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M344 Sale

(Synonyms: 4-(二甲氨基)-N-[7-(羟基氨基)-7-氧庚]苯甲酰胺,Histone Deacetylase Inhibitor III,MS344) 目录号 : GC16456

HDAC inhibitor

M344 Chemical Structure

Cas No.:251456-60-7

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥410.00
现货
5mg
¥378.00
现货
50mg
¥2,594.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

M344 is a potent inhibitor of HDAC with IC50 value of 100 nM and enable the induction of cell differentiation [1].

Treatment with M344 for 1 or 3 days induced a decreased relative p53 mRNA level and increased p21waf1/cip1 mRNA expression while no change in p53 protein. The result demonstrated the independent of p53 of inhibitory effects of M344 on MCF-7 cell growth. And the increased expression of the pro-apoptotic Puma, which can be induced by p53-independent pathways, is in accordance with the suppression of MCF-7 cell growth observed after the M344 treatment. On the other hand, M344 also show the ability in increasing the response to radiation in SCC-35 and SQ-20B human squamous carcinoma lines [2].

In MEL DS19 cells, M344 shows a much more significant effect on cell proliferation than the effect on cell differentiation. M344 exhibits toxic at concentrations of above 10 μM, when only 20% of the surviving cell population at most are induced to differentiate. M344 significantly inhibits proliferation of embryonic nervous system tumor cells, including medulloblastoma cells (D341 MED) with GI50 value of 0.65 μM and neuroblastoma cells (CH-LA 90) with GI50 value of 0.63 μM [1, 3].

M344 also plays an important role in the modification of histone and transcription factor of NF- kB in regulating HIV-1 LTR gene expression, showing the potential anti-latency therapies. Experiments were carried out in the cells, which latently infected Jurkat cells encoding the green fluorescence protein (GFP) under control of the HIV-1 LTR that act as a marker of expression of HIV-1 LTR, 72 hours after treatment with 200 nM M344, expression of HIV-1 activity was found, and the percentage of GFP-expressing cells was detected as high as 25.2% more than the cells which was subjected to mock treatment [4].

References:
[1].  Jung M, Brosch G , Kolle D, et al. Amide analogues of trichostatin A as inhibitors of histone deacetylase and inducers of terminal cell differentiation. JOURNAL OF MEDICINAL CHEMISTRY, 1999, 42 (22): 4669-4679.
[2].  Yeung A, Bhargava RK, Ahn, R, et al. HDAC inhibitor M344 suppresses MCF-7 breast cancer cell proliferation. BIOMEDICINE & PHARMACOTHERAPY, 2012, 66 (3): 232-236.
[3].  Furchert SE, Lanvers-Kaminsky C , Jurgens H , et al. Inhibitors of histone deacetylases as potential therapeutic tools for high-risk embryonal tumors of the nervous system of childhood. INTERNATIONAL JOURNAL OF CANCER, 2007, 120 (8): 1787-1794.
[4].  Ying H, Zhang YH , Zhou X , et al. Selective Histonedeacetylase Inhibitor M344 Intervenes in HIV-1 Latency through Increasing Histone Acetylation and Activation of NF-kappaB. PLOS ONE, 2012, 7 (11): e48832.

实验参考方法

Cell experiment [1]:

Cell lines

MCF-7 breast cancer cell line

Preparation method

The solubility of this compound in DMSO is > 14.75 mg/ml. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1 μM to 100 μM for 1–7 days

Applications

Bonferroni posthoc analysis indicated that treatment of MCF-7 cells with M344 for 1 day caused a significant inhibition at 50 μM, whereas treatment for 3 days showed significant inhibition at 10 μM, 50 μM and 100 μM, with a maximal inhibition of 40% at 100 μM. After 5 days, all concentrations of M344 caused a significant suppression of MCF-7 cell growth, with a maximal inhibition of 60% observed at 10 μM.

Ex-vivo animal experiment [2]:

Animal models

Brain slice from 5-day-old Wistar rats

Dosage form

Submicromolar doses

Application

Suberoylanilide hydroxamic acid (SAHA) increased survival motor neuron (SMN) levels in several neuroectodermal tissues, including rat hippocampal brain slices and motoneurone-rich cell fractions. SAHA activated survival motor neuron gene 2 (SMN2) and inhibited HDACs at submicromolar doses. In contrast to SAHA, M344 displayed unfavourable toxicity profiles.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Yeung A, Bhargava RK, Ahn, R, et al. HDAC inhibitor M344 suppresses MCF-7 breast cancer cell proliferation. BIOMEDICINE & PHARMACOTHERAPY, 2012, 66 (3): 232-236.

[2] Hahnen E et al. In vitro and ex vivo evaluation of second-generation histone deacetylase inhibitors for the treatment of spinal muscular atrophy. J Neurochem. 2006 Jul;98(1):193-202.

化学性质

Cas No. 251456-60-7 SDF
别名 4-(二甲氨基)-N-[7-(羟基氨基)-7-氧庚]苯甲酰胺,Histone Deacetylase Inhibitor III,MS344
化学名 4-(dimethylamino)-N-[7-(hydroxyamino)-7-oxoheptyl]benzamide
Canonical SMILES CN(C)C1=CC=C(C=C1)C(=O)NCCCCCCC(=O)NO
分子式 C16H25N3O3 分子量 307.39
溶解度 ≥ 14.75 mg/mL in DMSO, ≥ 12.88 mg/mL in EtOH with ultrasonic 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 3.2532 mL 16.266 mL 32.532 mL
5 mM 0.6506 mL 3.2532 mL 6.5064 mL
10 mM 0.3253 mL 1.6266 mL 3.2532 mL
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