CCT129957 是一种吲哚衍生物，也是一种有效的磷脂酶 C-γ (PLC-γ) 抑制剂，IC50 为 ~3 μM，GC50 为 15 μM。CCT129957 以约 15 μM 的浓度抑制鳞状细胞中 Ca2+ 的释放。
货号:ajcx37516
CAS:883098-58-6
分子式:C17H15N3O3
分子量：309.32
溶解度:DMSO : 100 mg/mL (323.29 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

CCT129957 is an indole derivative and a potent phospholipase C-γ (PLC-γ) inhibitor with an IC50 of ~3 μM and a GC50 of 15 μM. CCT129957 inhibits Ca2+ release in squamous carcinoma cells at ~15 μM[1][2].

The phenyl group on the left side sat in a lipophilic pocket formed of various amino acids. The predicted binding mode of CCT129957 displays a robust hydrogen bond pattern as well as a lipophilic contact[1].CCT129957 inhibits the cell growth of renal UO-31 and the breast T-47D cancer cell lines by ~60-70%[2].

[1]. Reynisson J, et al. The identification of novel PLC-gamma inhibitors using virtual high throughput screening. Bioorg Med Chem. 2009 Apr 15;17(8):3169-76.
[2]. Feng L, et al. The effect of PLC-γ2 inhibitors on the growth of human tumour cells. Eur J Med Chem. 2012 Aug;54:463-9.