MS37452

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MS37452  纯度: 99.22%

MS37452 是一种有效的 CBX7 chromodomain 与 H3K27me3 结合的抑制剂，Kd 为 27.7 μM。MS37452 可以通过置换 CBX7 与前列腺癌细胞中 INK4A/ARF 基因座的结合来抑制多梳抑制复合物靶基因 p16/CDKN2A 的转录。

MS37452

MS37452 Chemical Structure

CAS No. : 423748-02-1

规格 价格 是否有货 数量
5 mg ￥1500 In-stock
10 mg ￥2400 In-stock
25 mg ￥4800 In-stock
50 mg ￥7650 In-stock
100 mg ￥12200 In-stock
200 mg   询价  
500 mg   询价  

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MS37452 相关产品

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生物活性

MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a Kd of 27.7 μM. MS37452 can derepress transcription of polycomb repressive complex target gene p16/CDKN2A by displacing CBX7 binding to the INK4A/ARF locus in prostate cancer cells[1].

IC50 & Target

CBX7[1]
体外研究
(In Vitro)

MS37452 (125-500 μM; 12 hours) significantly increases INK4A/ARF transcript levels up to 25% and 60% for 250 μM and 500 μM, respectively, as compared to the DMSO control[1].
MS37452 (250 μM; 2 hours) treats human PC3 prostate cancer cells for 2 hours reducing CBX7 occupancy across the INK4A/ARF locus[1].
MS37452 (200 µM; 5 days) combined with doxorubicin results in consistently decreased cell viability compared to DMSO treated and single drug treatment[2].
MS37452 (200 µM; 5 days), which is a CBX7 chromodomain inhibitor (CBX7i), in combination with doxorubicin is a novel therapeutic strategy[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

RT-PCR[1]

Cell Line: PC3 cells
Concentration: 125-500 μM
Incubation Time: 12 hours
Result: Up-regulated INK4A/ARF expression up to 25% and 60% for 250 μM and 500 μM, respectively.

Cell Viability Assay[2]

Cell Line: Glioblastoma multiforme (GBM) U118MG cells
Concentration: PRT4165 40 µM, PTC209 200 nM, DZnep 25 µM, GSK343 400 nM, MS37452 200 µM, Doxorubicin 200 nM, temozolomide 50 µM, SAHA 1 µM
Incubation Time: 5 days
Result: Identified several combinations that resulted in consistently decreased cell viability compared to DMSO treated and single drug treatment: SAHA/TMZ and MS37452/doxorubicin.

分子量

398.45

Formula

C22H26N2O5
CAS 号

423748-02-1
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (250.97 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5097 mL 12.5486 mL 25.0972 mL
5 mM 0.5019 mL 2.5097 mL 5.0195 mL
10 mM 0.2510 mL 1.2549 mL 2.5097 mL

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.27 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Ren C, et al. Small-molecule modulators of methyl-lysine binding for the CBX7 chromodomain. Chem Biol. 2015;22(2):161-168.

    [2]. Connelly KE, et al. CBX Chromodomain Inhibition Enhances Chemotherapy Response in Glioblastoma Multiforme. Yale J Biol Med. 2016;89(4):431-440.

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