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M344

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Chemical Structure| 251456-60-7 同义名 : MS 344;D 237;Histone Deacetylase Inhibitor III
CAS号 : 251456-60-7
货号 : A201295
分子式 : C16H25N3O3
纯度 : 99%+
分子量 : 307.388
MDL号 : MFCD03453554
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(341.59 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • HDAC

    HDAC, IC50:100 nM
描述 Histone deacetylases are a family of enzymes that catalyze the removal of acetyl functional groups from the lysine residues. They are considered as conserved homologues of transcriptional regulators and nucleolar phosphoproteins. M344 is an inhibitor of histone deacetylase with an IC50 value of 100 nM. The treatment of MEL cells with 20 µM M344 inhibited the enzymatic activity of histone deacetylase[3]. M344 at 1 and 5 μM reduced the mRNA and protein expression of BRCA1 expression in breast and ovarian cancer cell lines. The treatment with M344 (1 μM) for 24h potentiated the effects of cisplatin and increased apoptosis in breast and ovarian cancer cells[4]. In a triple transgenic mouse model of Alzheimer’s disease (3xTg AD), repeated i.p. treatment with M344 (3 and 10 mg/kg) for 4 months dose-dependently increased spontaneous alternation in Y-maze (67.0% and 71.2%, respectively) compared to the vehicle controls. M344 at doses of 3 and 10 mg/kg also significantly decreased Aβ1-42 in the hippocampus of 3xTg AD mice (-42.7% and -35.6%, respectively)[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01064921 Stage III Squamous Cell Carcin... 展开 >>oma of the Oropharynx Stage IV Squamous Cell Carcinoma of the Oropharynx 收起 << Phase 1 Completed - United States, Ohio ... 展开 >> The Ohio State University Comprehensive Cancer Center Columbus, Ohio, United States, 43210 收起 <<
NCT00262834 Breast Cancer ... 展开 >> Stage I Breast Cancer Stage II Breast Cancer Stage III Breast Cancer 收起 << Not Applicable Completed - United States, Maryland ... 展开 >> Johns Hopkins University/Sidney Kimmel Cancer Center Baltimore, Maryland, United States, 21287 收起 <<
NCT01297764 Multiple Myeloma Phase 1 Phase 2 Active, not recruiting August 2019 United States, New Jersey ... 展开 >> Hackensack University Medical Center Hackensack, New Jersey, United States, 07601 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.25mL

0.65mL

0.33mL

16.27mL

3.25mL

1.63mL

32.53mL

6.51mL

3.25mL
参考文献

[1]Takai N, Ueda T, et al. M344 is a novel synthesized histone deacetylase inhibitor that induces growth inhibition, cell cycle arrest, and apoptosis in human endometrial cancer and ovarian cancer cells. Gynecol Oncol. 2006 Apr;101(1):108-13.

[2]Jung M, Brosch G, et al. Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation. J Med Chem. 1999 Nov 4;42(22):4669-79.

[3]Jung M, Brosch G, Kölle D, Scherf H, Gerhäuser C, Loidl P. Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation. J Med Chem. 1999;42(22):4669-4679. doi:10.1021/jm991091h

[4]Weberpals JI, O'Brien AM, Niknejad N, Garbuio KD, Clark-Knowles KV, Dimitroulakos J. The effect of the histone deacetylase inhibitor M344 on BRCA1 expression in breast and ovarian cancer cells. Cancer Cell Int. 2011;11(1):29. Published 2011 Aug 19. doi:10.1186/1475-2867-11-29

[5]Volmar CH, Salah-Uddin H, Janczura KJ, et al. M344 promotes nonamyloidogenic amyloid precursor protein processing while normalizing Alzheimer's disease genes and improving memory. Proc Natl Acad Sci U S A. 2017;114(43):E9135-E9144. doi:10.1073/pnas.1707544114