TNG-260 is a first-in-class, orally active, potent, and CoREST-selective deacetylase inhibitor. It inhibits HDAC1 with 10-fold selectivity over HDAC3 in cells, and 500-fold selectivity for the CoREST complex over the other HDAC1-containing complexes, NuRD and Sin3. TNG-260 reverses the immune evasion phenotype caused by loss of STK11 and induces tumor regressions in an STK11-mutant model in combination with α-PD1.

KEYWORDS: TNG-260 | Supplier | CoREST-selective deacetylase inhibitor | TNG260 | TNG 260 | TNG-260 | CAS [2935964-98-8] | Histone | HDAC | Inhibitor | Enzymes