Catalog No.
Product Name
Application
Product Information
Citations
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BRD4 PROTAC Degrader
PROTAC BRD4 Degrader-34 is a selective degrader that targets the bromodomain-containing protein 4 (BRD4) through a proteolysis-targeting chimera (PROTAC) mechanism. It induces the degradation of the BRD4-BD2 domain via the VHL E3 ubiquitin ligase system. This compound has significant potential for use in cancer research, enabling investigations into the therapeutic effects of targeting BRD4 in oncogenic pathways. -
BET bromodomain Ligand
TC AC 28 is a high-affinity ligand for bromodomain and extraterminal (BET) proteins, demonstrating Kd values of 40 nM for Brd2(2) and 800 nM for Brd2(1). This compound exhibits significant biological activity in regulating gene expression through the modulation of acetylated lysine recognition. TC AC 28 is applicable in research focusing on cancer, inflammation, and other diseases associated with BET protein function. -
BET Inhibitor
BRD4 Inhibitor-19 is a small molecule inhibitor targeting the bromodomain and extraterminal (BET) family, specifically inhibiting BRD4 with an IC50 of 55 nM at the BRD4-BD1 site. This compound exhibits significant anti-proliferative effects, making it a valuable tool in the study of multiple myeloma and related hematological malignancies. Researchers can utilize BRD4 Inhibitor-19 to explore the roles of BET proteins in cancer biology and evaluate potential therapeutic strategies in targeting aberrant gene expression. -
BET Inhibitor
BET-IN-27 is a potent inhibitor of bromodomain and extraterminal (BET) proteins, demonstrating IC50 values of 3.3 nM for BRD4-BD2, 3.4 nM for BRD4-BD1, 4.1 nM for BRD2-BD1, 20.4 nM for BRD3-BD1, and 42.0 nM for BRDT-BD1. This compound exhibits significant anti-proliferative effects, making it a valuable tool for research in cancer biology and therapeutic development targeting BET protein pathways. Its selective inhibition profile allows for further exploration of BET proteins in various disease models. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4 degrader-37 is a proteolysis-targeting chimera (PROTAC) that selectively degrades SMARCA2 and SMARCA4 proteins. It exhibits a potent inhibitory concentration (IC50) of ≤0.1 μM, highlighting its efficacy in disrupting these bromodomain-containing proteins. This reagent is suitable for applications in cancer research and therapeutic development, particularly in studies involving epigenetic modulation and chromatin remodeling. -
BET/BRD4 Probe
BiBET is a bivalent chemical probe targeting the BET family of bromodomain-containing proteins, specifically BRD4. It exhibits the ability to simultaneously bind to two bromodomains through a cis-binding mechanism. This unique interaction profile makes BiBET valuable for studying the role of BET proteins in cellular processes, particularly in cancer biology and inflammatory responses. Researchers can utilize BiBET to investigate the regulatory mechanisms of gene expression mediated by BRD4 and explore potential therapeutic strategies against related diseases. -
BET Inhibitor
BETi-211 is a potent BET inhibitor with a Ki value of less than 1 nM. It selectively inhibits the growth of triple-negative breast cancer (TNBC) cell lines, exhibiting an IC50 of less than 1 μM. BETi-211 effectively induces degradation of BET proteins, leading to significant suppression of tumor growth in xenograft models of breast cancer, making it a valuable tool for cancer research and therapeutic development. -
BRD4 Inhibitor
BRD4 Inhibitor-33 is a selective inhibitor of Bromodomain-containing protein 4 (BRD4), which plays a crucial role in regulating gene expression through the recognition of acetylated lysines. This compound has demonstrated significant potential in studies related to acute and chronic kidney diseases, making it valuable for researchers investigating therapeutic approaches for renal pathologies. Its mechanism of action may facilitate insights into the molecular underpinnings of kidney dysfunction and inform future treatment strategies. -
CBP/EP300 Inhibitor
