Catalog No.
Product Name
Application
Product Information
Citations
-
BRD4 Inhibitor
BRD4-IN-10 is a selective inhibitor of Bromodomain-containing protein 4 (BRD4), exhibiting an IC50 of 13.5 nM. This compound demonstrates anti-inflammatory and anti-fibrotic activities, making it a valuable tool in studies related to renal fibrosis. It also possesses favorable metabolic stability and pharmacokinetic properties, enhancing its suitability for research applications in exploring BRD4-related pathways and therapeutic interventions. -
BRD4 Inhibitor
Bi-magnolignan is an inhibitor of BRD4, a key regulator involved in the recognition of acetylated lysines on histones and non-histone proteins. This compound has been shown to induce DNA damage and promote apoptosis in cancer cells, specifically inhibiting the proliferation of HCT116 cells with an IC50 value of 2.9 μM. Bi-magnolignan may serve as a valuable tool for elucidating the role of BRD4 in cancer biology and for developing novel therapeutic strategies against BRD4-dependent malignancies. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-19 is a targeted protein degradative compound designed to degrade the SMARCA2 protein via a PROTAC mechanism. It demonstrates significant efficacy in A549 and MV411 cell lines with a DC50 of less than 100 nM. Additionally, this compound exhibits a reduced degradation effect on SMARCA4 in MV411 cells, with a DC50 exceeding 1000 nM. This specificity makes PROTAC SMARCA2 degrader-19 a valuable tool for studying the biological roles of SMARCA2 and its potential implications in cancer research. -
BRD4 BrD1 inhibitor
Olinone is a selective inhibitor of the bromodomain-containing proteins BRD4 and BrD1. This compound has been shown to accelerate the differentiation of primary oligodendrocyte progenitors derived from mouse models, making it a valuable tool for studying oligodendrocyte development and associated neural pathways. Its specificity for BRD4 and BrD1 further supports its use in research focusing on epigenetic regulation and potential neurodegenerative disease mechanisms. -
PROTAC SMARCA2 Degrader
PROTAC SMARCA2 degrader-20 (Compound I-40) is an innovative PROTAC molecule designed to selectively target and degrade the SMARCA2 protein. This compound facilitates the ubiquitination and subsequent proteasomal degradation of SMARCA2, offering a unique approach to modulate its biological activity. It is primarily utilized in cancer research to explore novel therapeutic pathways and to investigate the role of SMARCA2 in tumorigenesis and other related mechanisms. -
BET Inhibitor
EBET-590 is a potent bromodomain and extraterminal (BET) inhibitor that selectively targets BET proteins, disrupting their interactions with acetylated histones. This compound exhibits significant anti-proliferative activity in various cancer cell lines, making it a valuable tool for cancer research. It is particularly relevant for studies focused on epigenetic regulation and the development of targeted cancer therapies. -
BET Inhibitor
BET-IN-7 is a potent inhibitor of bromodomain and extra-terminal (BET) proteins, exhibiting a Ki value of 12.27 μM and a Kd of 89.3 μM. This compound demonstrates significant potential in research related to sepsis and other inflammatory conditions by modulating transcriptional regulation. Its ability to interfere with BET protein activity makes it a valuable tool for studying epigenetic processes and developing therapeutic strategies against related diseases. -
BET Inhibitor
BET-IN-21 is a selective BET inhibitor targeting the extra terminal domain, demonstrating a Ki of 230 nM. This compound effectively inhibits microglial activation and exhibits therapeutic benefits in models of experimental autoimmune encephalomyelitis. It serves as a valuable tool for research into neuroinflammation and related neurodegenerative disorders. -
BRD4 PROTAC Degrader,
LGF308 is a selective PROTAC degrader targeting BRD4, designed to promote the degradation of BRD4 through the formation of a ternary complex with DCAF11. This compound demonstrates potent cytotoxicity in cancer cells while sparing normal cells, effectively inducing apoptosis by upregulating apoptosis-related proteins. Additionally, LGF308 significantly inhibits tumor cell proliferation and migration in breast cancer and triple-negative breast cancer cell lines, making it a valuable tool for research in breast cancer biology. -
BRD4 Ligand-Linker Conjugate
