(2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮
中文名称:
(2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮
中文同义词:
(2E,5E)-2,5-二(2-噻吩基亚甲基)环戊酮;PPM1D抑制剂(CCT007093)
英文名称:
Cyclopentanone, 2,5-bis(2-thienylMethylene)-, (E,E)-
英文同义词:
(2E,5E)-2,5-Bis(2-thienylmethylene)cyclopentanone CCT007093;Cyclopentanone, 2,5-bis(2-thienylMethylene)-, (E,E)-;CCT007093;(2E,5E)-2,5-Bis(2-thienylmethylene)cyclopentanone;(2E,5E)-2,5-Bis(thiophen-2-ylmethylene)cyclopentanone;CCTOO7093;2,5-bis(2-thienylMethylene)-, (E,E)-Cyclopentanone;2,5-Bis(2-thienylmethylene)-cyclopentanone
CAS号:
176957-55-4
分子式:
C15H12OS2
分子量:
272.39
EINECS号:
相关类别:
细胞生物学试剂;小分子抑制剂;小分子抑制剂，天然产物;Inhibitors
Mol文件:
176957-55-4.mol
熔点
222-223℃
储存条件
2-8°C
溶解度
DMSO: >3mg/mL
形态
powder, yellow
敏感性
Light Sensitive
生物活性
CCT007093 是有效的蛋白磷酸酶 1D (PPM1D Wip1) 的抑制剂。Wip1 的抑制可激活mTORC1 通路，增强肝切除手术后肝细胞的增殖。
体外研究
CCT007093 (25 or 50 µM, 8 h) significantly increases the phosphorylation levels of mTOR at Ser2448, Ser2481 and Ser2159, and the phosphorylation levels of p70S6K (Thr389) and S6 (Ser235/236) are also up-regulated in transfected HEK293T cell line.
CCT007093 shows specificity for MCF-7 cells, reducing viability by 40% after 2 days with no observable effect on the growth of HeLa cells.
CCT007093 induces P38 phosphorylation at 4 h post exposure in MCF-7 cells (sensitive to PPM1D inhibition), and does not induce P38 phosphorylation in HeLa cells (relatively resistant to PPM1D inhibition).
Western Blot Analysis
Cell Line: HEK293T cell line.
Concentration: 25 or 50 µM.
Incubation Time: 8 h.
Result: The phosphorylation levels of mTOR at Ser2448, Ser2481 and Ser2159 were all significantly increased [1] .
The phosphorylation levels of p70S6K (Thr389) and S6 (Ser235/236) were also up-regulated [1] .
Cell Line:
HEK293T cell line.
Concentration:
25 or 50 µM.
Incubation Time:
8 h.
Result:
The phosphorylation levels of mTOR at Ser2448, Ser2481 and Ser2159 were all significantly increased [1] .
The phosphorylation levels of p70S6K (Thr389) and S6 (Ser235/236) were also up-regulated [1] .
体内研究
CCT007093 (6.4 mg/kg) enhances liver regeneration and increases the survival rate of mice following major hepatectomy.
Animal Model: Wild-type mice.
Dosage: 3.2 and 6.4 mg/kg.
Administration: Injected intraperitoneally 4 times (mice were sacrificed at 36 h post-PH).
Result: Significantly improved survival in mice following major hepatectomy (80% hepatectomy).
The level of PCNA was also significantly increased in the liver of CCT007093-treated mice at 36h, 48h and 72h post-PH.
Animal Model:
Wild-type mice.
Dosage:
3.2 and 6.4 mg/kg.
Administration:
Injected intraperitoneally 4 times (mice were sacrificed at 36 h post-PH).
Result:
Significantly improved survival in mice following major hepatectomy (80% hepatectomy).
The level of PCNA was also significantly increased in the liver of CCT007093-treated mice at 36h, 48h and 72h post-PH.
危险品标志
Xi
危险类别码
36/37/38
安全说明
26
WGK Germany
3
