Catalog No.
Product Name
Application
Product Information
Citations
-
BRD4 D1 Inhibitor
BRD4 D1-IN-2 is a selective inhibitor targeting BRD4 D1, exhibiting a potent IC50 of less than 0.092 µM. With an affinity of 15 nM for BRD4 D1, this compound demonstrates over 500-fold selectivity against both BRD2 D1 and BRD4 D2, as determined by isothermal titration calorimetry (ITC). BRD4 D1-IN-2 is valuable for research applications exploring the role of BRD4 in epigenetic regulation and its implications in cancer and other diseases. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-28 is a PROTAC (Proteolysis Targeting Chimeras) designed to target and degrade SMARCA2 and SMARCA4 proteins. This compound utilizes a combination of a CRL2VHL ligand, a linker, and a SMARCA-BD ligand to facilitate targeted degradation, thus modulating the expression of these critical chromatin remodeling factors. Its primary applications include studying the functional roles of SMARCA2 and SMARCA4 in cancer biology and epigenetic regulation, making it a valuable tool for researchers investigating therapeutic strategies in oncology and related fields. -
PROTAC BRD4 Degrader
(S)-GNE-987 is a selective PROTAC BRD4 degrader that functions by abrogating binding to von Hippel-Lindau while maintaining specific interactions with BRD4 bromodomains. With IC50 values of 4 nM for BD1 and 3.9 nM for BD2, (S)-GNE-987 facilitates targeted degradation of BRD4, making it a valuable tool in research focused on epigenetic regulation and cancer therapy. Additionally, it can be instrumental in the design of PROTAC-Antibody Conjugates (PAC) for enhanced therapeutic applications. -
BRD4 Inhibitor
BRD4-IN-5 is a selective inhibitor of the bromodomain protein BRD4. It demonstrates notable activity with Ki values of 9.7 nM for the first bromodomain (BDI) and 16.1 nM for the second bromodomain (BDII). This compound is valuable for use in cancer research, particularly in studies exploring the role of BRD4 in oncogenic transcriptional regulation and therapeutic interventions. -
BRDT-BD2 Inhibitor
CDD-1154 is an aminopyrimidine analog that functions as a specific inhibitor of the bromodomain testis-specific protein BRDT-BD2, with an IC50 of 139 nM. This compound is primarily utilized in male contraceptive research, providing valuable insights into fertility regulation and the development of novel contraceptive methods. Its selective activity against BRDT-BD2 supports investigations into potential therapeutic applications in reproductive health. -
BRD4 Inhibitor
BRD4 Inhibitor-29 is a selective bromodomain-containing protein 4 (BRD4) inhibitor with an IC50 of less than 100 nM. This compound exhibits notable antiproliferative effects against prostate cancer cells, making it a valuable tool for investigating the role of BRD4 in cancer biology and therapeutic applications. It can be utilized in research aimed at understanding the mechanisms of tumorigenesis and developing new treatment strategies for BRD4-dependent cancers. -
BRD4-DCAF1 Degrader
PROTAC BRD4-DCAF1 degrader-1 is a targeted protein degradation tool that recruits the E3 ligase complex for the ubiquitination and subsequent proteasomal degradation of BRD4-DCAF1. With a DC50 range of 10-100 nM, this compound effectively modulates BRD4 signaling pathways. It is particularly useful in cancer research and studies focused on the therapeutic potential of targeting bromodomain-containing proteins. -
BRD9 Binder
PROTAC BRD9-binding moiety 5 functions as a selective binder to the BRD9 protein, exhibiting an IC50 value of 4.20 μM. This compound is suitable for the synthesis of PROTACs, which target BRD9 for degradation. Additionally, PROTAC BRD9-binding moiety 5 demonstrates antiproliferative activity against various cancer cell lines, making it a valuable tool in cancer research and drug development. -
CBP Inhibitor
DC-CPin7 is a selective inhibitor of the CREB-binding protein (CBP) bromodomain, demonstrating an IC50 value of 2.5 μM. This compound modulates CBP-mediated signaling pathways, making it relevant for studies involving transcriptional regulation and epigenetic modifications. DC-CPin7 is suitable for research applications focused on cancer biology and other diseases linked to dysregulated gene expression. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-4 (Compound I-434) is a targeted PROTAC degrader that specifically promotes the degradation of the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It demonstrates robust biological activity, achieving degradation of SMARCA2 and SMARCA4 in MV411 and A549 cell lines with DC50 values below 100 nM. This compound is valuable for research applications focused on the modulation of chromatin remodeling processes and the elucidation of the roles of SMARCA proteins in cancer biology. -
