ERG245 | BCAT1 inhibitor | Probechem Biochemicals

Chemical Structure : ERG245

ERG245 (ERG-245)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt	347.21
Formula	C17H15BrO3
Appearance	Solid
CAS No.
Storage	Solide Powder -20°C 12 Months; 4°C 6 Months	In Solvent -80°C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	5-(4-bromophenyl)-5-oxo-4-phenylpentanoic acid

References

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

ERG245 (ERG-245)

Biological Activity

Physicochemical Properties

References

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