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BI-4732 is potent inhibitor against EGFR-activating mutations and on-target resistance mutations. It displays remarkable antitumor efficacy in vitro and in vivo as a single agent, as well as efficient activity in the central nervous system.
ACBI3 is a first in class VHL-recruiting PROTAC molecule, potently degrading multiple KRAS variants in vitro and in vivo.
BI-9787 is selective ketohexokinase (KHK) inhibitor. It inhibits both the A and C isoforms of KHK with high potency and is suitable for in vitro as well as in vivo studies.
AXPSP0056 is a selective allosteric GCH1 inhibitor that acts as a mimic of tetrahydrobiopterin (BH4). By occupying the latter’s binding site on GCH1, it triggers a feedback inhibition mechanism that decreases GCH1’s activity in the presence of elevated cellular concentrations of BH4.
BI-0474 is a selective and potent irreversible covalent KRASG12C inhibitor, developed using an NMR-based fragment screening approach pioneered at Vanderbilt University, whereby small molecules that bind reversibly to the KRAS switch II pocket were identified and optimized using structu