Table 3.

Description of FUBP1-inhibitors (top of the list) and activator (last in the list) identified so far

Compound	Chemical structure	Mechanism	Effect on FUBP1 target genes	IC50
Benzoyl anthranilic Acid [150]		Interacts with the hydrophobic region of the KH domain of FUBP1, leading to an impaired DNA-binding	↓ Binding on MYC	350 μM
Pyrazolo[1,5a] pyrimidine [11]		Inhibits or prevents the binding between FUBP1 and the FUSE	↓ Binding on P21 and ↑ P21 mRNA ↓ Binding on BIK and ↑ BIK mRNA ↓ CCND mRNA in Hep3B cells	11–24 μM depending on assays
GSK343 [128]		Competitive inhibitor	↓ MYC protein level in Saos-2 cells	Not available (4 nM for EZH2)
Camptothecin (CPT) [156]		Interferes with the transcriptional control of FUBP1	↑ P21 mRNA ↑ BIK mRNA ↓ CCND2 mRNA ↓ TCTP mRNA in Hep3B and HepG2 cells.	3.2 ± 0.6 mM
7-ethyl-10-hydroxycamptothecin (SN-38) [156]		Interferes with the transcriptional control of FUBP1	↑ P21 mRNA ↑ BIK mRNA ↓ CCND2 mRNA ↓ TCTP mRNA in Hep3B and HepG2 cells.	0.78 ± 0.2 mM - 1.9 ± 0.7 mM depending on assays
ACTIVATOR: pyrido-pyrimidinone SMN-C2 and SMN-C3 [144]		Binds to the AGGAAG motif on exon 7 of the SMN2 pre-mRNA Creates a new functional binding surface with FUBP1	↑ SMN2 splicing	EC50: 100 nM