| Description | Incyclinide (COL-3) is a matrix metalloproteinase (MMP) inhibitor. Thereby causing extracellular matrix degradation, tumor growth and invasion, and inhibiting angiogenesis, and metastasis. |
| In vitro | Incyclinide在细胞培养中已被证实可以实验性抑制前列腺癌、结肠腺癌和黑色素瘤的侵袭性。添加5至20μM的incyclinide可以抑制MT1-MMP的明胶酶和酪蛋白酶活性，阻断MT1-MMP对pro-MMP-2的激活，并减少HT-1080成纤维细胞瘤细胞的侵袭性[1]。大多数针对丝状真菌的CMT-3的最小抑制浓度（MICs）被发现在0.25至8μg/mL之间，且incyclinide对这些真菌的生存能力的抑制通常高于90%[2]。 |
| In vivo | Incyclinide 通过降低压缩侧的破骨细胞数量可能抑制大鼠的牙齿移动。Incyclinide 减少的 MMP 活性也可能直接抑制有机骨基质的降解。这可能是由于在激活的破骨细胞中引发凋亡或减少破骨细胞迁移的结果 [3]。 |
| Synonyms | COL-3, CMT-3 |
| molecular weight | 371.34 |
| Molecular formula | C19H17NO7 |
| CAS | 15866-90-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 95 mg/mL (255.83 mM) |
| References | 1. Lee HM, et al. CMT-3, a non-antimicrobial tetracycline (TC), inhibits MT1-MMPactivity: relevance to cancer. Curr Med Chem. 2001 Feb;8(3):257-60. 2. Liu Y, A chemically modified tetracycline (CMT-3) is a new antifungal agent. Antimicrob Agents Chemother. 2002 May;46(5):1447-54. 3. Bildt MM, et al. CMT-3 inhibits orthodontic tooth displacement in the rat. Arch Oral Biol. 2007 Jun;52(6):571-8. |