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AS1842856 Sale

(Synonyms: 5-氨基-7-(环己基氨基)-1-乙基-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸) 目录号 : GC19040

AS1842856是一种细胞渗透性抑制剂,抑制Foxo1转录活性,IC50=33 nM。

AS1842856 Chemical Structure

Cas No.:836620-48-5

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10mM (in 1mL DMSO)
¥495.00
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10mg
¥408.00
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50mg
¥1,428.00
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100mg
¥2,418.00
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200mg
¥3,882.00
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500mg
¥8,000.00
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1g
¥15,000.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment [1]:

Cell lines

3T3L1 preadipocytes

Preparation Method

Cell were cultured(with or without AS1842856) in basal medium (0-2 days), adipocyte differentiation was induced with differentiation medium I(3-4 days) and differentiation medium (5-6 days), and then the cells were maintained in basal medium (7-12 days).

Reaction Conditions

1.0 µM AS1842856; 0-12 days

Applications

AS1842856 continued to inhibit Foxo1, preventing adipocyte differentiation.

Animal experiment [2]:

Animal models

Foxc2 +/- mice(lymphedema-distichiasis mouse model )

Preparation Method

Mice were injected with AS1842856 for 2 weeks.

Dosage form

10 mg/kg AS1842856;i.p.;(P) 7-21(2 weeks)

Applications

AS1842856 treatment increases the valve number in Foxc2 heterozygous mice.

References:

[1]. Zou P, Liu L, et,al. Targeting Foxo1 with AS1842856 suppresses adipogenesis. Cell Cycle. 2014;13(23):3759-67. doi: 10.4161/15384101.2014.965977. PMID: 25483084; PMCID: PMC4613185.
[2]. Ogunsina O, Banerjee R, et,al. Pharmacological inhibition of Foxo1 promotes lymphatic valve growth in a congenital lymphedema mouse model. Front Cell Dev Biol. 2023 Jan 5;10:1024628. doi: 10.3389/fcell.2022.1024628. PMID: 36742198; PMCID: PMC9890395.

产品描述

AS1842856 is a cell permeable inhibitor that inhibits Foxo1 transcriptional activity with IC50=33 nM.AS1842856 can directly bind activated Foxo1, but does not bind Foxo1 phosphorylated at Ser256. AS1842856 reduces Foxo1 activity only by binding to Foxo1, without affecting its transcription and protein expression. AS1842856 can inhibit autophagy[1-3].

AS1842856(1.0 µM; 0-12 days) continued to inhibit Foxo1, preventing adipocyte differentiation[4]. Treatment of BBC and GBM cancer cells with AS1842856(0.2-1.0 µM)led to increases in FAS (FAS cell surface death receptor) and BIM (BCL2L11) gene expression, as well as increased positivity for markers for apoptosis such as annexin V and propidium iodide[5].

AS1842856-mediated(10 days ;5 mg/kg) chemical inhibition of Foxo1 reduced the expression of the atrophy-related ubiquitin ligases and significantly reversed the adverse cardiac remodeling while improving the contractile functions in the TLR2-KO mice[6].AS1842856(10 mg/kg;i.p.;(P) 7-21(2 weeks)) treatment increases the valve number in Foxc2 heterozygous mice[7].

References:
[1]. Nagashima T, Shigematsu N, et,al. Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice. Mol Pharmacol. 2010 Nov;78(5):961-70. doi: 10.1124/mol.110.065714. Epub 2010 Aug 24. PMID: 20736318.
[2]. He J, Zhang A, et,al. The resistant effect of SIRT1 in oxidative stress-induced senescence of rat nucleus pulposus cell is regulated by Akt- Foxo1 pathway. Biosci Rep. 2019 May 10;39(5):BSR20190112. doi: 10.1042/BSR20190112. PMID: 30967498; PMCID: PMC6509061.
[3]. Tanaka H, Nagashima T, et,al. Effects of the novel Foxo1 inhibitor AS1708727 on plasma glucose and triglyceride levels in diabetic db/db mice. Eur J Pharmacol. 2010 Oct 25;645(1-3):185-91. doi: 10.1016/j.ejphar.2010.07.018. Epub 2010 Jul 23. PMID: 20655898.
[4]. Zou P, Liu L, et,al. Targeting Foxo1 with AS1842856 suppresses adipogenesis. Cell Cycle. 2014;13(23):3759-67. doi: 10.4161/15384101.2014.965977. PMID: 25483084; PMCID: PMC4613185.
[5]. Flores D, Lopez A, et,al. The Foxo1 inhibitor AS1842856 triggers apoptosis in glioblastoma multiforme and basal-like breast cancer cells. FEBS Open Bio. 2023 Feb;13(2):352-362. doi: 10.1002/2211-5463.13547. Epub 2023 Jan 16. PMID: 36602390; PMCID: PMC9900086.
[6]. Spurthi KM, Sarikhani M, et,al.Toll-like receptor 2 deficiency hyperactivates the Foxo1 transcription factor and induces aging-associated cardiac dysfunction in mice. J Biol Chem. 2018 Aug 24;293(34):13073-13089. doi: 10.1074/jbc.RA118.001880. Epub 2018 Jun 21. PMID: 29929978; PMCID: PMC6109936.
[7]. Ogunsina O, Banerjee R, et,al.Pharmacological inhibition of Foxo1 promotes lymphatic valve growth in a congenital lymphedema mouse model. Front Cell Dev Biol. 2023 Jan 5;10:1024628. doi: 10.3389/fcell.2022.1024628. PMID: 36742198; PMCID: PMC9890395.

AS1842856是一种细胞渗透性抑制剂,抑制Foxo1转录活性,IC50=33 nM。它可以直接结合活化的Foxo1,但不结合Ser256磷酸化的Foxo1。AS1842856仅通过与Foxo1结合而降低FoxO1活性,而不影响其转录和蛋白表达。AS1842856可以抑制自噬[1-3]

AS1842856(1.0µM;0 ~ 12days)持续抑制Foxo1,阻止脂肪细胞分化[4]。AS1842856(0.2 ~ 1.0 µM)处理BBC和GBM癌细胞后,FAS (FAS细胞表面死亡受体)和BIM (BCL2L11)基因表达增加,凋亡标志物如膜联蛋白V和碘化丙啶阳性增加[5]

AS1842856介导(10days;5 mg/kg)的Foxo1化学抑制降低了TLR2-KO小鼠萎缩相关泛素连接酶的表达,改善心脏收缩功能,逆转心脏重构[6]。AS1842856(10 mg/kg;i.p;(P) 7 - 21)处理可增加Foxc2杂合小鼠的瓣膜数[7]

Chemical Properties

Cas No. 836620-48-5 SDF
别名 5-氨基-7-(环己基氨基)-1-乙基-6-氟-1,4-二氢-4-氧代-3-喹啉羧酸
Canonical SMILES O=C(C1=CN(CC)C2=C(C(N)=C(F)C(NC3CCCCC3)=C2)C1=O)O
分子式 C18H22FN3O3 分子量 347.38
溶解度 DMSO : 7.6 mg/mL (21.88 mM) 储存条件 Store at -20°C
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1 mM 2.8787 mL 14.3935 mL 28.7869 mL
5 mM 0.5757 mL 2.8787 mL 5.7574 mL
10 mM 0.2879 mL 1.4393 mL 2.8787 mL
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