ebc-1

MK-8033 is a new and selective dual ATP competitive c-Met/Ron inhibitor (IC50: 1 nM Wt c-Met).

OTUB1/USP8-IN-1 is a potent OTUB1/USP8 inhibitor with potential anticancer activity, demonstrating IC50 values of 0.17 nM for OTUB1 and 0.28 nM for USP8. OTUB1/USP8-IN-1 can be used in the study of non-small-cell lung cancer.

Inz-1 is an effective and fungal-selective inhibitor of mitochondrial cytochrome bc1 with IC50s of 8.092 and 45.320 μM for yeast and human. Inz-1 reverses Fluconazole or other triazole antifungals' resistance in the pathogenic fungus Candida albicans.

Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinase inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptors.

Atovaquone (Atavaquone) is a hydroxynaphthoquinone that has antimicrobial activity and is being used in antimalarial protocols.

Inz-5 is a fungal-selective inhibitor of mitochondrial cytochrome bc1 that impairs fungal virulence and prevents the evolution of drug resistance.

PROTACc-Met degrader-3 (Compound 22b) is a c-Met PROTAC degrader. It facilitates the ubiquitination and degradation of c-Met, with a DC50 of 0.59 nM in EBC-1 cells. PROTACc-Met degrader-3 is applicable in lung cancer research.

TrkC-IN-1 (Compound 6c) is an inhibitor of TrkC, with IC50 values of 3.3-7.1 and 7.3-10.2 μΜ for EBC-1 and HT-29 cells, respectively. This compound shows potential for research in the field of cancer therapeutics.

CDK2/FLT4/PDGFRA-IN-1 (Compound 4a) is a potent inhibitor of CDK2/cyclin A, FLT4 (VEGFR3), and PDGFRA, with IC50 values of 1.672, 0.554, and 0.629 μM respectively. This compound demonstrates significant antiproliferative effects on cancer cells, including lung cancer EBC-1, pancreatic ductal adenocarcinoma AsPC-1, and colorectal cancer HT-29 cells. Additionally, CDK2/FLT4/PDGFRA-IN-1 can induce apoptosis in these cancer cells.

PROTACc-Met degrader-5 (Compound D19) is an orally active c-Met PROTAC degrader, with a DC50 of 0.42 nM in EBC-1 cells and 0.32 nM in Hs746T cells. It effectively induces apoptosis, causes G1 cell cycle arrest, and inhibits cell migration and invasion. This compound shows strong antiproliferative and degradative effects on c-Met-dependent cancer cells and those resistant to Tepotinib.

PROTACc-Met degrader-6 is a potent and orally active c-Met PROTAC degrader. It effectively promotes the degradation of c-Met protein, with DC50 values of 0.52 nM in EBC-1 cells and 0.45 nM in Hs746T cells. This compound almost completely abolishes the migration and invasion capabilities of tumor cells, significantly induces apoptosis (apoptosis), and arrests the cell cycle at the G0/G1 phase. PROTACc-Met degrader-6 is useful for studying various cancers, including non-small cell lung cancer and gastric cancer.

Axl-IN-8 (NO.1) is a potent AXL inhibitor (IC50 < 1 nM) and also inhibits c-MET (IC50: 1-10 nM).

MET/PDGFRA-IN-1 (compound 8c) is an inhibitor of MET and PDGFRA proteins, with an IC50 of 36 μM against MET. It inhibits MET phosphorylation, induces apoptosis, and reduces proliferation in various MET-positive cell lines, showing IC50 values of 15.3 μM for AsPc-1, 19.0 μM for EBC-1, 22.0 μM for MKN-45, 25.6 μM for Mia-Paca-2, 21.0 μM for HT-29, and 31.5 μM for K562 [1].

MET/PDGFRA-IN-2 (compound 8h) is an inhibitor of MET and PDGFRA proteins that promotes apoptosis and impedes proliferation of MET-positive cells with IC50 values of 9.7, 6.1, 12.0, 11.5, 8.6, and 34.4 μM for AsPc-1, EBC-1, MKN-45, Mia-Paca-2, HT-29, and K562 cells, respectively [1].

N-Oleoyl serinol, a ceramide analog, plays a crucial role in stem cell therapy by inhibiting the development of teratomas in stem cells. It triggers apoptosis in remaining pluripotent embryoid body-derived cells (EBCs), thwarts teratoma formation, and promotes the enrichment of EBC cells that proceed to neural differentiation post-transplantation [1].