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CAY10602 Sale

(Synonyms: 1-(4-氟苯基)-3-(苯磺酰基)-1H-吡咯并[2,3-B]喹喔啉-2-胺) 目录号 : GC18228

A SIRT1 activator

CAY10602 Chemical Structure

Cas No.:374922-43-7

规格 价格 库存 购买数量
10mM 1 mL in DMSO
¥450.00
现货
5mg
¥405.00
现货
10mg
¥585.00
现货
50mg
¥1,710.00
现货
100mg
¥2,970.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

Sirtuin 1 (SIRT1) is an evolutionarily conserved NAD-dependent protein deacetylase that has been implicated in cell metabolism, differentiation, stress and DNA damage response, and the control of multidrug resistance in cancer. SIRT1 alters gene expression by deacetylating nuclear histones, NF-κB, p53, and FOXO transcription factors. CAY10602 was derived from high throughput screening for compounds that increase SIRT1-mediated deacetylation of a SIRT1-specific substrate. Functional assays show that CAY10602 dose-dependently suppresses the NF-κB-dependent induction of TNF-α by lipopolysaccharide in THP-1 cells, with approximately 75% inhibition achieved at 60 μM, without cytotoxicity. CAY10602 is at least 10 times more potent as a suppressor of TNF-α release than resveratrol. The effects of CAY10602 in other cellular processes remain to be determined.

实验参考方法

Cell experiment:

3T3L1 mouse fibroblasts and THP-1 leukemia cells are used and cultured following the supplier’s recommendations.THP-1 cells are treated first with representative compounds (including CAY10602/compound 1) followed by addition of lipopolysaccharide(LPS). THP-1 cells are plated at a density of 1.2×106 cells/mL in 0.4 mL (0.5×106 cells/treatment) in 24-well culture plates. The cells are preincubated with representative test compounds (including CAY10602) at 2 concentrations (20 or 60 μM) for 1 h under general tissue culture conditions[1].

References:

[1]. Nayagam VM, et al. SIRT1 modulating compounds from high-throughput screening as anti-inflammatory and insulin-sensitizing agents. J Biomol Screen. 2006 Dec;11(8):959-67.

化学性质

Cas No. 374922-43-7 SDF
别名 1-(4-氟苯基)-3-(苯磺酰基)-1H-吡咯并[2,3-B]喹喔啉-2-胺
化学名 1-(4-fluorophenyl)-3-(phenylsulfonyl)-1H-pyrrolo[2,3-b]quinoxalin-2-amine
Canonical SMILES Fc1ccc(cc1)n1c2nc3ccccc3nc2c(c1N)S(=O)(=O)c1ccccc1
分子式 C22H15FN4O2S 分子量 418.4
溶解度 DMF: 20 mg/ml,DMSO: 20 mg/ml,DMSO:PBS(pH 7.2) (1:3): 0.25 mg/ml 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.3901 mL 11.9503 mL 23.9006 mL
5 mM 0.478 mL 2.3901 mL 4.7801 mL
10 mM 0.239 mL 1.195 mL 2.3901 mL
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