货号 | 4857/50 |
别名 | 2-Amino-7-(1-methylethyl)-5-oxo-5H- |
供应商 | Tocris |
生物活性 | Selective inhibitor of TANK-binding kinase 1 (TBK1) and IKKε(IC50 values are ~1-2 μM). Displays no effect on IKKα or IKKβ at these concentrations. Reversibly lowers weight, increases insulin sensitivity, and reduces inflammation and steatosis in three mouse models of obesity. Exhibits antiallergic activity; inhibits the release of histamine from rat mast cells. Also binds to Hsp90 and inhibits C-terminal chaperone activity in vitro. |
运输条件 | Blue Ice |
存放说明 | -20℃ |
纯度 | >99 % |
计算分子量 | 298.29 |
分子式 | C16H14N2O4 |
可溶性/溶解性 | Soluble to 100 mM in DMSO |
参考文献 | Reillyet al (2012) An inhibitor of the protein kinases TBK1 and IKK-ε improves obesity-related metabolic dysfunctions in mice. Nat.Med. 19 313. PMID: 23396211. Okadaet al (2003) Hsp90 is a direct target of the anti-allergic drugs disodium cromoglycate and amlexanox. Biochem.J. 374 433. PMID: 12803546. Makinoet al (1987) Mechanism of action of an antiallergic agent, amlexanox (AA-673), in inhibiting histamine release from mast cells. Acceleration of cAMP generation and inhibition of phosphodiesterase. Int.Arch.Allergy Appl.Immunol. 82 66. PMID: 2433225. |