CAS:932749-62-7 Property

Melting point:

201-202 °C(Solv: isopropanol (67-63-0); water (7732-18-5))

Boiling point:

580.8±50.0 °C(Predicted)

Density 

1.733±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≤20mg/ml in ethanol;30mg/ml in DMSO;50mg/ml in dimethyl formamide

form 

crystalline solid

pka

7.89±0.35(Predicted)

color 

Light yellow to yellow

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

CAS:932749-62-7 Chemical Properties,Usage,Production

Uses

Histone Acetyltransferase Inhibitor II is a selective, cell-permeable p300/CBP HAT inhibitor, which may be used in the treatement of cystic fibrosis.

Biological Activity

hat inhibitor ii, a cell-permeable bis-arylidene cyclohexanone compound, selectively inhibits the histone acetyltransferase p300/creb-binding protein (cbp) with an ic50 value of 5 μm. it affects gcn5 and pcaf acetyltransferases only at much higher concentrations.histone acetyltransferase p300, a ubiquitously expressed global transcriptional coactivator, plays critical roles in a wide variety of cellular phenomena, involving in cell cycle control, differentiation, and apoptosis.

in vitro

hat inhibitor ii dose-dependently suppressed the proliferation of u251, u87, hs683 and shg44 cells. in hat inhibitor ii-treated u251 and shg44 cells, cell cycle arrest at the g2/m phase was triggered by hat inhibitor ii, significant levels of apoptosis, apoptotic body formation and dna fragmentation were induced, and cleavage of caspase-3, caspase-9 and parp were caused. additionally, hat inhibitor ii upregulated 965 genes and downregulated 984 genes in hat inhibitor ii-treated u251 cells [1].

in vivo

c57bl/6j mice were intraperitoneally administrated with hat inhibitor ii at a dose of 185 μg/g for 15 min. in muscle early postmortem, hat inhibitor ii inhibited protein acetylation, which reduced amp-activated protein kinase activation induced increase in the total acetylated proteins as well as glycolytic rate [2].

References

[1]. xu, l., li, z., tao, y., li, r., fang, f., & zhao, h. et al. histone acetyltransferase inhibitor ii induces apoptosis in glioma cell lines via the p53 signaling pathway. journal of experimental & clinical cancer research. 2014; 33:108.
[2]. li, q., li, z., lou, a., wang, z., zhang, d., & shen, q. histone acetyltransferase inhibitors antagonize amp-activated protein kinase in postmortem glycolysis. asian-australasian journal of animal sciences. 2016; 30(6): 857-864.