TMP269|cas:1314890-29-3|西域试剂

TMP269,98.23%

产品编号：Bellancom-18360| CAS NO：1314890-29-3| 分子式：C₂₅H₂₁F₃N₄O₃S| 分子量：514.52

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-18360	￥640.00	杭州北京（现货）
Bellancom-18360	￥1100.00	杭州北京（现货）
Bellancom-18360	￥1700.00	杭州北京（现货）
Bellancom-18360	￥3230.00	杭州北京（现货）
Bellancom-18360	￥5168.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

TMP269

产品介绍

TMP269 是一种有效的，选择性的脱乙酰化酶 (HDAC) 抑制剂，能够抑制 HDAC 4/HDAC 5/HDAC 7/HDAC 9，IC₅₀ 值分别为 157 nM，97 nM，43 nM 和 23 nM。

生物活性

TMP269 is a novel and selective class IIa histone deacetylase (HDAC) inhibitor with IC₅₀s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.

体外研究

TMP269 has no impact on the mitochondrial activity and/or the viability of human CD4⁺ T cells at 10 μM, and may be used as tools to identify the endogenous substrates of the class IIa HDAC enzymes. In IEC-18 intestinal epithelial cells, TMP269 prevents cell cycle progression, DNA synthesis, and proliferation induced in response to G protein-coupled receptor/PKD1 activation. As with HDAC4 knockdown, TMP269 significantly enhances cytotoxicity induced by CFZ in MM cell lines, upregulating ATF4 and CHOP and inducing apoptosis. TMP269 does not hyperacetylate histone H3K9 or α-tubulin in MM cell lines, confirming that it has no inhibitory effects on class I or IIb HDACs. In a dosedependent manner, TPM269-induced cytotoxicity is associated with cleavage of caspase-8, -9, -3 and PARP, consistent with apoptosis.

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

体内研究

In vivo angiogenesis assay, MDA-MB-231 cells are mixed with growth factor-reduced Matrigel and implanted subcutaneously into the flanks of nude mice. TMP269 (subcutaneous injection; 15 mg/kg; every other day; 10 days) shows an obvious antiangiogenic effect with 76% inhibition of angiogenesis in mice^[4].

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (194.36 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9436 mL	9.7178 mL	19.4356 mL
5 mM	0.3887 mL	1.9436 mL	3.8871 mL
10 mM	0.1944 mL	0.9718 mL	1.9436 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 (4.86 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.86 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