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Thalidomide
CAS No. : 50-35-1
MCE 国际站：Thalidomide
产品活性：Thalidomide 能够抑制 cereblon (cullin-4 E3 泛素连接酶复合物 CUL4-RBX1-DDB1 的一部分)，Kd 值约为 250 nM，具有免疫调节、抗炎、抗肿瘤作用。Thalidomide 可以作为分子胶来增强底物。
研究领域：PROTAC | Apoptosis | Autophagy
作用靶点：Ligands for E3 Ligase | Apoptosis | Autophagy
In Vitro: Thalidomide has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties, and targets cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ～250 nM.
Thalidomide (50 μg/mL) potentiates the anti-tumor activity of Icotinib against the proliferation of both PC9 and A549 cells, and this effect is correlated with apoptosis and cell migration. In addition, Thalidomide and Icotinib inhibits the EGFR and VEGF-R2 pathways in PC9 cells.
In Vivo: Thalidomide (100 mg/kg, p.o.) inhibits the collagen deposition, down-regulates the mRNA expression level of α-SMA and collagen I, and significantly reduces the pro-inflammatory cytokines in RILF mice. Thalidomide alleviates RILF via suppression of ROS and down-regulation of TGF-β/Smad pathway dependent on Nrf2 status.
Thalidomide (200 mg/kg, p.o.) combined with Icotinib shows synergistic anti-tumor effects in nude mice bearing PC9 cells, suppressing tumor growth and promoting tumor death.
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