Abcam, ab255734, NU 9056, KAT5 (Tip60) inhibitor

Size: 10mg
MW 232.4 Da. Selective KAT5 / Tip60 histone acetyl transferase inhibitor (IC 50 = <2 μM). Significantly less active towards p300 (IC 50 = 60 μM), pCAF (IC 50 = 36 μM) and GCN5 (IC 50 = >100 μM). Inhibits histone acetylation in prostate cancer cell lines. Inhibits proliferation of a range of prostate cancer cell lines. Induces apoptosis via a Caspase 3- and Caspase 9-dependent mechanism. Modulates epigenetic regulation of cytosolic phospholipase A2 expression in SH-SY5Y cells.
Key facts
CAS number:1450644-28-6,
Form:LiquidSee storage information,
Molecular weight:232.4 Da,
Molecular formula:C6H4N2S4,
PubChem:72201043,
Nature:Synthetic,
Biochemical name:5-(1,2-Thiazol-5-yldisulfanyl)-1,2-thiazole,
Biological description:Selective KAT5 / Tip60 histone acetyl transferase inhibitor (IC50 = <2 μM). Significantly less active towards p300 (IC50 = 60 μM), pCAF (IC50 = 36 μM) and GCN5 (IC50 = >100 μM). Inhibits histone acetylation in prostate cancer cell lines. Inhibits proliferation of a range of prostate cancer cell lines. Induces apoptosis via a Caspase 3- and Caspase 9-dependent mechanism. Modulates epigenetic regulation of cytosolic phospholipase A2 expression in SH-SY5Y cells.,
Canonical smiles:C1=C(SN=C1)SSC2=CC=NS2,
InChi:InChI=1S/C6H4N2S4/c1-3-7-9-5(1)11-12-6-2-4-8-10-6/h1-4H,
InChiKey:MLRAMCAHIWHWRM-UHFFFAOYSA-N,
IUPAC Name:5-(1,2-thiazol-5-yldisulfanyl)-1,2-thiazole

Product details:
Physical Appearance: Yellow liquid

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions--20°C, Appropriate long-term storage conditions--20°C, Storage information-Store in the dark

Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
KAT2B also known as PCAF (p300/CBP-associated factor) and KAT5 known as Tip60 are histone acetyltransferases that play important roles in chromatin modification. KAT2B has a molecular mass of about 92 kDa while KAT5 is approximately 60 kDa. Both are expressed in various tissues with high levels in the brain and reproductive organs. Mechanically they facilitate the transfer of acetyl groups to lysine residues on histones leading to changes in chromatin structure and influencing gene expression.
Biological function summary
PCAF and Tip60 are involved in the regulation of transcription and the cellular response to DNA damage. They participate in the formation of multi-protein complexes that mediate acetylation of both histones and non-histone proteins which is important for transcriptional activation and repair mechanisms. PCAF associates with the SAGA complex while Tip60 is part of the NuA4 complex. These complexes play a significant role in processes such as gene silencing and activation depending on the context of the cell situation.
Pathways
These acetyltransferases are integral to the p53 signaling pathway and the PI3K/AKT signaling pathway. The p53 pathway wherein KAT2B and KAT5 acetylate p53 enhances its ability to function as a tumor suppressor. These acetyltransferases collaborate with other proteins like CBP/p300 to regulate transcription and maintain genomic stability. Meanwhile in the PI3K/AKT pathway Tip60's action affects cell survival and proliferation by modulating acetylation status of components involved in it.
Alterations in the functions of PCAF and Tip60 link to cancer and neurodegenerative diseases. Their role in the modulation of p53 activity implicates them in tumorigenesis and progression of cancers such as breast cancer. Likewise disturbances in their normal activities are associated with Alzheimer’s disease where Tip60 interacts with proteins like APP (amyloid precursor protein) influencing the pathogenesis of neurodegeneration. The connection between these proteins and disorders highlights their importance in maintaining cellular integrity and how their dysfunction can contribute to disease development.