BET Inhibitor
XL-126 is a selective inhibitor of the bromodomain and extraterminal (BET) protein family, specifically targeting BD1 with a Kd of 8.9 nM. This compound demonstrates significant anti-inflammatory properties while preserving platelet function, making it a valuable tool for research into inflammatory disorders and hematological conditions. XL-126 is particularly useful in studies aimed at understanding the role of BET proteins in disease pathways and therapeutics. -
BRD9 PROTAC Degrader
dBRD9 dihydrochloride is a selective degrader of BRD9, targeting the protein for degradation through the PROTAC mechanism. This compound demonstrates efficacy in inhibiting the proliferation of acute myeloid leukemia (AML) cell lines, making it a valuable tool for research in cancer biology and therapeutic development. Its utility in studying BRD9's role in oncogenic processes positions dBRD9 dihydrochloride as a significant reagent for investigators exploring targeted protein degradation strategies. -
BRD4 Inhibitor
Penipanoid C is a selective BRD4 inhibitor derived from the marine sediment-derived fungus Penicillium paneum SD-44. This compound exhibits anti-inflammatory properties and demonstrates cytotoxic effects on SMMC-7721 cells. Penipanoid C serves as a valuable tool for research into inflammatory diseases and related therapeutic applications. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-27 is a PROTAC-based degrader that specifically targets the SMARCA2 and SMARCA4 proteins. This compound induces targeted protein degradation, facilitating the selective modulation of these chromatin remodelers. It is essential for research applications exploring the roles of SMARCA2 and SMARCA4 in cancer and other diseases, allowing for valuable insights into epigenetic regulation and therapeutic strategies. -
BRD4-BD1 Inhibitor
BRD4-BD1-IN-2 is a selective inhibitor of BRD4-BD1, exhibiting an IC50 of 2.51 µM, demonstrating a 20-fold selectivity over BD2. This compound is valuable in research focused on cancer and cardiovascular diseases, facilitating the investigation of BRD4’s role in oncogenic processes and cardiac function. Its specificity makes it a useful tool for probing the biological mechanisms underlying these conditions. -
PROTAC SMARCA2 Degrader
PROTAC SMARCA2 degrader-30 is an investigative PROTAC designed for targeted degradation of SMARCA2 protein. It demonstrates potent biological activity with a DC50 of less than 100 nM in H1299 cells, making it a valuable tool for research in cancer biology and therapeutic development. This compound may facilitate studies on the role of SMARCA2 in cellular processes and its potential as a therapeutic target in oncogenic pathways. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-3 is a targeted protein degradation compound that operates through the recruitment of von Hippel-Lindau (VHL) ligands to promote the ubiquitination and subsequent proteasomal degradation of the BRD4 protein. This compound demonstrates significant efficacy in downregulating BRD4, a key regulator in various cancers and inflammatory diseases. Research applications for PROTAC BRD4 Degrader-3 include the investigation of therapeutic strategies for cancer treatment and exploring the role of BRD4 in gene expression and signaling pathways. -
BET Inhibitor
XY153 is a BD2-selective BET inhibitor that primarily targets the bromodomain 2 (BD2) of the BRD4 protein. It exhibits potent binding affinity to BRD4 BD2, BRD3 BD2, and BRD2 BD2, with IC50 values of 0.79 nM, 5.31 nM, and 5.09 nM, respectively. XY153 demonstrates significant antiproliferative effects across various tumor cell lines and is applicable in research focused on acute myeloid leukemia (AML) and cancer therapeutics. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-5 is a PROTAC degrader targeting the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It effectively degrades SMARCA2 in MV411 and A549 cell lines with a DC50 of less than 100 nM, and targets SMARCA4 in MV411 with a DC50 ranging from 100 to 500 nM. This compound is instrumental for research applications focused on epigenetic regulation and oncogenic pathways involving SWI/SNF complex alterations. -
SMARCA2-BRD Inhibitor
DCSM06-05 is a potent inhibitor of the SMARCA2-BRD interaction, exhibiting an IC50 value of 9 µM and a Kd value of 22.4 µM. This compound is instrumental in studies focused on chromatin remodeling and precision oncology, as it modulates the activity of the SWI/SNF complex. Research applications include investigating the role of SMARCA2 in tumorigenesis and therapeutic resistance in various cancers. -
BET Bromodomain Inhibitor
