MPT0G211

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MPT0G211

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2151853-97-1

MPT0G211 是一种高效、口服活性和选择性的HDAC6抑制剂 (IC₅₀=0.291 nM)。MPT0G211 对 HDAC6 的选择性是其他 HDAC 亚型的 1000 倍。MPT0G211 可以透过血脑屏障。MPT0G211 改善阿尔茨海默病模型中 tau 磷酸化和认知缺陷。MPT0G211 具有抗转移和神经保护作用。抗癌活性。

生物活性

MPT0G211 is a potent, orally active and selectiveHDAC6inhibitor (IC₅₀=0.291 nM). MPT0G211 displays >1000-fold selective forHDAC6over otherHDACisoforms. MPT0G211 can penetrate the blood-brain barrier. MPT0G211 ameliorates tau phosphorylation and cognitive deficits in an Alzheimer’s disease model. MPT0G211 has anti-metastatic and neuroprotective effects. Anticancer activities^[1]^[2]^[3].

IC₅₀& Target^[1]

HDAC6

0.291 μM (IC₅₀)

体外研究
(In Vitro)

MPT0G211 (0.1 μM; cells were transfected with pCAX APP 695 and pRK5-EGFP-Tau P301L for 24 h) significantly inhibits the phosphorylation of tau Ser396^[1].
MPT0G211 inhibits HDAC6/Hsp90 binding and causes subsequent proteasomal degradation of polyubiquitinated proteins^[1].
MPT0G211 significantly decreases the phosphorylation of tau by GSK3β inactivation^[1].
MPT0G211 (0.1 μM; 24 hours) significantly attenuates the phosphorylation of tau Ser396 and Ser404 in both cell lines (SH-SY5Y and Neuro-2a cells were transfected for 24 h with pCAX APP 695 and pRK5-EGFP-Tau P301L)^[1].
MPT0G211 inhibits MDA-MB-231 and MCF-7 cells growth (GI₅₀=16.19 and 5.6 μM, respectively)^[2].
In AML cells, MPT0G211 potentiated the cytotoxic effects of DOXO by impairing DNA repair machinery and activating Bcl-2-associated X protein (BCL-XL)-dependent cell apoptosis^[3].

体内研究
(In Vivo)

MPT0G211 (50 mg/kg; p.o.; daily for 3 months) significantly ameliorates the spatial memory impairment^[1].
MPT0G211 (25 mg/kg; i.p. ; qd; day 73 post-tumor injection) reduces numbers of nodules and lung weights^[2].
MPT0G211 treatment not only diminishes tau phosphorylation by inhibition GSK3β activity but also enhances the acetylation of Hsp90, which causes the downregulation of HDAC6/Hsp90 binding and facilitates proteasomal degradation of polyubiquitinated p-tau^[1].

Animal Model:	Triple transgenic (3×Tg-AD) mice (harboring APP_Sweand tau_P301Lmutant transgenes^[1]
Dosage:	50 mg/kg
Administration:	P.o.; daily for 3 months
Result:	Significantly ameliorated the spatial memory impairment.

Animal Model:	Female SCID mice (bearing MDA-MB-231 cells)^[2]
Dosage:	25 mg/kg
Administration:	I.p.; qd; day 73 post-tumor injection
Result:	Significantly reduced numbers of nodules and lung weights.

分子量

293.32

性状

Solid

Formula

C₁₇H₁₅N₃O₂

CAS 号

2151853-97-1

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(340.92 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	3.4092 mL	17.0462 mL	34.0925 mL
5 mM	0.6818 mL	3.4092 mL	6.8185 mL
10 mM	0.3409 mL	1.7046 mL	3.4092 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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 90% (20%SBE-β-CDin saline)
Solubility: ≥ 2.5 mg/mL (8.52 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (8.52 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 μL20% 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本网站选购。