hm4

HM43239 is an orally active and selective FLT3 inhibitor with IC 50 s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. HM43239 directly inhibits the kinase activity of FLT3 as a reversible Type I inhibitor and effectively modulates downstream p-STAT5 and p-ERK. HM43239 also demonstrated inhibition of SYK, JAK1 2 and TAK1. HM43239 inhibits the proliferation and induces the apoptosis of leukemic cells [1] [2] [3].

DREADD agonist 21 is a potent agonist of human muscarinic acetylcholine M3 receptors (EC50=1.7 nM).

VU6028418 is a highly selective, potent, orally active M4mAChR antagonist that acts on hM4 (IC50: 4.1 nM).

VU6008677 is a positive allosteric modulator (PAM) of M4 with an EC50 of 120 nM for hM4. It inhibits cytochrome P450 (cytochrome P450) and exhibits a high microsomal clearance rate and high plasma protein binding in rats.