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首页-小分子抑制剂&激动剂-Others-Other Targets-ERG245
ERG245

Chemical Structure : ERG245

CAS No.:

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ERG245 (ERG-245)

货号: PC-26615Not For Human Use, Lab Use Only.

ERG245 is a potent, selective BCAT1 inhibitor with IC50 of 0.5 nM for recombinant human BCAT1 (rhBCAT1), >2000-fold selectivity for BCAT1 over BCAT2.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ERG245 is a potent, selective BCAT1 inhibitor with IC50 of 0.5 nM for recombinant human BCAT1 (rhBCAT1), >2000-fold selectivity for BCAT1 over BCAT2.
ERG245 completely suppressed production of IFNg and granzyme B (GZMB) in activated CD8+ T cells, shows partial inhibition of CD8+ T cell expansion for murine CD8+ (mCD8+).
ERG245 metabolically reprograms the cells towards increased OXPHOS. suppresses activation of CD8+ T cells in DSS colitis leading to improved disease outcomes.
ERG245 dramatically increases anti-PD-1 efficacy inducing complete and durable tumor regressions in the moderately immunogenic CT26 tumor model.

物理化学性质&存储条件

分子量 347.21
分子式 C17H15BrO3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

5-(4-bromophenyl)-5-oxo-4-phenylpentanoic acid

参考文献

1. Lodi F, et al. bioRxiv, 2023: 2023.02. 25.530034.

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