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EX229

Catalog No. TQ0028 CAS 1219739-36-2

Synonyms: Compound 991, C991

EX229 (C991) is an allosteric activator of AMPK, with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1, and α1β2γ1, respectively.

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EX229, CAS 1219739-36-2

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 68.00
10 mg	In stock	$ 113.00
25 mg	In stock	$ 233.00
50 mg	In stock	$ 396.00
100 mg	In stock	$ 595.00
1 mL * 10 mM (in DMSO)	In stock	$ 77.00

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Purity: 99.36%

Purity: 99.22%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	EX229 (C991) is an allosteric activator of AMPK, with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1, and α1β2γ1, respectively.
Targets&IC50	AMPK α1β1γ1:0.06 μM (Kd), AMPK α1β2γ1:0.51 μM (Kd), AMPK α2β1γ1:0.06 μM (Kd)
In vitro	Treatment of hepatocytes with EX229 (991) alone results in a slight increase in the phosphorylation of AMPK and RAPTOR only at 0.3 μM, whereas a robust increase in ACC phosphorylation is readily observed and saturated at a concentration of 0.03 μM EX229. AICAR or C13 alone robustly increases T172 phosphorylation of AMPKα, and when 991 is coincubated, there is a modest additional dose-dependent increase in AMPKα phosphorylation. RAPTOR phosphorylation is modestly increased by AICAR or C13 alone, and it is dose-dependently increased when coincubation is carried out with EX229. EX229 also dose-dependently (0.01 and 0.1 μM) inhibits lipogenesis (34% and 63%, respectively), which is further reduced when it is coincubated with a low dose of AICAR (0.03 mM) or C13 (1 μM). Treatment with EX229 promotes dose-dependent increases in ACC and RAPTOR phosphorylation. Similar to the observations in hepatocytes [2].

Synonyms	Compound 991, C991
Molecular Weight	431.87
Formula	C24H18ClN3O3
CAS No.	1219739-36-2

Storage

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

Solubility Information

DMSO: 12 mg/mL (27.78 mM), Sonification and heating are recommended.

References and Literature

1. Xiao B, et al. Structural basis of AMPK regulation by small molecule activators. Nat Commun. 2013;4:3017. 2. Bultot L, et al. Benzimidazole derivative small-molecule 991 enhances AMPK activity and glucose uptake induced by AICAR or contraction in skeletal muscle. Am J Physiol Endocrinol Metab. 2016 Oct 1;311(4):E706-E719.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Prostate Cancer Compound Library Epigenetics Compound Library AMPK-Targeted Compound Library Oxidation-Reduction Compound Library Anti-Cancer Metabolism Compound Library Anti-Diabetic Compound Library Anti-Breast Cancer Compound Library Bioactive Compound Library Anti-Lung Cancer Compound Library

Related Products

Related compounds with same targets

N-[(4-Aminophenyl)methyl]adenosine AMPK-IN-3 MK-3903 Ampkinone Palmitelaidic Acid Gomisin J GSK621 AICAR

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Keywords

EX229 1219739-36-2 Chromatin/Epigenetic PI3K/Akt/mTOR signaling AMPK EX 229 AMP-activated protein kinase inhibit Inhibitor C 991 Compound 991 C991 C-991 EX-229 inhibitor

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