CPI-203-PEG1-C3-O-COOH is a BRD4 ligand-linker conjugate, designed to facilitate the synthesis of PROTAC (proteolysis-targeting chimera) molecules, specifically the BRD4 degrader ARV-771. This compound serves as a crucial component in targeted protein degradation research, enabling the selective modulation of BRD4 protein levels and aiding in the understanding of its biological functions. Its application is significant in therapeutic development for diseases associated with dysregulated BRD4 activity. -
BET Bromodomain Inhibitor
BET-IN-18 is a pan-BET bromodomain inhibitor targeting Brd4 and BrdT. It exhibits potent competitive inhibition of the binding of acetylated histone substrates as well as the known BET inhibitor (+)-JQ1, with IC50 values of 1.0 μM and 2.3 μM for Brd4 and BrdT, respectively. This compound is useful for investigating BET bromodomain functions in various biological contexts, particularly in the study of multiple myeloma. -
SMARCA2 Degrader
PROTAC SMARCA2 degrader-31 is a targeted degrader of the SMARCA2 protein, utilizing a proteolysis-targeting chimera (PROTAC) approach. This compound has demonstrated an impressive degradation rate of up to 99% in H929 cells at a concentration of 100 nM. It exhibits significant anti-proliferative activity, making it a valuable tool for cancer research and investigations into SMARCA2-related pathways. -
SMARCA2 Degrader
JP-2-249 is a selective SMARCA2 degrader that functions as a molecular glue. It has been demonstrated to significantly reduce SMARCA2 protein levels in MV-4-11 cells at concentrations ranging from 1 to 10 μM. This compound is valuable for research applications focused on the modulation of cancer-related pathways involving SMARCA2. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-7 (Compound I-428) selectively targets and degrades the SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A, specifically SMARCA2. It has demonstrated effective degradation of both SMARCA2 and SMARCA4 in the MV411 cell line, with DC50 values of less than 100 nM and between 100-500 nM, respectively. This compound serves as a valuable tool for studying chromatin remodeling and its implications in cancer biology and therapeutic development. -
BRD 4/p38α/BRDT Inhibitor
SB-284851-BT is a selective inhibitor of BRD4, p38α, and BRDT. It effectively inhibits BRD4-BD1 with an IC50 of 1.7 µM, p38α with a Kd of 0.47 nM, and exhibits additional inhibitory activity against BRDT and BRD4 with IC50 values of 18 µM and 3.7 µM, respectively. SB-284851-BT significantly reduces IL-8 production through p38α inhibition and downregulates crucial oncogenic pathways such as c-Myc and NF-κB via BRD4 inhibition. This compound has potential applications in cancer research and therapeutic development targeting cellular signaling pathways. -
BRD4 BD1 Inhibitor
3-Methylcarbostyril is a selective inhibitor of the bromodomain protein BRD4 BD1, exhibiting a pIC50 value of 4.4. This compound has been utilized in research to investigate the role of BRD4 in various cellular processes, including transcription regulation and oncogenic signaling. Its inhibitory activity makes it a valuable tool for studies focused on cancer therapy and epigenetic modulation. -
BRD4 BD1 Inhibitor
ZL0516 is a selective inhibitor of the BRD4 bromodomain 1 (BD1), demonstrating potent activity in modulating epigenetic regulation. It effectively suppresses inflammatory bowel disease (IBD) through inhibition of the BRD4/NF-κB signaling pathway, which plays a critical role in inflammation and immune responses. This compound is primarily utilized in research focusing on the development of therapeutic strategies for IBD and related inflammatory conditions. -
BRDT-BD2 Inhibitor
CDD-1132 is a potent BRDT-BD2 inhibitor with an IC50 of 13 nM, demonstrating significant selectivity for this target. It plays a crucial role in research applications focused on nonhormonal contraceptive agents by interfering with the bromodomain's function. This compound offers potential insights into the development of innovative reproductive health solutions. -
SMARCA2 Degrader
PROTAC SMARCA2 degrader-18 is a synthetic molecule designed to selectively target and degrade the SMARCA2 protein. This compound exhibits promising activity in modulating SMARCA2 levels and has potential applications in the study of non-small cell lung cancer (NSCLC). Researchers can utilize PROTAC SMARCA2 degrader-18 to investigate the implications of SMARCA2 degradation in cancer biology and therapeutic development. -
BRD4 Degrader
BRD4 degrader-4 is a selective degrader targeting the bromodomain-containing protein BRD4, facilitating its proteasomal degradation. This compound exhibits significant biological activity by disrupting BRD4 function, which is implicated in epigenetic regulation and oncogenic gene expression. BRD4 degrader-4 is utilized in cancer research and the study of diseases associated with bromodomain proteins, providing valuable insights into potential therapeutic strategies. -
