2935964-98-8
Chemical Structure
TNG260
- CAS No.: 2935964-98-8
- Formula:C20H18FN3O2S
- Molecular Weight:383.44
IUPAC Name: (R)-N-(4-amino-4'-fluoro-[1,1'-biphenyl]-3-yl)-4-(S-methylsulfonimidoyl)benzamide
InChIKey: JPFMYSJUFUEHBI-HHHXNRCGSA-N
SMILES: NC1=CC=C(C=C1NC(C2=CC=C(C=C2)[S@](=O)(C)=N)=O)C3=CC=C(C=C3)F
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
TNG260 | 99.33% | 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. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
-
Similarity Score 1.00
HY-153358A(S)-TNG260 -
Similarity Score 0.67
HY-124053BRD2492 -
Similarity Score 0.62
HY-100719RBRD-6929 (Standard) -
Similarity Score 0.58
HY-139733β-N-Acetyl-D-hexosaminidase-IN-1 -
Similarity Score 0.58
HY-179654ST13 -
Similarity Score 0.57
HY-145009SN-008 -
Similarity Score 0.57
HY-124337BG48 -
Similarity Score 0.57
HY-162487HDAC-IN-72 -
Similarity Score 0.57
HY-182697RTICBM-74 -
Explore the MedChemAI to find more analogs