MS170 is a PROTAC AKT Degrader
The alternative name of serine/threonine kinase AKT is protein kinase B (PKB). Three closely related genes in humans: AKT1 (PKB-α), AKT2 (PKB-β), and AKT3 (PKB-γ) encode PKB. AKT is an…
Indoximod, An Immunometabolic Adjuvant, is an IDO Pathway Inhibitor
Indoleamine 2,3-dioxygenase (IDO) is an enzyme of interest in immuno-oncology. It has immunosuppressive effects that result from its role in tryptophan catabolism. IDO1 catalyzes the initial rate-limiting step in the…
Lomeguatrib is a O6-Methylguanine-DNA Methyltransferase (MGMT) Inhibitor
O6-alkylguanine DNA alkyltransferase (also known as AGT, MGMT or AGAT) is a protein that in humans is encoded by the O6-methylguanine DNA methyltransferase (MGMT) gene. MGMT repairs the naturally occurring…
VAL-083 Creates DNA N7 Methylation with Antitumor Activity
Glioblastoma (GBM) is one of the most difficult tumors. Many new agents fail to cross the blood-brain barrier (BBB) and it has intrinsic drug resistance. VAL-083 is an alkylating agent…
Hesperadin is an ATP Competitive Indolinone Inhibitor of Aurora A and B
Aurora kinases (AURK) are a group of serine/threonine kinases. And they participate in the cellular division through the regulation of chromatid segregation. what's more, AURK has three subclasses: AURKA, AURKB,…
PFM39 is a Selective MRE11 Exonuclease Inhibitor
Double-strand break repair protein MRE11 is an enzyme that in humans is encoded by the MRE11 gene. The MRE11/Rad50/NBS1 (MRN) complex maintains genomic stability by bridging DNA ends, and initiating…
HM43239 is an Orally Active and Selective FLT3 Inhibitor
Acute myeloid leukemia (AML) is the most common acute leukemia in adults, with an incidence of over 20 000 cases per year in the United States alone. Large chromosomal translocations,…
GS-493 is a Selective Protein Tyrosine Phosphatase SHP2 (PTPN11) Inhibitor
The protein tyrosine phosphatase SHP2 (also called SH-PTP2, Syp, PTP1D, and PT-P2C) is a ubiquitously expressed 68 kDa non-receptor PTP. In the inactive state, the SH2 domains of SHP2 auto-inhibit the…