Inhibitor | Type | Malignancies | Class | EC50/IC50/Dose | Reference |
---|---|---|---|---|---|
TAK-981 | Clinical: phase 1 | BCL and colorectal carcinoma | Adenosine sulfamate | SUMOylation assays: 0.005–0.026 μM; MCL cell lines: 17–62.5 nM; dose in mice: 5–10 mg/kg, i.v., twice weekly; 15 mg once weekly | Berger et al., 2019; Hanel et al., 2019; Hatton et al., 2019; Khattar et al., 2019; Nakamura et al., 2019 |
ML-792 | Experimental | Cell-free and cellular activity in colorectal, breast, and melanoma cancer cells | Adenosine sulfamate | SUMOylation assays: 0.003–0.051 μM; cytotoxicity: 0.03–0.45 μM | He et al., 2017 |
COH000 | Experimental | Cell-free and cellular activity in lymphoma, colorectal, and ovarian cancer cells in vitro and in vivo | Oxabicycloheptadiene | Cell-free RanGAP1 SUMOylation: 0.2 µM; dose in mice: 10 mg/kg once daily | Lv et al., 2018b; Li et al., 2019 |
Davidiin | Experimental | Cell-free and cellular activity in gastric, prostate, lung, and hepatocellular cancer cells | Natural compound; ellagitannin | Cell-free RanGAP1-C2 SUMOylation: 0.15 µM; cytotoxicity: 8.3–16.4 µM; dose in mice: 10 mg/kg 3 times weekly | Takemoto et al., 2014; Wang et al., 2014 |
Ginkgolic acid | Experimental | Cell-free and cellular activity | Natural compound; alkyl phenol derivative | Cell-free substrate SUMOylation: 3 µM | Fukuda et al., 2009a |
Kerriamycin B (Urdamycin A) | Experimental | Cell-free and cellular activity | Natural compound; polycyclic antibiotic | Cell-free RanGAP1-C2 SUMOylation: 11.7 µM | Fukuda et al., 2009b |
Tannic acid | Experimental | Cell-free and cellular activity (no cytotoxicity in liver cancer cells) | Natural compound; gallotannin | Cell-free rhLRH-1 SUMOylation: 12.8 µM | Suzawa et al., 2015 |
Anacardic acid | Experimental | Cell-free and preclinical activity in AML | Natural compound; alkyl phenol derivative | Cell-free substrate SUMOylation: 2.2 µM; median IC50 (primary AML samples): 42 µM; dose in mice: 2 mg/kg/d | Fukuda et al., 2009a; Bossis et al., 2014 |
Compound 21 | Experimental | Cell-free activity | Biaryl urea derivative | Cell-free RanGAP1-C2 SUMOylation: 14.4 µM | Kumar et al., 2013b |
SUMO-AMSN | Experimental | Cell-free activity | Semisynthetic SUMO adenylate | NA | Lu et al., 2010; Olsen et al., 2010 |
SUMO-AVSN | Experimental | Cell-free activity | Semisynthetic SUMO adenylate | NA | Lu et al., 2010; Olsen et al., 2010 |
pS50 (YSFVSGG) | Experimental | Cell-free activity | Synthetic heptameric SUMO-mimicking peptides | Cell-free thioester formation: 125 µM | Zhao et al., 2014 |
pS90 (YQYVSGG) | Experimental | Cell-free activity | Synthetic heptameric SUMO-mimicking peptides | Cell-free thioester bond formation: 131 µM | Zhao et al., 2014 |
BCL, B-cell lymphoma; NA, not available; rhLRH-1, recombinant human liver receptor homolog-1.