Epigenetics
Epigenetics research delves into the molecular mechanisms that control gene expression and cellular traits without altering the underlying DNA sequence. One crucial aspect of this field is the role of small molecules, which act as powerful regulators of epigenetic modifications. These small compounds, typically comprising a few dozen to a few hundred atoms, have emerged as essential tools in understanding and manipulating the epigenome.
- DNA Methylation Inhibitors: Small molecules like 5-azacytidine and 5-aza-2'-deoxycytidine are DNA methyltransferase inhibitors. They block the addition of methyl groups to DNA, leading to DNA demethylation. This can reactivate silenced genes, potentially offering therapeutic avenues for conditions like cancer.
- HDAC inhibitors: HDACs remove acetyl groups from histone proteins, contributing to gene repression. Small molecule HDAC inhibitors, such as Vorinostat and Romidepsin, can reverse this process by increasing histone acetylation, allowing genes to be more accessible for transcription. These inhibitors are being explored for cancer therapy and other conditions.
- Histone Methyltransferase Inhibitors: Small molecules like GSK126 inhibit specific histone methyltransferases, affecting histone methylation patterns. This can alter gene expression, making them promising candidates for cancer and other diseases with epigenetic dysregulation.
- RNA Modulators: Small molecules can also target non-coding RNAs involved in epigenetic regulation. For instance, small molecules called small interfering RNAs (siRNAs) can be designed to target and degrade specific long non-coding RNAs, influencing gene expression.
- Epigenetic Reader Domain Inhibitors: These small molecules target proteins that recognize and bind to specific epigenetic marks. Examples include inhibitors of bromodomain-containing proteins (BET inhibitors), which can disrupt gene regulation by interfering with protein-DNA interactions.
Small molecules in epigenetics research not only provide insights into the fundamental biology of gene regulation but also hold immense promise for developing novel therapeutics. Their ability to selectively modulate specific epigenetic marks and pathways has led to ongoing clinical trials and drug development efforts for various diseases, including cancer, neurological disorders, and inflammatory conditions. Understanding and harnessing the power of these small molecules is at the forefront of modern epigenetics research, offering new hope for precision medicine and targeted therapies.
3 key components involved in the regulation of epigenetic modifications
Epigenetics Writer
Epigenetics writers are enzymes responsible for adding chemical marks or modifications to DNA or histone proteins. These marks include DNA methylation (addition of methyl groups to DNA) and histone modifications (such as acetylation, methylation, phosphorylation, etc.).
Epigenetics Reader
Function: Epigenetics readers are proteins that can recognize and bind to specific epigenetic marks on DNA or histones. These reader proteins interpret the epigenetic code and facilitate downstream cellular processes, such as gene activation or repression.
Epigenetics Eraser
Function: Epigenetics erasers are enzymes responsible for removing or reversing epigenetic marks on DNA or histones. This process allows for the dynamic regulation of gene expression and the resetting of epigenetic states during various stages of development and in response to environmental changes.
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Catalog No.
Product Name
Application
Product Information
Citations
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PRMT5 Inhibitor
PF-06939999 is a potent, orally active inhibitor of protein arginine methyltransferase 5 (PRMT5), functioning as a S-adenosylmethionine (SAM) competitive antagonist. It effectively suppresses the expression of symmetric dimethylarginine (SDMA) protein, with an IC50 value of 1.1 nM in A427 cells. Due to its ability to inhibit PRMT5 activity, PF-06939999 demonstrates significant antitumor effects, making it valuable for cancer research focused on epigenetic regulation and methylation pathways. -
JMJD1C Inhibitor
JMJD1C-IN-1 is a selective inhibitor of JMJD1C with an IC50 of 0.59 μM and a Kd of 1.96 μM. This compound effectively disrupts the binding of JMJD1C to the H3K9me2 peptide substrate as demonstrated in the HTRF assay, showing an IC50 of 1.47 μM. JMJD1C-IN-1 enhances tumor immunotherapy research by impairing intratumoral regulatory T (Treg) cell fitness through the accumulation of H3K9me2, which downregulates PD1 expression, and by reducing STAT3 demethylation, thereby promoting STAT3 activation. Furthermore, it exhibits dose-dependent antitumor efficacy across various mouse cancer models, including fibrosarcoma, melanoma, lung cancer, hepatocellular carcinoma, and colorectal cancer. -
