M4205 (IDRX-42) is an oral, selective inhibitor of KIT with broad activity against mutations in KIT exons 11, 13, and 17. It exhibits significant and dose-dependent antitumor activity in the xenograft model of GIST.

CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.

dTAG-13(FKBP12 PROTAC dTAG-13) is an ortho-substituted, heterobifunctional selective degrader of FKBP12F36V that effectively engage FKBP12F36V and CRBN leading to rapid and selective CRBN-mediated degradation of FKBP12F36V.It can useful for target validation in the context of drug discovery.

dTAG-13(FKBP12 PROTAC dTAG-13) is an ortho-substituted, heterobifunctional selective degrader of FKBP12F36V that effectively engage FKBP12F36V and CRBN leading to rapid and selective CRBN-mediated degradation of FKBP12F36V.It can useful for target validation in the context of drug discovery.

dTAG-13(FKBP12 PROTAC dTAG-13) is an ortho-substituted, heterobifunctional selective degrader of FKBP12F36V that effectively engage FKBP12F36V and CRBN leading to rapid and selective CRBN-mediated degradation of FKBP12F36V.It can useful for target validation in the context of drug discovery.

ME-344 is a synthetic metabolite of NV-128, a potent inhibitor of mitochondrial oxidative phosphorylation (OXPHOS) complex I, disrupting ATP generation and oxygen consumption. It also inhibits mTOR by downregulating the AKT/mTOR pathway, exhibiting anticancer activity by inhibiting cell growth and viability in leukemia cell lines with IC50 values of 70–260 nM.

Deruxtecan is an ADC drug-linker conjugate composed of the cleavable glycine-glycine-phenylalanine-glycine tetrapeptide-based linker, a self-immolative amino methylene spacer, and a novel topoisomerase 1 inhibitor payload that is a derivative of exatecan (DX-8951).

dTAG-13(FKBP12 PROTAC dTAG-13) is an ortho-substituted, heterobifunctional selective degrader of FKBP12F36V that effectively engage FKBP12F36V and CRBN leading to rapid and selective CRBN-mediated degradation of FKBP12F36V.It can useful for target validation in the context of drug discovery.

ME-344 is a synthetic metabolite of NV-128, a potent inhibitor of mitochondrial oxidative phosphorylation (OXPHOS) complex I, disrupting ATP generation and oxygen consumption. It also inhibits mTOR by downregulating the AKT/mTOR pathway, exhibiting anticancer activity by inhibiting cell growth and viability in leukemia cell lines with IC50 values of 70–260 nM.

Vecabrutinib (SNS-062) is a potent, noncovalent BTK and ITK inhibitor, with Kd values of 0.3 nM and 2.2 nM, respectively. Vecabrutinib shows an IC50 of 24 nM for ITK.