生產(chǎn)地：品牌：MedChemExpress （MCE）

移動電話：18019480960公司傳真：86-021-53700325

更新時間：2019-06-26

MedChemExpress (MCE) 專注于為全球科學(xué)家提供高品質(zhì)的生物活性小分子化合物，化合物庫及各類試劑盒，總部位于美國新澤西。
 MedChemExpress (MCE) 產(chǎn)品作用于 20 多個熱門信號通路及研究領(lǐng)域的300多個細(xì)分靶點，擁有 10000 特異性抑制劑、激動劑，以及 30 活性化合物篩選庫；
 我們堅持對所有產(chǎn)品進(jìn)行嚴(yán)格質(zhì)檢，確保產(chǎn)品的高品質(zhì)和高純度；
 MedChemExpress (MCE) 產(chǎn)品已被全球數(shù)萬名科學(xué)家信賴，并被大量Top文獻(xiàn)和Patent引用；
 我們擁有專業(yè)的技術(shù)團隊追蹤全球前沿科技進(jìn)展，不斷豐富各個靶點的特異性產(chǎn)品，堅持做 您身邊的抑制劑大師 ；
 MedChemExpress (MCE) 與全球眾多知名藥企和科研機構(gòu)保持深度合作；
 大量產(chǎn)品有中國庫存，工作日 16:00 前訂單確保當(dāng)日發(fā)貨，次日送達(dá)。
MCE 中國：www.MedChemExpress.cn

Hotline: 400-820-3792
Tel: 021-58955995
Email: sales@MedChemExpress.cn
Tech Support: 021-58950656

產(chǎn)品活性：GNE-049 是一種高效的選擇性 CBP 抑制劑，在 TR-FRET 實驗中 IC50 為 1.1 nM。GNE-049 還抑制 BRET 和 BRD4 (1)，IC50 分別為 12 nM 和 4200 nM。

研究領(lǐng)域：Epigenetics

作用靶點：Epigenetic Reader Domain | Histone Acetyltransferase

In Vitro: GNE-049 is selected for further profiling as it has the best balance of liver microsomes (LM) stability, selectivity, and cellular potency GNE-049 has excellent potency in the BRET cellular assay and, in an orthogonal measure of the target engagement, GNE-049 is shown to inhibit the expression of MYC (MV4-11 cell line) with an EC50 of 14 nM.

In Vivo: GNE-049 demonstrates acceptable PK in mouse, rat, dog, and monkey. Determination of potency versus a selection of bromodomains revealed that GNE-049 is selective for CBP/P300 and, importantly, quite selective (3820-fold) over BRD4(1). GNE-049 is further evaluated in a rat single dose (30-250 mg/kg QD) toxicokinetic study. Adverse central nervous system (CNS)-related signs (e.g., marked hyperactivity and vocalization) are observed in several of the rats at the 250 mg/kg dose level. Furthermore, at the 250 mg/kg dose level, the ratio of the unbound drug concentration in brain to unbound drug concentration in plasma (Kp,uu) 3 h post dose is determined to be 0.43, indicating that GNE-049 is penetrating into the CNS and potentially resulting in the observed toxicity.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus | (+)-JQ-1 | A-485 | Birabresib | Curcumin | ARV-825 | ARV-771 | Molibresib | BI 2536 | C646 | 666-15 | I-BET151 | dBET1 | CPI-637 | dBET6 | Mivebresib | UNC1999 | MZ 1 | I-BRD9 | IACS-9571 Hydrochloride | SGC-CBP30 | WM-1119 | ABBV-744 | CPI-203 | KG-501 | GNE-272 | PLX51107 | PFI-3 | Anacardic Acid