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

666-15

CAS No. : 1433286-70-4

產(chǎn)品活性：666-15 is a potent and selective CREB inhibitor with an IC₅₀ of 81 nM. 666-15 suppresses tumor growth in a breast cancer xenograft model.

研究領(lǐng)域：Epigenetics

作用靶點(diǎn)：Epigenetic Reader Domain

In Vitro: 666-15 (73 nM; for 12 hours) significantly blocks the effects caused by MSN overexpression, including cell proliferation, invasion, soft agar colony formation ability, and the expression of CREB downstream genes. 666-15 inhibits MSN overexpression-induced CREB phosphorylation.
666-15 (1μM; pretreated 2 hour) effectively inhibits PE-induced CREB phosphorylation. 666-15 significantly decreases the protein expression of ANP and β-MHC and inhibits the activation of ER stress, including the expression of GRP78, CHOP, ATF6, and the phosphorylation of IRE1 in PE?+?siRNA?+?666-15 group and PE?+?si-CTRP3?+?666-15 group.
666-15 potently inhibits cancer cell growth. In MDA-MB-231 and MDA-MB-468 cells, the GI₅₀ for 666-15 is 73 and 46 nM, respectively. In A549 and MCF-7 cells, it exhibits robust activity as well with GI₅₀ of 0.47 and 0.31 μM. 666-15 is also found to be a rather weak inhibitor of CREB-CBP interaction with IC₅₀ of 18.27 μM. 666-15 inhibits CREB’s transcription activity in living cells independent of direct CREB or CBP binding interaction. 666-15 is very potent in inhibiting CREB’s transcription activity. 666-15 also inhibits endogenous CREB target gene expression, the transcript level of nuclear receptor related 1 protein (Nurr1/NR4A2).

In Vivo: 666-15 (10 mg/kg; IP; once a week; for 11 weeks) alone can play a good role in inhibiting the growth of breast cancer, and the combination with RP-56976 (DOC) shows a better effect.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Reprogramming Compound Library  |  Endoplasmic Reticulum Stress Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Anti-Obesity Compound Library  |  Transcription Factor-Targeted Library  |  Anti-Prostate Cancer Compound Library  |  Pain-Related Compound Library  |  BRD4 Inhibitor-18  |  ACBI2  |  BI01826025  |  Curcumin  |  GSK6853  |  MI-1  |  GSK 4027  |  ZL0590  |  BRD4 Inhibitor-26  |  Apabetalone  |  PROTAC BRD2/BRD4 degrader-1  |  MS645  |  OF-1  |  I-CBP112  |  BRM/BRG1 ATP Inhibitor-2  |  UMB-32  |  Ziftomenib  |  GSK761  |  KB02-JQ1  |  CD235  |  I-BET151  |  VZ185  |  BET-IN-6  |  PLK1/BRD4-IN-1  |  MI-136  |  SF2523  |  SNIPER(BRD)-1  |  Anacardic Acid  |  NI-42

熱門(mén)產(chǎn)品線：重組蛋白  |  化合物庫(kù)  |  天然產(chǎn)物  |  熒光染料  |  PROTAC  |  同位素標(biāo)記物  |  寡核苷酸  |  抗體  |  點(diǎn)擊化學(xué)

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種全球僅有化合物庫(kù)，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(dòng)劑涉及各熱門(mén)信號(hào)通路及疾病領(lǐng)；
•   產(chǎn)品種類(lèi)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(xiàng)目；
•   提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測(cè)分析，藥物篩選等專(zhuān)業(yè)技術(shù)服務(wù)；
•   設(shè)有專(zhuān)業(yè)的實(shí)驗(yàn)中心和嚴(yán)格的質(zhì)控、驗(yàn)證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項(xiàng)質(zhì)檢報(bào)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(guó)客戶實(shí)驗(yàn)驗(yàn)證；
•   Nature, Cell, Science 等多種頂級(jí)期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專(zhuān)業(yè)團(tuán)隊(duì)跟蹤最新的制藥及生命科學(xué)研究進(jìn)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(jī)構(gòu)建立了長(zhǎng)期的合作。