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组蛋白去乙酰化酶
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4-(二甲氨基)-N-[7-(羟基氨基)-7-氧庚]苯甲酰胺 /M344 {[allProObj[0].p_purity_real_show]}

货号：A201295 同义名： MS 344;D 237

M344 is HDAC inhibitor with IC50 of 100 nM and can induce cell differentiation.

M344 化学结构 CAS号：251456-60-7
M344 化学结构
CAS号：251456-60-7
M344 3D分子结构
CAS号：251456-60-7
M344 化学结构 CAS号：251456-60-7
M344 3D分子结构 CAS号：251456-60-7
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M344 纯度/质量文件 产品仅供科研

货号：A201295 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 HD1 ↓ HD2 ↓ HDAC ↓ HDAC1 ↓ HDAC10 ↓ HDAC11 ↓ HDAC2 ↓ HDAC3 ↓ HDAC4 ↓ HDAC5 ↓ HDAC6 ↓ HDAC7 ↓ HDAC8 ↓ HDAC9 ↓ 其他靶点 纯度
Givinostat HCl monohydrate ++++

HD1-A, IC50: 16 nM

HD1-B, IC50: 7.5 nM

 		+++

HD2, IC50: 10 nM

 		99%+
MC1568 ++

HD1-A (Maize), IC50: 100 nM

HD1-B (Maize), IC50: 3.4 μM

 		96%
Trichostatin A ++++

HDAC, IC50: ~1.8 nM

 		99%+
Scriptaid ✔ 99%+
Valproic acid sodium ✔ Autophagy 97%
AR-42 +++

HDAC, IC50: 30 nM

 		99%+
Dacinostat +++

HDAC, IC50: 32 nM

 		98+%
CUDC-101 ++++

HDAC, IC50: 4.4 nM

 		++++

HDAC1, IC50: 4.5 nM

 		+++

HDAC10, IC50: 26.1 nM

 		+++

HDAC2, IC50: 12.6 nM

 		++++

HDAC3, IC50: 9.1 nM

 		+++

HDAC4, IC50: 13.2 nM

 		+++

HDAC5, IC50: 11.4 nM

 		++++

HDAC6, IC50: 5.1 nM

 		+

HDAC7, IC50: 373 nM

 		++

HDAC8, IC50: 79.8 nM

 		++

HDAC9, IC50: 67.2 nM

 		EGFR,HER2 99%+
M344 ++

HDAC, IC50: 100 nM

 		99%+
Splitomicin +

Sir2p, IC50: 60 μM

 		95%
Panobinostat ++++

HDAC (Reh cells), IC50: 20 nM

HDAC (MOLT-4 cells), IC50: 5 nM

 		98%
Sodium 4-Phenylbutyrate ✔ 98%
Vorinostat +++

HDAC, IC50: ~10 nM

 		98%
Curcumin ✔ Nrf2,NF-κB 98%
Belinostat +++

HDAC, IC50: 27 nM

 		98%
RG-2833 ++

HDAC1, Ki: 32 nM

 		++

HDAC3, Ki: 5 nM

 		98%
Valproic acid +

HDAC1, IC50: 0.4 mM

 		98%
BG45 +

HDAC1, IC50: 2 μM

 		+

HDAC2, IC50: 2.2 μM

 		+

HDAC3, IC50: 289 nM

 		99%+
Entinostat +

HDAC1, IC50: 0.51 μM

 		+

HDAC3, IC50: 1.7 μM

 		98%
Resminostat +++

HDAC1, IC50: 42.5 nM

 		++

HDAC3, IC50: 50.1 nM

 		++

HDAC6, IC50: 71.8 nM

 		98+%
Romidepsin +++

HDAC1, IC50: 36 nM

 		+++

HDAC2, IC50: 47 nM

 		99%+
Parthenolide ✔ p53,NF-κB 97% HPLC
Tacedinaline +

HDAC1, IC50: 0.9 μM

 		+

HDAC2, IC50: 0.9 μM

 		+

HDAC3, IC50: 1.2 μM

 		98%
Mocetinostat ++

HDAC1, IC50: 0.15 μM

 		+

HDAC11, IC50: 0.59 μM

 		+

HDAC2, IC50: 0.29 μM

 		+

HDAC3, IC50: 1.66 μM

 		98%
WT-161 ++++

HDAC1, IC50: 8.35 nM

 		+++

HDAC2, IC50: 15.4 nM

 		++++

HDAC6, IC50: 0.4 nM

 		99%+
Fimepinostat ++++

HDAC1, IC50: 1.7 nM

 		++++

HDAC10, IC50: 2.8 nM

 		++++

HDAC11, IC50: 5.4 nM

 		++++

HDAC2, IC50: 5.0 nM

 		++++

HDAC3, IC50: 1.8 nM

 		+++

HDAC6, IC50: 27 nM

 		99%+
Tucidinostat ++

HDAC1, IC50: 95 nM

 		++

HDAC10, IC50: 78 nM

 		++

HDAC2, IC50: 160 nM

 		++

HDAC3, IC50: 67 nM

 		99%+
Santacruzamate A ++++

HDAC2, IC50: 119 pM

 		99%+
(E,E)-RGFP966 ++

HDAC3, IC50: 80 nM

 		99%+
LMK-235 +++

HDAC4, IC50: 11.9 nM

 		++++

HDAC5, IC50: 4.2 nM

 		99%+
Tasquinimod ✔ 99%+
