2. Signaling Pathways
  3. Epigenetics
  4. Histone Acetyltransferase
  5. TIP60 Isoform

TIP60

Histone acetyltransferase TIP60 (KAT5) is a member of the MYST family of lysine acetyltransferases and functions as the catalytic core of the evolutionarily conserved NuA4 chromatin-modifying complex, where it promotes histone acetylation and transcriptional regulation[1][2]. Mechanistically, TIP60 plays a central role in the DNA damage response by interacting with and acetylating key DNA repair regulators, including ataxia-telangiectasia mutated (ATM), thereby facilitating ATM activation following DNA double-strand breaks[1][3][4]. Following DNA damage, the NuA4/TIP60 complex is recruited to chromatin surrounding DNA lesions and contributes to chromatin remodeling events that support efficient DNA repair[1][5]. TIP60 also regulates the acetylation of multiple non-histone proteins involved in genome maintenance, highlighting its broad role in preserving cell viability and genomic stability[2]. In disease contexts, reduced TIP60 activity or expression has been associated with genomic instability, and experimental evidence supports a tumor-suppressive role for TIP60 in breast cancer models[6]. Beyond cancer, genetic studies demonstrate that TIP60 is required for neural stem cell maintenance, neurogenesis, and normal brain development, indicating functions that extend beyond canonical DNA repair pathways[7]. Compared with related MYST acetyltransferases, TIP60 is distinguished by its direct coupling of chromatin sensing and ATM-dependent DNA damage signaling, making it a widely used experimental model for investigating chromatin-regulated genome surveillance mechanisms[1][3][4].

TIP60 Related Products (5):

Cat. No. Product Name Effect Purity
  • HY-15887
    MG 149
    		Inhibitor 99.60%
    MG149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50 = 47 uM); little potent for PCAF and p300 (IC50 >200 uM). MG 149 inhibits KAT8 and blocks PINK1 kinase activity. MG149 inhibits the phosphorylation of Parkin and ubiquitin, thereby suppressing the initiation of PINK1-dependent mitophagy. MG 149 can reverse chronic restraint stress (CRS) induced hypertension and related molecular changes. MG 149 commonly used in research on diseases such as hypertension and Parkinson's disease.
  • HY-123604
    TH1834
    		Inhibitor 99.79%
    TH1834 is a specific Tip60 (KAT5) histone acetyltransferase (HAT) inhibitor. TH1834 induces apoptosis and increases DNA damage in breast cancer. TH1834 does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
  • HY-123604A
    TH1834 dihydrochloride
    		Inhibitor 99.89%
    TH1834 dihydrochloride is a specific Tip60 (KAT5) histone acetyltransferase inhibitor. TH1834 dihydrochloride induces apoptosis and increases DNA damage in breast cancer. TH1834 dihydrochloride does not affect the activity of related histone acetyltransferase MOF. Anticancer activity.
  • HY-112610
    CF53
    		Inhibitor 99.81%
    CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
  • HY-143440
    CBP/p300-IN-16
    		Inhibitor
    CBP/p300-IN-16 (compound 1) is a potent EP300/CBP HAT inhibitor with IC50s of 0.61, 2.24 µM for HAT EP300 and LK2 H3K27, respectively.