Catalog No.
Product Name
Application
Product Information
Citations
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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.- Kevin Bohm, .et al. , Arch Pharm (Weinheim), 2023, Jul;356(7):e2200661 PMID: 37196427
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CBP/beta-catenin antagonist
PRI-724 is the second-generation, potent and specific inhibitor of CBP/β-Catenin complex, and a modulator of the β-Catenin dependent canonical Wnt signaling pathway in cancer stem cells.
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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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.- Thibaud Reyser, .et al. , Pharmaceutics, 2023, Oct 10;15(10):2440 PMID: 37896200
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p300/CBP inhibitor
C646 is a selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM).- Thibaud Reyser, .et al. , Pharmaceutics, 2023, Oct 10;15(10):2440 PMID: 37896200
- Zhifeng Zhang, .et al. , PLoS One, 2017, 12(10): e0186900 PMID: 29049411
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p300/CBP bromodomain inhibitor
Inobrodib (CCS-1477) is a potent p300/CBP bromodomain inhibitor.
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p300/CBP histone acetyltransferase inhibitor
P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor. -
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. -
NAT10 inhibitor
Remodelin Hydrobromide is a potent acetyl-transferase NAT10 inhibitor. -
KAT5 (Tip60), p300/PCAF inhibitor
Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. -
Tip60 HAT Inhibitor
TH1834 dihydrochloride is a selective inhibitor of Tip60 (KAT5), a histone acetyltransferase involved in the regulation of gene expression and DNA repair. This compound has been shown to induce apoptosis and enhance DNA damage in breast cancer cells, demonstrating its potential as a therapeutic agent in cancer research. Importantly, TH1834 dihydrochloride does not inhibit the activity of the structurally related histone acetyltransferase MOF, suggesting a targeted approach in modulating histone acetylation and cellular responses. -
p300 Activator
CTB is a potent activator of the p300 histone acetyltransferase, known for its role in regulating gene expression through histone acetylation. This compound has demonstrated the ability to induce apoptosis in MCF-7 breast cancer cells, making it a valuable tool for research into cancer biology and therapeutic approaches targeting acetylation pathways. Its specificity for p300 highlights its potential in studies of transcriptional regulation and chromatin dynamics. -
Tip60 HAT Inhibitor
TH1834 is a selective inhibitor of the Tip60 (KAT5) histone acetyltransferase (HAT). This compound has demonstrated the ability to induce apoptosis and enhance DNA damage in breast cancer cells. Notably, TH1834 does not interfere with the activity of the related MOF HAT, making it a valuable tool for investigating the role of Tip60 in cancer biology and exploring potential therapeutic applications. -
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. -
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. -
histone acetyltransferase Gcn5 inhibitor
Butyrolactone 3 (MB-3) is a specific small-molecule inhibitor of the histone acetyltransferase Gcn5, exhibiting an IC₅₀ of 100 μM and binding affinity comparable to that of its natural substrate, histone H3. It displays weak inhibitory activity against CBP (IC₅₀ = 0.5 mM), indicating high selectivity for Gcn5. By modulating histone acetylation and epigenetic regulation, Butyrolactone 3 serves as a valuable research tool for exploring the roles of Gcn5 in cancer, metabolic disorders, autoimmune diseases, and neurological conditions. -
p300/CBP inhibitor
NEO2734 (EP31670) is an orally active dual inhibitor of p300/CBP and BET bromodomains, with IC₅₀ values of <30 nM for both targets. It is effective in both SPOP-mutant and wild-type prostate cancer models. -
CBP/p300 inhibitor
CBP/p300-IN-8 is a potent inhibitor of the CBP/p300 family of bromodomains, with an IC₅₀ of 0.01–0.1 µM for CBP. It also inhibits BRD4 activity with significantly lower potency (IC₅₀ = 1–1000 µM). -
