Chemical Structure : LC427
货号: PC-25905Not For Human Use, Lab Use Only.
LC427 (LC-427) is a specific small molecule inhibitor of LRBA-CTLA4 interaction with IC50 of 0.18 uM, facilitates the lysosomal degradation of CTLA4, binds directly to PH-BEACH domain of LRBA with Kd of 19.6 uM.
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LC427 (LC-427) is a specific small molecule inhibitor of LRBA-CTLA4 interaction with IC50 of 0.18 uM, facilitates the lysosomal degradation of CTLA4, binds directly to PH-BEACH domain of LRBA with Kd of 19.6 uM.
LC427 mainly inhibits the interaction of LRBA with intracellular CTLA4, but not with the surface CTLA4 or soluble CTLA4.
LC427 disrupts LRBA-CTLA4 interactions in HEK293T cells transfected with LRBA PH and CTLA4, and human PBMCs.
LC427 triggers CTLA4 lysosomal degradation in a time-dependent manner and a dose-dependent manner in HEK293T cells overexpressing LRBA and CTLA4 proteins.
LC427 reduces CTLA4 expression in mouse and human T cells.
LC427 inhibits apoptosis and enhances the functions of activated T cells.
LC427 promotes antitumor immunity in multiple tumor models, triggers antitumor immunity in an LRBA/CTLA4-dependent manner.
| 分子量 | 291.36 | |
| 分子式 | C17H17N5 | |
| 外观性状 | Solid | |
| 储存条件 |
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| Solubility |
10 mM in DMSO |
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1. Ge X, et al. Nat Commun. 2025 Dec 14. doi: 10.1038/s41467-025-67365-5.
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