天堂网亚洲,天天操天天搞,91视频高清,菠萝蜜视频在线观看入口,美女视频性感美女视频,95丝袜美女视频国产,超高清美女视频图片

Birabresib (OTX015)

別名: MK 8628 中文名稱：比拉瑞塞

Birabresib (OTX015, MK 8628) 是一種有效的BET bromodomain抑制劑，在無細胞試驗中對BRD2，BRD3，和BRD4的EC50范圍為10 到 19 nM。Birabresib 可抑制 Nuclear receptor binding SET domain protein 3 (NSD3) 的靶基因表達。

Birabresib (OTX015) Chemical Structure

Birabresib (OTX015) Chemical Structure

CAS: 202590-98-5

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1613.43 現(xiàn)貨
2mg 647.01 現(xiàn)貨
10mg 1941.03 現(xiàn)貨
100mg 9582.3 現(xiàn)貨
1g 16134.3 現(xiàn)貨
更大包裝 有超大折扣

400-668-6834

info@selleck.cn
免費分裝
免費預溶

Birabresib (OTX015)相關(guān)產(chǎn)品

相關(guān)信號通路圖

Epigenetic Reader Domain Signaling Pathways

Epigenetic Reader Domain信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
MV4-11 Cell cycle assay 125 nM 24 hrs Cell cycle arrest in human MV4-11 cells assessed as increase in accumulation at G1-phase at 125 nM measured after 24 hrs by propidium iodide staining based flow cytometry 32208600
MV4-11 Function assay 500 nM 6 to 24 hrs Inhibition of BRD4 in human MV4-11 cells assessed as reduction in c-Myc expression at 500 nM measured after 6 to 24 hrs by Western blot analysis 32208600
MV4-11 Function assay 31.25 to 125 nM 6 hrs Inhibition of BRD4 in human MV4-11 cells assessed as reduction in c-Myc mRNA level at 31.25 to 125 nM measured after 6 hrs by SYBR green dye based RT-qPCR analysis 32208600
MV4-11 Function assay 31.25 to 125 nM 6 hrs Inhibition of BRD4 in human MV4-11 cells assessed as reduction in BCL2 mRNA level at 31.25 to 125 nM measured after 6 hrs by SYBR green dye based RT-qPCR analysis 32208600
MV4-11 Function assay 31.25 to 125 nM 6 hrs Inhibition of BRD4 in human MV4-11 cells assessed as reduction in CDK6 mRNA level at 31.25 to 125 nM measured after 6 hrs by SYBR green dye based RT-qPCR analysis 32208600
MV4-11 Function assay 10 to 100 nM 24 hrs Inhibition of BRD4 in human MV4-11 cells assessed as reduction in c-Myc mRNA level at 10 to 100 nM after 24 hrs by real time qPCR analysis 31490070
RKO Cell cycle assay 100 nM 24 hrs Induction of cell cycle arrest in human RKO cells assessed as increase in accumulation at G1 phase at 100 nM after 24 hrs by propidium iodide staining based flow cytometric analysis 31490070
Rosetta2 DE3 Function assay 30 mins Displacement of FAM-labeled ZBA248 from BRD3 BD2 (306 to 417 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki=0.004μM. 26080064
Rosetta2 DE3 Function assay 30 mins Displacement of FAM-labeled ZBA248 from BRD2 BD2 (349 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki=0.0054μM. 26080064
Rosetta2 DE3 Function assay 30 mins Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki=0.006μM. 26080064
MM1S Antiproliferative assay 72 hrs Antiproliferative activity against human MM1S cells after 72 hrs by CCK8 or SRB assay, IC50=0.0063μM. 31490070
Rosetta2 DE3 Function assay 30 mins Displacement of FAM-labeled ZBA248 from BRD3 BD1 (24 to 144 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki=0.0107μM. 26080064
Rosetta2 DE3 Function assay 30 mins Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki=0.0109μM. 26080064
Rosetta2 DE3 Function assay 30 mins Displacement of FAM-labeled ZBA248 from BRD2 BD1 (72 to 205 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, Ki=0.0166μM. 26080064
Rosetta2 DE3 Function assay 30 mins Displacement of FAM-labeled ZBA248 from BRD4 BD2 (333 to 460 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, IC50=0.0166μM. 26080064
MV4-11 Antiproliferative assay 4 days Antiproliferative activity against human MV4-11 cells assessed as cell growth inhibition after 4 days by CCK8 assay, IC50=0.0176μM. 31461688
MM1S Antiproliferative assay 4 days Antiproliferative activity against human MM1S cells assessed as cell growth inhibition after 4 days by CCK8 assay, IC50=0.0227μM. 31461688
Rosetta2 DE3 Function assay 30 mins Displacement of FAM-labeled ZBA248 from BRD4 BD1 (44 to 168 amino acid residues) (unknown origin) expressed in Rosetta2 DE3 cells after 30 mins by fluorescence polarization assay, IC50=0.0255μM. 26080064
BL21(DE3) Function assay 4 hrs Displacement of 5-FITC labelled (+)-JQ1 from His6-tagged human BRD4 bromodomain 1 expressed in Escherichia coli BL21(DE3) )-codon plus-RIL cells incubated for 4 hrs in dark condition by fluorescence anisotropy binding assay, IC50=0.0343μM. 31490070
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay, IC50=0.0463μM. 32208600
Kasumi-1 Antiproliferative assay 72 hrs Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay, IC50=0.135μM. 32208600
MM1S Antiproliferative assay 72 hrs Antiproliferative activity against human MM1S cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay, IC50=0.137μM. 32208600
RS4:11 Antiproliferative assay 72 hrs Antiproliferative activity against human RS4:11 cells assessed as reduction in cell viability measured after 72 hrs by Celltitre-glo luminescence assay, IC50=0.416μM. 32208600
TY82 Antiproliferative assay 72 hrs Antiproliferative activity against human TY82 cells after 72 hrs by CCK8 or SRB assay 31490070
MV4-11 Antiproliferative assay 72 hrs Antiproliferative activity against human MV4-11 cells after 72 hrs by CCK8 or SRB assay 31490070
MV4-11 Apoptosis assay 24 hrs Induction of apoptosis in human MV4-11 cells after 24 hrs by Annexin V staining based assay 31490070
THP1 Antiproliferative assay Antiproliferative activity against human THP1 cells, IC50=0.033μM. 28939121
TY82 Antiproliferative assay Antiproliferative activity against human TY82 cells, IC50=0.067μM. 28939121
insect cells Function assay Inhibition of recombinant full length human N-terminal His6-tagged BRD4 (2 to 1362 residues) expressed in baculovirus infected insect cells using histone H4 peptide as substrate by alpha screen assay, IC50=0.092μM. 30529546
LNCAP Antiproliferative assay Antiproliferative activity against human LNCAP cells, IC50=0.1114μM. 29758518
點擊查看更多細胞系數(shù)據(jù)

