Description
Key facts
CAS number:328968-36-1,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:445.4 Da,
Molecular formula:C24H19N3O6,
PubChem:2871948,
Nature:Synthetic,
Solubility:Soluble in DMSO to 25 mM,
Biochemical name:4-(4-((5-(4,5-Dimethyl-2-nitrophenyl)furan-2-yl)methylene)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl)benzoic acid,
Biological description:Cell-permeable, competitive, selective, potent p300/CBP histone acetyltransferase inhibitor (Ki = 400 nM). Blocks dynamic acetylation. Anticancer agent. Active in vitro and in vivo.,
Canonical smiles:CC1=CC(=C(C=C1C)[N+](=O)[O-])C2=CC=C(O2)C=C3C(=NN(C3=O)C4=CC=C(C=C4)C(=O)O)C,
InChi:InChI=1S/C24H19N3O6/c1-13-10-20(21(27(31)32)11-14(13)2)22-9-8-18(33-22)12-19-15(3)25-26(23(19)28)17-6-4-16(5-7-17)24(29)30/h4-12H,1-3H3,(H,29,30),
InChiKey:HEKJYZZSCQBJGB-UHFFFAOYSA-N,
IUPAC Name:4-[4-[[5-(4,5-dimethyl-2-nitrophenyl)furan-2-yl]methylidene]-3-methyl-5-oxopyrazol-1-yl]benzoic acid
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 under desiccating conditions, The product can be stored for up to 12 months
Supplementary Information:
This supplementary information is collated from multiple sources and compiled automatically.
KAT3B also known as p300 is a histone acetyltransferase with a molecular weight of approximately 300 kDa. Known for its ability to acetylate histone and non-histone proteins p300 modulates gene expression by altering chromatin structure. The protein is ubiquitously expressed across various tissues impacting numerous cellular processes by its mechanical functions of modifying chromatin.
Biological function summary
KAT3B/p300 influences multiple cellular activities like cell growth differentiation and apoptosis. It functions as a transcriptional coactivator and integrates various signaling pathways into the cell's gene expression program. p300 often forms complexes with other transcription factors enhancing or repressing their activity based on the cellular context. By modifying transcription factors it plays an essential role in controlling cell fate decisions.
Pathways
P300 participates in the regulation of significant cellular processes including the Wnt signaling pathway and the p53 pathway. In the Wnt signaling pathway p300 acts alongside beta-catenin to regulate gene expression while in the p53 pathway it acetylates the p53 protein influencing the cell’s response to DNA damage. These pathways highlight p300's interaction with important proteins such as CBP (CREB-binding protein) which shares a similar functional repertoire and works synergistically in gene regulation.
P300 is implicated in cancers and congenital disorders. In cancer aberrant regulation or mutation of p300 can lead to uncontrolled cell proliferation and tumor growth; p300 inhibitors like C646 are researched for their therapeutic potential. Additionally Rubinstein-Taybi syndrome a congenital disorder results from mutations in the p300 gene showcasing p300’s importance in developmental processes. The interplay of p300 with proteins such as CBP is also relevant in these conditions where disrupted interactions may lead to disease manifestation.
