Table 4 Description of CHD1L-inhibitors identified so far
From: Diversity roles of CHD1L in normal cell function and tumorigenesis
| Compound | Chemical structure | Molecular Weight | Mechanism | Effect on CHD1L target genes | IC50 | References |
|---|---|---|---|---|---|---|
| 2-(4-Methoxyphenyl)-5-(methylsulfonyl)-4-(phenylsulfonyl)-1,3-oxazole |
| 393.43 | Inhibit that CHD1L binds the TCF complex, reverse TCF-driven EMT | TCF complex WNT response elements (WRE) (eg. c-Myc, vimentin, slug, LEF1, and N-cadherin) | 3 μmol/L | [115] |
| N-(4-{[6-Methyl-2-(1-pyrrolidinyl)-4-pyrimidinyl]amino}phenyl)-2-(2-thienyl)acetamide |
| 393.51 | 5.5 μmol/L | [115] | ||
| 2-(4-{4-[(3-Chloro-4-methylphenyl)amino]-2-pteridinyl}-1-piperazinyl)ethanol |
| 399.88 | 4 μmol/L | [115] | ||
| Olaparib |
| 434.46 | suppresses the DNA damage repair signaling, repress the key pluripotent transcriptional factors | DNA damage repair genes (eg. SSRP1,ERCC3,CHD1L,TP53BP1,TRIP13), the key pluripotent transcriptional factors (eg. SOX2, OCT4, c-MYC) |
5–50 μM depending on Assays (HCC cells), 10–50 mg/kg (xenograft mouse model) |
[113] [114] |
| Niraparib |
| 492.59 | suppresses the DNA damage repair signaling | DNA damage repair genes (eg. SSRP1,ERCC3,CHD1L,TP53BP1,TRIP13) | Not available (10 μM treated HCC cells) | [114] |