TNG260

TNG260 is a selective, orally effective inhibitor of HDAC1 and CoREST complex, with a 10-fold selectivity for HDAC1 over HDAC3 and a 500-fold selectivity for CoREST complex over NuRD and Sin3 complex. TNG260 reshapes the tumor immune microenvironment, reduces immunosuppressive neutrophil infiltration, promotes effector T cell recruitment, and reverses anti-PD-1 resistance caused by STK11 deficiency by inhibiting the activity of the CoREST-HDAC1 complex. TNG260 induces durable tumor regression in combination with α-PD1 in MC38 tumor-bearing mice with STK11 mutations, and has lower toxicity to bone marrow cells than non-selective HDAC inhibitors[1].

Product Specifications

CAS Number

[2935964-98-8]

UNSPSC

12352005

Target

HDAC

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/tng260.html

Purity

99.33

Solubility

DMSO : 2.22 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

NC1=CC=C(C2=CC=C(F)C=C2)C=C1NC(C3=CC=C([S@](=O)(C)=N)C=C3)=O

Molecular Formula

C20H18FN3O2S

Molecular Weight

383.44

References & Citations

[1]Ahronian L, et al. TNG260, a CoREST-selective deacetylase inhibitor, reverses anti-PD1 resistance driven by loss of STK11[J]. J Immunother, 2022, 10 (2) : A1-A1595.|[2]Patel Ayushi, et al. TNG260, a small molecule CoREST inhibitor, sensitizes STK11-mutant NSCLC to anti-PD1 immunotherapy. Cancer Research 84.6_Supplement (2024) : 3916-3916.