ft

FT827 is a covalent inhibitor of selective ubiquitin-specific protease 7 (USP7) (Ki=4.2 µM, Kd=7.8 µM) targeting the catalytic center of the autoinhibitory apolipoprotein form of USP7 for cancer research.

FT113 is a novel potent inhibitor of fatty acid synthase (fasn, IC50 : 213 nM),and exhibits anti-cancer activity

FT-1518 is an orally available, selective and potent mTORC1 and mTORC2 inhibitor with anticancer and antitumor activity for cancer research.

FT895 is a selective and potent HDAC11 inhibitor with antifungal and antitumor activity, inhibiting HDAC11 expression and limiting EV71 replication in vitro (in vitro).

FT671 is a non-covalent, selective USP7 inhibitor (IC50=52 nM) that binds to the catalytic domain of USP7 (Kd=7.8 µM). It disrupts the stability of USP7 substrates including MDM2, elevates p53, induces p21, and inhibits tumor growth in mice.

Notoginsenoside Ft1 is a saponin originally isolated from P. notoginseng with diverse biological activities

FT709 is a selective USP9X deubiquitinating enzyme inhibitor (IC50=82 nM) that reduces Makorin and ZNF598 levels, impairing ribosomal quality control pathways.

FT385 is a novel USP30 inhibitor, recapitulating genetic loss of USP30 and setting the trigger for PINK1-PARKIN amplification of mitochondrial ubiquitylation.

FT-1101 is an orally bioavailable, potent and selective BET inhibitor. FT-1101 binds to the acetylated lysine recognition motifs in the bromodomain sites of BET proteins, thereby preventing the interaction between the BET proteins and acetylated histones. This disrupts chromatin remodeling and gene expression. Prevention of the expression of certain growth-promoting genes may lead to the inhibition of tumor cell growth. BET proteins, comprised of BRD2, BRD3, BRD4 and BRDT, are transcriptional regulators that play an important role during development and cellular growth.

FT011, a direct anti-fibrotic agent,attenuates cardiac remodelling and dysfunction in experimental diabetic cardiomyopathy.

FTI-2148 diTFA, a dual inhibitor targeting both farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1), functions as a RAS C-terminal mimetic. It exhibits potent inhibitory capabilities with IC50 values of 1.4 nM for FT-1 and 1.7 μM for GGT-1, respectively.

FTI-2148 is an inhibitor of RAS C-terminal mimetic dual farnesyl transferase (FT-1) and geranylgeranyl transferase-1 (GGT-1) (IC50s: 1.4 nM and 1.7 μM, respectively).

FGTI-2734 is a dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT-1) inhibitor, exhibiting IC50 values of 250 nM and 520 nM for FT and GGT-1, respectively. It effectively prevents the membrane localization of KRAS, addressing the issue of KRAS resistance and inhibiting the growth of mutant KRAS patient-derived pancreatic tumors.

FGTI-2734 mesylate, a RAS C-terminal mimetic compound with dual farnesyl transferase (FT) and geranylgeranyl transferase-1 (GGT) inhibitory activities (IC50s of 250 nM and 520 nM for FT and GGT, respectively), mitigates KRAS resistance by preventing its membrane localization, effectively impeding mutant KRAS patient-derived pancreatic tumors.

Pocenbrodib (FT-7051) is a potent inhibitor of the bromodomain of the CBP/p300 family with potential antitumour activity and is palatable for cancer research.

(Rac)-Etavopivat ((Rac)-FT-4202), an isomer of Etavopivat, is an orally active erythrocyte pyruvate kinase-R (PKR) activator used in sickle cell disease and haemoglobinopathy research [1].

Tegafur (FT 207) is a congener of the antimetabolite fluorouracil with antineoplastic activity. Tegafur is a prodrug that is gradually converted to fluorouracil in the liver by the cytochrome P-450 enzyme.

Geranylgeraniol (FT0626663) is an isoprenoid found in fruits, vegetables, and grains, including rice. Geranylgeraniol (FT0626663) inhibits growth and induces apoptosis of various tumor cells. Geranylgeraniol (FT0626663) protects monocytes against statin-induced cytotoxicity and suppresses the growth of Mycobacterium.

Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Olutasidenib is a highly effective, brain penetrant, and selective inhibitor of the mutant Isocitrate dehydrogenase 1 (IDH1) (IC50: 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively).

Luvesilocin (Example 6) is a tryptamine prodrug that converts into an active form acting as a 5HT2A receptor agonist in vivo. It is utilized for research concerning mental disorders.

Etavopivat is a potent, selective, and orally active activator of erythrocyte pyruvate kinase (PKR) that enhances red blood cell glycolytic flux and energy metabolism, exhibiting strong antisickling effects by improving erythrocyte deformability and reducing hemoglobin polymerization. Etavopivat is therefore widely applied in translational and mechanistic studies of sickle cell disease and other inherited haemoglobinopathies.

EP-7041 is a novel, potent, and selective Factor XIa inhibitor.

2"-O-Galloylhyperin (FT-0689359) found in Pyrola. It increases ruminal fiber fermentability by formed wall-bound lignin in primary maize cell walls.

1. Protosappanin B (Q-100961) significantly increases cell viability, inhibits cell apoptosis and up-regulates the expression of growth-associated protein 43. 2. Protosappanin B induces the degradation of p53 protein, via activation of a MDM2-dependent ubiquitination process.