MS67,2407452-77-9

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

MS67

CAS No. : 2407452-77-9

MCE 国际站：MS67

产品活性：MS67 是一种有效的选择性 WD40 重复域蛋白 5 (WDR5) 降解剂，K_d 为 63 nM。MS67 对其他蛋白质甲基转移酶、激酶、GPCR、离子通道和转运蛋白无活性。MS67 显示出有效的抗癌作用。

研究领域：Epigenetics  |  PROTAC

作用靶点：Histone Methyltransferase  |  PROTACs

In Vitro: MS67 (0.001-1 μM) induces WDR5 degradation at a concentration as low as 1 nM. MS67 induces WDR5 depletion much more effectively in all six mixed lineage leukemia (MLL)-r acute myeloid leukemia (AML) and four pancreatic ductal adenocarcinoma (PDAC) cell lines without a hook effect and in a concentration-dependent manner in PDAC cells.
MS67 decreases H3K4me2/3 in both MV4;11 and MIA PaCa-2 cells, whereas other examined histone methylation marks such as H3K9me3, H3K27me3, and H3K36me3 are not affected . MS67 is effective in suppressing both WDR5-related gene expression programs and WDR5/MLL-induced H3K4 methylations on chromatin.
The GI₅₀ values of MS67 in the two most sensitive AML lines, MV4;11 and EOL-1, are 15 nM and 38 nM, respectively. MLL-r acute leukemia cell lines including MV4;11, EOL-1, MOLM13, KOPN8, RS4;11, and THP-1 are sensitive to MS67, whereas leukemia cell lines that did not harbor MLL-r (including K562, HL60, and a murine AML line transformed by Hoxa9 plus Meis1) are insensitive to MS67.
. MS67 binds to VCB (VHL-Elongin C-Elongin B ternary complex), with a K_d of 140 nM.

In Vivo: MS67 (75 mg/kg; i.p.; twice daily; 5 days a week; for 20 days) significantly inhibits tumor growth in vivo and prolongs survival of the treated mice.
After a single intraperitoneal (i.p.) injection of MS67 at a dose of 75 mg/kg, the Cmax reached at about 4.2 μM, and the concentration of MS67 retained above 0.5 μM over 12 hours.

相关产品：Tazemetostat  |  GSK126  |  GSK3326595  |  Pinometostat  |  3-Deazaneplanocin A hydrochloride  |  MZ 1  |  ARV-825  |  GSK3368715 dihydrochloride  |  dBET6  |  EPZ015666  |  dBET1  |  JNJ-64619178  |  EED226  |  GSK343  |  ARV-771  |  UNC0642  |  UNC1999  |  Chaetocin  |  EZM 2302  |  BIX-01294  |  MS023  |  ACBI1  |  UNC0379  |  ARV-471  |  CM-272  |  LC-2  |  SD-36  |  MM-102 TFA  |  PROTAC K-Ras Degrader-1  |  UNC0638

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  染料试剂  |  PROTAC  |  同位素标记物  |  寡核苷酸

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Dye Reagents  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种TOP期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪前沿的制药及生命科学研究进展，为您提供全球前沿的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。