BET bromodomain inhibitor 3 selectively inhibits BET bromodomains, demonstrating an inhibitory effect against BrdT with a Ki value greater than 40 µM. This compound is instrumental in studying various biological processes and has potential applications in research related to contraception, cancer, and cardiovascular diseases. Its mechanism of action makes it a valuable tool for investigating the role of BET proteins in gene regulation and associated pathologies. -
SMARCA2 ATPase Inhibitor
SMARCA2-IN-10 is a selective inhibitor of the SMARCA2 ATPase domain, with an IC50 value of 17.676 μM. This compound has been shown to induce cell death in tumors lacking SMARCA4, making it a valuable tool for investigating SMARCA4-mutant non-small cell lung cancer, small cell ovarian carcinoma, and melanoma. Its targeting of the SMARCA2 ATPase offers significant potential for advancing research in these cancer types. -
SMARCA2/4 Inhibitor
SMARCA2/4-IN-1 is a selective inhibitor targeting SMARCA2 and SMARCA4, with reported IC50 values of 3.8 µM and 1.7 µM, respectively. This compound demonstrates significant inhibition of these chromatin remodeling factors, making it a valuable tool for studying epigenetic regulation and its impact on gene expression. It has potential applications in cancer research and therapeutic investigations aimed at manipulating chromatin dynamics. -
PBRM1 Bromodomain Inhibitor
PBRM1-BD2-IN-4 is a selective inhibitor of the PBRM1 bromodomain, exhibiting Kd values of 5.5 μM and 11.1 μM for PBRM1-BD2 and PBRM1-BD5, respectively, with an IC50 of 0.2 μM for PBRM1-BD2. This compound is instrumental in studying the role of PBRM1 in cancer biology and may contribute to the development of anticancer therapies targeting bromodomain-containing proteins. Its high potency and specificity make it a valuable tool for research focused on epigenetic regulation in cancer contexts. -
BRD4 Inhibitor
BRD4 Inhibitor-34 is a selective inhibitor of the bromodomain and extraterminal (BET) protein BRD4, exhibiting an IC50 value of 24 μM. This compound effectively disrupts BRD4's interaction with acetylated lysines, leading to the modulation of gene expression and cellular signaling pathways. BRD4 Inhibitor-34 is utilized in research applications involving cancer biology, inflammation, and epigenetic regulation, providing valuable insights into the therapeutic potential against various diseases. -
SMARCA Inhibitor
SMARCA2-IN-4 is a selective inhibitor of the SWI/SNF chromatin remodeling complex, specifically targeting the bromodomains of SMARCA proteins. This compound demonstrates high binding affinity for PB1, SMARCA2B, and SMARCA4, with dissociation constants (Kd) of 124 nM, 262 nM, and 417 nM, respectively. SMARCA2-IN-4 is valuable for studies investigating the roles of chromatin remodeling in gene expression and cellular processes, offering potential insights into cancer biology and epigenetic regulation. -
BRD4 PROTAC Degrader
NEP108 is a GID4 E3 ligase-based PROTAC degrader specifically targeting BRD4. With a DC50 value of approximately 3.8 μM, NEP108 demonstrates a strong affinity for GID4, exhibiting a KD value of 0.22 μM, while the KD value for its trimeric complex is 2.85 μM. This compound is suitable for research applications in cancer biology, facilitating the study of BRD4 degradation and its implications in therapeutic strategies. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-22 is a PROTAC-based degrader targeting the bromodomain-containing protein 4 (BRD4). This compound demonstrates significant biological activity with a pDC50 value of 9.2 in MOLT4 cells after 24 hours of treatment. It is primarily utilized in research applications focused on exploring the therapeutic potential of targeted protein degradation in various cancers and other BRD4-related disorders. -
BET Inhibitor
BET-IN-1 is a potent inhibitor of bromodomain and extraterminal (BET) proteins, which play a crucial role in regulating gene expression through acetylated lysine recognition. It demonstrates significant brain penetration and favorable metabolic stability, making it a valuable tool for studying the role of BET proteins in various cellular processes. BET-IN-1 is particularly applicable in research related to cancer biology and neurodegenerative disorders, aiding in the exploration of therapeutic strategies targeting epigenetic regulation. -
BRD4 Inhibitor
CeMMEC2 is a potent inhibitor of the bromodomain-containing protein 4 (BRD4) with an IC50 of 0.9 μM. This compound effectively disrupts BRD4-driven transcriptional programs, making it a valuable tool for studying epigenetic regulation. CeMMEC2 is particularly useful in cancer research and the investigation of inflammatory diseases, providing insights into therapeutic strategies targeting BRD4-mediated pathways. -
BRD4 Inhibitor
