UNC10142 is a selective CHD1 antagonist with an IC50 of 1.7 μM and a K d of 4.3 μM. UNC10142 exhibits anticancer activity against PTEN-deficient prostate cancer but shows no effect on PTEN-intact prostate cancer. UNC10142 can be used in studies related to PTEN-deficient prostate cancer [1].
In Vitro, UNC10142 (1 h) inhibits the interaction between recombinant CHD1 tandem chromatin domains and H3K4me2 peptide in TR-FRET assays, with an IC50 of 1.7 μM[1]. UNC10142 (750-1000 μM) binds directly to the tandem chromatin domains of recombinant CHD1, with a measured Kd value of 4.3 μM determined by ITC[1]. UNC10142 exhibits much higher selectivity for CHD1 than most of the tested Kme reader domains, with only 6-fold weaker binding affinity for the PHF19 Tudor domain[1]. UNC10142 (75 μM; 24 h) selectively reduces the viability of PTEN-deficient PC-3 and LNCaP prostate cancer cells, while exerting minimal effects on PTEN-intact DU145 prostate cancer cells[1].
References:
[1]. Johnson RL, et al. Discovery of CHD1 Antagonists for PTEN-Deficient Prostate Cancer. Journal of medicinal chemistry. 2024 Nov 28;67(22):20056-20075.
In Vitro, UNC10142 (1 h) inhibits the interaction between recombinant CHD1 tandem chromatin domains and H3K4me2 peptide in TR-FRET assays, with an IC50 of 1.7 μM[1]. UNC10142 (750-1000 μM) binds directly to the tandem chromatin domains of recombinant CHD1, with a measured Kd value of 4.3 μM determined by ITC[1]. UNC10142 exhibits much higher selectivity for CHD1 than most of the tested Kme reader domains, with only 6-fold weaker binding affinity for the PHF19 Tudor domain[1]. UNC10142 (75 μM; 24 h) selectively reduces the viability of PTEN-deficient PC-3 and LNCaP prostate cancer cells, while exerting minimal effects on PTEN-intact DU145 prostate cancer cells[1].
References:
[1]. Johnson RL, et al. Discovery of CHD1 Antagonists for PTEN-Deficient Prostate Cancer. Journal of medicinal chemistry. 2024 Nov 28;67(22):20056-20075.