CBP/p300 Inhibitor

CBP/p300 Inhibitors (34):

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 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-13823

C646	Inhibitor	99.78%
C646 is a selective and competitive histone acetyltransferase p300 inhibitor with K_i of 400 nM, and is less potent for other acetyltransferases.

HY-15826

SGC-CBP30	Inhibitor	99.83%
SGC-CBP30 is a potent and highly selective CBP/p300 bromodomain (K_ds 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-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-N2020

Anacardic Acid	Inhibitor	98.86%
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-15887

MG 149	Inhibitor	99.86%
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).

HY-124696

PU139	Inhibitor	99.14%
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-136938

NEO2734	Inhibitor	99.79%
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-136285

CPI-1612	Inhibitor	99.85%
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-19999A

PF-CBP1 hydrochloride	Inhibitor	99.99%
PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC₅₀ of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1β, IL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.

HY-132197

CBP/p300-IN-12	Inhibitor	99.70%
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.

HY-100734

Histone Acetyltransferase Inhibitor II	Inhibitor	99.01%
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-120028

GNE-207	Inhibitor
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-131035

Lys-CoA TFA	Inhibitor	99.42%
Lys-CoA TFA is a selective p300 histone acetyltransferase (HAT) inhibitor (IC₅₀=50-500 nM). Lys-CoA TFA displays >100-fold selectivity for p300 over PCAF (IC₅₀=200 μM). Lys-CoA TFA inhibits p300 HAT activity-dependent transcriptional activation.

HY-104068

Naphthol AS-E	Inhibitor	≥98.0%
Naphthol AS-E is a potent and cell-permeable inhibitor of KIX-KID interaction. Naphthol AS-E directly binds to the KIX domain of CBP (K_d:8.6 µM), blocks the interaction between the KIX domain and the KID domain of CREB with IC₅₀ of 2.26 µM. Naphthol AS-E can be used for cancer research.

HY-100697

TPOP146	Inhibitor	98.98%
TPOP146 is a selective CBP/P300 benzoxazepine bromodomain inhibitor with K_d values of 134 nM and 5.02 μM for CBP and BRD4.

HY-128875

CBP/p300-IN-10	Inhibitor	98.69%
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.

HY-112610

CF53	Inhibitor	99.78%
CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K_i of <1 nM, K_d 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, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.

HY-139149

NiCur	Inhibitor	99.11%
NiCur is a potent and selective CBP histone acetyltransferase (HAT) inhibitor with an IC₅₀ value of 0.35 μΜ. NiCur, which blocks CBP HAT activity and downregulates p53 activation upon genotoxic stress. NiCur can be used for performing mechanistic studies without affecting the expression of target proteins.

HY-110263

EML 425	Inhibitor	98.16%
EML425 is a potent and selective CREB binding protein (CBP)/p300 inhibitor with IC₅₀s of 2.9 and 1.1 μM, respectively.

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