BRD4-IN-6 is a selective inhibitor of the Bromodomain-containing protein 4 (BRD4), a critical regulator of gene expression and a key target in cancer research. This compound effectively disrupts the BRD4-dependent transcriptional activation, leading to decreased cell proliferation in various cancer models. Its application extends to studying the mechanisms of BRD4 in epigenetic regulation and the development of potential therapeutic strategies for cancer treatment. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-30 is a targeted protein degradation agent specifically designed to degrade the catalytic subunits of the SWI/SNF complex, SMARCA2 and SMARCA4. This compound demonstrates effective degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, with a DC50 of less than 100 nM for both targets. It serves as a valuable tool for investigating the biological roles of SMARCA2 and SMARCA4 in various cancer models and for exploring potential therapeutic strategies in malignant conditions involving these proteins. -
BRD4 PROTAC Degrader
PROTAC BRD4 Degrader-35 is a PROTAC degrader specifically designed to target BRD4. This compound facilitates the ubiquitination and subsequent degradation of BRD4, making it a valuable tool in anti-cancer research. Its mechanism of action enables the modulation of BRD4-dependent pathways, providing insights into the therapeutic potential of BRD4 inhibition in various malignancies. -
CBP Bromodomain Inhibitor
Y08284 is a potent and selective inhibitor of the CBP bromodomain, exhibiting an IC50 of 4.21 nM. This compound effectively suppresses the proliferation of prostate cancer cell lines, including LNCaP, C4-2B, and 22Rv1. Its significant antitumor activity makes Y08284 a valuable tool for research focused on prostate cancer biology and bromodomain-related processes. -
CBP Bromodomain Inhibitor
Y08175 is a highly potent inhibitor of the CBP bromodomain, demonstrating significant inhibitory capacity with IC50 values of 37 nM and 178.15 nM in AlphaScreen and HTRF assays, respectively. This compound is valuable for investigating the role of CBP in oncogenic processes, particularly in the context of prostate cancer research. Its ability to selectively target the CBP bromodomain makes it a useful tool for studying bromodomain-mediated transcriptional regulation and associated pathways. -
BET Bromodomain Inhibitor
BET Bromodomain Inhibitor 2 selectively targets the bromodomains of BET proteins, exhibiting a potent inhibitory effect with an IC50 of 14.1 µM. This compound is critical for modulating gene expression linked to cancer and inflammation by disrupting the interaction between acetylated histones and BET proteins. It is applicable in various research contexts, including oncology and epigenetics studies, providing invaluable insights into therapeutic strategies targeting bromodomain-containing proteins. -
BRD4 Inhibitor
BRD4-IN-9 is a potent inhibitor of BRD4, exhibiting an IC50 value of 9.4 nM. It demonstrates significant efficacy in suppressing tumor growth, specifically in a mouse melanoma xenograft model. This compound is valuable for research focusing on cancer biology and epigenetic regulation. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2/4-degrader-8 is a specialized PROTAC targeting the catalytic subunit SMARCA2 of the SWI/SNF complex. This compound effectively degrades SMARCA2 with a DC50 of less than 100 nM in A549 cells, while also targeting SMARCA4 with equivalent efficiency in MV411 cells. It serves as a valuable tool in research focused on understanding the roles of these proteins in chromatin remodeling and their implications in various cancer types. -
Bromodomain Inhibitor
Bromodomain inhibitor-10 is a selective bromodomain inhibitor that targets BRD4-1 and BRD4-2 with Kd values of 15.0 nM and 2500 nM, respectively. This compound effectively inhibits the production of IL-12p40, making it valuable in studies related to immune response and inflammation. It is suitable for research applications investigating the roles of bromodomain proteins in various biological processes and disease states. -
p300/CBP Bromodomain Inhibitor
CZL-077 is a selective and potent inhibitor of the bromodomains of p300 and CBP, with IC50 values of 0.034 μM and 0.052 μM, respectively. It demonstrates high specificity for p300/CBP over BET proteins, making it a valuable tool in the study of epigenetic regulation. CZL-077 effectively inhibits the growth of multiple myeloma and prostate cancer cell lines, with IC50 values of 0.024 μM in OPM-2 and 5.6 μM in 22RV1 cells. Additionally, it exhibits significant antitumor activity in xenograft mouse models, supporting its potential use in cancer research. -
BRD4 Inhibitor
