CBP/p300-IN-19 is a potent p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 shows antitumor activity[1].
Remodelin HBr salt is a novel potent and selective inhibitor of the acetyl-transferase protein NAT10.IC50 value:Target: NAT10 inhibitorRemodelin can improve nuclear architecture, chromatin organization, and fitness of both human lamin A/C-depleted cells and HGPS-derived patient cells, and decrease markers of DNA damage in these cells. Using a combination of chemical, cellular, and genetic approaches, acetyl-transferase protein NAT10 was identified as the target of Remodelin that mediated nuclear shape rescue in laminopathic cells via microtubule reorganization. Down-regulation and mutations of the nuclear-architecture proteins lamin A and C cause misshapen nuclei and altered chromatin organization associated with cancer and laminopathies, including the premature-aging disease Hutchinson-Gilford progeria syndrome (HGPS). Remodelin is a useful chemical tool to study how NAT10 affects nuclear architecture and suggest alternative strategies for treating laminopathies and aging.
CBP/p300-IN-10 is a highly potent histone acetyltransferase EP300 and CREBBP with IC50 values of 26 nM and 39 nM, respectively. CBP/p300-IN-10 can be used to research anticancer[1].
NSC 694623 is a potent histone acetyltransferase (HAT) inhibitor with an IC50 value of 15.9 μM for recombinant HAT p300/CBP-associated factor (PCAF). NSC 694623 has antiproliferative activity against certain cancer cells. NSC 694623 can be used for researching anticancer[1].
GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
CBP/p300-IN-19 hydrochloride is a potent and selective p300/CBP HAT inhibitor with IC50s of 1.4, 2.2, >100, >100 µM for p300-HAT, CBP-HAT, PCAF, Myst3, respectively. CBP/p300-IN-19 hydrochloride shows antitumor activity[1].
Curcumin is a natural phenolic compound with diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin is an inhibitor of p300 histone acetylatransferase ((HATs)) and also shows inhibitory effects on NF-κB and MAPKs.
C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
Butyrolactone 3 is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM)[1]
HAT-IN-1 is an inhibitor of HAT, used in the research of cancer.
CPI-637 is a potent and selective CBP/EP300 bromodomains inhibitor with IC50 of 0.03±0.01μM and 11.0±0.6 μM for CBP/EP300 and BRD4, respectively.IC50:0.03±0.01μM (CBP/EP300)[1]IC50:11.0±0.6 μM(BRD4)[1]CPI-637, which demonstrated substantial biochemical potency that was confirmed by isothermal titration calorimetry. A cocrystal structure of CPI-637 in the CBP bromodomain indicated that the compound recapitulated the key hydrogen bonding interactions observed with the parent compound, with the substituted indazole filling space above Pro1110 and the Pro/Arg cleft . As expected, CPI-637 was also potent against EP300, and its opposite enantiomer displayed a >200-fold loss in potency. The biochemical potency of CPI-637 translated well into cells (CBP BRET EC50 = 0.3 μM), and the compound demonstrated a >700-fold selectivity over the BET family of bromodomains (BRD4 IC50 = 11.0 ± 0.6 μM).CPI-637 was also highly selective against other bromodomains (detailed list in the Supporting Information), displaying substantial biochemical activity only against BRD9, which is acceptable, since inhibition of the BRD9 bromodomain has not been shown to produce a pronounced cellular phenotype . In a cellular assay, CPI-637 inhibits the expression of MYC, a transcription factor widely expressed in human cancer,with an EC50 of 0.60 μM, providing an orthogonal measure of the target engagement of the compound .The inactive enantiomer of CPI-637 displayed an EC50 in the same assay of >10 μM.[1]
Windorphen is a Wnt/β-catenin signal inhibitor that specifically targets the function of the c-terminal transactivation domain of β-catenin-1 but not β-catenin-2. Windorphen selectively targets p300, disrupting the association of the mammalian β-catenin with p300 but not CBP[1].
NEO2734 (EP31670) is an orally active dual p300/CBP and BET bromodomain selective inhibitor, with IC50 values of <30 nM for both p300/CBP and BET bromodomains[1]. NEO2734 is active in SPOP mutant and wild-type prostate cancer[2].
Acetaminophen-13C2,15N is the 13C and 15N labeled Acetaminophen[1]. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM;is a widely used antipyretic and analgesic agent[2][3][4]. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor[5].
CBP/p300-IN-14 is a potent inhibitor of CBP/EP300 (lysine acetyltransferase) with an IC50 of 3.3 nM (extracted from patent WO2021213521A1, compound 27)[1].
PF-9363 (CTx-648) is a first-in-class potent and high selective KAT6A/KAT6B inhibitor. PF-9363 can be used for the research of cancer[1][2].
WM-1119 is a highly potent and selective KAT6A inhibitor, with an IC50 of 0.25 μM for KAT6A in lymphoma cells, the binding KD values of WM-1119 with KAT6A, KAT5 and KAT7 are 2 nM, 2.2 μM, 0.5 μM , respectively.
A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP, respectively.
NSC 228155 is a potent inhibitor of KIX-KID interaction, inhibits kinase-inducible domain (KID) from CREB and KID-interacting domain (KIX) from CBP, with an IC50 of 0.36 μM. NSC 228155 is not selective against CREB-mediated gene transcription in living HEK 293T cells[1].
CPTH2 hydrochloride is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 hydrochloride selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 hydrochloride induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B)[1][2].
NSC 694621 is a potent PCAF inhibitor, with an IC50 of 5.71 µM (PCAF/H31-21). NSC 694621 exhibits good activity of inhibiting the proliferation of cancer cells[1].
WM-8014 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.
PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain.Target: CREBin vitro: PF-CBP1 modulates key inflammatory genes in primary macrophages. PF-CBP1 downregulates RGS4 in neurons, a target linked to Parkinson's disease. PF-CBP1 is 139-fold selective over BRD4 in the biochemical assays and >105-fold selective by ITC. F-CBP1 is also a potent inhibitor of EP300 (a result observed for other CBP inhibitors. [1]
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 nΜ, respectively.
GNE-272 is a potent and selective in vivo probe for the bromodomains of CBP/EP300 with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively.
P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1[1].
SPV106 is histone acetylase (HAT) and GCN5-related N-acetyltransferases (GNAT) activator. SPV106 can be used for the research of type 2 diabetes (T2D)[1].
CTB (Cholera Toxin B subunit) is a potent p300 histone acetyltransferase activator[1]. CTB can effectively induce apoptosis in MCF-7 cells[2].
TTK21 (CBP-p300 activator TTK21) is a small molecule activator of CBP/p300 histone acetyltransferase activity with a maximal effect at a concentration of 275 uM; induces acetylation of histones H3 and H4 in vitro but not H2B and H2A; promotes neurogenesis and extends memory duration in adult mice, promotes regeneration and sprouting of sensory and motor axons, as well as recovery of sensory and motor functions in both the mouse and rat model of spinal cord injury.
CBP/p300-IN-15 (compound 13a) is a potent p300/CBP inhibitor, with IC50 values of 2.50 and 28.0 nM, respectively. CBP/p300-IN-15 shows good activity against OVCAR-3 and A2780 cell line, with EC50 values of 0.865 and 2.71 μM, respectively. CBP/p300-IN-15 can be used for ovarian cancer research[1].