生物活性

產(chǎn)品描述 Birabresib (OTX015, MK 8628) 是一種有效的BET bromodomain抑制劑，在無細胞試驗中對BRD2，BRD3，和BRD4的EC50范圍為10 到 19 nM。Birabresib 可抑制 Nuclear receptor binding SET domain protein 3 (NSD3) 的靶基因表達。
特性 口服生物可利用的BRD2/3/4選擇性抑制劑，處于臨床I期臨床試驗，用于治療血液學惡性腫瘤。
靶點
BRDs [1]
(Cell-free assay)
10-19 nM(EC50)
體外研究(In Vitro)
體外研究活性 OTX015抑制BRD2，BRD3，和BRD4與AcH4的結(jié)合，IC50的范圍為92到112 nM，并抑制各種人癌細胞系的生長，GI50的范圍為60到200 nM。[1] OTX015導致c-MYC表達快速下調(diào)，并且在ALKpos ALCL細胞系中，表現(xiàn)出與ALK抑制劑結(jié)合的協(xié)同抗增殖作用。[2]
激酶實驗 TR-FRET 試驗[1]
為了評估OTX015與BRD2，BRD3，以及BRD4的結(jié)合，BRD表達的CHO細胞裂解物(來自感染表達質(zhì)粒的CHO細胞， Flag標記的BRD2，BRD3，或BRD4 或僅載體)，銪共軛的抗Flag抗體，XL-665共軛的鏈霉親和素，和生物素化的OTX015在室溫下培育0.2到2小時。熒光性通過TR-FRET使用EnVision 2103多標閱讀器測量，結(jié)合的EC50使用5.02版PRISM通過非線性回歸計算。
細胞實驗 細胞系 人腫瘤細胞
濃度 ~2 μM
孵育時間 72小時
方法

OTX015對癌細胞增殖的作用通過將人腫瘤細胞在逐漸增加濃度的OTX015下培育72小時進行評估，并使用基于四唑鹽(WST-8)的比色測定評估。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot BRD4 c-Myc

感谢您访问我们的网站，您可能还对以下资源感兴趣：

天堂网亚洲,天天操天天搞,91视频高清,菠萝蜜视频在线观看入口
日韩中文字幕免费观看,狠狠色丁香久久婷婷综合丁香,91在线视频免费看,蜜桃视频在线 亚洲色p,快活影院在线毛片,婷婷六月丁香色婷婷网,你懂的视频在线观看 国产91精品在线观看,成人一区专区在线观看,中文字幕网站在线观看,在线播放免费人成毛片试看 中文性按摩1区2区3区,国产网站在线看,八戒影视在线观看免费,四虎国产精品高清在线观看 毛片特级,美女撒尿毛片免费看,久久大尺度,人人玩人人添人人澡免费