fd-1

Tegadifur (40497S) is an orally available antitumor compound with antimetabolic effects, often used with uracil and in the treatment of rectal adenocarcinoma.

DS18561882 is an orally available, selective and potent inhibitor of methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) with antitumor activity, inhibits MTHFD1 activity and can be used in the study of breast cancer.

Panadiplon (FG 10571) is a selective gamma-aminobutyric acid receptor agonist and partial agonist of 5GABAA, a benzodiazepine receptor, used in the treatment of anxiety disorders.Panadiplon exhibits selectivity for 5GABAA receptors versus 1GABAA receptors.

FD 12-9, Anti-glioblastoma activity. is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively.

LY 345899 is a folate analog that inhibits methylenetetrahydrofolate dehydrogenase and MTHFD2, with IC50 values of 96 nM and 663 nM, respectively, and a Ki of 18 nM for MTHFD1.

TH9028 is an inhibitor of MTHFD2, featuring an IC50 value of 11 nM. It demonstrates specific inhibitory activity with IC50 values of 7.97 nM, 27 nM, and 0.5 nM against hMTHFD2, MTHFD2L, and MTHFD1, respectively.

TH9028 TFA is an effective MTHFD2 inhibitor (IC50=11 nM) that suppresses proliferation in HL-60 cells, AML cells, and T-ALL Jurkat cells.

FD1024 is a potent PIM inhibitor, displaying inhibitory concentrations (IC50s) of 1.96 nM, 38.9 nM, and 4.17 nM for PIM1, PIM2, and PIM3, respectively. It demonstrates significant antiproliferative effects on several AML cell lines, with IC50 values of 0.16 μM for EOL-1, 0.12 μM for MV-4-11, 1.05 μM for KG-1, and 1.39 μM for MOLM-16. Additionally, FD1024 has shown antitumor efficacy in murine models [1].

FD-IN-1 (Compound 12) is an orally active Factor D (FD) inhibitor (IC50=12 nM) that also inhibits Factor XIa (FXIa) and Tryptase β2 with IC50 values of 7.7 and 6.5 μM, respectively.

Complement factor D-IN-1 is a potent and selective small-molecule reversible Factor D inhibitor, with IC50 values of 0.006 μM in the FD Thioesterolytic Fluorescent Assay and 0.05 μM in the MAC Deposition Assay.

FD-211 is a δ lactone originally isolated from M. lutea with anticancer activity.1 It is cytotoxic to adriamycin-susceptible P388, T-24, HeLa, A549, and HL-60 cancer cells (IC50s = 4, 0.5, 1, 1, and 0.2 μg/ml, respectively), as well as adriamycin-resistant HL-60/ADR cells (IC50 = 0.1 μg/ml). FD-211 also inhibits DNA, RNA, and protein synthesis in HeLa cells (IC50 = 1.25 μg/ml for all). |1. Nozawa, O., Okazaki, T., Sakai, N., et al. A novel bioactive δ lactone FD-211. Taxonomy, isolation and characterization. J. Antibiot. (Tokyo) 48(2), 113-118 (1995).