MS417-GTPL7512-DataSheet-生命科學(xué)試劑-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) Ethanol : 50 mg/mL (

2、120.51 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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

3、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% EtOH 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.03 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% EtOH 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.03 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% EtOH 90% corn oil1/2 Master of Sma

4、ll Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.03 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 MS417BET 特異性蛋 BRD4 的抑制劑，能夠與 BRD4-BD1 和 BRD4-BD2 結(jié)合，IC50 值分別為 30，46nM，Kd 值分別為 36.1，25.4 nM; MS417 對(duì) CBP BRD 的選擇性較低，IC50 值為 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體外研究 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.體內(nèi)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