85-2073-48　Histone Acetyl Transferase Inhibitor VII, CTK7A (HBC, Na 4-(3,5-bis-(2-(4-Hydroxy-3-methoxy-phenyl)-ethyl)-4,5-dihydro-pyrazol-1-yl)-benzoic Acid, Na Salt Hydroxy-methoxy-phenyl-ethyl-dihydro-pyrazolyl-benzoic acid, Na Salt Sodium-4-(3,5-bis(4-hydroxy-3-methoxystyryl)-1H-pyrazol-1-yl)benzoate, HAT Inhibitor VII, p300/CBP Inhibitor V, PCAF Inhibitor III, ) 10mg　217427

特徴

• A cell-permeable and water soluble hydrazinobenzoylcurcumin (HBC) compound that acts as a selective, reversible and mixed mode inhibitor of p300/CBP and PCAF histone acetyltransferases (IC50<25 and 50uM, respectively) with minimal activity towards other histone modifying enzymes like, G9a, CARM1, HDAC1, SIRT2 and TIP60 (IC50>100uM). Blocks the autoacetylation of p300 and PCAF and histone acetylation, downregulates cyclin E expression and induces senescence-like growth arrest at 100uM in KB cells. Further, suppresses tumor growth in xenograft oral tumor nude mouse model (100mg/kg, i.p., b.i.d.) and reduces H3K14 and H3K9 acetylation levels. Reported to potently inhibit bFGF-induced bovine aortic endothelial cells (BAECs) invasion and tube formation with an IC50 of 0.93uM and binds to Ca2+/calmodulin with high-affinity (=8.11uM) and antagonize its functions in HCT15 cells.
• Molecular Formula:C28H23N2NaO6
• Molecular Weight:506.5
• Solubility (100mg/ml):DMSO
• Method for Determining Identity:Proton NMR Spectroscopic and Mass Spectrometric analysis
• Microanalysis:%C: ≥0.00%%H: ≥0.00%%N: ≥0.00%
• Water by CHN (mol):≥0.0mol
• Storage and Stability:Lyophilized and reconstituted products are stable for 6 months after receipt at -20°C. Reconstitute with DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap.