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CCT129957

Names

[ CAS No. ]:
883098-58-6

[ Name ]:
CCT129957

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Metabolic Enzyme/Protease >> Phospholipase

[Target]

IC50: ~3 μM (Phospholipase C-γ (PLC-γ))[1]


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C17H15N3O3

[ Molecular Weight ]:
309.32

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds