Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC p300/CBP Degrader
dCBP-1 is a potent and selective heterobifunctional PROTAC degrader of p300/CBP, utilizing a cereblon ligand for E3 ligase recruitment. It effectively eliminates oncogenic enhancer activity driving MYC expression and demonstrates strong cytotoxicity against multiple myeloma cells, making it a valuable tool for epigenetic and cancer research. -
PROTAC BRD4 Degrader
GNE-987 is a highly potent PROTAC degrader of BRD4, composed of a BET inhibitor, a von Hippel-Lindau (VHL) ligand, and a ten-methylene linker. It binds both BD1 and BD2 bromodomains of BRD4 with low nanomolar affinity (IC₅₀ = 4.7 and 4.4 nM) and induces BRD4 degradation with a DC₅₀ of 0.03 nM in EOL-1 AML cells. GNE-987 is also suitable for use in PROTAC–Antibody Conjugates (PAC), making it a valuable tool for targeted protein degradation and epigenetic cancer research. -
PROTAC SMARCA2/SMARCA4 degrader
AU-15330 is a PROTAC degrader targeting the SWI/SNF chromatin remodeling ATPase subunits SMARCA2 and SMARCA4. It effectively suppresses tumor growth in prostate cancer xenograft models and enhances the therapeutic efficacy of the AR antagonist enzalutamide. AU-15330 also induces remission in castration-resistant prostate cancer models, demonstrating strong antitumor activity with a favorable safety profile. -
SMARCA2/SMARCA4/PBRM1 Degrader
ACBI1 is a potent and cooperative PROTAC degrader targeting SMARCA2, SMARCA4, and PBRM1, with DC₅₀ values of 6 nM, 11 nM, and 32 nM, respectively. It exhibits strong anti-proliferative activity and induces apoptosis, making it a valuable tool for studying chromatin remodeling and cancer therapeutics. -
SMARCA2/SMARCA4/PBRM1 Degrader
AU-24118 is an orally bioavailable PROTAC degrader targeting the mSWI/SNF chromatin remodeling complex ATPases SMARCA2 and SMARCA4, as well as PBRM1. It offers a powerful approach for modulating epigenetic regulation and holds promise for the treatment of cancers driven by alterations in SWI/SNF complex components. -
PROTAC BRD9 Degrader
CFT8634 is an orally bioavailable PROTAC that targets the E3 ubiquitin ligase CRBN to degrade BRD9. This heterobifunctional molecule effectively inhibits the growth of tumor cells reliant on BRD9, making it a valuable tool for researching synovial sarcoma and SMARCB1-deficient solid tumors. CFT8634 facilitates targeted degradation through its unique binding properties, offering a strategic approach to investigate the role of BRD9 in SMARCB1-related cancers, including malignant rhabdoid tumors. -
PI3K/BRD4 Inhibitor
PI3Kα-IN-28 is a potent dual-target inhibitor of PI3K and BRD4. This compound effectively suppresses cell proliferation in various cancer cell lines, including KYSE180 and KYSE450, while also inhibiting migration and colony formation. Additionally, PI3Kα-IN-28 induces G0/G1 phase cell cycle arrest and promotes cellular senescence by enhancing the proportion of senescent cells. Mechanistically, it decreases the levels of p-AKT and c-Myc, while activating the AMPK-p27 pathway, making it a valuable tool for cancer research, particularly in esophageal cancer studies. -
BET/HDAC Inhibitor
TW9 is a potent dual inhibitor that targets bromodomain and extraterminal (BET) proteins and histone deacetylases (HDAC) with KDs of 0.069 μM and 0.231 μM for BRD4(1) and BRD4(2), respectively, and an IC50 of 0.29 μM for HDAC1. This compound is a novel derivative of the BET inhibitor (+)-JQ1 and the class I HDAC inhibitor CI994. TW9 demonstrates significant anti-tumor activity in pancreatic ductal adenocarcinoma (PDAC) and enhances the efficacy of the chemotherapeutic agent Gemcitabine, making it a valuable tool for cancer research applications. -
CBP/EP300 Inhibitor
CBP/EP300 bromodomain receptor-IN-1 is a selective inhibitor of the CBP/EP300 bromodomain. This compound demonstrates high-affinity binding to bromodomain-containing proteins at nanomolar concentrations. Its primary application lies in research focused on epigenetic regulation and oncogenesis, making it a valuable tool for studying gene expression modulation and therapeutic interventions in cancer biology. -
BRD4/CBP/p300 Inhibitor
CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor that specifically targets the bromodomain and extraterminal (BET) family members BRD4, as well as the acetyltransferases CBP and p300. This compound functions by competitively binding to the functional domains of these proteins, preserving critical interactions. CBP/p300/BRD4 ligand-1 is suitable for the development of dual-target PROTAC degraders, making it valuable for research in prostate cancer and various other malignancies. -
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/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. -
EP300/CBP Inhibitor
EP300/CBP-IN-1 is a highly selective inhibitor targeting the EP300 and CBP bromodomain proteins, exhibiting IC50 values of 2.3 nM and 2.1 nM for CBP and EP300, respectively. This compound demonstrates significant anti-proliferative effects on CWR22RV1 prostate cancer cells, making it a valuable tool for research in cancer biology and epigenetic regulation. Its application extends towards elucidating the roles of EP300 and CBP in various cellular processes and disease states. -
CBP/p300 Inhibitor
CBP/p300 Ligand 3 is a selective inhibitor targeting the CBP/p300 proteins, which function as histone acetyltransferases (HATs). By binding to specific domains within CBP/p300, this compound effectively inhibits their enzymatic activity and modulates interactions with transcription factors. This inhibition alters chromatin structure and gene expression, making CBP/p300 Ligand 3 a valuable tool for studying the role of CBP/p300 in various biological processes, including cancer progression and neurodegenerative diseases, where dysregulation of CBP/p300 is implicated. -
CBP/p300 Inhibitor
PU141 is a selective inhibitor of the histone acetyltransferases CBP and p300. This compound induces cellular histone hypoacetylation, leading to significant inhibition of cell growth in various neoplastic cell lines derived from multiple tissue types. PU141 is primarily utilized in cancer research to explore mechanisms of transcriptional regulation and therapeutic interventions. -
p300/CBP HAT Inhibitor
CBP/p300-IN-19 hydrochloride is a selective inhibitor of the histone acetyltransferases (HAT) p300 and CBP, exhibiting IC50 values of 1.4 µM and 2.2 µM, respectively. It demonstrates significant antitumor activity, making it a valuable tool for cancer research. This compound can be applied in studies investigating the roles of acetylation in gene regulation and cell proliferation, as well as in the development of targeted therapies. -
PROTAC p300/CBP Degrader
QC-182 is a potent PROTAC degrader targeting p300/CBP, facilitating the degradation of these proteins. It effectively reduces p300 protein levels in SK-HEP-1 cells, with a DC50 of 93 nM. Additionally, QC-182 demonstrates significant growth inhibition in SK-HEP-1 and JHH7 cell lines, with IC50 values of 0.733 μM and 0.477 μM, respectively. This reagent is valuable for research focused on hepatocellular carcinoma (HCC). -
CBP HAT Inhibitor
NiCur is a potent and selective inhibitor of CBP histone acetyltransferase (HAT) with an IC50 value of 0.35 μM. By targeting CBP HAT activity, NiCur effectively downregulates p53 activation in response to genotoxic stress. This compound is suitable for mechanistic studies, allowing researchers to investigate pathways involving histone acetylation without altering the expression of target proteins. -
P300/CBP Inhibitor
Pocenbrodib is a potent inhibitor of the P300/CBP transcriptional coactivators. By blocking the function of these coactivators, Pocenbrodib effectively inhibits the acetylation of both histone and non-histone proteins, impacting gene expression regulation. This compound is particularly valuable for research into castration-resistant prostate cancer and other cancer types that are associated with dysregulated acetylation processes. -
p300/CBP Inhibitor
CBP/p300-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase, demonstrating an IC50 value of 18.8 nM. This compound serves as a valuable tool for studying the role of histone acetylation in gene regulation and various biological processes. Its application is significant in cancer research and therapeutic development, where modulation of acetylation pathways is of interest. -
p300/CBP HAT Inhibitor
B026 is a selective and potent inhibitor of the p300/CBP histone acetyltransferase (HAT) with IC50 values of 1.8 nM for p300 and 9.5 nM for CBP. This compound exhibits significant anticancer activity against androgen receptor-positive (AR+) prostate cancer cell lines, making it a valuable tool for research in cancer biology and epigenetic regulation. Its oral bioavailability enables easy administration for in vivo studies targeting p300/CBP-mediated pathways. -
CBP/p300 Inhibitor
CBP/p300-IN-20 is a selective inhibitor of the p300/CBP transcriptional coactivators, displaying a high potency with a pIC50 of 10.1 for p300. This compound is useful in cancer research, providing insights into the role of p300/CBP in oncogenic transcriptional regulation and potential therapeutic interventions. Its specificity towards p300 allows for targeted studies in related signaling pathways and tumor biology. -
CBP/EP300 Inhibitor
CBP/p300-IN-14 is a highly potent inhibitor of CBP/EP300, a lysine acetyltransferase, with an IC50 of 3.3 nM. This compound is utilized to study the role of CBP/EP300 in various biological processes, including transcriptional regulation and cellular signaling pathways. Its application is critical in research focused on cancer, metabolic disorders, and other diseases where histone acetylation plays a significant role. -
EP300/CBP HAT Inhibitor
CBP/p300-IN-18 is a potent inhibitor of the EP300 and CBP histone acetyltransferases (HATs), exhibiting IC50 values of 0.056 µM and 0.46 µM for EP300 and LK2 H3K27, respectively. This compound serves as a valuable tool for investigating the role of histone acetylation in various biological processes and disease states. It is particularly useful in studies focused on chromatin remodeling, gene expression, and potential therapeutic applications in cancer and other disorders associated with dysregulated acetylation. -
CBP/p300 Inhibitor
CBP/p300-IN-21 is a selective inhibitor of the CBP/p300 transcriptional co-activators, exhibiting IC50 values of 0.07 μM for p300 and 1.755 μM for CBP. This compound effectively reduces the acetylation level of histone H3 at lysine 18 (H3K18Ac), implicating a potential role in modulating gene expression. Furthermore, CBP/p300-IN-21 has demonstrated efficacy in inhibiting the growth of 4T1 tumors in murine models, highlighting its relevance in cancer research and therapeutic applications. -
CBP/p300 Inhibitor
CBP/p300-IN-15 is a potent inhibitor of the CBP/p300 coactivators, exhibiting IC50 values of 2.50 nM for p300 and 28.0 nM for CBP. This compound demonstrates significant biological activity in ovarian cancer cell lines, with EC50 values of 0.865 μM for OVCAR-3 and 2.71 μM for A2780. CBP/p300-IN-15 is a valuable tool for investigating the role of CBP/p300 in ovarian cancer research and could provide insights into therapeutic strategies targeting these coactivators. -
BRD4/CBP/p300 PROTAC Degrader
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader that specifically targets BRD4, CBP, and p300, achieving DC50 values of 8.8 pM, 6.55 nM, and 1.05 nM, respectively. This compound promotes CRBN- and proteasome-mediated degradation of BRD4 and CBP/p300, leading to the downregulation of c-Myc and acetyl-H3K27, and inducing apoptosis. It exhibits significant antiproliferative and antitumor effects, demonstrated by tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 is a valuable tool for research focused on prostate and colorectal cancer. -
EP300/CBP Inhibitor
CPI-1612 is a potent, orally active inhibitor of EP300/CREB-binding protein (CBP) histone acetyltransferase, exhibiting an IC50 of 8.1 nM for EP300 HAT. This compound demonstrates significant anticancer activity, making it a valuable tool for cancer research. Its ability to modulate acetylation pathways enables investigations into epigenetic regulation and therapeutic strategies targeting malignancies. -
EP300/CBP Inhibitor
DS17701585 is a selective inhibitor of EP300 and CBP, demonstrating IC50 values of 0.040 µM for CBP, 0.15 µM for EP300, 0.45 µM for H3K27, and 0.70 µM for SOX2. This compound is orally active and is primarily utilized in cancer research to explore the roles of histone acetyltransferases and related transcriptional regulators in tumorigenesis. Its specificity and potency make it a valuable tool for investigating the epigenetic mechanisms underlying various cancers. - Phoenixin-20 (PNX-20) is a bioactive peptide with hormone-like actions in vertebrates, and can stimulates hypothalamo-pituitary-gonadal hormones and regulate reproductive processes in mammals. Phoenixin-20 promotes neuronal mitochondrial biogenesis via CREB-PGC-1α pathway. Phoenixin-20 has anxiolytic effect.
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BRD2/BRD4 Inhibitor
KB-0118 is a selective inhibitor of the bromodomains BRD2 and BRD4, exhibiting Kd values of 36.7 μM and 47.4 μM, respectively. This orally active compound effectively inhibits the production of pro-inflammatory cytokines, such as TNF, IL-1β, and IL-23a, and selectively reduces Th17 cell differentiation. The compound modulates Th17-driven inflammatory processes through the epigenetic suppression of BRD4, leading to decreased expression of STAT3 and other target genes. KB-0118 demonstrates potential therapeutic benefits in models of inflammatory bowel disease (IBD). -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-35 is a selective degrader targeting SMARCA2 with a DC50 potency of less than 0.1 μM. This compound exhibits significant anticancer activity by regulating cell proliferation and growth, primarily through mechanisms of cell cycle arrest and inhibition of DNA replication in SMARCA4-deleted cancer cells. It is a valuable tool for research focused on targeted protein degradation and its implications in cancer therapy. -
BAZ2A Bromodomain Inhibitor
4-Chloro-N-methylpicolinamide is a selective inhibitor of the BAZ2A bromodomain, exhibiting a Kd of over 500 μM. This compound interacts through a weak hydrogen bond with the carbonyl oxygen of Pro1817, offering insights into bromodomain-targeted therapies. It is applicable in the study of invasive prostate cancer, contributing to research focused on cancer biology and therapeutic strategies. -
PB1(5)/SMARCA2/4 Inhibitor
SGC-SMARCA-BRDVIII is a potent and selective inhibitor targeting SMARCA2/4 and PB1(5) with dissociation constants (Kds) of 35 nM, 36 nM, and 13 nM, respectively. This compound also demonstrates inhibitory activity against PB1(2) and PB1(3), with Kds of 3.7 μM and 2.0 μM, respectively. SGC-SMARCA-BRDVIII effectively inhibits adipogenesis in 3T3-L1 murine fibroblasts, making it a valuable tool for research in epigenetics and obesity-related studies. -
BRD4 Inhibitor
Biotinylated-JQ1 is a biotinylated derivative of JQ1 that selectively inhibits BRD4 by binding with high affinity to its bromodomain. This compound exhibits significant anti-proliferative activity in MM1.S multiple myeloma cells, with an EC50 value of 0.4 μM. Biotinylated-JQ1 is suitable for research applications targeting BRD4-mediated pathways in cancer biology and epigenetic regulation studies. -
BRD9 Degradation Agent
dBRD9 is a targeted proteolysis-tethering compound that selectively induces the degradation of BRD9. By enhancing bromodomain binding, dBRD9 demonstrates reduced binding activity across the entire BET family of proteins. This compound serves as a valuable tool for researchers studying the role of BRD9 in various biological processes and its implications in diseases such as cancer. -
BET Inhibitor
Trotabresib is a reversible and orally active Bromodomain and Extra-Terminal (BET) inhibitor. It demonstrates significant inhibition of BET proteins, which play a crucial role in regulating gene expression associated with cancer progression. Trotabresib is primarily utilized in research focused on advanced solid tumors, providing insights into potential therapeutic strategies for tackling malignancies driven by aberrant transcriptional regulation. -
SMARCA4/SMARCA2/PBRM1 Inhibtor
GNE-064 is a selective inhibitor targeting the bromodomains of SMARCA4, SMARCA2, and PBRM1. This compound exhibits an IC50 of 0.035 μM for SMARCA4 and an EC50 of 0.10 μM for SMARCA2, demonstrating potent inhibition. With binding affinities (Kd) of 0.01 μM, 0.016 μM, 0.018 μM, and 0.049 μM for SMARCA4, SMARCA2, and the two bromodomains of PBRM1 respectively, GNE-064 serves as an effective chemical probe for investigating chromatin regulation and related biological processes in research settings. -
BRD4 Inhibitor
MS645 is a bivalent inhibitor targeting the bromodomains of BRD4 with a Ki value of 18.4 nM for BRD4-BD1/BD2. This compound effectively spatially constrains bivalent inhibition, leading to sustained repression of BRD4 transcriptional activity in solid tumor cells. MS645 is suitable for research applications exploring the regulation of gene expression and potential therapeutic strategies in oncology. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-5 is a selective inhibitor targeting the bromodomain of the PBRM1 protein, demonstrating Kd values of 1.5 μM for PBRM1-BD2 and 3.9 μM for PBRM1-BD5. It exhibits an IC50 of 0.26 μM for PBRM1-BD2, effectively disrupting the interaction between PBRM1 and acetylated histone peptides within the PBAF complex in cell lysates. This compound is valuable for investigating the role of PBRM1 in cancer biology and may contribute to the development of novel anticancer therapeutics. -
Pan-BD2 BET Inhibitor
GSK973 is a highly selective pan-BD2 bromodomain and extraterminal (BET) inhibitor that targets the second bromodomains of the BET protein family. It exhibits potent inhibitory activity with a pIC50 of 7.8 for BRD4 BD2 and notable selectivity, showing a 1600-fold preference for BRD4 BD2 over BRD4 BD1. Additionally, GSK973 demonstrates efficacy against BRD2 BD2, BRD3 BD2, and BRDT BD2, with pIC50 values ranging from 7.4 to 7.8. This compound is valuable for research applications focused on epigenetic regulation and BET protein functions in various disease models, including cancer. -
BET Inhibitor
PROTAC BRD4 ligand-1 functions as a potent inhibitor of Bromodomain and Extra-Terminal (BET) proteins, targeting the BRD4 protein. This compound is utilized in research applications aimed at investigating BET inhibition and its implications in various cancers and inflammatory diseases. By facilitating the targeted degradation of BRD4, PROTAC BRD4 ligand-1 serves as a valuable tool for studying the role of BET proteins in gene regulation and cellular processes. -
BRD4 BD1 Inhibitor
ZL0590 is a potent, orally bioavailable inhibitor of the bromodomain-containing protein 4 (BRD4) BD1 with an IC50 value of 90 nM for human BRD4 BD1. This compound demonstrates significant anti-inflammatory properties, effectively reducing mucosal inflammation in animal models of inflammatory bowel disease and restoring tissue architecture. ZL0590 is suitable for research applications targeting inflammatory diseases, particularly those associated with the gastrointestinal tract. -
BD2-Selective BET Inhibitor
RVX-297 is a selective bromodomain inhibitor targeting the BD2 domain of BET proteins. This compound demonstrates potent inhibition with IC50 values of 0.08 μM for BRD2, 0.05 μM for BRD3, and 0.02 μM for BRD4 at the BD2 site. RVX-297 effectively suppresses inflammatory gene expression in various immune cell types and shows promise in models of acute inflammation and autoimmune disorders, making it a valuable tool for research in inflammatory diseases. -
BRD7/9 Inhibitor
BRD7-IN-1 is a selective inhibitor of the bromodomain-containing protein 7 (BRD7) and bromodomain-containing protein 9 (BRD9). This compound effectively disrupts BRD7/9 interactions and exhibits notable biological activity with DC50 values of 4.5 nM and 1.8 nM, respectively. BRD7-IN-1 serves as a valuable tool for research focused on understanding the roles of BRD7 and BRD9 in cellular processes and is applicable in studies related to epigenetic regulation and cancer therapy. -
Molecular Glue BRD4 Degrader
BRD4 degrader-1 is a monovalent, covalent molecular glue that specifically targets BRD4, a key regulator in various cellular processes. By engaging DCAF16, an E3 ubiquitin ligase, this compound facilitates the degradation of both long and short isoforms of BRD4 within the cellular context. Its mechanism of action makes BRD4 degrader-1 a valuable tool for research applications aimed at understanding and manipulating BRD4-related pathways in cancer and other diseases. -
BRD4 Degrader
MMH1 is a novel BRD4 molecular glue degrader that effectively recruits the CUL4 and DCAF16 ligases to the second bromodomain of BRD4 (BRD4BD2). This targeted degradation mechanism allows for the selective reduction of BRD4 levels, which is crucial for studying its role in various biological processes. MMH1 is particularly useful in research applications focusing on cancer biology and epigenetic regulation, enabling the exploration of therapeutic strategies targeting BRD4-associated pathways. -
BRD4 Ligand
BRD4 ligand 6 TFA is the trifluoroacetic acid (TFA) salt form of a potent BRD4 ligand, specifically designed for investigating the bromodomain and extraterminal (BET) family of proteins. This compound serves as a valuable building block for the synthesis of targeted protein degraders, including BRD4 PROTACs like PROTAC BRD4 Degrader-26. It is instrumental in research related to epigenetic regulation and cancer biology. -
BRD4 Degrader
BRD4 degrader-3 is a selective bromodomain-containing protein 4 (BRD4) degrader, showcasing potent activity with IC50 values of 15.5 nM and 12.3 nM for BRD4-BD1 and BRD4-BD2, respectively. This compound employs the PROTAC technology to facilitate targeted degradation of BRD4. Additionally, it features an alkyne functional group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for chemical biology applications in studying BRD4-related pathways and functions. -
BRD9 PROTAC Degrader
dBRD 9-A is a selective BRD9 PROTAC degrader that targets the E3 ubiquitin ligase CRBN for the near-complete degradation of BRD9. This compound disrupts BRD9 chromatin binding on a genome-wide scale, leading to downregulation of oncogenic transcriptional programs driven by SS18-SSX and the depletion of GBAF complex members from SS18-SSX complexes. dBRD 9-A also induces cell cycle arrest and promotes apoptosis in synovial sarcoma cells, making it a valuable tool for research focused on synovial sarcoma.
