The histone acetyltransferase (HAT) enzymes p300 and CBP are closely related paralogs that serve as transcriptional coactivators. The p300 and CBP catalyze the acetylation of Lys residues in histones and other proteins. Serving as transcriptional coactivators, p300 and CBP participate in numerous ways to regulate cell growth, differentiation, and gene expression across many organ systems and physiologic pathways. Dysregulation of p300/CBP by mutation, altered expression, or other mechanisms has been linked to disease states, including various malignancies such as acute leukemias and prostate cancer. Furthermore, p300/CBP is critical in development as evidenced by the genetic disorder Rubinstein-Taybi syndrome, which occurs with loss of function mutations in single alleles of either p300 or CBP. Inhibitors of p300/CBP HAT activity have been developed and are under investigation as therapeutics for a number of diseases.


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Butyrolactone 3

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]

  • CAS Number: 778649-18-6
  • MF: C9H12O4
  • MW: 184.189
  • Catalog: Histone Acetyltransferase
  • Density: 1.2±0.1 g/cm3
  • Boiling Point: 386.2±42.0 °C at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 158.5±21.4 °C

PF-9363

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].

  • CAS Number: 2569009-58-9
  • MF: C20H20N4O6S
  • MW: 444.46
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

WM 1119

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.

  • CAS Number: 2055397-28-7
  • MF: C18H13F2N3O3S
  • MW: 389.38
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CPTH2 hydrochloride

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].

  • CAS Number: 2108899-91-6
  • MF: C14H15Cl2N3S
  • MW: 328.260
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NSC 694621

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].

  • CAS Number: 104857-29-6
  • MF: C13H10N2O2S
  • MW: 258.30
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PF-CBP1 hydrochloride

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]

  • CAS Number: 2070014-93-4
  • MF: C29H36N4O3·HCl
  • MW: 525.08
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE-781

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.

  • CAS Number: 1936422-33-1
  • MF: C27H33F2N7O2
  • MW: 525.59
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE-272

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.

  • CAS Number: 1936428-93-1
  • MF: C22H25FN6O2
  • MW: 424.47
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

P300/CBP-IN-3

P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1[1].

  • CAS Number: 2299226-01-8
  • MF: C24H29N7O
  • MW: 431.53
  • Catalog: Histone Acetyltransferase
  • Density: 1.23±0.1 g/cm3(Predicted)
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

SPV 106

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].

  • CAS Number: 1036939-38-4
  • MF: C22H40O4
  • MW: 368.55100
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CTB

CTB (Cholera Toxin B subunit) is a potent p300 histone acetyltransferase activator[1]. CTB can effectively induce apoptosis in MCF-7 cells[2].

  • CAS Number: 451491-47-7
  • MF: C16H13ClF3NO2
  • MW: 343.73
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PU-141

PU-141 is a potent, selective CBP/p300 inhibitor that inhibits SK-N-SH cell growth with GI50 of 0.48 uM; blocks growth of SK-N-SH neuroblastoma xenografts in mice, also reduces histone lysine acetylation in vivo at concentrations that block neoplastic xenograft growth.

  • CAS Number: 168334-34-7
  • MF: C14H9F3N2OS
  • MW: 310.294
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

GNE-049

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 nΜ, respectively.

  • CAS Number: 1936421-41-8
  • MF: C27H32F2N6O2
  • MW: 510.58
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

BET inhibitor CF53

CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, Kds are 1.1 nM (BRD2 BD1), 0.6 nM (BRD2 BD2), 0.52 nM (BRD3 BD1), 0.49 nM (BRD3 BD2), 0.8 nM (BRD4 BD2), 2 nM (BRDT BD1), 2.1 nM (BRDT BD2), 47 nM (CREBBP), 570 nM (CECR2), 110 nM (EP300), respectively, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo[1].

  • CAS Number: 1808160-52-2
  • MF: C24H25N7O2
  • MW: 443.50
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Ep300/CREBBP-IN-2

Ep300/CREBBP-IN-2 (Example 73) is a potent and orally active Ep300 and CREBBP inhibitor with IC50s of 0.052 and 0.148 μM, respectively. Ep300/CREBBP-IN-2 can be used for the research of cancer[1].

