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Histone acetyltransferase (HAT) inhibitors target the writers of lysine acetylation on histones and other proteins. Acetylation neutralizes the positive charge of histone tails and favors transcription. In 1996 a Tetrahymena HAT was found to be related to a yeast transcriptional regulator, which linked histone acetylation to gene activation. In the same year the coactivators p300 and CREB-binding protein (CBP) were shown to be histone acetyltransferases. C646, found in 2010 by virtual ligand screening, is a selective inhibitor of the p300/CBP HAT domain. MG149 and NU 9056 target lysine acetyltransferase 5 (KAT5, Tip60), and garcinol is a natural product with broad HAT inhibition. SGC-CBP30 and I-CBP112 bind the CBP/p300 bromodomain rather than the catalytic site.
C646 is a selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM).
SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.
Synonyms: MG 149,MG-149
MG149 is a potent histone acetyltransferase inhibitor with IC50 of 74 uM and 47 uM for Tip60 and MOF.
Synonyms: PRI 724
PRI-724 is the second-generation, potent and specific inhibitor of CBP/β-Catenin complex, and a modulator of the β-Catenin dependent canonical Wnt signaling pathway in cancer stem cells.
Histone Acetyltransferase Inhibitor II is a potent and cell permeable p300 inhibitor, with an IC50 of 5μM; Histone Acetyltransferase Inhibitor II can be used in cancer research.
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
Synonyms: camboginol
Garcinol is a polyisoprenylated benzophenone derivative isolated from Garcinia indica. It is a potent inhibitor of histone acetyltransferases (HATs) p300 (IC50=7μM) and PCAF (IC50=5μM) both in vitro and in vivo.
I-CBP112 is a highly potent and selective p300/CBP bromodomain inhibitor (IC50 ~0.14-0.17 uM for CBP and ~0.625 uM for p300).
NU9056 is an selective KAT5 (Tip60) HAT inhibitor. IC50 values are < 2, 60, 36, and >100 μM for KAT5, p300, pCAF and GCN5, respectively. Inhibits protein acetylation in prostate cancer cell lines and blocks DNA damage response. Decreases proliferation of LNCaP cells; induces apoptosis via caspase activation.
Remodelin Hydrobromide is a potent acetyl-transferase NAT10 inhibitor.
Synonyms: 6-pentadecylsalicylic Acid
Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases.
EML 425 is a reversible and non-competitive CBP/p300 inhibitor that is cell permeable (IC50 values are 1.1 and 2.9 uM, respectively).
CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
WM-1119 is a highly potent, selective inhibitor of lysine acetyltransferase KAT6A with IC50 of 0.25 μM. It is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively.
A-485 is a potent and selective HAT inhibitor of p300/CBP in vitro with an IC50 of 10 nM in a p300 TR-FRET assay and 3 nM in a CBP TR-FRET assay with selectivity > 1000-fold over closely related HATs.
CBL0137 is a FACT inhibitor that functionally inactivates the facilitates chromatin transcription complex (FACT), driving the effects on p53 and NF-κB and promoting cancer cell death.
P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor.
GNE-207 is a novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP. GNE-207 has excellent CBP potency (CBP IC50 = 1 nM, MYC EC50 = 18 nM), and it exhibits a good pharmacokinetic profile.
GNE-781 is a highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively.
HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
WM-8014 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.
MOZ-IN-2 is an inhibitor of protein MOZ, a member of histone acetyltransferases, with an IC50 of 125 μM.
Synonyms: CCS-1477
Inobrodib (CCS-1477) is a potent p300/CBP bromodomain inhibitor.
GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively.
L002 is a novel potent, specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 uM.
