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2738688-57-6

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2738688-57-6 Structure

2738688-57-6 Structure
IdentificationBack Directory
[Name]

INDEX NAME NOT YET ASSIGNED
[CAS]

2738688-57-6
[Synonyms]

[Molecular Formula]

C33H29F4N5O6
[Molecular Weight]

667.61
Chemical PropertiesBack Directory
[density ]

1.46±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : 250 mg/mL (374.47 mM; Need ultrasonic)
[form ]

Solid
[pka]

13.36±0.70(Predicted)
[color ]

Off-white to light yellow
Hazard InformationBack Directory
[Biological Activity]

CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450[1]. CBP/p300-IN-12 (Compound 2) shows antiproliferative effect against androgen receptor (AR)-positive LnCaP-FGC cells (EC50 of 87 nM), while displaying significantly less activity in the AR-negative cell line DU-145 (EC50 of 1.37 μM).
[References]

[1]. Anthony Mastracchio, et al. Discovery of a Potent and Selective Covalent p300/CBP Inhibitor. ACS Med Chem Lett. 2021 Apr 5;12(5):726-731.
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