Lys-CoA TFA  (Synonyms: Lys-coenzyme A)

Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC₅₀=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC₅₀=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation^[1][2].

Lys-CoA TFA (0.1 and 1 mM; 60 hours) induces a senescent phenotype in human normal melanocytes^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

1108.82

C₃₃H₅₄F₃N₁₀O₂₁P₃S

Solid

White to off-white

O[C@@H]1[C@H](OP(O)(O)=O)[C@@H](COP(OP(OCC(C)(C)[C@@H](O)C(NCCC(NCCSCC(NCCCC[C@@H](C(N)=O)NC(C)=O)=O)=O)=O)(O)=O)(O)=O)O[C@H]1N2C=NC3=C(N)N=CN=C32.O=C(O)C(F)(F)F

Room temperature in continental US; may vary elsewhere.

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

• [1]. Cebrat M, et al. Synthesis and analysis of potential prodrugs of coenzyme A analogues for the inhibition of the histone acetyltransferase p300. Bioorg Med Chem. 2003;11(15):3307-3313.  [Content Brief]

  [2]. Lau OD, et al. HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol Cell. 2000;5(3):589-595.  [Content Brief]