Terameprocol (Synonyms: EM-1421)

目录号: HY-10447 纯度: 99.33%: Data Sheet SDS COA 产品使用指南
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Terameprocol 是转录因子 Sp1 的抑制剂，可选择性抑制依赖 Sp1 的基因转录。Terameprocol 通过抑制 Sp1 介导的基因转录，如抑制 CDC2、survivin 和 HMGB1 等基因的表达，进而阻滞细胞周期、诱导细胞凋亡以及抑制炎症反应。Terameprocol 可发挥抗增殖、促凋亡和抗炎活性，可用于癌症和肺动脉高压等疾病领域的研究。

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Terameprocol Chemical Structure

CAS No. : 24150-24-1

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥610	In-stock
5 mg	￥343	In-stock
10 mg	￥550	In-stock
25 mg	￥1000	In-stock
50 mg	￥1600	In-stock
100 mg	￥2600	In-stock
200 mg		询价
500 mg		询价

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Terameprocol 相关产品

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COX COX-1 COX-2 COX-3

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TNFRSF1A/CD120a TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

生物活性
纯度 & 产品资料
参考文献

生物活性

Terameprocol is an inhibitor targeting the Sp1 transcription factor, which can selectively inhibit the transcription of Sp1-dependent genes. Terameprocol exerts its effects by inhibiting Sp1-mediated gene transcription, such as reducing the expression of genes like CDC2, survivin and HMGB1, thereby arresting the cell cycle, inducing apoptosis, and suppressing the inflammatory response. Terameprocol exhibits anti-proliferative, pro-apoptotic, and anti-inflammatory activities and is currently mainly used in the research of diseases such as cancer and pulmonary arterial hypertension[1][2][3].

IC₅₀ & Target

COX-2

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
786-0	GI₅₀	4.54 μM Compound: Terameprocol, M4N, EM-1421	Cytotoxicity against human 786-0 cells after 72 hrs by MTT assay Cytotoxicity against human 786-0 cells after 72 hrs by MTT assay	[PMID: 24080463]
A-375	IC₅₀	16.6 μM Compound: 1a, M4N	Cytotoxicity against human A375 cells after 5 days by MTT assay Cytotoxicity against human A375 cells after 5 days by MTT assay	[PMID: 19615898]
BXPC-3	GI₅₀	17.1 μM Compound: Terameprocol, M4N, EM-1421	Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay Cytotoxicity against human BxPC3 cells after 72 hrs by MTT assay	[PMID: 24080463]
C8166	CC₅₀	28.8 μM Compound: 21	Cytotoxicity against human C8166 cells by MTT assay Cytotoxicity against human C8166 cells by MTT assay	[PMID: 19413342]
HeLa	GI₅₀	> 50 μM Compound: Terameprocol, M4N, EM-1421	Cytotoxicity against human HeLa cells after 72 hrs by MTT assay Cytotoxicity against human HeLa cells after 72 hrs by MTT assay	[PMID: 24080463]
Hep 3B2	IC₅₀	≤ 10 μM Compound: 3, M4N	Cytotoxicity against human Hep3B cells after 3 days by MTT assay Cytotoxicity against human Hep3B cells after 3 days by MTT assay	[PMID: 21123067]
HepG2	IC₅₀	44.5 μM Compound: 1a, M4N	Cytotoxicity against human HepG2 cells after 5 days by MTT assay Cytotoxicity against human HepG2 cells after 5 days by MTT assay	[PMID: 19615898]
HT-29	IC₅₀	≤ 10 μM Compound: 3, M4N	Cytotoxicity against human HT-29 cells after 3 days by MTT assay Cytotoxicity against human HT-29 cells after 3 days by MTT assay	[PMID: 21123067]
HT-29	IC₅₀	61.5 μM Compound: 1a, M4N	Cytotoxicity against human HT-29 cells after 5 days by MTT assay Cytotoxicity against human HT-29 cells after 5 days by MTT assay	[PMID: 19615898]
K562	IC₅₀	5.87 mg/L Compound: 2, EM-1421, M4N, Terameprocol	Inhibition of growth metabolism of human K562 cells at 37 degC by TAM air microcalorimetry Inhibition of growth metabolism of human K562 cells at 37 degC by TAM air microcalorimetry	[PMID: 23434529]
LNCaP	IC₅₀	≤ 10 μM Compound: 3, M4N	Cytotoxicity against human LNCAP cells after 3 days by MTT assay Cytotoxicity against human LNCAP cells after 3 days by MTT assay	[PMID: 21123067]
MCF7	IC₅₀	≤ 10 μM Compound: 3, M4N	Cytotoxicity against human MCF7 cells after 3 days by MTT assay Cytotoxicity against human MCF7 cells after 3 days by MTT assay	[PMID: 21123067]
MCF7	IC₅₀	42.4 μM Compound: 1a, M4N	Cytotoxicity against human MCF7 cells after 5 days by MTT assay Cytotoxicity against human MCF7 cells after 5 days by MTT assay	[PMID: 19615898]
NCI/ADR-RES	IC₅₀	≤ 10 μM Compound: 3, M4N	Cytotoxicity against human NCI/ADR-RES cells after 3 days by MTT assay Cytotoxicity against human NCI/ADR-RES cells after 3 days by MTT assay	[PMID: 21123067]
T47D	GI₅₀	5.36 μM Compound: Terameprocol, M4N, EM-1421	Cytotoxicity against human T47D cells after 72 hrs by MTT assay Cytotoxicity against human T47D cells after 72 hrs by MTT assay	[PMID: 24080463]
T98G	GI₅₀	> 50 μM Compound: Terameprocol, M4N, EM-1421	Cytotoxicity against human T98G cells after 72 hrs by MTT assay Cytotoxicity against human T98G cells after 72 hrs by MTT assay	[PMID: 24080463]
U-87MG ATCC	GI₅₀	> 50 μM Compound: Terameprocol, M4N, EM-1421	Cytotoxicity against human U87 cells after 72 hrs by MTT assay Cytotoxicity against human U87 cells after 72 hrs by MTT assay	[PMID: 24080463]

