Histone Acetyltransferases
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CBP/p300 bromodomain inhibitor
SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.
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CBP/p300 bromodomain inhibitor
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).
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p300 inhibitor
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.
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CBP/P300 benzoxazepine bromodomain inhibitor
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with Kd values of 134 nM and 5.02 μM for CBP and BRD4.
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CBP 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.
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CBP/p300 inhibitor
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).
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CBP/EP300 bromodomain inhibitor
CPI-637 is a selective and cell-active benzodiazepinone CBP/EP300 bromodomain inhibitor.
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p300/CBP inhibitor
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.
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CBP/beta-catenin modulator
E-7386 is an orally active CBP/beta-catenin modulator.
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CBP bromodomain 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.
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p300 HAT activator
CTPB is an activator of p300 HAT (histone acetyltransferase) without PCAF (p300/CBP-associated factor) HAT activities.
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lysine acetyltransferase KAT6A 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.
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histone acetyltransferase activator
YF-2 is a highly selective, blood-brain-barrier permeable histone acetyltransferase activator, acetylates H3 in the hippocampus, with EC50s of 2.75 μM, 29.04 μM and 49.31 μM for CBP, PCAF, and GCN5, respectively, shows no effect on HDAC. Anti-cancer and anti-Alzheimer's disease.
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acetyl-transferase protein NAT10 inhibitor
Remodelin is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.
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p300/CBP histone acetyltransferase inhibitor
P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor.
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HAT inhibitor
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.
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KAT5 (Tip60) HAT inhibitor
MG149 is a potent histone acetyltransferase inhibitor with IC50 of 74 uM and 47 uM for Tip60 and MOF.
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NAT10 inhibitor
Remodelin Hydrobromide is a potent acetyl-transferase NAT10 inhibitor.
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KAT5 (Tip60), p300/PCAF inhibitor
Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases.
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KAT5 (Tip60) HAT inhibitor
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.
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p300/CBP inhibitor
C646 is a selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM).
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- Zhifeng Zhang, .et al. XRCC5 cooperates with p300 to promote cyclooxygenase-2 expression and tumor growth in colon cancers, PLoS One, 2017, 12(10): e0186900 PMID: 29049411