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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. -
GSPT1/BRD4 Degrader
DP-15 is a targeted degrader for GSPT1 and BRD4, demonstrating DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits potent anti-proliferative effects against acute myeloid leukemia (AML) and non-Hodgkin lymphoma (NHL) cells, with IC50 values in the nanomolar range. Additionally, DP-15 induces G1 phase cell cycle arrest and promotes apoptosis in MOLM13 cells. In vivo studies have shown its effective anti-leukemia activity in MOLM-13 xenograft mouse models, supporting its potential application in cancer research. -
HDAC/JAK/BRD4 Inhibitor
HDAC/JAK/BRD4-IN-1 is a potent inhibitor targeting histone deacetylases (HDAC), Janus kinases (JAK), and bromodomain-containing protein 4 (BRD4). This compound demonstrates significant anti-proliferative effects and promotes apoptosis in MDA-MB-231 breast cancer cells. Additionally, HDAC/JAK/BRD4-IN-1 exhibits promising anticancer activity in vivo, making it a valuable tool for research in cancer therapeutics and the study of epigenetic and signaling pathways. -
SMARCA2 Degrader
A947 is a selective SMARCA2 proteolysis-targeting chimera (PROTAC) that functions as a potent degrader of SMARCA2. It exhibits a binding affinity to the SMARCA2 bromodomain with a Kd value of 93 nM, establishing its effectiveness in mediating targeted protein degradation. This compound has significant applications in cancer research, facilitating studies on the role of SMARCA2 in tumorigenesis and potential therapeutic interventions. -
CBP Inhibitor
DC-CPin711 is a potent and selective inhibitor of the CREB-binding protein (CBP) bromodomain, demonstrating an IC50 of 0.0626 μM. This compound effectively induces apoptosis and arrests the cell cycle at the G1 phase, making it a valuable tool for research into cellular proliferation and death pathways. Its specificity for CBP enhances its utility in investigating the role of bromodomain-containing proteins in various biological processes and diseases. -
BRD4 Inhibitor
BRD4 Inhibitor-18 is a potent inhibitor of the Bromodomain-containing protein 4 (BRD4), exhibiting an IC50 value of 110 nM. This compound features a hydrophobic acetylcyclopentanyl side chain and significantly reduces the proliferation of MV-4-11 leukemia cells, which are characterized by high BRD4 expression. In addition, BRD4 Inhibitor-18 promotes apoptosis and induces G0/G1 cell cycle arrest, making it a valuable tool for research into cancer therapeutics and cell cycle regulation. -
CDK6/BRD4 Inhibitor
BC13 is a selective inhibitor of CDK6 and BRD4, demonstrating IC50 values of 234 nM and 36 nM, respectively. This compound exhibits notable antiproliferative effects, facilitating cell apoptosis and inducing DNA damage in various cell lines. Additionally, BC13 has been shown to elevate reactive oxygen species (ROS) levels, making it a valuable tool for research in cancer biology and therapeutic development targeting cell cycle regulation. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-17 is a potent protein degrader targeting bromodomain-containing protein 4 (BRD4). It exhibits IC50 values of 29.54 nM for BRD4 (BD1) and 3.82 nM for BRD4 (BD2). This compound effectively inhibits G2/M cell cycle progression, leading to decreased expression of Cyclin B1, and significantly induces apoptosis in MV-4-11 cells. PROTAC BRD4 Degrader-17 is valuable for research applications focused on cancer cell biology and the development of targeted degraders in therapeutic strategies. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-5 is a potent inhibitor targeting both PLK1 and BRD4, exhibiting IC50 values of 0.3 nM and 60.8 nM, respectively. This compound effectively induces cell cycle arrest in the S phase and promotes apoptosis in MV4-11 cells in a dose-dependent manner. PLK1/BRD4-IN-5 is a valuable tool for cancer research, facilitating studies on mechanisms of tumorigenesis and therapeutic responses. -
p300/CBP Inhibitor
DCH36_06 is a selective inhibitor of the p300/CBP acetyltransferases, exhibiting IC50 values of 0.6 μM for p300 and 3.2 μM for CBP. This compound induces hypoacetylation of histone H3 at lysine 18 (H3K18) in leukemic cells, contributing to its anti-tumor properties. DCH36_06 is useful for investigating the role of p300/CBP in transcriptional regulation and potential therapeutic applications in cancer research. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4 degrader-38 is a dual-targeted PROTAC degrader designed to promote the ubiquitination and subsequent degradation of the SMARCA2 and SMARCA4 proteins. With DC50 values of 3.0 nM and 4.0 nM for SMARCA2 and SMARCA4 respectively, this compound effectively blocks the G0/G1 cell cycle phase and induces apoptosis in cancer cells. It has significant potential for use in research focused on acute myeloid leukemia (AML) and other malignancies involving these chromatin remodeling factors. -
PROTAC FLT3/JAK2/BRD4 Degrader
PROTAC FLT3/JAK2/BRD4 Degrader-1 is a potent PROTAC degrader that simultaneously targets FLT3, JAK2, and BRD4, exhibiting DC50 values of 5.23 nM, 0.678 nM, and 1.17 nM, respectively. It demonstrates significant antiproliferative activity against MV4;11 cells with an IC50 of 0.79 nM, inducing apoptosis in these cells. Additionally, PROTAC FLT3/JAK2/BRD4 Degrader-1 shows marked anti-tumor efficacy in MV4;11 xenograft models in NOD SCID mice. This compound is valuable for research into acute myeloid leukemia (AML). -
BRD4 Inhibitor
