生物活性
CCT007093 is an effective protein phosphatase 1D (PPM1D Wip1) inhibitor. Wip1 inhibition can activate the mTORC1 pathway and enhance hepatocyte proliferation after hepatectomy[1][2].
体外研究
(In Vitro)
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[1].
CCT007093 shows specificity for MCF-7 cells, reducing viability by 40% after 2 days with no observable effect on the growth of HeLa cells[2].
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)[2].
Western Blot Analysis[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(In Vivo)
CCT007093 (6.4 mg/kg) enhances liver regeneration and increases the survival rate of mice following major hepatectomy[1].
Animal Model: Wild-type mice[1].
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.
分子量
272.39
性状
Solid
Formula
C15H12OS2
CAS 号
176957-55-4
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMF : 3.33 mg/mL (12.23 mM; Need ultrasonic)
DMSO : ≥ 2.8 mg/mL (10.28 mM)
* "≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 3.6712 mL 18.3560 mL 36.7121 mL
5 mM 0.7342 mL 3.6712 mL 7.3424 mL
10 mM 0.3671 mL 1.8356 mL 3.6712 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。