I-CBP112 hydrochloride is a selective inhibitor of CBP and EP300, acting through direct binding to their bromodomains with dissociation constants of 142 nM and 625 nM, respectively. This compound has been shown to significantly diminish the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells both in vitro and in vivo, demonstrating dose-dependent efficacy. Additionally, I-CBP112 enhances the cytotoxic effects of the BET bromodomain inhibitor JQ1 and doxorubicin, making it a valuable tool for research in cancer therapeutics and epigenetic regulation. -
BRD4 Inhibitor
BRD4 Inhibitor-32 is a potent inhibitor of the Bromodomain-containing protein 4 (BRD4), targeting the interaction between BRD4 and acetylated histones. This compound exhibits significant biological activity in the modulation of inflammatory pathways and has potential applications in the study of acute and chronic kidney diseases. It serves as a valuable tool in research aimed at understanding the role of BRD4 in renal pathophysiology and therapeutic intervention. -
BET Inhibitor
BET-IN-24 is a bromodomain and extra-terminal (BET) inhibitor that selectively targets BET proteins. This compound is known to modulate gene expression and has demonstrated significant biological activity in various research contexts, including virology, heart failure, inflammation, central nervous system (CNS) diseases, and cancer. Its ability to inhibit BET proteins makes it a valuable tool for exploring the underlying mechanisms of these conditions and assessing potential therapeutic strategies. -
CBP/p300 Inhibitor
XDM-CBP is a potent inhibitor of the CBP/p300 transcriptional co-activators. This compound effectively disrupts CBP/p300-mediated signaling pathways, making it valuable for investigating the role of these proteins in various malignancies, including malignant melanoma, breast cancer, and leukemia. XDM-CBP serves as an important tool in cancer research, aiding in the understanding of tumorigenesis and potential therapeutic strategies. -
SMARCA2/4 Ligand
SMARCA2/4-ligand-5 is a selective ligand targeting the SMARCA2 and SMARCA4 proteins, functioning as a crucial component in the PROTAC SMARCA2/4 degrader-37. This compound demonstrates potent biological activity, achieving an IC50 of ≤0.1 μM, making it suitable for applications in targeted protein degradation studies. Research utilizing SMARCA2/4-ligand-5 contributes to understanding the roles of these chromatin remodelers in various biological processes and cancer biology. -
BRDT-BD2 Inhibitor
CDD-1147 is a selective inhibitor of the BRDT-BD2 domain, exhibiting an IC50 of 94 nM. This compound is primarily utilized in research investigating non-hormonal contraceptive methods for males. Its ability to hinder BRDT interactions facilitates the exploration of reproductive targets, contributing to the advancement of male contraceptive solutions. -
CBP bromodomain Inhibitor
CBP/p300-IN-24 is a selective inhibitor of the CBP bromodomain, exhibiting an IC50 of 32 μM and demonstrating notable selectivity over the BRD4 BD-1 bromodomain. This compound interacts with the acetyl lysine binding pocket, establishing hydrogen bonds with Asn1168 and a solvent-mediated hydrogen bond with Tyr1125, alongside hydrophobic interactions with Leu1120, Ile1122, and Val1174. CBP/p300-IN-24 is useful for investigating the role of CBP in various signaling pathways and disease states, particularly in cancer research and epigenetic studies. -
SMARCA2 PROTAC Degrader
PRT3789 is a selective PROTAC degrader targeting SMARCA2, exhibiting a DC50 of 0.72 nM in HeLa cells for SMARCA2 and 14 nM for SMARCA4. By forming a stable ternary complex with Von Hippel-Lindau (VHL) E3 ligase, PRT3789 facilitates polyubiquitination and subsequent proteasomal degradation of SMARCA2. This compound effectively disrupts the integrity of the SWI/SNF chromatin remodeling complex, leading to the downregulation of oncogenic gene expression, decreased chromatin accessibility, and enhanced expression of genes related to antigen processing and presentation. PRT3789 is applicable in research on SMARCA4-mutated solid tumors, including non-small cell lung cancer, endometrial cancer, and several other malignancies. -
SMARCA2 Inhibitor
FHD-909 is a selective inhibitor of SMARCA2 (BRM), exhibiting IC50 values of 2.5 nM for SMARCA2 and 123.7 nM for SMARCA4. This compound serves as a valuable tool for the investigation of BAF complex-related disorders, including various cancer types. Researchers can leverage FHD-909 to elucidate the role of SMARCA2 in oncogenesis and other pathological conditions associated with chromatin remodeling. -
