Drug intelligence / Profile preview

KT203

Development stage
Preclinical
Lead developer
Ono Pharmaceutical
Modality
Small Molecules
Administration
Intraperitoneal (preclinical), Oral (possible, Preclinical)
01

Overview

**KT203** is a potent and highly selective small-molecule inhibitor of **α/β-hydrolase domain-containing protein 6 (ABHD6)**, with IC50 values in the subnanomolar range (as low as 0.31 nM in Neuro2A cells)[4][7][16][18][20]. ABHD6 is an enzyme expressed in tissues such as brain, liver, kidney, and brown adipose tissue that hydrolyzes monoacylglycerols, including the endocannabinoid 2-arachidonoylglycerol (2-AG), affecting lipid signaling and metabolic pathways[1][4][5][6][10]. KT203 acts by irreversibly inhibiting ABHD6 via carbamoylation of the enzyme's active serine[6]. It displays excellent selectivity for peripheral ABHD6 and limited brain penetration, making it a useful tool for probing peripheral endocannabinoid and lipid signaling in vivo with minimized CNS effects[6]. KT203 has shown potential anti-inflammatory and antiviral activity and may modulate metabolic and immunological responses, such as macrophage polarization, cytokine release, and lipid metabolism[5][10][16]. It is primarily utilized for preclinical research; there is no evidence it has entered clinical trials or human therapeutic development as of 2025[1][6].

Brand names
KT203KT-203KT 203
Other names
1402612-64-93-[4-[1-(2-benzylpiperidine-1-carbonyl)triazol-4-yl]phenyl]benzoic acid4'-(1-(2-benzylpiperidine-1-carbonyl)-1H-1,2,3-triazol-4-yl)-[1,1'-biphenyl]-3-carboxylic acid4'-[1-[(2-Benzyl-1-piperidinyl)carbonyl]-1H-1,2,3-triazole-4-yl]-1,1'-biphenyl-3-carboxylic acid4'-[1-[[2-(phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1'-biphenyl]-3-carboxylicacid
02

Targets

ABHD6 (Alpha/beta-hydrolase domain-containing protein 6)

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