10mM.
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PK11007 is a p53 targeting compound, has anti-tumor activities through activation of unstable p53.
PK11007 (15-30 µM) reduces the viability of mutant p53 cell lines MKN1 (V143A), HUH-7 (Y220C), NUGC-3 (Y220C), and SW480 (R273H/P309S). PK11007 also shows inhibitory activities against the p53 wt cancer cell lines HUH-6 and NUGC-4, as well as the fibroblast cell line WI-38 only at high concentrations (60 and 120 µM). PK11007 increases levels of p53 target genes and activates the unfolded protein response pathway. PK11007 also increases p53 activity in HUH-6 and NUGC-4 cells. PK11007 induces cell death via caspase-independent pathways. PK11007 (30, 60 µM) induces reactive oxygen species (ROS) especially in mutant p53 cells[1]. PK11007 inhibits the proliferation of a panel of 17 breast cell lines, with IC50s ranging from 2.3 to 42.2 μM[2].
[1]. Bauer MR, et al. 2-Sulfonylpyrimidines: Mild alkylating agents with anticancer activity toward p53-compromised cells. Proc Natl Acad Sci U S A. 2016 Sep 6;113(36):E5271-80. [2]. Synnott NC, et al. Mutant p53 as a therapeutic target for the treatment of triple-negative breast cancer: Preclinical investigation with the anti-p53 drug, PK11007. Cancer Lett. 2018 Feb 1;414:99-106
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