Top/HDAC-IN-1

Top/HDAC-IN-1 (Compound 29b) is a topoisomerase/HDAC dual inhibitor with IC50s of 18, 230, 790, 87, and 5250 nM for HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8, respectively. Top/HDAC-IN-1 exhibits potent antitumor activities against the HCT116 cell line with the IC50 of 180 nM. Top/HDAC-IN-1 efficiently induces apoptosis with G2 cell cycle arrest in HCT116 cells[1].

Product Specifications

CAS Number

[2775446-49-4]

UNSPSC

12352005

Target

Apoptosis; HDAC; Topoisomerase

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Epigenetics

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/top-hdac-in-1.html

Solubility

10 mM in DMSO

Smiles

CN1C2=C(C(N3CCC4=C(C13)NC5=C4C=C(C=C5)O)=O)C=C(C=C2)NCC6=CC=C(C=C6)/C=C/C(NO)=O

Molecular Formula

C29H27N5O4

Molecular Weight

509.56

References & Citations

[1]Fugui Zhu, et al. Design, Synthesis, and Structure-Activity relationships of Evodiamine-Based topoisomerase (Top) /Histone deacetylase (HDAC) dual inhibitors. Bioorg Chem. 2022 May;122:105702.