PRMT1 Inhibitor
Furamidine dihydrochloride is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), exhibiting an IC50 of 9.4 μM. This compound demonstrates significant selectivity for PRMT1 over PRMT5, PRMT6, and PRMT4, making it an essential tool for studying PRMT-related biological processes. In addition, Furamidine dihydrochloride inhibits tyrosyl-DNA phosphodiesterase 1 (TDP-1) competitively and reversibly, showing enhanced activity with duplex DNA substrates. Furthermore, it possesses antiparasitic properties, expanding its potential applications in chemical and biological research. -
SETD2 Inhibitor
EPZ-719 is a selective inhibitor of the SETD2 enzyme, exhibiting an IC50 value of 0.005 μM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development. EPZ-719 may be utilized to explore the role of SETD2 in tumorigenesis and to evaluate potential treatment strategies targeting this pathway. -
DOT1L Inhibitor
Dot1L-IN-4 is a potent inhibitor of the DOT1L enzyme, exhibiting an IC50 of 0.11 nM. It effectively disrupts the activity of the telomeric silencing 1-like protein, making it a valuable tool for research into epigenetic regulation and gene expression modulation. Its application extends to studies on leukemia and other cancer types where DOT1L is implicated, facilitating investigations into therapeutic approaches targeting this pathway. -
HDAC Inhibitor
HDAC-IN-48 is a potent inhibitor of histone deacetylases (HDACs) that exhibits significant cytotoxicity, with a GI50 of approximately 20 nM. This hybrid molecule incorporates pharmacophores from SAHA and CETZOLE, effectively inducing ferroptosis while inhibiting HDAC activity. Additionally, HDAC-IN-48 features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a valuable tool for click chemistry applications in chemical biology and therapeutic research. -
HDAC11 Inhibitor
HDAC11-IN-3 is a selective inhibitor of HDAC11, exhibiting an IC50 of 4.1 nM. This compound demonstrates potent anti-acute myeloid leukemia (AML) activity against U937 and OCI-AML2 cell lines with an IC50 of 10 μM. It effectively induces apoptosis, cell cycle arrest, and differentiation while upregulating iron transporters transferrin (TF) and transferrin receptor (TFRC). Additionally, HDAC11-IN-3 activates the p62-Keap1-Nrf2-HMOX1 pathway, resulting in elevated intracellular iron levels and subsequent ferroptosis in AML cells. This reagent is suited for studies investigating the molecular mechanisms of AML and can be utilized alone or in combination with other therapeutic agents like Cytarabine. -
LSD1 Inhibitor
Higenamine hydrochloride is a selective inhibitor of LSD1, with an IC50 value of 1.47 μM. This compound exhibits anti-inflammatory and antibacterial properties, and has been shown to attenuate IL-1β-induced apoptosis via the ROS-mediated PI3K/Akt signaling pathway. Additionally, Higenamine hydrochloride protects brain cells from oxygen deprivation and promotes bone formation in osteoporosis through the SMAD2/3 pathway. Its versatile applications make it suitable for research in cancer, inflammation, cardiorenal syndrome, and related diseases. -
PAD Inhibitor
BB-Cl-Amidine hydrochloride is a selective peptidylarginine deiminase (PAD) inhibitor. It demonstrates significant inhibitory activity against PAD enzymes, influencing protein citrullination processes. This compound is utilized in research focused on the role of PAD enzymes in various diseases, such as rheumatoid arthritis and neurodegenerative disorders, as well as for exploring mechanisms of protein modification. -
PAD2 Inhibitor
AFM32a hydrochloride is a selective inhibitor of protein arginine deiminase 2 (PAD2), derived from a benzimidazole structure. It demonstrates high potency and a remarkable selectivity profile, exhibiting a 95-fold preference for PAD2 over PAD4 and a 79-fold preference over PAD3. This compound is valuable for research applications focusing on the regulatory mechanisms of PAD2 in various biological processes. -
PAD4 Inhibitor
GSK484 is a selective inhibitor of peptidylarginine deiminase 4 (PAD4), effectively blocking the enzyme's catalytic activity to inhibit protein citrullination and neutrophil extracellular trap (NET) formation. This compound demonstrates anti-inflammatory properties by reducing histone H3 production, modulating MHC-I expression, and inhibiting CD8+ T cell activation and proliferation. Research applications include studies on rheumatoid arthritis, sickle cell disease, myocardial ischemia-reperfusion injury, and colitis, as well as investigations into intestinal microbial homeostasis and ferroptosis-related dysbiosis. -
