666-15 _Epigenetic Reader Domain 抑制劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemE666-15Cat. No.: HY-101120CAS No.: 1433286-70-4分式: CHClNO分量: 620.52作靶點(diǎn): Epigenetic Reader Domain作通路: Epigenetics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 : 30 mg/mL (48.35 mM)* means sol

2、uble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.6116 mL 8.0578 mL 16.1155 mL5 mM 0.3223 mL 1.6116 mL 3.2231 mL10 mM 0.1612 mL 0.8058 mL 1.6116 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，

3、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 (4.03 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.03 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTI

4、VITY物活性 666-15是有效選擇性的CREB抑制劑，IC50值為81 nM。IC50 & Target IC50: 81 nM (CREB) 1體外研究 666-15 potently inhibits cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI50 for 666-15 is73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibits robust activity as well with GI50 of 0.47 and0.31 M.

5、 666-15 is also found to be a rather weak inhibitor of CREB-CBP interaction with IC50 of 18.27 M.666-15 inhibits CREBs transcription activity in living cells independent of direct CREB or CBP bindinginteraction. 666-15 is very potent in inhibiting CREBs transcription activity. 666-15 also inhibits e

6、ndogenousCREB target gene expression, the transcript level of nuclear receptor related 1 protein (Nurr1/NR4A2) 1.體內(nèi)研究 Preliminary toxicity studies show that intraperitoneal (ip) injection of 10 mg/kg of 666-15 is well tolerated inmice. The tumor growth in the mice treated with 666-15 is efficaciousl

7、y inhibited with complete tumor stasis.During the same period, the tumor volume in the vehicle-treated group is more than tripled. The body weightsof 666-15-treated animals and vehicle-treated ones are indistinguishable from each other during the entiretreatment period 1.PROTOCOLCell Assay 1 Cells a

8、re plated into 96-well plates and the cells are allowed to attach to the bottom of the plates overnight.Then the cells are treated with different concentrations of different drugs (666-15) for 72 h. The media areremoved, and MTT reagent in complete tissue culture media is added to each well and incu

9、bated at 37 C for3 h. The incubation media are removed and 100 L of DMSO is added to each well. The absorbance of theformed purple formazan solution is read at 570 nm using a plate reader 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: 66

10、6-15 is dissolved in 1% N-methylpyrrolidone (NMP), 5% Tween-80 in water. Each 6- to 8-week oldAdministration 1 BALB/c nude mouse is inoculated subcutaneously at the right flank with MDA-MB-468 cells. Mice are treatedwith either vehicle or 666-15 at 10 mg/kg. The mice are treated once a day for 5 con

11、secutive days a week,and the treatment lasted for 5 weeks 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Br J Pharmacol. 2019 Aug;176(16):2962-2976. Cell Death Dis. 2019 Jul 8;10(7):520. Sci Rep. 2019 Mar 5;9(1):3462. Cell Mol Neurobiol.

12、2019 Mar;39(2):265-286.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Xie F, et al. Identification of a Potent Inhibitor of CREB-Mediated Gene Transcription with Efficacious in Vivo Anticancer Activity. J MedChem. 2015 Jun 25;58(12):5075-87.McePdfHeightCaution: