CQ211 is a Potent and Selective RIOK2 Inhibitor
RIOK2 is a typical kinase implicated in multiple human cancers. The right open reading frame (RIO) kinases belong to the atypical kinases family. RIO kinases contain a C-terminal RIO domain that…
Lapatinib is a Potent Inhibitor of the ErbB-2 and EGFR Tyrosine Kinase Domains
Growth factors and their transmembrane receptor tyrosine kinase play important roles in cell proliferation, survival, migration, and differentiation. Additionally, Epidermal growth factor (EGF)-like proteins stimulates cells to divide by activating members…
Rebeccamycin, an Antitumor Antibiotic, Inhibits DNA Topoisomerase I
Rebeccamycin, a yellow crystalline product, is isolated from the mycelium. It has activity against P388 leukemia, L1210 leukemia, and B16 melanoma implanted in mice. Rebeccamycin is also an antitumor antibiotic…
DS17701585 is a Highly Selective, Orally Active EP300 and CBP Inhibitor
DS17701585 (Compound 11) is a highly selective, orally active EP300 and CBP inhibitor with IC50 values of 0.15, 0.040, 0.45 and 0.70 µM against CBP, EP300, H3K27 and SOX2. Besides, DS17701585 has the…
Pitstop 2 is a Clathrin Inhibitor which Inhibits Clathrin-Mediated Endocytosis (CME)
Clathrin is a protein that plays a major role in the formation of coated vesicles. It forms a triskelion shape composed of three clathrin heavy chains and three light chains.…
Actinomycin D Inhibits DNA Repair and Induces Autophagy
Actinomycin D is isolated from Streptomyces species, containing a phenoxazine chromophore and two cyclic pentapeptide lactone rings. Besides, Actinomycin D can inhibit DNA repair, DNA-directed RNA synthesis, or DNA synthesis via…
LTX-315 is an Oncolytic Peptide with Potent Anticancer Activity
Oncolytic peptides offer yet a new therapeutic modality. Their membranolytic mode of action includes the release of danger-associated molecular pattern molecules (DAMPs) and tumor antigens from cancer cells. Therefore, it…
β-Amanitin is a cyclic peptide toxin, inhibits eukaryotic RNA polymerase II and III and protein synthesis.
β-Amanitin is a cyclic peptide toxin in the poisonous Amanita phalloides mushroom. Besides, β-Amanitin inhibits eukaryotic RNA polymerase II and III. It inhibits DNA transcription and protein synthesis. Moreover, β-Amanitin…
Vatalanib (PTK787) is an Inhibitor of VEGFR2/KDR
Vascular endothelial growth factor receptor (VEGFR) is the receptor for VEGF. VEGF is an important signaling protein involved in both vasculogenesis and angiogenesis. VEGFRs consist of three subtypes, the fms-like…
Gardiquimod is a TLR7/8 Agonist and Could Inhibit HIV-1 Infection
Toll-like receptors (TLR) are a family of highly conserved pattern recognition receptors. They participate in innate immune responses to pathogen infection. Some of the more than two dozen members of…