1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEJSH-23Cat. No.: HY-13982CAS No.: 749886-87-1分式: CHN分量: 240.34作靶點(diǎn): NF-B作通路: NF-B儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 56 mg/mL (233.00 mM)* means soluble, but saturation unknown.Ma

2、ss Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 4.1608 mL 20.8039 mL 41.6077 mL5 mM 0.8322 mL 4.1608 mL 8.3215 mL10 mM 0.4161 mL 2.0804 mL 4.1608 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的

3、百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.40 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (10.40 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 JSH-23NF-B 抑制劑，作于脂多糖

4、刺激的巨噬細(xì)胞 RAW 264.7，抑制 NF-B 轉(zhuǎn)錄活性，IC50 為 7.1 M。JSH-23 抑制 NF-B p65 的核易位不影響 IB 降解 1。IC50 & Target NF-B7.1 M (IC50, in RAW 264.7 cells)體外研究 JSH-2 (1-300 M; 24 hours) at 1.Nuclear amount of NF-B p65 is markedly increased upon exposure to LPS for 1 h. Treatment of JSH-23 (30M; 1 hours) to LPS- stimulated RA

5、W 264.7 cells decreases nuclear content of NF-B p65 in a dose-dependent manner 1.Cell Cytotoxicity Assay 1Cell Line: Macrophages RAW 264.7Concentration: 1, 3, 10, 30, 100, 300 MIncubation Time: 24 hoursResult: Did not show significant cytotoxic effects at 100 M.Western Blot Analysis 1Cell Line: Macr

6、ophages RAW 264.7 with LPS-stimulatedConcentration: 30 MIncubation Time: 1 hourResult: Decreased nuclear content of NF-B p65 in a dose-dependent manner, corresponding to494% inhibition at 3 M, 757% at 10 M and 958% at 30 M.體內(nèi)研究 JSH-23 (1 mg/kg, 3 mg/kg; orally administered; daily; for 2 weeks) signi

7、ficantly reverses the nerve conductionand nerve blood flow deficits seen in diabetic rats 1.Animal Model: Male Sprague Dawley diabetic rats (250-270 g) 1Dosage: 1 mg/kg, 3 mg/kgAdministration: Orally administered; daily; for 2 weeksResult: Produced significant improvement in motor nerve conduction v

8、elocity (MNCV).戶使本產(chǎn)品發(fā)表的科研獻(xiàn)2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE Sci Transl Med. 2019 Feb 6;11(478). pii: eaau5266. EBioMedicine. 2019 May;43:188-200. Cancer Lett. 2018 Aug 1;428:77-89. J Invest Dermatol. 2019 Jan;139(1):224-234. J Mol Cell Biol. 2018 Oct 15.See more customer validations

9、on HYPERLINK / www.MedChemEREFERENCES1. Shin HM, et al. Inhibitory action of novel aromatic diamine compound on lipopolysaccharide-induced nuclear translocation of NF-kappaBwithout affecting IkappaB degradation. FEBS Lett. 2004 Jul 30;571(1-3):50-4.2. Kumar A, et al. JSH-23 targets nuclear factor-kappa B and reverses various deficits in experimental diabetic neuropathy: effect onneuroinflammation and antioxidant defence. Diabetes Obes Metab. 2011 Aug;13(8):750-8.McePdfHeightCaution: Product has not been fully validated f