MGH-CP1|cas:896657-58-2|西域试剂

MGH-CP1,99.21%

产品编号：Bellancom-139330| CAS NO：896657-58-2| 分子式：C₂₀H₂₄N₄OS| 分子量：368.50

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货号	价格	库存与货期
Bellancom-139330	￥700.00	杭州北京（现货）
Bellancom-139330	￥1100.00	杭州北京（现货）
Bellancom-139330	￥2400.00	杭州北京（现货）
Bellancom-139330	￥4200.00	杭州北京（现货）
Bellancom-139330	￥6800.00	杭州北京（现货）

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MGH-CP1

产品介绍

MGH-CP1 是一种有效且具有口服活性的 TEAD2 和 TEAD4 自棕榈酰化抑制剂， IC₅₀ 分别为 710 nM 和 672 nM。MGH-CP1 可降低细胞内源性或异位表达的 TEAD 蛋白棕榈酰化水平。MGH-CP1 与 Lats1/2 缺失，可抑制 Myc 表达，抑制上皮细胞过度增殖，诱导细胞凋亡 (apoptosis)。

生物活性

MGH-CP1 is a potent and orally active TEAD2 and TEAD4 auto-palmitoylation inhibitor with IC₅₀s of 710 nM and 672 nM, respectively. MGH-CP1 can decrease the palmitoylation levels of endogenous or ectopically expressed TEAD proteins in cells. MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion.

体外研究

MGH-CP1 (0-100 μM) inhibits auto-palmitoylation of recombinant TEAD2 and TEAD4 in a dose-dependent manner.
MGH-CP1 (0-2 μM) inhibits TEAD-binding sites (TBS)-Luc reporter activity in a dose-dependent manner in YAP-expressing HEK293 cells.
MGH-CP1 does not affect YAP nuclear localization or protein levels but potently inhibits TEAD-mediated transcription in a dose-dependent manner and effectively blocks cell over-proliferation.
MGH-CP1 can suppress Myc expression, inhibit epithelial over-proliferation, and induce apoptosis when together with Lats1/2 deletion.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

MGH-CP1 (75mg/kg; PO; daily, for 2 weeks) inhibits the palmitoylation of TEAD proteins in the intestinal epithelium in wild-type mice, but inhibits upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO mice intestine.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice (induced high-dose Cre recombination by intraperitoneal injection of 120mg/kg Tamoxifen for two consecutive days)
Dosage:	75 mg/kg
Administration:	PO; daily, for 2 weeks
Result:	Effectively inhibited the palmitoylation of TEAD proteins in the intestinal epithelium in wild-type mice, but effectively inhibited upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO mice intestine.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Mice (induced high-dose Cre recombination by intraperitoneal injection of 120mg/kg Tamoxifen for two consecutive days)
Dosage:	75 mg/kg
Administration:	PO; daily, for 2 weeks
Result:	Effectively inhibited the palmitoylation of TEAD proteins in the intestinal epithelium in wild-type mice, but effectively inhibited upregulation of the TEAD target genes, CTGF and ANKRD1, in Lats1/2 KO mice intestine.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (271.37 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7137 mL	13.5685 mL	27.1370 mL
5 mM	0.5427 mL	2.7137 mL	5.4274 mL
10 mM	0.2714 mL	1.3569 mL	2.7137 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 (sealed storage, away from moisture and light)。-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 (6.78 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.78 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 (6.78 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.78 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.78 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.78 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。