p300/CBP inhibitor
CBP/p300-IN-12 is a potent and selective covalent inhibitor of the histone acetyltransferases p300 and CBP, with an IC₅₀ of 166 nM for p300. It reduces H3K27Ac levels in PC-3 cells with an EC₅₀ of 37 nM and forms a covalent adduct with cysteine residue C1450. -
KIX-KID interaction inhibitor
Naphthol AS-E is a potent, cell-permeable inhibitor of the KIX-KID interaction. It binds directly to the KIX domain of CBP with a Kd of 8.6 μM and inhibits the interaction between the KIX domain and the KID domain of CREB with an IC₅₀ of 2.26 μM. Naphthol AS-E is applicable in cancer research. -
PROTAC CBP/p300 Degrader
CBPD-409 is an orally active PROTAC degrader targeting CBP/p300, with a DC₅₀ of 0.2–0.4 nM. It shows potent antiproliferative activity in AR⁺ prostate cancer cell lines (VCaP, LNCaP, 22Rv1) with IC₅₀ values of 1.2–2.0 nM and demonstrates significant antitumor efficacy. -
PROTAC CBP/p300 degrader
JET-209 is a potent PROTAC degrader targeting CBP and p300, with DC₅₀ values of 0.05 nM and 0.2 nM, respectively. It is composed of lenalidomide, a linker, and the bromodomain inhibitor GNE-207. JET-209 is a valuable tool for cancer research involving epigenetic regulation. -
PROTAC EP300 Degrader
JQAD1 is a CRBN-dependent PROTAC selectively targeting EP300 for degradation. It effectively reduces EP300 protein levels and H3K27ac histone acetylation, resulting in apoptosis. JQAD1 is a valuable tool for investigating EP300 function and epigenetic regulation in cellular processes. -
EP300/CBP HAT Inhibitor
CBP/p300-IN-17 is a potent inhibitor of the EP300 and CBP histone acetyltransferases (HATs), exhibiting IC50 values of 0.18 µM and 0.69 µM for EP300 and LK2 H3K27, respectively. This compound demonstrates significant biological activity in modifying histone acetylation, making it valuable for research in epigenetics, cancer biology, and transcriptional regulation. Its selective inhibition of EP300 and CBP provides a critical tool for investigating their roles in various cellular processes and disease states. -
P300 HAT Inhibitor
P300-IN-6 is an orally bioavailable inhibitor targeting the histone acetyltransferase p300 HAT domain, exhibiting a human IC50 of 7 nM. This compound effectively suppresses c-Myc expression and reduces acetylation levels of histones H3K18 and H3K27, leading to inhibition of cancer cell proliferation. P300-IN-6 demonstrates significant antitumor activity in xenograft mouse models, making it a valuable tool for investigating therapeutic strategies in multiple myeloma research. -
HAT Inhibitor
SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor with specific activity against various HAT enzymes. This compound plays a critical role in the regulation of gene expression and cellular processes by modulating acetylation levels on histones. SYY-B085-1 is utilized in research to explore the effects of HAT inhibition in cancer biology and epigenetic regulation. Its unique mechanism offers valuable insights for studies focused on transcriptional modulation and potential therapeutic interventions. -
p300/CBP HAT Inhibitor
CBP/p300-IN-19 is a potent inhibitor of the histone acetyltransferase (HAT) activity of p300 and CBP, exhibiting IC50 values of 1.4 µM and 2.2 µM, respectively, while showing limited inhibition of PCAF and Myst3 (>100 µM). This compound demonstrates significant anti-tumor activity, making it valuable for research into cancer biology and epigenetic regulation. Its ability to selectively target p300/CBP HAT provides a useful tool for investigating the role of acetylation in various cellular processes and disease states. -
HAT Inhibitor
DS-9300 is a selective inhibitor of the EP300/CBP histone acetyltransferases (HATs) with a potent IC50 value of 28 nM. This compound demonstrates significant anticancer activity and is applicable in prostate cancer research, providing valuable insights into the mechanisms of acetylation in tumorigenesis. DS-9300 serves as a critical tool for studying the role of HATs in cancer progression and therapeutic resistance.
