pip4k2c

UNC3230 is a potent, selective, and ATP-competitive PIP5K1C inhibitor with an IC50 of approximately 41 nM. UNC3230 (UNC 3230) also inhibits PIP4K2C.

LRK-4189 is an orally active and highly selective PIP4K2C PROTAC degrader. In MOLT-4 cells, its DC₅₀ for PIP4K2C is lower than 500 nM. This compound exhibits significant anti-tumor effects, inducing endogenous apoptosis in cells and activating the interferon signaling pathway, thereby triggering immune-mediated tumor cell killing in immunologically inert microsatellite stable (MSS) colorectal cancer (CRC) cells. Therefore, LRK-4189 can be used to study the molecular mechanisms and treatment strategies of MSS-type colorectal cancer and related cancers.

MMV390048 is an antimalarial agent and is a representative of a new chemical class of Plasmodium PI4K inhibitor (Kdapp=0.3 μM). MMV390048 binds to the ATP binding site of Plasmodium PI4K and does not bind to other P. falciparum and human kinases apart from human PIP4K2C, thus alleviating potential kinase-mediated safety concerns.

TMX-4153 is a bivalent degrader that selectively targets and rapidly degrades endogenous PIP4K2C through recruitment of the von Hippel-Lindau (VHL) E3 ligase complex, demonstrating a K D of 42 nM. It is applicable in the synthesis of PROTAC [1].

WX8 (Ro 91-4714) is an ATP-competitive inhibitor of PIKFYVE, displaying Kd values of 0.9 nM for PIKFYVE and 340 nM for PIP4K2C. This compound inhibits lysosomal fission without affecting homotypic lysosome fusion. WX8 (Ro 91-4714) is applicable in research on autophagy-dependent cancers.