TH1834

• CAT Number: I014994
• CAS Number: 2108830-08-4
• Molecular Formula: C₃₃H₄₀N₆O₃
• Molecular Weight: 568.71
• Purity: ≥95%
• Target: Apoptosis
• IUPAC Name: 2-[5-[4-[[2-phenylethyl-[4-[4-(pyrrolidin-1-ylmethyl)phenoxy]butyl]amino]methyl]phenyl]tetrazol-2-yl]acetic acid
• InChI: InChI=1S/C33H40N6O3/c40-32(41)26-39-35-33(34-36-39)30-14-10-28(11-15-30)25-38(22-18-27-8-2-1-3-9-27)21-6-7-23-42-31-16-12-29(13-17-31)24-37-19-4-5-20-37/h1-3,8-17H,4-7,18-26H2,(H,40,41)
• InChIKey: XERATECPNBWJFP-UHFFFAOYSA-N
• SMILES: C1CCN(C1)CC2=CC=C(C=C2)OCCCCN(CCC3=CC=CC=C3)CC4=CC=C(C=C4)C5=NN(N=N5)CC(=O)O

TH1834 (Cat No.:I014994) is a specific inhibitor of the histone acetyltransferase Tip60 (KAT5). It demonstrates potent anticancer activity by inducing apoptosis and increasing DNA damage in breast cancer cells. TH1834 selectively targets Tip60 without affecting the activity of the related histone acetyltransferase MOF. Treatment with TH1834 leads to reduced cell viability and increased cytotoxicity in MCF7 cells. It also induces caspase 3 activation, further supporting its apoptotic effects. In vitro studies demonstrate the inhibition of Tip60 activity by TH1834, resulting in apoptosis and increased unrepaired DNA damage in breast cancer cells. These findings suggest TH1834 as a potential therapeutic agent for breast cancer targeting Tip60 histone acetyltransferase.

Reference

[1]. Gao C, et al. Rational design and validation of a Tip60 histone acetyltransferase inhibitor. Sci Rep. 2014 Jun 20;4:5372.