BET Inhibitor
BET-IN-29 is a bromodomain and extraterminal motif (BET) inhibitor that modulates protein-protein interactions involved in gene regulation. It exhibits potent anti-cancer activity by disrupting the function of BET proteins, which play a critical role in cellular proliferation and survival. This compound is applicable in various research areas, including cancer biology, inflammation, metabolic disorders, neurological diseases, and infectious diseases, making it a valuable tool for elucidating underlying mechanisms in these fields. -
BRD4-BD1/2 Inhibitor
BRD4-BD1/2-IN-1 is a potent inhibitor targeting the bromodomain receptor BRD4, exhibiting IC50 values of less than 100 nM for both BRD4 BD-1 and BD-2. This compound plays a crucial role in modulating gene expression through its interactions with chromatin. It is commonly utilized in research applications focused on cancer biology and therapeutic strategies targeting epigenetic regulation. -
BET Inhibitor
BET-IN-15 is a potent bromodomain and extraterminal (BET) inhibitor that targets BRD4 with IC50 values of 0.64 nM and 0.25 nM for BRD4-BD1 and BRD4-BD2, respectively. This compound exhibits significant antiproliferative activity, making it an important tool for studying the role of BET proteins in cancer and other diseases. Researchers can utilize BET-IN-15 in investigations of transcriptional regulation and the therapeutic potential of BET inhibition in oncology. -
BRD4 PROTAC Degrader
TrimTAC1 is a TRIM21-based PROTAC designed to target BRD4 for selective degradation. This compound effectively promotes the degradation of NUP98FG-mEGFP-BRD4BD2 nuclear condensates without affecting soluble mEGFP-BRD4BD2 in A549 cells. TrimTAC1 is valuable for research applications aimed at studying the dynamics of protein degradation and the role of BRD4 in various cellular processes. -
BRD4 Ligand
BRD4 Inhibitor-12 is a selective ligand for the bromodomain-containing protein 4 (BRD4). It exhibits potent inhibitory activity, making it a valuable tool for investigating the role of BRD4 in cancer and inflammatory pathways. This compound facilitates research into the modulation of gene expression and potential therapeutic interventions in various diseases associated with aberrant BRD4 activity. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-20 is a novel PROTAC degrader targeting the catalytic subunits of the SWI/SNF complex, specifically SMARCA2 and SMARCA4. This compound effectively induces degradation of SMARCA2 in A549 and MV411 cell lines with a DC50 of less than 100 nM, while degrading SMARCA4 in MV411 cells with a DC50 range of 100-500 nM. It serves as a valuable tool for studying the functional roles of SWI/SNF complex components in various biological processes and disease states. -
BRD4 Inhibitor
BRD4 Inhibitor-17 is a potent BRD4 inhibitor with an IC50 of 0.33 μM. This compound is involved in the regulation of transcription associated with inflammatory responses, cellular proliferation, and cell cycle progression. BRD4 Inhibitor-17 holds potential as a therapeutic agent for counteracting the effects of arsenical compounds in research applications. -
BET Inhibitor
BET-IN-12 is an orally active inhibitor of bromodomain and extra-terminal (BET) proteins, specifically targeting BRD4 with an IC50 of 0.9 nM. This compound demonstrates significant ability to disrupt BET protein interactions with acetylated lysines, thereby influencing gene expression and cellular signaling pathways. BET-IN-12 is utilized in research exploring therapeutic strategies for various cancers and inflammatory diseases, making it a valuable tool for studying the role of BET proteins in these conditions. -
BRD4 PROTAC Degrader
JV8 is a potent BRD4 PROTAC degrader that facilitates the ubiquitination and subsequent degradation of the BRD4 protein, leading to induced apoptosis. This compound exhibits significant antitumor activity, demonstrated in a 4T1 orthotopic tumor model in mice. JV8 serves as a valuable tool for research in cancer therapeutics and the study of protein degradation pathways. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-15 is a potent PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It demonstrates efficient degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, with DC50 values below 100 nM. This compound is valuable for researchers investigating the role of these proteins in epigenetic regulation and cancer biology. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2/4-degrader-9 is a targeted protein degrader that specifically targets the catalytic subunits of the SWI/SNF complexes, SMARCA2 and SMARCA4. This compound effectively degrades SMARCA2 in MV411 and A549 cell lines with a DC50 value of less than 100 nM, while also demonstrating similar potency against SMARCA4 in MV411 cells. PROTAC SMARCA2/4-degrader-9 serves as a valuable tool for studying the biological functions of these proteins and their roles in cancer research and therapeutic development. -
