HDAC3-IN-2

HDAC3-IN-2 (compound 4i) is a pyrazinyl hydrazide-based HDAC3 inhibitor (IC50: 14 nM) that efficiently targets triple-negative breast cancer cells. HDAC3-IN-2 is cytotoxic with an IC50 of 0.55 μM against 4T1 and an IC50 of 0.74 μM against MDA-MB-231. HDAC3-IN-2 has anti-tumor efficacy in vivo in tumor-bearing mouse models, selectively increasing the acetylation levels of H3K9, H3K27 and H4K12, increasing the contents of apoptosis-related caspase-3, caspase-7 and cytochrome c, and reducing Proliferation-related Bcl-2, CD44, EGFR, and Ki-67 levels[1].

Product Specifications

CAS Number

[3033039-28-7]

UNSPSC

12352005

Target

Apoptosis; Caspase; DNA/RNA Synthesis; HDAC; Histone Methyltransferase

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/hdac3-in-2.html

Purity

99.64

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

COC1=CC=C(CNC2=CN=C(C(NNCCC)=O)C=N2)C=C1

Molecular Formula

C16H21N5O2

Molecular Weight

315.37

References & Citations

[1]Pulya S, et al. Selective HDAC3 Inhibitors with Potent In Vivo Antitumor Efficacy against Triple-Negative Breast Cancer. J Med Chem. 2023 Sep 14;66 (17) :12033-12058.. .