SMARCA2 PROTAC Degrader
NEP202 is a potent SMARCA2 PROTAC degrader that engages the GID4 E3 ligase to facilitate targeted protein degradation. This reagent is valuable for cancer research, enabling the selective degradation of SMARCA2, a key protein implicated in various oncogenic processes. NEP202 offers researchers a powerful tool for studying the role of SMARCA2 in tumor biology and therapeutic responses. -
SMARCA2 Ligand
SMARCA2 ligand-11 is a specific ligand for the chromatin remodeling factor SMARCA2, facilitating the development of PROTACs such as SMARCA2 degrader-32. This compound is instrumental in research applications focused on targeted protein degradation, particularly in studies aimed at elucidating the role of SMARCA2 in various biological processes and diseases. Its ability to selectively engage with SMARCA2 allows for investigations into novel therapeutic strategies in cancer and other conditions where SMARCA2 activity is implicated. -
SMARCA2 Degrader
PROTAC SMARCA2 degrader-32 is a targeted protein degradation agent that selectively degrades SMARCA2 with a DC50 of 1.3 nM. This compound demonstrates significant inhibitory activity against lung cancer cell line NCI-H838, with a GI50 of 34 nM. Its application in research includes studies on the role of SMARCA2 in cancer biology and therapeutic strategies leveraging PROTAC technology for targeted degradation. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-24 is a selective degrader targeting the SMARCA2 protein through a PROTAC mechanism. It exhibits potent biological activity with a DC50 value of less than 0.1 µM in HeLa cells, facilitating effective degradation of SMARCA2. Additionally, it demonstrates lower activity against SMARCA4, with a DC50 greater than 10 μM in the same cellular context. This compound serves as a valuable tool for studying the functional roles of SMARCA2 in various biological processes and disease models. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-22 is a potent proteolysis-targeting chimera (PROTAC) specifically designed to degrade the SMARCA2 protein. It exhibits a degradation efficacy of 94% at a concentration of 100 nM. Additionally, PROTAC SMARCA2 degrader-22 demonstrates effective inhibition of A549 cell proliferation with an EC50 of less than 250 nM, making it a valuable tool for research into cancer biology and therapeutic applications targeting the chromatin remodeling complex. -
PROTAC SMARCA2 Degrader
PROTAC SMARCA2 Degrader-27 is a proteolysis-targeting chimera (PROTAC) that selectively degrades the SMARCA2 protein. By utilizing a VHL ligand, it engages the ubiquitin-proteasome system to induce targeted degradation of SMARCA2, demonstrating significant potential for research in cancer biology. This compound allows for the investigation of SMARCA2's role in oncogenesis and therapeutic resistance, contributing to the development of novel cancer treatments. -
SMARCA2 PROTAC Degrader
PROTAC A515 is a targeted protein degradation agent that selectively degradas the SMARCA2 protein. By promoting the ubiquitination of SMARCA2, it facilitates its subsequent degradation via the proteasome pathway. This compound is valuable for cancer research, allowing for the investigation of SMARCA2's role in tumorigenesis and potential therapeutic applications. -
SMARCA2 Ligand
SMARCA2 ligand-8 acts as a selective ligand for the target protein SMARCA2, facilitating the synthesis of the PROTAC SMARCA2/4-degrader-35. This compound is instrumental in research applications focused on targeted protein degradation, offering insights into the modulation of gene regulation and chromatin remodeling. Its utility in developing innovative degraders highlights its significance in the study of cancer biology and potential therapeutic interventions. -
BRD4 PROTAC
Lenalidomide-CO-C7-NH2 is a CRBN-dependent intermediate designed as a BRD4-targeting PROTAC degrader. This compound facilitates the selective degradation of the oncoprotein BRD4, leading to decreased cancer cell proliferation, cell cycle arrest, and enhanced apoptosis. It demonstrates noteworthy anti-tumor efficacy in xenograft models, making Lenalidomide-CO-C7-NH2 a valuable tool for investigating mechanisms in acute myeloid leukemia research. -
