Skip to main content

Table 1 List of the validated small molecule inhibitors of the FA pathway

From: Non-specific chemical inhibition of the Fanconi anemia pathway sensitizes cancer cells to cisplatin

Chemicals Primary known functions IC50 (μM)
Lactacystin Proteasome inhibitor 1.7
MG132 Proteasome and calpain inhibitor 0.8
ALLN Proteasome, calpain, cathepsin L inhibitor 9.2
5929407 Proteasome inhibitor (this study) 6.5
Curcumin Proteasome, protein kinase C (PKC), EGF-receptor tyrosine kinase, IkappaB kinase and mTOR inhibitor 18.6
H-9 PKA, PKC, PKG inhibitor 34.2
Gö6976 PKC, CHK1 inhibitor > 50
SB218078 CHK1, Cdc2, PKC inhibitor 1.4
UCN-01 PKC, CHK1, CDK, AKT inhibitor 0.14
Alsterpaullone CDK, GSK3 inhibitor 1.6
Roscovitine CDK, ERK1,2 inhibitor 27.5
Geldanamycin HSP90 inhibitor 0.15
17-AAG HSP90 inhibitor 0.6
CA-074-Me CathepsinB inhibitor 16.7
Chloroquine Lysosome permeabilisation, inhibition of drug efflux pumps (ATP-binding cassette transporters) 67.5
Wortmannin Casein kinase II, phosphatidylinositol 3-kinase (PI 3-kinase), polo-like kinase 1 (PLK1) inhibitor 84.4
DRB Casein kinase II, RNA pol II inhibitor 11
HNMPA-(AM)3 Insulin receptor tyrosine kinase inhibitor 4.7
Puromycin Protein synthesis inhibitor 5.2
TPEN Heavy metal chelator 5
5656325 Unknown 0.83
5315179 Unknown 5.9
7012246 Unknown 7
5195243 Unknown 2.2
5373662 Unknown 1.3
  1. The identified chemicals are presented with their major known functions and the dose required to inhibit 50% of IR-induced EGFP-FANCD2 foci formation (IC50) in PD20-EGFP-FANCD2 cells. Chemical structures of 5195243 (2-nitro-9,10-phenanthrenedione 10-oxime), 5373662 (2-(2-pyrinylmethylene)quinuclidin-3-one), 5656325 (1-(2-methoxy-1-naphtyl)-3-(3-pyridinyl)-2-propen-1-one), 5929407 (5-[4-(dietylamino)benzylidene]-3-{[(3-methylphenyl)amino]methyl}-2-thioxo-1,3-thiazolidin-4-one), 5315179 (1-(2,4-dimethoxyphenyl)-3-(3-pyridinyl)-2-propen-1-one) and 7012246 (1-(5-bromo-2-hydroxyphenyl)-3-(3-pyridinyl)-2-propen-1-one)) are shown in Additional file 2: Figure S1.