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. 2023 Jul 24;13(12):4247–4265. doi: 10.7150/thno.86528

Table 2.

Small molecule inhibitor of IGF2BPs

IGF2BPs Inhibitors Cancer types Target site Effect Ref
IGF2BP1 BTYNB Melanoma, Ovarian cancer Unknown Disrupting the interaction between 117, 118
IGF2BP1 and target mRNAs
7773 Lung cancer A hydrophobic surface at the Reducing the level of mRNA targets 119
boundary of KH3 and KH4 domain
Cucurbitacin B HCC The Cys253 site in the KH1-2 domain A pharmacological allosteric effect to inhibit 73
recognition of target mRNAs
C646 Intrahepatic H3K27ac in the promoter of IGF2BP1 Decreasing the IGF2BP1 mRNA and protein 45
cholangiocarcinoma expression
IGF2BP2 Ten compounds, CRC, Liver cancer RRM1 and KH3-4 (Compounds Reducing tumor cell proliferation 120
belonging to the from benzamidobenzoic acid class),
benzamidobenzoic acid class Unknown (Compounds from
and ureidothiophene class ureidothiophene class)
JX5 Leukemia KH3-4 domain Suppressing the cancer progression without 121
influencing the IGF2BP2 mRNA levels
CWI1-2 Leukemia The hydrophobic pocket within Decreasing downstream RNA and protein levels of 122
the KH4 domain IGF2BP2 to exert anti-tumor efficacy
IGF2BP3 JQ1 and I-BET151 Leukemia, Unknown Decreasing levels of IGF2BP3 and its mRNA 27, 123
Ewing Sarcoma targets to hinder tumor growth
Berberine CRC Unknown Down-regulating IGF2BP3 at the protein level to 105, 124
inhibit CRC growth
Isoliquiritigenin Non-small cell lung cancer Unknown Reducing IGF2BP3 at the mRNA and protein level 125
to inhibit lung cancer progression
RIG Lung adenocarcinoma Unknown Reducing IGF2BP3 expression and tumor growth 57