PAD4 Inhibitor
JBI-589 is a non-covalent inhibitor selectively targeting the PAD4 isoform. This compound effectively reduces CXCR2 expression and inhibits neutrophil chemotaxis, making it instrumental in the study of inflammatory processes. JBI-589 demonstrates potential in diminishing primary tumors and metastases while enhancing the efficacy of checkpoint inhibitors. It is suitable for various applications in cancer research. -
PAD4 Inhibitor
BMS-P5 free base is a selective inhibitor of peptidylarginine deiminase 4 (PAD4), demonstrating an IC50 of 98 nM. This compound exhibits specificity for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 free base effectively inhibits multiple myeloma (MM)-induced neutrophil extracellular trap (NET) formation and has been shown to delay the progression of MM in syngeneic mouse models, making it a valuable tool for research in cancer and inflammation. -
PAD4 Inhibitor
BMS-P5 is a selective inhibitor of peptidylarginine deiminase 4 (PAD4), demonstrating an IC50 of 98 nM. This compound exhibits notable selectivity for PAD4 over PAD1, PAD2, and PAD3. BMS-P5 effectively inhibits neutrophil extracellular trap (NET) formation induced by multiple myeloma (MM) and has been shown to delay the progression of MM in syngeneic mouse models, making it a valuable tool for research in cancer biology and the study of inflammatory responses. -
PAD4 Inhibitor
PAD-IN-2 is a potent inhibitor of pad4 with an IC50 of less than 1 μM. This compound is valuable in the investigation of various autoimmune diseases and cancers, including rheumatoid arthritis, vasculitis, systemic lupus erythematosus, cutaneous lupus erythematosus, ulcerative colitis, cystic fibrosis, asthma, multiple sclerosis, and psoriasis. Its ability to modulate pad4 activity makes it a significant tool for research aimed at understanding these complex conditions. -
PAD2 inhibitor
KP-302 is a selective inhibitor of protein arginine deiminase PAD2, exhibiting a Ki value of 60 μM. This compound demonstrates significant biological activity by reversing physical disability in the experimental autoimmune encephalomyelitis (EAE) mouse model of multiple sclerosis (MS), as well as reducing T cell infiltration in the central nervous system. KP-302 serves as a valuable research tool for investigating disease-modifying therapies in the context of MS. -
PAD2 Inhibitor
AFM-30a is a selective inhibitor of protein arginine deiminase 2 (PAD2), exhibiting an EC50 of 9.5 μM for PAD2 binding. This compound effectively inhibits H3 citrullination with an EC50 value of 0.4 μM. AFM-30a is useful for investigating the role of PAD2 in various biological processes, particularly in cancer research and the study of autoimmune diseases such as rheumatoid arthritis, multiple sclerosis, lupus, and ulcerative colitis. -
PAD2 Inhibitor
AFM32a is a selective inhibitor of protein arginine deiminase 2 (PAD2), characterized by its benzimidazole structure. This compound demonstrates a remarkable selectivity, exhibiting a 95-fold preference for PAD2 over PAD4 and a 79-fold preference over PAD3. Its potential applications in biochemical research include investigations into the role of PAD2 in various physiological and pathological processes, making it a valuable tool for studying citrullination and related signaling pathways. -
PAD4 Inhibitor
PAD4-IN-2 is a selective inhibitor of the peptidyl arginine deiminase 4 (PAD4) enzyme, with an IC50 value of 1.94 μM. This compound has been shown to inhibit tumor growth in mouse models by specifically targeting the PAD4-H3cit-neutrophil extracellular traps (NETs) pathway in neutrophils. PAD4-IN-2 is useful for research applications exploring cancer biology, inflammation, and neutrophil function. -
PAD4 Inhibitor
TDFA is an irreversible inhibitor of protein arginine deiminase 4 (PAD4), a crucial enzyme involved in the modification of arginine residues to citrulline. This compound exhibits significant biological activity by affecting histone modifications and autoimmunity-related processes. TDFA is valuable for research applications focusing on rheumatoid arthritis, cancer biology, and neurodegenerative diseases, providing insights into the role of PAD4 in various disease mechanisms. -
PAD inhibitor
(Rac)-Cl-amidine is a potent inhibitor of protein arginine deiminase (PAD), demonstrating oral bioavailability and effective inhibition of PAD activity. This compound serves as a valuable tool for investigating PAD functions in cellular contexts, influencing critical biological processes such as gene transcription, cell differentiation, and innate immune responses. Its ability to stabilize epigenetic modifications makes (Rac)-Cl-amidine an important reagent for research in immunology and epigenetics. -
