Protein Information

Name liver carboxylesterase
Synonyms ACAT; Cholesteryl ester hydrolase; CES1; SES 1; SES1; ANAE; Acid esterase; Acyl coenzyme A cholesterol acyltransferase…

Compound Information

Name piperazine
CAS piperazine

Reference List

PubMed Abstract RScore(About this table)
12736497 Ohishi K, Sawada H, Yoshida Y, Hatano H, Aiyama R, Watanabe T, Yokokura T: The metabolic stability of acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitors, N-(4-benzyloxy-3, 5-dimethoxycinnamoyl)-N'-(2, 4-dimethylphenyl) piperazine (YIC-708-424) and its derivatives in rat liver and intestinal epithelium. Biol Pharm Bull. 2003 May;26(5):600-7.
63(0,2,2,3) Details
12913263 Ohishi K, Sawada H, Yoshida Y, Yokoi W, Hatano H, Aiyama R, Watanabe T, Yokokura T: Inhibitory effects of N-(3,5-dimethoxy-4-n-octyloxycinnamoyl)-N'-(3,4-dimethylphenyl) piperazine (YIC-C8-434), an acyl-CoA:cholesterol O-acyltransferase inhibitor, on cholesterol esterification in the intestine and liver. Biol Pharm Bull. 2003 Aug;26(8):1125-8.

The effects of an acyl-CoA:cholesterol O-acyltransferase (ACAT) inhibitor, N-(3,5-dimethoxy-4-n-octyloxycinnamoyl)-N'-(3,4-dimethylphenyl) piperazine (YIC-C8-434), on cholesterol esterification in the intestine and liver were investigated in vitro and in vivo.
32(0,1,1,2) Details
11456087 Ohishi K, Aiyama R, Hatano H, Yoshida Y, Wada Y, Yokoi W, Sawada H, Watanabe T, Yokokura T: Structure-activity relationships of N-(3,5-dimethoxy-4-n-octyloxycinnamoyl)-N'-(3,4-dimethylphenyl) piperazine and analogues as inhibitors of acyl-CoA: cholesterol O-acyltransferase. Chem Pharm Bull. 2001 Jul;49(7):830-9.

A novel series of acyl-CoA: cholesterol O-acyltransferase (ACAT) inhibitors were synthesized from a lead compound, 1-(4-hydroxy-3-methoxyphenyl)-7-phenylhept-1-en-3-one (1, Yakuchinone B) through a modification of three regions (A, B, C) in the molecule.
4(0,0,0,4) Details
18448139 Bate C, Tayebi M, Williams A: Cholesterol esterification reduces the neurotoxicity of prions. Neuropharmacology. 2008 Jun;54(8):1247-53. Epub 2008 Apr 9.


Here we report that three acyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitors, TMP-153, FR179254 or YIC-C8-434, were more toxic to prion-infected neuronal cell lines (ScGT1 and ScN2a cells) than to their uninfected equivalents (GT1 and N2a cells).
2(0,0,0,2) Details
15299073 Yoon KJ, Hyatt JL, Morton CL, Lee RE, Potter PM, Danks MK: Characterization of inhibitors of specific carboxylesterases: development of carboxylesterase inhibitors for translational application. Mol Cancer Ther. 2004 Aug;3(8):903-9.

A secondary goal was to develop molecules that specifically inhibit activation of CPT-11 by a rabbit liver carboxylesterase (rCE). rCE is the most efficient CPT-11-activating enzyme thus far identified, and this enzyme is being developed for viral-directed enzyme prodrug therapy applications.
Lead compounds are derivatives of nitrophenol having 4-(furan-2-carbonyl)-piperazine-1-carboxylic acid or 4-[(4-chlorophenyl)-phenylmethyl]-piperazine-1-carboxylic acid substitutions in the p position.
1(0,0,0,1) Details
11719709 Kaneko K, Uchida K, Kobayashi T, Miura K, Tanokura K, Hoshino K, Kato I, Onoue M, Yokokura T: Sex-dependent toxicity of a novel acyl-CoA:cholesterol acyltransferase inhibitor, YIC-C8-434, in relation to sex-specific forms of cytochrome P450 in rats. Toxicol Sci. 2001 Dec;64(2):259-68.


YIC-C8-434 is a novel inhibitor of acyl coenzyme A:cholesterol acyltransferase (ACAT).
1(0,0,0,1) Details