DC-S239 is a Selective SET7 Inhibitor With Anti-Cancer Activity
SET7 is a protein lysine methyltransferase (PKMT), which methylates a plethora of proteins and regulates diverse biological processes. Meanwhile, SET7 plays a significant role in transcriptional regulation, cell cycle control, differentiation, DNA repair, and DNMT1 stability. Specifically, researches show that SET7 is closely associated with various diseases. Particularly, SET7...
MS159 is a First-In-class NSD2 PROTAC degrader for Multiple Myeloma Research
Proteolytic targeting chimera (PROTAC) is a heterobifunctional small molecule, including two active domains, and a linker. Importantly, it can remove specific unwanted proteins. PROTAC is a technology based on the ligand binding of TAP and then the degradation of TAP. PROTAC provides an alternative approach to those so-called non-druggable...
BM-1074 is a Potent and Specific Bcl-2/Bcl-xL Inhibitor
Bcl-2 (B-cell lymphoma 2) and Bcl-xL (B-cell lymphoma-extra large) are members of the Bcl-2 family of proteins. BCL-2 is localized to the outer membrane of mitochondria, where it plays an important role in promoting cell survival and inhibiting the actions of pro-apoptotic proteins. As well as, Bcl-xL acts as an...
FL118, a Camptothecin Analogue, is a Survivin Inhibitor with Anti-Cancer Activity
Survivin is the smallest member of the inhibitor of apoptosis (IAP) protein family. Specifically, survivin is a 142 amino acid, 16.5 kDa protein. Survivin participates in the inhibition of apoptosis and the regulation of the cell cycle. Besides, survivin can inhibit caspase and block cell death. Moreover, survivin was...
BNS-22 is a DNA Topoisomerase II Catalytic Inhibitor
Topoisomerases (DNA topoisomerases) are enzymes that catalyze changes in the topological state of DNA, regulating the overwinding or underwinding of DNA. Topoisomerases play essential roles in DNA replication, transcription, chromosome segregation, and recombination. The winding problem of DNA arises due to the intertwined nature of its double-helical structure. All...
BI-1622 is an Orally active and Selective HER2 Inhibitor
BI-1622 is an orally active, potent, and highly selective HER2 (ERBB2) inhibitor, with IC50 values of 7.8, 7.1, <5.3 nM for HER2WT, HER2YVMA, EGFRWT, respectively. Besides, BI-1622 shows greater than 25-fold selectivity over EGFR. Moreover, BI-1622 shows high antitumor efficacy in vivo in xenograft mouse tumor models. HER2 is a member...
Vamotinib (PF-114) is a Potent, Selective and Orally Active Tyrosine Kinase Inhibitor
BCR-ABL, a fusion gene, is a mutation that is formed by the combination of two genes, BCR and ABL. The BCR gene is normally on chromosome number 22. The ABL gene is normally on chromosome number 9. The BCR-ABL mutation happens when pieces of BCR and ABL genes break...