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. Synonyms: Sodium-4-(3,5-bis(4-hydroxy-3-methoxystyryl)-1H-pyrazol-1-yl)benzoate, HBC, Na, HAT Inhibitor VII, p300/CBP Inhibitor V, PCAF Inhibitor III 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 -20C. Reconstitute with DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap.
Molekulargewicht:
506.5
Reinheit:
99% (HPLC)
Formulierung:
Supplied as a tan powder.
* Mehrwertsteuer und Versandkosten nicht enthalten. Irrtümer und Preisänderungen vorbehalten
