2. Signaling Pathways
  3. Epigenetics
  4. Histone Acetyltransferase
  5. CBP/p300 Isoform
  6. CBP/p300 Inhibitor

CBP/p300 Inhibitor

CBP/p300 Inhibitors (45):

Cat. No. Product Name Effect Purity
  • HY-N0005
    Curcumin
    		Inhibitor 98.84%
    Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin is a photosensitizer against microorganisms. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
  • HY-107455
    A-485
    		Inhibitor 99.87%
    A-485, a chemical probe, is a potent and selective catalytic inhibitor of p300/CBP with IC50s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively.
  • HY-13823
    C646
    		Inhibitor 99.88%
    C646 is a selective and competitive histone acetyltransferase p300 inhibitor with Ki of 400 nM, and is less potent for other acetyltransferases.
  • HY-15826
    SGC-CBP30
    		Inhibitor 99.83%
    SGC-CBP30, a chemical probe, is a potent and highly selective CBP/p300 bromodomain (Kds of 21 nM and 32 nM for CBP and p300, respectively) inhibitor, displaying 40-fold selectivity over the first bromodomain of BRD4 [BRD4(1)] bound. SGC-CBP30 strongly reduces secretion of IL-17A in Th17 cells and has anti-inflammatory effects.
  • HY-N2020
    Anacardic Acid
    		Inhibitor 98.49%
    Anacardic Acid, extracted from cashew nut shell liquid, is a histone acetyltransferase inhibitor, inhibits HAT activity of p300 and PCAF, with IC50s of ∼8.5 μM and ∼5 μM, respectively.
  • HY-174866
    BT-O2C
    		Inhibitor
    BT-O2C is a highly selective p300 PROTAC degrader. BT-O2C can significantly degrade the level of p300 in HAP1 cells. BT-O2C has significant cytotoxicity in CIC:DUX4 sarcoma (CDS) cell lines (IC50 ranges from 152 to 221 nM) and significantly reduces the expression of CDS target genes (ETV1, ETV4, ETV5). BT-O2C can be used for research on cancer. (Pink: p300 Ligand (HY-174868); Blue: CRBN Ligand (HY-W023573); Black: Linker; CRBN Ligand+Linker (HY-174869)).
  • HY-175180
    Conophyllidine
    		Inhibitor
    Conophyllidine, a bisindole alkaloid, is a selective M2 polarization inhibitor. Conophyllidine inhibits histone acetylation by targeting the histone acetyltransferase domain of the P300/CBP proteins. Conophyllidine inhibits IL-4-induced arginase with an IC50 of 0.31 μM. Conophyllidine effectively induces a phenotypic switch in tumor-associated macrophages (TAMs) from an anti-inflammatory to an inflammatory type, thereby enhancing cytotoxic CD8+ T cell recruitment and functionality within the tumor microenvironment. Conophyllidine can be used for the study of TAMs.
  • HY-15887
    MG 149
    		Inhibitor 99.24%
    MG149 (Tip60 HAT inhibitor) is a selective and potent Tip60 inhibitor with IC50 of 74 uM, similar potentcy for MOF (IC50 = 47 uM); little potent for PCAF and p300 (IC50 >200 uM). MG 149 inhibits KAT8 and blocks PINK1 kinase activity. MG 149 can induce mitochondrial depolarization and promote PINK1 dependent mitochondrial clearance. MG 149 can reverse chronic restraint stress (CRS) induced hypertension and related molecular changes. MG 149 commonly used in research on diseases such as hypertension and Parkinson's disease.
  • HY-101084
    NSC 228155
    		Inhibitor 98.0%
    NSC 228155 is an activator of EGFR, binds to the extracellular region of EGFR and enhance tyrosine phosphorylation of EGFR. NSC 228155 is also 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.
  • HY-124696
    PU139
    		Inhibitor 99.51%
    PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor. PU139 blocks the HATs Gcn5, p300/CBP-associated factor (PCAF), CREB (cAMP response element-binding) protein (CBP) and p300 with IC50s of 8.39, 9.74, 2.49 and 5.35 μM, respectively.
  • HY-108435
    GNE-049
    		Inhibitor 98.01%
    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.
  • HY-136285
    CPI-1612
    		Inhibitor 99.74%
    CPI-1612 is a highly potent, orally active EP300/CBP histone acetyltransferase (HAT) inhibitor with an IC50 of 8.1 nM for EP300 HAT. CPI-1612 has an anticancer activity.
  • HY-136938
    NEO2734
    		Inhibitor 99.63%
    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. NEO2734 is active in SPOP mutant and wild-type prostate cancer.
  • HY-120028
    GNE-207
    		Inhibitor 99.94%
    GNE-207 is a potent, selective and orally bioavailable inhibitor of the bromodomain of CBP, with an IC50 of 1 nM, exhibits a selectively index of >2500-fold against BRD4 (1). GNE-207 shows excellent CBP potency, with an EC50 of 18 nM for MYC expression in MV-4-11 cells.
  • HY-100726
    GNE-272
    		Inhibitor 99.60%
    GNE-272 is a potent and selective CBP/EP300 inhibitor with IC50 values of 0.02, 0.03 and 13 μM for CBP, EP300 and BRD4, respectively. GNE-272 is also a selective in vivo probe for CBP/EP300.
  • HY-100671
    L002
    		Inhibitor 99.44%
    L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an IC50 of 1.98 μM. L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation. L002 has the potential for hypertension-induced cardiac hypertrophy and fibrogenesis treatment.
  • HY-N2345
    Procyanidin B3
    		Inhibitor 99.92%
    Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis.
  • HY-100734
    Histone Acetyltransferase Inhibitor II
    		Inhibitor 98.70%
    Histone Acetyltransferase Inhibitor II (compound 2c) is a potent, selective and cell permeable p300 histone acetyltransferase inhibitor, with an IC50 of 5 µM. Histone Acetyltransferase Inhibitor II shows anti-acetylase activity in mammalian cells.
  • HY-128876
    CBP/p300-IN-3
    		Inhibitor 98.01%
    CBP/p300-IN-3, a p300/CBP histone acetyltransferase inhibitor, Compound 6, is sourced from patent WO 2019049061 A1.
  • HY-132197
    CBP/p300-IN-12
    		Inhibitor 99.72%
    CBP/p300-IN-12 is a potent and selective covalent histone acetyltransferases p300 (IC50 of 166 nM) and CBP inhibitor. CBP/p300-IN-12 decreases the levels of H3K27Ac of PC-3 cells (EC50 of 37 nM). CBP/p300-IN-12 forms a covalent adduct with C1450.