Dihydrocytochalasin B (H2CB) 是一种细胞分裂抑制剂,抑制胞质分裂并改变细胞的形态,破坏 Swiss 3T3 小鼠成纤维细胞的肌动蛋白结构,抑制血清生长因子在静止培养物中刺激 DNA 合成的能力,瓦解肌动蛋白细胞结构并抑制 3T3 细胞中 DNA 合成的启动。低剂量的 H2CB 会导致细胞变圆和肌动蛋白微丝束的丢失。
Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms. It effectively induces the translocation of nPKC-delta, -epsilon, and -theta as well as PKC-mu from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].
YW3-56 is a potent peptidylarginine deiminase (PAD) inhibitor, with an IC50 of 1-5 μM for PAD4. Compared with Cl-amidine, YW3-56 shows >60-fold increase in cell growth inhibition efficacy (IC50 about 2.5 μM) but only 5-fold increase in PAD4 inhibition (IC sub>50 about 1-5 μM). At 2-4 μM concentrations, YW3-56 displays mainly cytostatic effects by slowing cell division, whereas at higher concentrations, it exerts cytotoxic effects by altering cell morphology and killing cells[1]. [1]. Wang Y, et al. Anticancer peptidylarginine deiminase (PAD) inhibitors regulate the autophagy flux and t he mammalian target of rapamycin complex 1 activity. J Biol Chem. 2012 Jul 27;287(31):25941-53.
SMAP-29 is a broad spectrum antibacterial and antifungal α-helical cathelicidin-derived peptide with strong potential as an antiinfective agent. It effectively permeabilizes bacterial membranes and induces significant alterations in the surface morphology of susceptible microorganisms.
RAD16-I hydrochloride is a self-assembling peptide with nanofibrous morphology that provides an optimal microenvironment for the proliferation and differentiation of human mesenchymal stem cells (hMSC) into chondrocytes. This peptide, known as RAD16-I, has been extensively studied and serves as a model to assess the amyloid-like staining properties of self-assembling peptide nanofibers (SAPNFs).
Antitumor agent-38 is a highly effective antitumor compound that exhibits antiproliferative activity towards cancer cells. It induces cell cycle arrest specifically at the late S and G2 M phase, while not impeding microtubule formation or altering cell morphology [1].
RO314724 is a HDAC inhibitor. RO314724 is also a a reversible, tightly binding, MMP inhibitor with a Ki of 26 nm. Matrix metalloproteinases (MMPs) belong to the key enzymes of the proteolytic destruction of cartilage matrix during chronic rheumatic diseases. Ro314724 displayed MMP-proteoglycanase inhibitory activity both in vitro and ex vivo and proved to be not harmful to the morphology, viability and proteoglycan biosynthesis of bovine articular cartilage explants.