A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
IC-87114 is a compound that inhibits the p110δ isoform of PI3K selectively, p110δ(IC50 = 0.13 µM) vs. p110α(IC50 = 200 µM), p110β(IC50 = 16 µM) and p110γ(IC50 = 61 µM).
A-196 is a potent selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively, and biochemically inhibits SUV4-20 in a substrate-competitive manner. In addition, A-196 is a first-in-class chemical probe for SUV4-20, which can be used to study the role of histone methyltransferases in genome integrity.
Saruparib (AZD5305) is a potent and oral active, second-generation PARP (highly selective PARP1) inhibitor with IC50 values of 3 nM and 1400 nM for PARP1 and PARP2, respectively.
Y15 is a novel small molecule FAK phosphorylation inhibitor; specifically block phosphorylation of Y397-FAK and total phosphorylation of FAK.
Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines.
Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
PP2 is a selective inhibitor of Src-family tyrosine kinases with >10,000-fold selectivity over ZAP-70 and JAK2.
CADD522 is a novel small molecule inhibitor of RUNX2, downregulates RUNX2-mediated transcription of downstream target genes by inhibiting RUNX2-DNA binding, with an IC50 of 10 nM.
4-Phenylbutyric acid is an inhibitor of HDAC, inhibits the growth of NSCLC Cell Lines at 2 mM.
γ-Glu-Cys is a dipeptide containing cysteine and glutamate, and is also a precursor of glutathione (GSH). In addition, γ-Glu-Cys is a cofactor in the increase of GSH levels by glutathione peroxidase (GPx).