Methacycline hydrochloride 

Methacycline hydrochloride is a tetracycline antibiotic and can inhibits bacterial protein synthesis. Methacycline hydrochloride is a potent epithelial-mesenchymal transition (EMT) inhibitor. Methacycline hydrochloride blocks EMT in vitro and fibrogenesis in vivo without directly affecting TGF-β1 Smad signaling. Methacycline hydrochloride is an antimicrobial and has the potential for pulmonary fibrosis^[1].

Methacycline hydrochloride is an inhibitor of A549 EMT with an IC50 of roughly 5 μM^[1].
In vitro, Methacycline hydrochloride (10, 20 μM; for 48 hours) inhibits TGF-β1-induced α-smooth muscle actin, Snail1, and collagen I of primary alveolar epithelial cells. Methacycline hydrochloride inhibits TGF-β1–induced non-Smad pathways, including c-Jun N-terminal kinase, p38, and Akt activation, but not Smad or β-catenin transcriptional activity. Methacycline has no effect on baseline c-Jun N-terminal kinase, p38, or Akt activities or lung fibroblast responses to TGF-β1^[1].

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

In vivo, Methacycline hydrochloride (100 mg/kg/day; ip; beginning 10 days after intratracheal Bleomycin) improves survival at Day 17. Bleomycin-induced canonical EMT markers, Snail1, Twist1, collagen I, as well as fibronectin protein and mRNA, ARE attenuated by Methacycline hydrochloride (Day 17)^[1].

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

478.88

Solid

C₂₂H₂₃ClN₂O₈

3963-95-9

O[[email protected]@](C(O)=C(C(C1=C2C=CC=C1O)=O)[[email protected]](C2=C)([H])[[email protected]@H]3O)(C(C(C(N)=O)=C4O)=O)[[email protected]]3([H])[[email protected]@H]4N(C)C.Cl

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Ying Xi, et al. Inhibition of epithelial-to-mesenchymal transition and pulmonary fibrosis by methacycline. Am J Respir Cell Mol Biol. 2014 Jan;50(1):51-60.  [Content Brief]