Terameprocol  (Synonyms: EM-1421)

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].

Terameprocol (25 μM; 16 h) inhibited the production of prostaglandins (PGE2), some cytokines and chemokines induced by lipopolysaccharide (LPS) in RAW 264.7 cells, and also inhibited the expression and activity of COX-2, and inhibited the growth of RAW264.7 cells, but did not induce cell apoptosis^[1]. Terameprocol (10 μM; 24 h, 48 h) downregulated survivin transcription and protein expression in HCC2429 and H460 non-small cell lung cancer cell experiments, while enhancing the sensitivity of cells to radiotherapy, but did not induce cell apoptosis and did not affect the cell cycle^[2]. Terameprocol (0.1-20 μM; 24 h) inhibited cell proliferation in a dose-dependent manner in rat pulmonary artery smooth muscle cells (PASMCs) experiments, and induced cell apoptosis at 20 μM^[3].

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

Terameprocol (1 mg; intraperitoneal injection; 1 time; administered 1 hour before lipopolysaccharide (LPS) injection) reduces the levels of TNF-α and MCP-1 in the serum of C57BL6/J mice in the endotoxemia model^[1].
Terameprocol (166mg/kg; intraperitoneal injection; on days 7, 12, and 17; for 21 days) improves cardiac function, alleviates cardiac and pulmonary remodeling, inhibits the proliferation and induces the apoptosis of pulmonary artery smooth muscle cells in the monocrotaline (MCT)-induced pulmonary hypertension model of male Wistar rats (weighing 180-200g, age not mentioned)^[3].

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

358.47

C₂₂H₃₀O₄

24150-24-1

Solid

White to off-white

COC1=CC(C[C@H](C)[C@H](C)CC2=CC=C(OC)C(OC)=C2)=CC=C1OC

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

• [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]