体外研究
(In Vitro)

Terameprocol (25 μM；16 h) 在 RAW 264.7 细胞实验中，抑制脂多糖 (LPS) 诱导的前列腺素 (PGE2)、部分细胞因子和趋化因子的产生，还抑制 COX-2 的表达和活性，且抑制 RAW264.7 细胞生长，但不诱导细胞凋亡^[1]。
Terameprocol (10 μM；24 h，48 h) 在 HCC2429 和 H460 非小细胞肺癌细胞实验中，下调 survivin 转录和蛋白表达，同时增强细胞对放疗的敏感性，但不诱导细胞凋亡，不影响细胞周期^[2]。
Terameprocol (0.1-20 μM；24 h) 在大鼠肺动脉平滑肌细胞 (PASMCs) 实验中，以剂量依赖方式抑制细胞增殖，20 μM 时诱导细胞凋亡^[3]。

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

Cell Viability Assay^[1]

Cell Line:	RAW 264.7 cells
Concentration:	25 μM
Incubation Time:	16 h
Result:	Inhibited the LPS-induced production of prostaglandins, including PGE2, PGF2α, and 6-keto - PGF1α. Suppressed the production of several cytokines and chemokines, such as TNF-α and MCP-1. Reduced the expression of COX-2 mRNA and protein, inhibited the enzymatic activity of COX-2, and inhibited the growth of RAW 264.7 cells, but did not induce apoptosis.

Cell Cycle Analysis^[2]

Cell Line:	HCC2429 and H460 cells
Concentration:	10 μM
Incubation Time:	24 h or 48 h
Result:	Down-regulated the transcription and protein expression of survivin. Enhanced the radiosensitivity of both HCC2429 and H460 cells. Did not induce apoptosis in either cell line and had no significant effect on the cell cycle.

