Table 1. Small Molecule HuR Inhibitors:
Small molecules that have been identified as inhibitors of HuR in vitro and in vivo. These drugs are categorized by their mechanism of action, and whether they have been utilized in vitro, in vivo or both.
| Published HuR inhibitors | Mechanism of action | IC50 (in vitro)* | Status | Reference |
|---|---|---|---|---|
| MS-444 | HuR translocation | 2.1-40.7 μM | In vitro/ in vivo | (Blanco, Jimbo, et al., 2016; Blanco, Preet, et al., 2016; Meisner et al., 2007) |
| Pyrvinium Pamoate | HuR translocation | 1.093 μM | In vitro/ in vivo | (Guo et al., 2016) |
| Cryptotanshinone | HuR translocation | 6.0 μM | In vitro/ in vivo | (Z. Zhu et al., 2016) |
| MPT0B098 | HuR translocation | 0.08 - 0.51 μM | In vitro/ in vivo | (Cheng et al., 2013) |
| Dehydromutactin | HuR translocation | 39.0 - 130.0 μM | In vitro only | (Meisner et al., 2007) |
| Okicenone | HuR translocation | 0.53 - 2.9 μg/ml | In vitro only | (Meisner et al., 2007) |
| SP600125 | HuR translocation | 0.12 - 16.0 μM | In vitro/ in vivo | (Hostetter et al., 2008) |
| 5-aza 2’ deoxycytidine / trichostatin A | HuR translocation | 0.1 uM - 0.5 uM | In vitro/ in vivo | (Hostetter et al., 2008) |
| N-Benzylcantharidinamide | HuR translocation | 50.0 - 100.0 μM | In vitro only | (Lee et al., 2014) |
| Triptolide | HuR translocation | 0.01 - 0.03 μM | In vitro/ in vivo | (L. Sun et al., 2011) |
| Leptomycin B | HuR translocation | 0.01 μM | In vitro/ in vivo | (Mutka et al., 2009) |
| Selinexor | HuR translocation | 0.12 - 0.22 μM | In vitro/ in vivo | (Hing et al., 2015) |
| Latrunculin A | HuR trafficking | 0.33 - 0.76 μM | In vitro/ in vivo | (Doller et al., 2015) |
| Blebbistatin | HuR trafficking | 0.43 - 22.8 μM | In vitro/ in vivo | (Doller et al., 2015) |
| CMLD2 | HuR target mRNA binding inhibition | 25.9 - 28.8 μM | In vitro only | (Muralidharan, Mehta, et al., 2017) |
| AZA-9 | HuR target mRNA binding inhibition | 51.9 - 67.6 μM | In vitro only | (Kaur et al., 2017) |
| 15,16-dihydrotanshinone-I (DHTS) | HuR target mRNA binding inhibition | 0.84 - 1.2 μM | In vitro/ in vivo | (D’Agostino et al., 2015; P. Lal et al., 2017) |
| Quercetin | HuR target mRNA binding inhibition | 5.78 - 31.04 μg/ml | In vitro/ in vivo | (Chae et al., 2009) |
| B-40 | HuR target mRNA binding inhibition | 0.38 μM | In vitro only | (Chae et al., 2009) |
| B-41 | HuR target mRNA binding inhibition | 6.21 μM | In vitro only | (Chae et al., 2009) |
| Tanshinone II | HuR target mRNA binding inhibition | 4.0 μM | In vitro only | (D’Agostino et al., 2015) |
| Cetylpyridinium choride | HuR target mRNA binding inhibition | 0.8-2.1 μg/ml | In vitro only | (D’Agostino, Adami, & Provenzani, 2013) |
|
Mitoxantrone |
HuR target mRNA binding inhibition | 0.01 - 1.13 μM | In vitro/ in vivo | (D’Agostino et al., 2013) |
| Suramin | HuR target mRNA binding inhibition | 732 μM | In vitro/in vivo | (Kakuguchi et al., 2018) |
| NSC# 5836 | HuR target mRNA binding inhibition | 14.7 μM | In vitro | (Z. Wang, Bhattacharya, & Ivanov, 2015) |
| NSC# 7572 | HuR target mRNA binding inhibition | 41.0 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 44750 | HuR target mRNA binding inhibition | 26.9 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 50648 | HuR target mRNA binding inhibition | 97.4 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 62685 | HuR target mRNA binding inhibition | 16.7 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 84126 | HuR target mRNA binding inhibition | 2.7 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 91438 | HuR target mRNA binding inhibition | 4.6 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 109292 | HuR target mRNA binding inhibition | 44.4 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 123418 | HuR target mRNA binding inhibition | 69.6 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 143491 | HuR target mRNA binding inhibition | 21.7 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 227186 | HuR target mRNA binding inhibition | 41.9 μM | In vitro | (Z. Wang et al., 2015) |
| NSC# 651084 | HuR target mRNA binding inhibition | 17.4 μM | In vitro | (Z. Wang et al., 2015) |
| KH-3 | Unknown | Unknown | In vitro/in vivo | (Green et al., 2019) |
*
IC50 values obtained in vitro through HuR binding inhibition and/or inhibition of cell proliferation/viability.