MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)。

NHWD-870

產(chǎn)品活性：NHWD-870 是一種高效、口服活性和選擇性的 BET family bromodomain 抑制劑，僅與 BRD2、BRD3、BRD4 (IC₅₀=2.7 nM) 和 BRDT 結(jié)合。NHWD-870 具有較強的抑癌作用，并能抑制癌細胞與巨噬細胞的相互作用。

研究領(lǐng)域：Epigenetics  |  Apoptosis

作用靶點：Epigenetic Reader Domain  |  Apoptosis

In Vitro: NHWD-870 (0.01-10000 nM) inhibits melanoma cells (A375) with an IC₅₀ of 2.46 nM.
NHWD-870 (0-10000 nM; 5 dys) suppressed cell growth.
NHWD-870 (0-50 nM; 24?hours) inhibits BRD4 phosphorylation and c-MYC expression.
NHWD-870 exhibits mild inhibition of hERG channel (IC₅₀?=?5.4?µM).NHWD-870 shows robust activities inducing apoptosis and suppressing cell proliferation.

In Vivo: NHWD-870 (0.75-3 mg/kg; p.o.) has strong anti-tumor activities in mouse models.
NHWD-870 reduces the number of tumor associated macrophages (TAMs) in subcutaneously implanted H526 and A2780 tumors. NHWD-870 downregulated CSF1 expression in tumor cells to inhibit TAM proliferation.
NHWD-870 manifests diverse mechanisms of action in different cancer settings. These include: 1) inhibition of tumor cell growth by downregulating the PDGFRβ, MEK1/2 and STAT1/MYC signaling in tumor cells; 2) inhibition of tumor angiogenesis by decreasing PDGF production in tumor cells and the PDGFRβ and MEK1/2 signaling in endothelial cells. NHWD-870 has potent tumor suppressive efficacies in xenograft mouse models of small cell lung cancer, triple negative breast cancer and ovarian cancer.

相關(guān)產(chǎn)品：Covalent Screening Library Plus  |  Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Covalent Screening Library  |  Reprogramming Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Heterocyclic Compound Library  |  SY-5609  |  BRD4 Inhibitor-18  |  8α-Tigloyloxyhirsutinolide 13-O-acetate  |  AAPK-25  |  Dutasteride-¹³C₆  |  Oleic acid-¹³C  |  ACBI2  |  Abacavir sulfate  |  Meloxicam-d₃-1  |  Thailanstatin D  |  SB-218078  |  Toyocamycin  |  Sorafenib-d₄  |  Busulfan  |  PTC-028  |  Dinaciclib  |  CR-1-31-B  |  BI01826025  |  142I5  |  Farudodstat  |  Ecteinascidin 770  |  AT9283  |  Staurosporine  |  SNS-032  |  AZA1  |  Bleomycin A5  |  Xevinapant  |  Mangiferin  |  Cambinol  |  hGGPPS-IN-1

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種全球僅有化合物庫，我們致力于為全球科研客戶提供前沿的高品質(zhì)小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動劑涉及各熱門信號通路及疾病領(lǐng)；
•   產(chǎn)品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產(chǎn)品，廣泛應(yīng)用于新藥研發(fā)、生命科學(xué)等科研項目；
•   提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測分析，藥物篩選等專業(yè)技術(shù)服務(wù)；
•   設(shè)有專業(yè)的實驗中心和嚴格的質(zhì)控、驗證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項質(zhì)檢報告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實驗驗證；
•   Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業(yè)團隊跟蹤最新的制藥及生命科學(xué)研究進展，為您提供全球新的活性化合物；
•   與世界各大制藥公司及著名科研機構(gòu)建立了長期的合作。