Apoptosis Analysis^[3]

Cell Line:	Rat pulmonary artery smooth muscle cells (PASMCs)
Concentration:	0.1 μM, 1 μM, 10 μM, 20 μM
Incubation Time:	24 h
Result:	Inhibited the proliferation of PASMCs in a dose-dependent manner. At 20μM, induced apoptosis of PASMCs.

体内研究
(In Vivo)

Terameprocol (1 mg/100 μL；ip；1 次；在注射 LPS 前 1 小时给药) 在 C57BL6/J 小鼠内毒素血症模型中，降低小鼠血清中 TNF-α 和 MCP-1 水平^[1]。
Terameprocol (166 mg/kg；腹腔注射；第 7、12、17 天；21 天) 在野百合碱 (HY-N0750) 诱导的大鼠肺动脉高压模型中，改善心脏功能，减轻心脏和肺部重塑，抑制肺动脉平滑肌细胞增殖并诱导其凋亡^[3]。

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

Animal Model:	C57BL6/J mice (15-16g, 6-8 weeks old)^[1]
Dosage:	1 mg (in CPE vehicle)
Administration:	Intraperitoneal injection, 1 time, 1 hour before LPS injection
Result:	Offset the increase in serum TNF-α induced by LPS by 41% and significantly suppressed the LPS-induced accumulation of MCP-1 in serum.

Clinical Trial

分子量

358.47

Formula

C₂₂H₃₀O₄

CAS 号

24150-24-1

性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (278.96 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7896 mL	13.9482 mL	27.8963 mL
5 mM	0.5579 mL	2.7896 mL	5.5793 mL
10 mM	0.2790 mL	1.3948 mL	2.7896 mL

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.33%

选择批次：

Data Sheet (624 KB) SDS (459 KB)

COA (283 KB) HNMR (241 KB) LCMS (89 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Eads D, et al. Terameprocol, a methylated derivative of nordihydroguaiaretic acid, inhibits production of prostaglandins and several key inflammatory cytokines and chemokines. J Inflamm (Lond). 2009 Jan 8;6:2. [Content Brief]

[2]. Sun Y, et al. Terameprocol (tetra-O-methyl nordihydroguaiaretic acid), an inhibitor of Sp1-mediated survivin transcription, induces radiosensitization in non-small cell lung carcinoma. J Thorac Oncol. 2011 Jan;6(1):8-14. [Content Brief]

[3]. Nogueira-Ferreira R, et al. HMGB1 down-regulation mediates terameprocol vascular anti-proliferative effect in experimental pulmonary hypertension. J Cell Physiol. 2017 Nov;232(11):3128-3138. [Content Brief]

Terameprocol 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7896 mL	13.9482 mL	27.8963 mL	69.7408 mL
	5 mM	0.5579 mL	2.7896 mL	5.5793 mL	13.9482 mL
	10 mM	0.2790 mL	1.3948 mL	2.7896 mL	6.9741 mL
	15 mM	0.1860 mL	0.9299 mL	1.8598 mL	4.6494 mL
	20 mM	0.1395 mL	0.6974 mL	1.3948 mL	3.4870 mL
	25 mM	0.1116 mL	0.5579 mL	1.1159 mL	2.7896 mL
	30 mM	0.0930 mL	0.4649 mL	0.9299 mL	2.3247 mL
	40 mM	0.0697 mL	0.3487 mL	0.6974 mL	1.7435 mL
	50 mM	0.0558 mL	0.2790 mL	0.5579 mL	1.3948 mL
	60 mM	0.0465 mL	0.2325 mL	0.4649 mL	1.1623 mL
	80 mM	0.0349 mL	0.1744 mL	0.3487 mL	0.8718 mL
	100 mM	0.0279 mL	0.1395 mL	0.2790 mL	0.6974 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Terameprocol24150-24-1EM-1421EM1421EM 1421SurvivinCOXTNF ReceptorApoptosisCyclooxygenaseTumor Necrosis Factor ReceptorTNFRInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Terameprocol (Synonyms: EM-1421)

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