Chemical Structure : UNC10142
CAS No.:
UNC10142
(UNC-10142)
Catalog No.: PC-23450Not For Human Use, Lab Use Only.
UNC10142 is a first-in-class, specific, cell-active small molecule antagonist of the tandem chromodomains of CHD1 (Chromodomain-Helicase DNA-Binding Protein 1) with binding IC50 of 1.7 uM in TR-FRET assays.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
UNC10142 is a first-in-class, specific, cell-active small molecule antagonist of the tandem chromodomains of CHD1 (Chromodomain-Helicase DNA-Binding Protein 1) with binding IC50 of 1.7 uM in TR-FRET assays.
UNC10142 dispalys >30-fold selective for CHD1 against other Kme readers MPP8, PHF19, and SETDB1.
UNC10142 binds to the tandem chromodomains of CHD1 with ITC Kd of 4.3 uM.
UNC10142 engages endogenous CHD1 and leads to loss of viability in PTEN-deficient cells.
UNC10142 phenocopies genetic loss of CHD1 in PTEN-deficient prostate cancer cells.
UNC10142 treatment results in synthetic lethality in PTEN-deficient prostate cancer cells while sparing PTEN-intact prostate cancer cells.
Physicochemical Properties
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M.Wt
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580.82
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Formula
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C33H52N6O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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1-(4-((2-(Azonan-1-yl)-6-methoxy-7-(3-(piperidin-1-yl)propoxy)quinazolin-4-yl)(methyl)amino)piperidin-1-yl)ethan-1-one
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References
1. Johnson RL, et al. J Med Chem. 2024 Nov 7. doi: 10.1021/acs.jmedchem.4c01172.
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