CAY10603 ++++

HDAC6, IC50: 2 pM

 		98%
Tubastatin A +++

HDAC6, IC50: 15 nM

 		98%
Tubacin ++++

HDAC6, IC50: 4 nM

 		99%+
ACY-738 ++++

HDAC6, IC50: 1.7 nM

 		99%+
Nexturastat A ++++

HDAC6, IC50: 5 nM

 		99%+
BRD73954 +++

HDAC6, IC50: 36 nM

 		++

HDAC8, IC50: 120 nM

 		98%
Tubastatin A HCl +++

HDAC6, IC50: 15 nM

 		+

HDAC8, IC50: 854 nM

 		98%
PCI-34051 +++

HDAC8, IC50: 10 nM

 		99%+
Ricolinostat ++

HDAC1, IC50: 58 nM

 		++

HDAC2, IC50: 48 nM

 		++

HDAC3, IC50: 51 nM

 		++++

HDAC6, IC50: 4.7 nM

 		++

HDAC8, IC50: 100 nM

 		99%+
Droxinostat +

HDAC3, IC50: 16.9 μM

 		+

HDAC6, IC50: 2.47 μM

 		+

HDAC8, IC50: 1.46 μM

 		99%+
Abexinostat ++++

HDAC1, Ki: 7 nM

 		+++

HDAC10, IC50: 24 nM

 		+++

HDAC2, Ki: 19 nM

 		++++

HDAC3/SMRT, Ki: 8.2 nM

 		+++

HDAC6, Ki: 17 nM

 		+

HDAC8, IC50: 280 nM

 		98%+
Citarinostat +++

HDAC1, IC50: 35 nM

 		+++

HDAC2, IC50: 45 nM

 		+++

HDAC3, IC50: 46 nM

 		++++

HDAC6, IC50: 2.6 nM

 		++

HDAC8, IC50: 137 nM

 		99%+
HPOB +

HDAC1, IC50: 2.9 μM

 		+

HDAC10, IC50: 3.0 μM

 		+

HDAC2, IC50: 4.4 μM

 		+

HDAC3, IC50: 1.7 μM

 		++

HDAC6, IC50: 56 nM

 		+

HDAC8, IC50: 2.8 μM

 		97%
Quisinostat 2HCl ++++

HDAC1, IC50: 0.11 nM

 		++++

HDAC10, IC50: 0.46 nM

 		++++

HDAC11, IC50: 0.37 nM

 		++++

HDAC2, IC50: 0.33 nM

 		++++

HDAC3, IC50: 4.86 nM

 		++++

HDAC4, IC50: 0.64 nM

 		++++

HDAC5, IC50: 3.69 nM

 		++++

HDAC8, IC50: 4.26 nM

 		99+%
Domatinostat +

HDAC1, IC50: 1.20 μM

 		+

HDAC10, IC50: 21 μM

 		+

HDAC11, IC50: 9.7 μM

 		+

HDAC2, IC50: 1.12 μM

 		+

HDAC3, IC50: 0.57 μM

 		+

HDAC5, IC50: 11.3 μM

 		+

HDAC9, IC50: 50 μM

 		99%+
TMP269 ++

HDAC4, IC50: 157 nM

 		++

HDAC5, IC50: 97 nM

 		+++

HDAC7, IC50: 43 nM

 		+++

HDAC9, IC50: 23 nM

 		99%+
Pracinostat ++

HDAC1, IC50: 49 nM

 		+++

HDAC10, IC50: 40 nM

 		++

HDAC11, IC50: 93 nM

 		++

HDAC2, IC50: 96 nM

 		+++

HDAC3, IC50: 43 nM

 		++

HDAC4, IC50: 56 nM

 		+++

HDAC5, IC50: 47 nM

 		+

HDAC6, IC50: 1.008 μM

 		++

HDAC7, IC50: 137 nM

 		++

HDAC8, IC50: 140 nM

 		++

HDAC9, IC50: 70 nM

 		99%+
TMP195 ++

HDAC4, Ki: 59 nM

 		++

HDAC5, Ki: 60 nM

 		+++

HDAC7, Ki: 26 nM

 		+++

HDAC9, Ki: 15 nM

 		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

M344 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].

M344 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 <<

M344 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

M344 实验方案

计算器
存储液制备 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

M344 技术信息

CAS号251456-60-7
分子式C16H25N3O3
分子量 307.388
别名 MS 344;D 237;Histone Deacetylase Inhibitor III
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

Tags: M344 | 251456-60-7 | D 237 | MS 344 | M 344 | M-344 | D237 | D-237 | MS344 | MS 344 | MS-344 | HDAC Inhibitor | Cell Cycle/DNA Damage | Epigenetics | HDAC | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | M344 纯度/质量文件 | M344 亚型比较 | M344 生物活性 | M344 临床数据 | M344 参考文献 | M344 实验方案 | M344 技术信息

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