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KT203
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
KT203图片
CAS NO:1402612-64-9
包装与价格：
包装价格(元)
1mg电议
5mg电议
10mg电议
25mg电议

产品介绍
KT203 是一种有效且选择性的 α/β-水解酶结构域含有 6 (ABHD6) 的抑制剂，在 Neuro2A 细胞中的 IC50 为 0.31 nM。
Cas No.1402612-64-9
别名ML-296
化学名4'-[1-[[2-(phenylmethyl)-1-piperidinyl]carbonyl]-1H-1,2,3-triazol-4-yl]-[1,1'-biphenyl]-3-carboxylic acid
Canonical SMILESO=C(N1N=NC(C2=CC=C(C3=CC=CC(C(O)=O)=C3)C=C2)=C1)N4C(CC5=CC=CC=C5)CCCC4
分子式C28H26N4O3
分子量466.5
溶解度≤10mg/ml in DMSO;10mg/ml in dimethyl formamide
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

IC50:< 5 nM

KT203 is an ABHD6 inhibitor.

ABHD6, a unique and highly conserved enzyme in mammals, is prominently expressed in brain, liver, kidney, and brown adipose tissue based on global gene expression analysis and activitybased protein profiling (ABPP).

In vitro: The in-vitro potency of KT203 was studied and it was found that KT203 was able to potently inhibit ABHD6 as measured by gelbased competitive ABPP and 2-AG hydrolysis assays. Moreover, the in-situ potency was then measured by treating Neuro2A cells with varying concentrations of KT203 for 4 h and the results showed that KT203 inhibited ABHD6 with IC50 values in the subnanomolar range [1].

In vivo: In a previous animal study, mice were treated intraperitoneally with KT203 at various doses (0.1-1 mg/kg) for 4 h. Results showed that KT203 had near-complete blockade of ABHD6 in the liver at the highest dose tested. At lower doses, KT203 showed about 80% inhibition of ABHD6 in the liver. Notably, KT203 exhibited impressive selectivity in the mouse liver even at higher doses, showing little cross-reactivity against the numerous carboxylesterase enzymes that are common off-targets of mechanism-based SH inhibitors in rodents. In addition, KT203 showed good selectivity against other brain and liver SHs as judged by gelbased ABPP, suggesting a single major off-target, carboxylesterase-1 (CES1) [1].

Clinical trial: Up to now, KT203 is still in the preclinical development stage.

Reference:
[1] Hsu KL, Tsuboi K, Chang JW, Whitby LR, Speers AE, Pugh H, Cravatt BF.  Discovery and optimization of piperidyl-1,2,3-triazole ureas as potent, selective, and in vivo-active inhibitors of α/β-hydrolase domain containing 6 (ABHD6). J Med Chem. 2013 Nov 14;56(21):8270-9.