  • CAS Number: 2259641-59-1
  • MF: C26H27F3N4O4
  • MW: 516.51
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CPTH2

CPTH2 is a potent histone acetyltransferase (HAT) inhibitor. CPTH2 selectively inhibits the acetylation of histone H3 by Gcn5. CPTH2 induces apoptosis and decreases the invasiveness of a clear cell renal carcinoma (ccRCC) cell line through the inhibition of acetyltransferase p300 (KAT3B)[1][2].

  • CAS Number: 357649-93-5
  • MF: C14H14ClN3S
  • MW: 291.79900
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CTPB

CTPB is a good activator of p300 histone acetyl transferase (HAT) enzyme[1].

  • CAS Number: 586976-24-1
  • MF: C31H43ClF3NO2
  • MW: 554.12700
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Curcumin D6

Curcumin D6 (Diferuloylmethane D6) is a deuterium labeled Curcumin (Turmeric yellow). Curcumin (Turmeric yellow) 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.

  • CAS Number: 1246833-26-0
  • MF: C21H14D6O6
  • MW: 374.41700
  • Catalog: Influenza Virus
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DCH36_06

DCH36_06 is a potent and selective p300/CBP inhibitor with IC50s of 0.6 μM and 3.2 μM for p300 and CBP, respectively. DCH36_06 mediated p300/CBP inhibition leading to hypoacetylation on H3K18 in leukemic cells. Anti-tumor activity[1].

  • CAS Number: 593273-05-3
  • MF: C18H13ClN2O3S
  • MW: 372.83
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

JQAD1

JQAD1 is a CRBN-dependent PROTAC that selectively targets EP300 for degradation. JQAD1 suppresses EP300 expression and the H3K27ac modification. JQAD1 induces apoptosis. JQAD1 can be used in research of cancer[1].

  • CAS Number: 2417097-18-6
  • MF: C48H52F4N6O9
  • MW: 932.95
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

YF-2

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[1].

  • CAS Number: 1311423-89-8
  • MF: C20H22ClF3N2O3
  • MW: 430.84800
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

PCAF-IN-2

PCAF-IN-2 (compound 17) is a potent PCAF inhibitor with an IC50 value of 5.31 µM. PCAF-IN-2 shows anti-tumour activity. CAF-IN-2 induces apoptosis and arrest the cell cycle at the G2/M phase[1].

  • CAS Number: 56173-05-8
  • MF: C10H7F3N6
  • MW: 268.20
  • Catalog: Apoptosis
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

NSC 694623

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].

  • CAS Number: 907957-34-0
  • MF: C16H16N2OS
  • MW: 284.38
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Curcumin

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.

  • CAS Number: 458-37-7
  • MF: C21H20O6
  • MW: 368.380
  • Catalog: Autophagy
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 593.2±50.0 °C at 760 mmHg
  • Melting Point: 183 °C
  • Flash Point: 209.7±23.6 °C

C646

C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.

  • CAS Number: 328968-36-1
  • MF: C24H19N3O6
  • MW: 445.424
  • Catalog: Autophagy
  • Density: 1.4±0.1 g/cm3
  • Boiling Point: 662.6±65.0 °C at 760 mmHg
  • Melting Point: 224-226℃
  • Flash Point: 354.5±34.3 °C

NEO2734

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].

  • CAS Number: 2081072-29-7
  • MF: C22H24F3N3O3
  • MW: 435.44
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

CBP/p300-IN-14

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].

  • CAS Number: 2725036-10-0
  • MF: C30H31F2N7O2
  • MW: 559.61
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

A 485

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.

  • CAS Number: 1889279-16-6
  • MF: C25H24F4N4O5
  • MW: 536.48
  • Catalog: Epigenetic Reader Domain
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

MOZ-IN-3

WM-8014 is an inhibitor of MOZ, a member of histone acetyltransferases, with an IC50 of 55 nM.

  • CAS Number: 2055397-18-5
  • MF: C20H17FN2O3S
  • MW: 384.42
  • Catalog: Histone Acetyltransferase
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

4-Acetamidophenol

Acetaminophen (paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic drug.

  • CAS Number: 103-90-2
  • MF: C8H9NO2
  • MW: 151.163
  • Catalog: Bacterial
  • Density: 1.3±0.1 g/cm3
  • Boiling Point: 387.8±25.0 °C at 760 mmHg
  • Melting Point: 168-172 °C(lit.)
  • Flash Point: 188.4±23.2 °C