BRD4-IN-41 is a selective BRD4 inhibitor that targets the acetyl-lysine binding site with an IC50 of 34 nM. In addition to inhibiting BRD4, it also affects multiple kinases, including JAK2, FLT3, and NTRK3, with IC50 values ranging from 0.9 nM to 43 nM. This compound downregulates c-MYC, lowers phosphorylated STAT3 levels, and induces G1 cell cycle arrest and apoptosis, demonstrating significant anti-cancer activity. BRD4-IN-41 is particularly relevant for research on hematological malignancies such as multiple myeloma and acute myeloid leukemia. -
FLT3/JAK2/BRD4 Ligand
FLT3/JAK2/BRD4 ligand-1 is a specific ligand for the FLT3, JAK2, and BRD4 proteins. This compound facilitates the design and synthesis of proteolysis-targeting chimeras (PROTACs), specifically PROTAC FLT3/JAK2/BRD4 Degrader-1. It demonstrates potential applications in targeted protein degradation and cancer research, enabling innovative therapeutic strategies against malignancies associated with these targets. -
BD2-selective BET Inhibitor
BET-IN-23 is a BD2-selective BET inhibitor with a reported IC50 of 2.9 nM. This compound exhibits anticancer properties, effectively inhibiting the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 cell cycle arrest and apoptosis in vitro. BET-IN-23 serves as a valuable tool for research in cancer biology, specifically in the study of leukemia and other malignancies involving BET protein dysregulation. -
CBP Bromodomain Inhibitor
Ischemin is a selective inhibitor of the CBP bromodomain, effectively disrupting the interaction between p53 and CBP, consequently reducing transcriptional activity. With an IC50 value of 5 µM, Ischemin demonstrates the ability to inhibit p53-induced p21 activation. Additionally, it has been shown to protect against apoptosis in ischemic cardiomyocytes. This reagent is valuable for investigating mechanisms involved in cardiovascular diseases, particularly myocardial ischemia. -
PARP1/BRD4 Inhibitor
PARP1/BRD4-IN-1 is a selective inhibitor targeting both PARP1 and BRD4, demonstrating IC50 values of 49 nM and 202 nM, respectively. This compound effectively represses the expression and activity of these proteins, leading to synergistic inhibition of malignant pancreatic cancer cell growth. PARP1/BRD4-IN-1 is a valuable tool for exploring therapeutic strategies in cancer research, particularly in the context of PARP and BRD4 signaling pathways. -
BRD4 Inhibitor
BET-IN-20 is a selective BRD4 bromodomain inhibitor with an IC50 of 1.9 nM. This compound demonstrates significant anticancer activity by inducing apoptosis in acute myeloid leukemia (AML) cells and effectively arresting the cell cycle in the G0/G1 phase. Additionally, BET-IN-20 inhibits c-Myc and CDK6, while enhancing PARP cleavage, making it a valuable tool for cancer research and therapeutic development. -
BRD4 PROTAC Degrader
NEP162 is a potent BRD4 PROTAC degrader, demonstrating DC50 values of 1.2 and 1.6 μM in SW480 and U2OS cell lines, respectively. It exhibits significant antiproliferative activity, effectively inhibiting tumor growth and promoting apoptosis in various cancer models. NEP162 is particularly relevant for research applications in osteosarcoma, colorectal cancer, and non-small cell lung cancer. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-16 is an effective degrader specifically targeting BRD4, with IC50 values of 34.58 nM for BRD4 (BD1) and 40.23 nM for BRD4 (BD2). This compound is known to significantly reduce Cyclin B1 expression, which is associated with G2/M cell cycle progression. Additionally, PROTAC BRD4 Degrader-16 effectively induces apoptosis in MV-4-11 cells, contributing to its potential utility in cancer research and therapeutic applications. -
PARP1/BRD4 Inhibitor
PARP1/BRD4-IN-2 is a selective inhibitor of PARP1 and BRD4, demonstrating IC50 values of 197 nM and 238 nM, respectively. This compound effectively impedes DNA damage repair mechanisms, inhibits the G0/G1 cell cycle transition, and induces apoptotic cell death. PARP1/BRD4-IN-2 has shown significant anti-tumor efficacy in the MDA-MB-468 xenograft mouse model, making it a valuable tool for research in triple-negative breast cancer (TNBC). -
Dual PLK1/BET Inhibitor
WNY0824 is a dual inhibitor targeting Polo-like kinase 1 (PLK1) and the Bromodomain and Extra-Terminal (BET) protein family. It demonstrates potent inhibitory activity, with IC50 values of 22 nmol/L for PLK1 and varying efficacy against BRD2, BRD3, BRD4, and BRDT. WNY0824 induces cell cycle arrest and apoptosis by disrupting AR- and MYC-mediated transcriptional processes, making it valuable for research in cancer biology. Furthermore, it has shown effectiveness in inhibiting tumor growth in Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenograft models, highlighting its potential in overcoming treatment resistance. -
BRD4 PROTAC Degrader
PROTAC BRD4 Degrader-21 is a targeted PROTAC that degrades the BRD4 protein through the induction of ubiquitination, achieving an IC50 of 59 nM. This compound effectively leads to BRD4 degradation via the proteasome pathway, and demonstrates moderate affinity for recombinant HSP90α with an IC50 range of 100-1000 nM. In preclinical studies, PROTAC BRD4 Degrader-21 has been shown to induce apoptosis in cancer cells and inhibit tumor growth in xenograft mouse models, making it a valuable tool for research into acute myeloid leukemia and diffuse large B-cell lymphoma. -
CBP/β-catenin Antagonist
C-82 is a selective antagonist of CBP/β-catenin interaction, designed to inhibit the binding of β-catenin to CBP while promoting its association with p300. This compound effectively modulates the Wnt signaling pathway, making it a valuable tool for research in cancer biology and developmental processes. C-82 serves as an important reagent for studies investigating the role of β-catenin in transcriptional regulation and related disease mechanisms. -
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.