BET Inhibitor
BET-IN-8 is a potent bromodomain and extraterminal (BET) inhibitor, with a Ki value of 0.83 μM and a Kd of 0.571 μM. This compound exhibits significant biological activity by ameliorating lipopolysaccharide (LPS)-induced sepsis in vivo. BET-IN-8 is valuable for research applications focused on understanding the role of BET proteins in inflammatory responses and sepsis pathophysiology. -
PROTAC SMARCA2 Degrader
PROTAC SMARCA2 Degrader-23 is a potent and selective degrader targeting the SMARCA2 protein. With a DC50 of less than 100 nM, it effectively induces degradation of SMARCA2. This compound is primarily utilized in cancer research, facilitating studies on the therapeutic potential of targeting SMARCA2 for oncological applications. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-14 is a targeted protein degradation compound designed to bind both von Hippel-Lindau (VHL) and the BRD4 protein. It demonstrates potent activity with IC50 values of 1.8 nM for BRD4 BD1 and 1.7 nM for BRD4 BD2. This reagent effectively induces degradation of BRD4 in PC3 prostate cancer cells, making it a valuable tool for studying BRD4-related pathways and potential therapeutic interventions in cancer research. -
SMARCA2 Inhibitor
SMARCA2-IN-1 is a selective inhibitor of the SWI/SNF chromatin remodeling complex, specifically targeting SMARCA2. With an IC50 of greater than 1000 nM in H1299 cell lines, this compound is useful for studying the role of SMARCA2 in chromatin dynamics and epigenetic regulation. It has potential applications in cancer research, particularly in understanding the implications of chromatin remodeling in tumor progression and therapeutic resistance. -
BRD4 Inhibitor
BRD4-IN-8 is a selective inhibitor of the bromodomain-containing protein 4 (BRD4). It modulates gene expression by disrupting the interaction between BRD4 and acetylated histones, leading to the inhibition of transcriptional elongation. This compound has been shown to exhibit anti-cancer activity and is utilized in research investigating the therapeutic potential of targeting the BRD4 pathway in various malignancies. -
BET Inhibitor
Repibresib is a selective Bromodomain and Extra-Terminal (BET) inhibitor that targets BET proteins involved in the regulation of gene expression. This compound exhibits significant antineoplastic activity, making it a valuable tool for cancer research. Its ability to disrupt the interaction between BET proteins and acetylated lysines can be utilized in the study of various malignancies and in the development of novel therapeutic strategies. -
BRD4 Inhibitor
BRD4-IN-4 is a selective inhibitor of the bromodomain-containing protein 4 (BRD4) with an IC50 of 6.83 μM. This compound effectively inhibits the proliferation of MV4-11 cells and induces cell cycle arrest in the G1 phase. BRD4-IN-4 is primarily utilized in research focused on MLL leukemia, providing insights into the therapeutic potential of targeting BRD4 in cancer treatment. -
BET Inhibitor
GSK-340 is a potent BET inhibitor that exhibits high affinity and selectivity for the bromodomain BD2 of BRD4, with a pIC50 value of 7.2. This compound effectively inhibits the release of MCP-1 in lipopolysaccharide-treated PBMCs and whole blood, demonstrating pIC50 values of 7.4 and 6.0, respectively. GSK-340's immunomodulatory properties make it a valuable tool for research applications in inflammation and cancer biology. -
Pan-BRD4-D1-Biased/BRD4-D2 Inhibitor
DW34 is a pan-BRD4-D1 biased inhibitor with concurrent inhibitory activity against BRD4-D2. It demonstrates potent biological activity with an EC50 of 0.14 μM, making it effective in modulating BRD4 pathways. DW34 significantly mitigates liver inflammation induced by lipopolysaccharide (LPS) and acetaminophen (APAP), primarily by reducing chemokine expression and cellular necrosis. This compound is suitable for research applications focused on inflammatory diseases and BRD4-related pathways. -
BRD4 Inhibitor