PAD inhibitor
2-PADQZ is a potent inhibitor targeting Protein Arginine Deiminase, demonstrating significant antiviral activity against influenza viruses. It specifically binds to the RNA promoter of the influenza A virus, creating a binding site within the internal loop, which disrupts viral replication. Research involving 2-PADQZ has shown notable inhibitory effects against H1N1, H3N2, and influenza B viruses, making it a valuable tool for investigations into antiviral therapeutics and influenza virus biology. -
PAD4 Inhibitor
PAD4-IN-5 is a potent inhibitor of the enzyme PAD4, exhibiting an IC50 of ≤10 nM under 50 µM Ca2+ conditions and between 101-500 nM under 1 mM Ca2+ conditions. This compound serves as a valuable tool for investigating the role of PAD4 in autoimmune diseases, particularly rheumatoid arthritis. Its specificity and efficacy make it suitable for research focused on the pathophysiology of these disorders and the development of targeted therapies. -
PAD4 Inhibitor
F-Amidine TFA is a selective inhibitor of Protein Arginine Deiminase 4 (PAD4), an enzyme crucial in the process of citrullination, which impacts various inflammatory and autoimmune conditions. This compound has demonstrated significant potential in the study of diseases such as rheumatoid arthritis by modulating PAD4 activity. F-Amidine TFA serves as a valuable tool for researchers exploring the role of PAD4 in immune system dysregulation and related pathologies. -
PAD3 Inhibitor
PAD3-IN-1 is a selective inhibitor of protein arginine deiminase 3 (PAD3), exhibiting over 10-fold selectivity compared to PAD isoforms 1, 2, and 4. With IC50 values of 120 μM for PAD1, 27.5 μM for PAD2, 4.5 μM for PAD3, and 30.5 μM for PAD4, PAD3-IN-1 is particularly effective for targeting PAD3. This isoform is implicated in neurodegenerative processes following spinal cord injury, allowing PAD3-IN-1 to serve as a valuable tool for investigating PAD-related neurological disorders. -
Peptidylarginine Deiminase 4 Inhibitor
GSK147 is a potent inhibitor of Peptidylarginine Deiminase 4 (PAD4), demonstrating a Kd of 0.47 µM. This compound effectively inhibits ionomycin-induced protein citrullination in isolated human neutrophils, making it a valuable tool for studying PAD4 activity and its role in various inflammatory conditions. GSK147 is applicable in research focusing on autoimmune diseases and the modulation of protein citrullination. -
PAD4 Inhibitor
PAD4-IN-3 is a potent inhibitor of protein arginine deiminase 4 (PAD4), exhibiting notable antitumor activity both in vitro and in vivo. It is designed to be covalently linked to an RGD sequence peptide-modified chitosan, resulting in an oxidative stress-responsive nanoagent. This composite, K-CRGDV-PAD4-IN-3, targets tumors effectively, inhibits PAD4 activity, and suppresses the formation of neutrophil extracellular traps (NETs), thereby enhancing the tumor immune microenvironment. Its applications in cancer research focus on improving therapeutic responses and understanding immune modulation within the tumor context. -
PAD Inhibitor
BB-Cl-Yne is a selective inhibitor of protein arginine deiminases (PADs), demonstrating Ki values of 6400, 3600, 10800, and 4900 M-1min-1 for PAD1 to PAD4, respectively. This compound serves as a valuable tool for studying PAD enzymatic activity and its role in various biological processes. Additionally, BB-Cl-Yne can be utilized as a click probe for labeling PAD, facilitating research in epigenetics and signal transduction. -
PAD Inhibitor
BB-F-Yne is a potent inhibitor of protein arginine deiminases (PADs), exhibiting Ki values of 2050, 1700, 1100, and 3100 M^-1 min^-1 for PAD1 through PAD4, respectively. This compound serves as an effective click probe for labeling PAD, facilitating research into its biological roles. BB-F-Yne is valuable for studies investigating the modulation of PAD activity and its implications in various physiological and pathological processes. -
PAD4 Inhibitor
F-Amidine is an inhibitor of Protein arginine deiminase 4 (PAD4), a key enzyme involved in the regulation of protein citrullination. This compound is valuable for studying its role in inflammatory and immune system disorders, particularly in conditions such as rheumatoid arthritis. Researchers can utilize F-Amidine to explore the molecular mechanisms underlying immune responses and identify potential therapeutic targets for related diseases. -
PAD4 Inhibitor
