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. Author manuscript; available in PMC: 2015 Feb 1.
Published in final edited form as: Cancer Treat Rev. 2013 Jul 5;40(1):10.1016/j.ctrv.2013.05.009. doi: 10.1016/j.ctrv.2013.05.009

Table 2.

Specificity and Activity of Histone Acetyltranferase Inhibitors

HATi COMPOUND NAMES HAT SPECIFICITY ACTIVITY( IC50) REF
SYNTHETIC HATis
graphic file with name nihms-491539-t0003.jpg Lys-CoA KAT3B (P300) 3.2μM 37
graphic file with name nihms-491539-t0004.jpg Lys-CoA-CH3 KAT2B (PCAF) 0.8μM 37
graphic file with name nihms-491539-t0005.jpg Ph-Lys-CoA KAT3B (P300/) 0.7μM 38
NATURAL HATis
graphic file with name nihms-491539-t0006.jpg Anacardic Acid KAT3B (P300)
KAT2B (PCAF)		 8.5μM
5.0μM		 39
graphic file with name nihms-491539-t0007.jpg Garcinol
(Toxic)		 KAT3B (P300)
KAT2B (PCAF)		 7.0μM
5.0μM		 40, 41
graphic file with name nihms-491539-t0008.jpg Isogarcinol (Toxic)
LTK14 (R = CH3/ -C(CH3)2)
(Non-Toxic)		 KAT3B (P300)
KAT2B (PCAF)
KAT3B (P300)		 7.0μM
5.0μM
5.0-7.0μM		 41
graphic file with name nihms-491539-t0009.jpg Curcumin
(R = OCH3)		 KAT3B (P300) 25μM 40, 42
graphic file with name nihms-491539-t0010.jpg Compound-11
R=Br		 KAT3B (P300) 5.0μM 42
SMALL MOLECULE HATis
graphic file with name nihms-491539-t0011.jpg γ-Butyrolactone
(R= nC3H7)		 KAT2A (hGCN5) 100μM 43
graphic file with name nihms-491539-t0012.jpg Isothiazolones
(R1 = H, R2 = NO2,
R3 = Cl, R4-6 = H)		 KAT2B (PCAF) 1.1μM 44
graphic file with name nihms-491539-t0013.jpg CCT077791 KAT3B (P300)
KAT2B (PCAF)		 3.0μM
7.3μM		 44

Red arrows or circles denote sites of side chain substitution