For research use only. Not for therapeutic Use.
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].
| Catalog Number | I045768 |
| Synonyms | [[(3R)-4-[[3-[2-[2-[[(5S)-5-acetamido-6-amino-6-oxohexyl]amino]-2-oxoethyl]sulfanylethylamino]-3-oxopropyl]amino]-3-hydroxy-2,2-dimethyl-4-oxobutoxy]-hydroxyphosphoryl] [(2R,3S,4R,5R)-5-(6-aminopurin-9-yl)-4-hydroxy-3-phosphonooxyoxolan-2-yl]methyl hydrogen phosphate;2,2,2-trifluoroacetic acid |
| Molecular Formula | C33H54F3N10O21P3S |
| Purity | ≥95% |
| InChI | InChI=1S/C31H53N10O19P3S.C2HF3O2/c1-17(42)40-18(27(33)47)6-4-5-8-34-21(44)13-64-11-10-35-20(43)7-9-36-29(48)25(46)31(2,3)14-57-63(54,55)60-62(52,53)56-12-19-24(59-61(49,50)51)23(45)30(58-19)41-16-39-22-26(32)37-15-38-28(22)41;3-2(4,5)1(6)7/h15-16,18-19,23-25,30,45-46H,4-14H2,1-3H3,(H2,33,47)(H,34,44)(H,35,43)(H,36,48)(H,40,42)(H,52,53)(H,54,55)(H2,32,37,38)(H2,49,50,51);(H,6,7)/t18-,19+,23+,24+,25-,30+;/m0./s1 |
| InChIKey | SGCAYGMHHNOYEY-JPBLFTSTSA-N |
| SMILES | CC(=O)NC(CCCCNC(=O)CSCCNC(=O)CCNC(=O)C(C(C)(C)COP(=O)(O)OP(=O)(O)OCC1C(C(C(O1)N2C=NC3=C(N=CN=C32)N)O)OP(=O)(O)O)O)C(=O)N.C(=O)(C(F)(F)F)O |
| Reference | [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. [2]. Lau OD, et al. HATs off: selective synthetic inhibitors of the histone acetyltransferases p300 and PCAF. Mol Cell. 2000;5(3):589-595. |