CN427 is a quinazoline-based compound that selectively inhibits the bromodomain-containing protein 4 (BRD4) with a Kd of 66 nM. This inhibition disrupts the interaction between BRD4 and acetylated histones, which can lead to altered transcriptional regulation. CN427 is primarily applicable in leukemia research, providing insights into epigenetic modulation and potential therapeutic strategies in this malignancy. -
pBrd4 PDID Binding Agent
DC-peptoid-1 is a selective binder targeting the phosphorylated Brd4 PDID domain, exhibiting a dissociation constant (Kd) of approximately 50-100 μM for human-derived substrates. This reagent specifically binds to phosphorylated PDID, showing no affinity for the non-phosphorylated variant or unrelated domains. Capable of crosslinking with its target in both solution and cell lysates, DC-peptoid-1 can efficiently capture phosphorylated PDID from complex biological samples through immobilization, while avoiding interactions with non-phosphorylated proteins or phosphoproteins from bacterial origins. Its unique selectivity positions DC-peptoid-1 as a potential alternative to phosphoprotein-specific antibodies in applications such as immunoaffinity purification. -
BRD4 BD2 Inhibitor
BRD4-BD1/2-IN-2 is a highly selective inhibitor targeting the BD2 domain of BRD4, demonstrating IC50 values of less than 0.5 nM for BRD4 BD2 and approximately 300 nM for BRD4 BD1. This compound exhibits significant biological activity in modulating BRD4-related pathways, making it a valuable tool for research in oncology and epigenetic regulation. Its potency and specificity support further exploration of BRD4 as a therapeutic target in various diseases. -
BET Inhibitor
BET-IN-10 is a potent BET inhibitor that selectively targets bromodomain and extraterminal (BET) proteins, crucial for regulating gene expression. This compound demonstrates significant anticancer activity, notably inhibiting the growth of MV4-11 leukemia cells with an IC50 value of 26.5 nM. BET-IN-10 is valuable for research applications focused on cancer biology and the mechanistic study of BET-mediated signaling pathways. -
BRD4 Inhibitor
BRD4 Inhibitor-28 is a selective inhibitor of the bromodomain protein BRD4, targeting the BRD4-BD1 and BRD4-BD2 domains with IC50 values of 15 nM and 55 nM, respectively. Additionally, it demonstrates inhibitory effects on BRD2-BD1, BRD3-BD1, and BRDT-BD1, with IC50 values of 19 nM, 25 nM, and 68 nM. This compound exhibits notable anti-melanoma activity, making it valuable for research in cancer therapeutics and epigenetic modulation. -
PROTAC SMARCA2 Degrader
PROTAC SMARCA2 degrader-3 is a PROTAC degrader specifically targeting the SWI/SNF ATPase subunit SMARCA2. This compound induces proteasomal degradation of SMARCA2, demonstrating significant anticancer activity. It is valuable for research applications focused on cancer biology and the exploration of therapeutic strategies targeting chromatin remodeling complexes. -
BET Inhibitor
SJ1461 is a potent BET inhibitor that selectively targets bromodomain-containing proteins BRD2 and BRD4. It demonstrates high affinity with IC50 values of 1.6 nM for BRD2 (BD1), 0.1 nM for BRD2 (BD2), 6.5 nM for BRD4 (BD1), and 0.2 nM for BRD4 (BD2). SJ1461 is utilized in research applications related to cancer, inflammation, and epigenetic regulation, making it a valuable tool for investigating the role of BET proteins in various biological processes. -
BRD9 Molecule Glue
BRD9 Degrader-3 is a molecular glue targeting BRD9, exhibiting a DC50 of less than 1.25 nM. This compound facilitates the proteolytic degradation of BRD9, effectively modulating protein levels within cellular systems. It is primarily utilized in research applications aimed at investigating the role of BRD9 in cancer biology and other disease contexts. -
BRD4 Inhibitor
Y02224 is a potent inhibitor of the bromodomain-containing protein 4 (BRD4), which plays a critical role in regulating gene expression and cellular proliferation. This compound exhibits significant antiproliferative activity against leukemia cells, highlighting its potential in cancer research. Additionally, Y02224 may be valuable in investigating therapeutic strategies for castration-resistant prostate cancer (CRPC). -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-15 is a proteolysis-targeting chimera (PROTAC) that utilizes ligands for von Hippel-Lindau (VHL) and BRD4, exhibiting IC50 values of 7.2 nM for the BRD4 BD1 domain and 8.1 nM for the BD2 domain. This compound effectively induces the degradation of the BRD4 protein in PC3 prostate cancer cells. Its ability to selectively target and eliminate BRD4 makes it a valuable tool for research in cancer biology and therapeutic applications aimed at modulating gene expression.