GSK199 analog hydrochloride is a potent inhibitor of protein arginine deiminase 4 (PAD4), an enzyme involved in the post-translational modification of arginine residues. This compound exhibits promising anti-inflammatory properties and is being explored for therapeutic applications in various autoimmune diseases, including rheumatoid arthritis, systemic lupus erythematosus, and vasculitis. Additionally, it shows potential in the treatment of oncological conditions and other disorders characterized by dysregulated citrullination, making it a valuable tool for researchers investigating these diseases. -
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. -
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. -
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. -
YTH domain Inhibitor
YTH-IN-1 is a pan-YTH domain inhibitor that targets various YTH domain-containing proteins. It exhibits IC50 values of 39 μM, 34 μM, 35 μM, 48 μM, and 30 μM for human YTHDF1, YTHDF2, YTHDF3, YTHDC1, and YTHDC2 respectively. This compound is utilized in research to explore the role of YTH domain proteins in RNA metabolism and epitranscriptomics, making it a valuable tool for studying gene regulation and cellular responses. -
BRD9 Inhibitor
GNE-375 is a highly selective inhibitor of BRD9, exhibiting an IC50 of 5 nM. It demonstrates more than 100-fold selectivity for BRD9 compared to BRD4, TAF1, and CECR2. GNE-375 effectively reduces the binding of BRD9 to chromatin, making it a valuable tool for studies of chromatin regulation and the role of BRD9 in epigenetic modulation. This compound is ideal for research applications involving cancer biology and cellular differentiation pathways. -
BRD4 Inhibitor
BRD4 Inhibitor-20 is a selective inhibitor of bromodomain protein 4 (BRD4), targeting both the BD1 and BD2 domains with IC50 values of 19 nM and 28 nM, respectively. This compound exhibits significant anti-proliferative effects in various cancer cell lines, making it useful for studying the role of BRD4 in oncogenesis. BRD4 Inhibitor-20 is particularly applicable in research focused on colon cancer and other malignancies associated with dysregulated BRD4 activity. -
BRD4 Inhibitor
dBRD4-BD1 is a selective BRD4 inhibitor that effectively induces degradation of the BRD4 protein, exhibiting a DC50 value of 280 nM (Dmax=77%). This compound not only selectively diminishes BRD4 levels but also promotes the upregulation of BRD2 and BRD3 protein levels, making it a valuable tool for studying the role of bromodomain proteins in cellular processes. Its low cytotoxicity profile compared to other BRD4 inhibitors highlights its potential for use in various research applications, including cancer biology and epigenetic regulation studies. -
PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-3 is a selective dual inhibitor targeting bromodomain 4 (BRD4) and polo-like kinase 1 (PLK1). This compound effectively inhibits BRD4-BD1, PLK1, and BRDT-BD1, exhibiting IC50 values of 0.059 µM, 0.127 µM, and 0.245 µM, respectively. PLK1/BRD4-IN-3 can be employed in research applications focused on cancer biology, particularly in studies investigating cell proliferation and transcriptional regulation. -
CREB-CBP Complex Inhibitor
Naphthol AS-MX phosphate is an inhibitor of the CREB-CBP transcription factor complex, functioning to disrupt its activity. This compound exhibits significant antitumor effects against lung cancer cells, demonstrating an IC50 value of 3.701 μmol/L for inhibiting cell proliferation, as well as reducing colony formation and anchorage-independent growth in soft agar assays. Naphthol AS-MX phosphate serves as a valuable tool for research on KRAS-mutated lung cancer, particularly in instances characterized by poor chemotherapy resistance and unfavorable prognoses. -
BET Inhibitor
I-BET787 is an orally active inhibitor of bromodomain and extraterminal (BET) proteins, specifically targeting BRD4 with pIC50 values of 7.1 for BD1 and 5.9 for BD2. This compound exhibits anti-inflammatory properties in murine models, making it a valuable tool for studying inflammatory pathways and the role of BET proteins in various diseases. I-BET787 is utilized in research focused on cancer, cardiovascular diseases, and autoimmune disorders. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-2 is a selective inhibitor targeting the bromodomain of the polybromo-1 (PBRM1) protein. With a binding affinity characterized by a Kd of 9.3 μM and an IC50 of 1.0 μM, this compound exhibits potent inhibitory activity against PBRM1-BD2. PBRM1-BD2-IN-2 is suitable for research focused on cancer biology and the investigation of epigenetic regulation mechanisms in tumorigenesis.
