CCT007093 是有效的蛋白磷酸酶 1D (PPM1D

CCT007093 

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。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。

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。
 

参考文献	[1]. Lingling Zhang, et al. Inhibition of wild-type p53-induced phosphatase 1 promotes liver regeneration in mice by direct activation of mammalian target of rapamycin. Hepatology. 2015 Jun;61(6):2030-41.  [Content Brief] [2]. S Rayter, et al. A chemical inhibitor of PPM1D that selectively kills cells overexpressing PPM1D. Oncogene. 2008 Feb 14;27(8):1036-44. [Content Brief]