BRD4 Inhibitor-27 targets the bromodomain protein BRD4, demonstrating inhibitory activity with IC50 values of 9.6 μM for BRD4 BD1 and 11.3 μM for BRD4 BD2. This compound is valuable for research in cancer biology, providing insights into the roles of BRD4 in tumorigenesis and potential therapeutic applications in cancer treatment. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-5 is a potent degrader specifically designed to target the catalytic subunit SMARCA2 of the SWI/SNF chromatin remodeling complex. This compound effectively induces degradation of SMARCA2 in MV411 and A549 cell lines, demonstrating a DC50 of less than 100 nM, while also degrading SMARCA4 with a DC50 between 100-500 nM. This reagent is essential for researchers investigating the functional role of SMARCA2 and its associated pathways in cancer biology and other cellular processes. -
SMARCA2/4 Inhibitor
SMARCA2-IN-6 is a potent inhibitor of SMARCA2 and SMARCA4, exhibiting IC50 values under 5 nM for both targets. This compound effectively suppresses KRT80 gene expression in H1299 cells with an IC50 of 26 nM, and demonstrates significant antiproliferative effects in BRG1-mutant SKMEL5 cells, with an IC50 of 13 nM. SMARCA2-IN-6 serves as a valuable tool for research applications focused on chromatin remodeling and associated oncogenic pathways. -
BRD4 Inhibitor
BRD4-IN-7 is a selective inhibitor of the bromodomain-containing protein 4 (BRD4). By targeting BRD4, this compound plays a crucial role in modulating gene expression and has been shown to disrupt the interaction between BRD4 and acetylated histones. Its primary applications include cancer research and investigations into various diseases involving epigenetic regulation, making it a valuable tool for further studies on transcriptional control and associated pathways. -
BRD4-1 Inhibitor
Bromodomain inhibitor-9 is a selective inhibitor of BRD4-1, exhibiting a Kd of 12 nM. This compound has been shown to play a significant role in modulating biological pathways related to systemic and tissue inflammation, lipid metabolism, fibrosis, and chronic autoimmune diseases. Its application in research provides valuable insights into the therapeutic potential for addressing these conditions. -
BET Inhibitor
Y08060 is a selective inhibitor of Bromodomain and Extra-Terminal (BET) proteins. It demonstrates significant anti-proliferative effects on C4-2B and LNCaP prostate cancer cell lines, with IC50 values of 3.23 μM and 4.41 μM, respectively. Additionally, Y08060 effectively suppresses colony formation and androgen receptor (AR) expression in these cell lines, making it a valuable tool for research applications targeting prostate cancer biology. -
Bromodomain Inhibitor
Bromodomain inhibitor-13 is a selective inhibitor targeting bromodomain-containing proteins (BCPs), including SMARCA2, SMARCA4, and the bromodomain of PB1. It exhibits potent binding affinity with KD values of 37 nM for SMARCA2, 53 nM for SMARCA4, and 30 nM for PB1(5), alongside a KD of 190 nM for PB1(2). This compound is valuable for research into epigenetic regulation and the role of bromodomains in various cellular processes, making it a useful tool for studying gene expression modulation and protein interactions in cancer and other diseases. -
BRD4 PROTAC
WWL0245 is a highly selective BRD4 PROTAC that effectively induces degradation of BRD4 with a sub-nanomolar DC50 of less than 1 nM, while demonstrating significantly lower potency against BRD2/3 and PLK1 (DC50 > 1 μM). This compound exhibits remarkable cytotoxicity in BET inhibitor-sensitive cancer cell lines, particularly in androgen receptor-positive prostate cancer models. WWL0245 serves as a valuable research tool for exploring the biological functions of BRD4 and holds potential as a therapeutic candidate in the context of AR-positive prostate cancer. -
PROTAC BRD9 Degrader
(S,R)-CFT8634 is a selective PROTAC-class degrader targeting BRD9, designed for oral administration. This compound facilitates the ubiquitination and subsequent degradation of BRD9, which is implicated in various diseases characterized by abnormal cell proliferation. The structure comprises a BRD9 ligand, a CRBN ligase ligand, and a PROTAC linker, enabling effective recruitment of the E3 ligase for degradation. (S,R)-CFT8634 is a valuable tool for investigating BRD9-related biological processes and therapeutic strategies. -
Bromodomain Inhibitor
Bromodomain inhibitor-12 is a selective bromodomain inhibitor that interferes with the interaction between bromodomain-containing proteins and acetylated lysines. This compound exhibits significant biological activity in modulating chromatin dynamics and has potential applications in the study of autoimmune and inflammatory diseases. Its ability to inhibit bromodomain-mediated signaling pathways makes it a valuable tool for investigating therapeutic strategies in these conditions.
