TH1834 dihydrochloride

• CAT Number: I017157
• CAS Number: 2108830-09-5
• Molecular Formula: C₃₃H₄₂Cl₂N₆O₃
• Molecular Weight: 641.63
• 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;dihydrochloride
• InChI: InChI=1S/C33H40N6O3.2ClH/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);2*1H
• InChIKey: HYXIFSOROZPMMU-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.Cl.Cl

TH1834 dihydrochloride (Cat No.:I017157) is a specific inhibitor of the histone acetyltransferase Tip60 (KAT5). It demonstrates anticancer activity by inducing apoptosis and increasing DNA damage in breast cancer cells, specifically MCF7 cells. Treatment with TH1834 dihydrochloride leads to a significant reduction in cell viability and a highly significant increase in cytotoxicity. It also induces caspase 3 activation, indicating apoptotic cell death. TH1834 dihydrochloride specifically inhibits Tip60 activity without affecting the activity of related histone acetyltransferase MOF. These findings highlight the potential of TH1834 dihydrochloride as a therapeutic agent for breast cancer by targeting Tip60 and promoting apoptosis while inducing DNA damage.

Reference

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