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LI-2242

Catalog No. T72034 CAS 2762762-17-2

LI-2242 is a potent inositol hexakisphosphate kinase (IP6K) inhibitor with IC50s of 31 nM, 42 nM, 8.7 nM, and 1944 nM for IP6K1, IP6K2, IP6K3, and IPMK, respectively.LI-2242 ameliorated hepatic steatosis by reducing the expression of genes that enhance lipid uptake, lipid stabilization, and adipogenesis, and enhanced mitochondrial oxygen consumption rate (OCR) and insulin signaling in adipocytes and hepatocytes in vitro. LI-2242 ameliorated diet-induced obesity, hyperglycemia and hepatic steatosis in mice.LI-2242 can be used to study type II diabetes, obesity, metabolic complications, venous thrombosis and psychiatric disorders.

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LI-2242, CAS 2762762-17-2

Pack Size	Availability	Price/USD
25 mg	Inquiry	$ 1,820.00
50 mg	Inquiry	$ 2,380.00
100 mg	Inquiry	$ 3,100.00

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Biological Description

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Description	LI-2242 is a potent inositol hexakisphosphate kinase (IP6K) inhibitor with IC50s of 31 nM, 42 nM, 8.7 nM, and 1944 nM for IP6K1, IP6K2, IP6K3, and IPMK, respectively.LI-2242 ameliorated hepatic steatosis by reducing the expression of genes that enhance lipid uptake, lipid stabilization, and adipogenesis, and enhanced mitochondrial oxygen consumption rate (OCR) and insulin signaling in adipocytes and hepatocytes in vitro. LI-2242 ameliorated diet-induced obesity, hyperglycemia and hepatic steatosis in mice.LI-2242 can be used to study type II diabetes, obesity, metabolic complications, venous thrombosis and psychiatric disorders.
Targets&IC50	IP6K1:31 nM, IP6K2:42 nM, IP6K3:8.7 nM, IPMK:1944 nM
In vitro	LI-2242 exhibits inhibitory effects on IP6K1, IP6K2, IP6K3, and IPMK with IC50 values of 31 nM, 42 nM, 8.7 nM, and 1944 nM, respectively.[1]
In vivo	We tested the efficacy of LI-2242 in DIO WT C57/BL6J mice. LI-2242 (20 mg/kg/BW daily, i.p.) reduced body weight in DIO mice by specifically reducing the accumulation of body fat. It also improved glycemic parameters and reduced hyperinsulinemia. LI-2242-treated mice displayed reduced the weight of various adipose tissue depots and an increased expression of metabolism- and mitochondrial-energy-oxidation-inducing genes in these tissues. LI-2242 also ameliorated hepatic steatosis by reducing the expression of genes that enhance lipid uptake, lipid stabilization, and lipogenesis. Furthermore, LI-2242 enhances the mitochondrial oxygen consumption rate (OCR) and insulin signaling in adipocytes and hepatocytes in vitro. In conclusion, the pharmacologic inhibition of the inositol pyrophosphate pathway by LI-2242 has therapeutic potential in obesity and NAFLD.[2]

Molecular Weight	405.27
Formula	C20H18Cl2N2O3
CAS No.	2762762-17-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Liao G, et al. Identification of Small-Molecule Inhibitors of Human Inositol Hexakisphosphate Kinases by High-Throughput Screening. ACS Pharmacol Transl Sci. 2021;4(2):780-789. 2. Mukherjee S, et al. The IP6K Inhibitor LI-2242 Ameliorates Diet-Induced Obesity, Hyperglycemia, and Hepatic Steatosis in Mice by Improving Cell Metabolism and Insulin Signaling. Biomolecules. 2023;13(5):868.

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Keywords

LI-2242 2762762-17-2 Others LI2242 LI 2242 inhibitor inhibit

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