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TH 1834
- Parent CAS: 2108830-08-4
- Soluble in water and DMSO
- MF: C33H40N6O3.2HCl
- MW: 641.63
Description
TH1834 is a selective Tip60 histone acetyltransferase (HAT) inhibitor that suppresses Tip60-dependent acetylation and downstream cellular signaling. TH1834 has been shown to induce apoptosis and increase unrepaired DNA damage following ionizing radiation treatment in breast cancer cell lines.
Tip60 (KAT5) is a member of the MYST family of histone acetyltransferases and plays critical roles in chromatin remodeling, transcriptional regulation, DNA damage response, DNA repair, and apoptosis. Aberrant Tip60 activity has been implicated in cancer progression and therapeutic resistance. TH1834 selectively targets Tip60 without affecting the activity of the related MYST family acetyltransferase MOF, as demonstrated by the absence of changes in H4K16 acetylation. This selectivity makes TH1834 a valuable tool for investigating Tip60-dependent epigenetic regulation and DNA damage repair mechanisms.
Key Features
- Selective Tip60 (KAT5) histone acetyltransferase inhibitor
- Induces apoptosis in breast cancer cell models
- Increases unrepaired DNA damage following ionizing radiation
- Selective over the related HAT MOF
- Useful tool for DNA damage response and epigenetics research
Applications
- Tip60 and MYST family HAT research
- DNA damage response and DNA repair studies
- Epigenetics and chromatin biology investigations
- Cancer biology and radiosensitization research
- Apoptosis and transcriptional regulation studies
More Information
| Parent CAS No. | 2108830-08-4 |
|---|---|
| Chemical Name | 2-(5-(4-((phenethyl(4-(4-(pyrrolidin-1-ylmethyl)phenoxy)butyl)amino)methyl)phenyl)-2H-tetrazol-2-yl)acetic acid dihydrochloride |
| SMILES | C1C=C(OCCCCN(CC2C=CC(C3=NN(CC(O)=O)N=N3)=CC=2)CCC2C=CC=CC=2)C=CC=1CN1CCCC1.Cl.Cl |
| MFCD | N.A. |
| 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 |
| CID | 91826511 |
| Short Description | Tip60 HAT inhibitor |
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