smad4

Kartogenin (KGN) 是一种人间充质干细胞分化为软骨细胞的诱导剂(EC50:100 nM)。它能够结合纤维蛋白 A，破坏其与转录因子核心结合因子 β 亚基 (CBFβ) 的相互作用，并通过调节 CBFβ-RUNX1 转录程序，诱导软骨形成，可用于研究骨关节炎。

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4 SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

MY-673是CBSI（秋水仙碱结合位点抑制剂），可抑制微管蛋白聚合。该化合物还可阻断ERK信号通路，进而调节TGF-β SMAD通路中的SMAD4蛋白表达。MY-673已经证实能在体内外有效抑制细胞的增殖和迁移，同时诱导apoptosis（细胞凋亡）。