MS37452 | whatman (沃特曼)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

MS37452 纯度: 99.22%

MS37452 是一种有效的 CBX7 chromodomain 与 H3K27me3 结合的抑制剂，K_d 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 Chemical Structure

CAS No. : 423748-02-1

规格	价格	是否有货
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

* Please select Quantity before adding items.

MS37452 相关产品

•相关化合物库:

Bioactive Compound Library Plus
Epigenetics Compound Library
Histone Modification Research Compound Library
Anti-Cancer Compound Library
Reprogramming Compound Library
Anti-Blood Cancer Compound Library

生物活性

MS37452 is a potent inhibitor of CBX7 chromodomain binding to H3K27me3, with a K_d 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].

上海金畔生物科技有限公司 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上海金畔生物科技有限公司网站选购。

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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