MS417-GTPL7512-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMS417Cat. No.: HY-111139CAS No.: 916489-36-6Synonyms: GTPL7512分式: CHClNOS分量: 414.91作靶点: Epigenetic Reader Domain作通路: Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 Ethanol : 50 mg/mL (

2、120.51 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4102 mL 12.0508 mL 24.1016 mL5 mM 0.4820 mL 2.4102 mL 4.8203 mL10 mM 0.2410 mL 1.2051 mL 2.4102 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天

3、使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.03 mM); Clear solution2. 请依序添加每种溶剂： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.03 mM); Clear solution3. 请依序添加每种溶剂： 10% EtOH 90% corn oil1/2 Master of Sma

4、ll Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (6.03 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 MS417BET 特异性蛋 BRD4 的抑制剂，能够与 BRD4-BD1 和 BRD4-BD2 结合，IC50 值分别为 30，46nM，Kd 值分别为 36.1，25.4 nM; MS417 对 CBP BRD 的选择性较低，IC50 值为 32.7 M。IC50 & Target IC50: 30 nM (BRD4-BD1), 46 nM (BRD4-BD2), 32.7 M (CBP B

5、RD) 1Kd: 36.1 nM (BRD4-BD1), 25.4 nM (BRD4-BD2) 1体外研究 MS417 is a BET-specific BRD4 inhibitor, binds to BRD4-BD1 and BRD4-BD2 with IC50s of 30, 46 nM andKds of 36.1, 25.4 nM, respectively, with less selectivity at CBP BrD (IC50, 32.7 M). MS417 effectively blocksBRD4 binding to NF-B, almost completely

6、 suppresses TNF-induced NF-B transcription activation inhuman embryonic kidney 293T cells at 1 M and also reduces NF-B p65 acetylation in the HIV-infectedRTECs. MS417 (1 M) modulation of gene transcription in HIV-infected human primary renal tubularepithelial cells. In addition, MS417 suppresses NF-

7、B-targeted cytokines and chemokines 1.体内研究 MS417 (0.08 mg/kg) markedly improves renal function, reduces proteinuria and decreasesglomerulosclerosis, tubular injury, and infiltration of inflammatory cells in the kidney of Tg26 mice 1.REFERENCES1. Zhang G, et al. Down-regulation of NF-B transcriptional activity in HIV-associated kidney disease by BRD4 inhibition. J Biol Chem.2012 Aug 17;287(34):28840-51.McePdfHeightCaution: Product has not been fully validated for medical applications.For resea