BRD4 BD2 Inhibitor
BRD4-BD1/2-IN-3 is a selective inhibitor of the BRD4 bromodomain 2 (BD2), exhibiting an IC50 of 0.41 nM for BRD4 BD2 compared to BRD4 BD1. This compound effectively inhibits LPS-induced expression of IL-6, demonstrating significant anti-inflammatory properties through modulation of the TNF and NF-κB signaling pathways. BRD4-BD1/2-IN-3 is valuable for research focused on inflammatory diseases. -
SMARCA2 PROTAC degrader
YD54 is a PROTAC designed to induce degradation of the SMARCA2 protein, exhibiting a DC50 of 3.5 nM. This compound utilizes a targeted approach to promote the ubiquitination and proteasomal degradation of SMARCA2, making it a valuable tool for studying SMARCA2-dependent biological processes. YD54 is suitable for applications in cancer research and cellular signaling investigations, where modulation of SWI/SNF complex activity is critical. -
SMARCA2 Degrader
PROTAC SMARCA2 degrader-8 is a selective degrader targeting the SMARCA2 protein, exhibiting a DC50 of 28 nM in A375 cells. This compound facilitates the ubiquitination and subsequent proteasomal degradation of SMARCA2, thereby effectively reducing its cellular levels. It is particularly useful for studies investigating the role of SMARCA2 in various cancer types and for elucidating its mechanisms of action in cellular processes. -
BRD4 PROTAC
MS83 is a novel PROTAC that employs a KEAP1 ligand to target and degrade BRD4, along with its homologs BRD3 and BRD2. By harnessing the ubiquitin-proteasome system, MS83 facilitates targeted protein degradation, providing a powerful tool for dissecting the functional roles of BRD4 in cellular processes. This compound is particularly relevant for research on cancer and epigenetic regulation, offering insights into therapeutic strategies that leverage targeted protein degradation. -
BRD9 Degrader PROTAC
PROTAC BRD9 Degrader-5 is a proteolysis-targeting chimera (PROTAC) that facilitates the targeted degradation of the bromodomain-containing protein BRD9. This compound employs the cellular ubiquitin-proteasome pathway to promote the selective elimination of BRD9, leading to the modulation of biological pathways associated with cancer and other diseases. It serves as a valuable tool for researchers investigating the role of BRD9 in various cellular processes and therapeutic interventions. -
SMARCA2 Degrader degrader
SMARCA2 degrader-20 is a potent PROTAC that targets the SMARCA2 protein for degradation, exhibiting a DC50 of less than 100 nM in A549 cells. This degrader is valuable for studying the functional consequences of SMARCA2 depletion in cancer biology and epigenetic regulation. Its high efficacy facilitates research into targeted protein degradation strategies and their therapeutic potential in oncology. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-17 (compound I-290) is a potent PROTAC degrader designed to selectively target and degrade the SMARCA2 protein. It demonstrates effective degradation in A549 cells with a DC50 value of less than 100 nM and achieves a maximum degradation rate exceeding 90% after 24 hours of treatment. This reagent is valuable for research in cancer biology and the investigation of SMARCA2-related pathways. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-16 (compound I-278) is a PROTAC designed to selectively degrade the SMARCA2 protein. It demonstrates significant biological activity by efficiently reducing SMARCA2 levels in A549 cells, achieving a DC50 value of less than 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. This compound is invaluable for research applications involving the modulation of SMARCA2 in cancer biology and therapeutic development. -
SMARCA2 Degrader
PROTAC SMARCA2 degrader-25 is a potent heterobifunctional molecule that targets SMARCA2 for degradation via the proteasome pathway. With a DC50 value of less than 0.01 μM, this compound efficiently engages the target protein using a specific ligand, a link to facilitate the interaction, and an E3 ligase ligand to promote ubiquitination. Its high efficiency makes it a valuable tool in investigating the role of SMARCA2 in various biological processes and diseases. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-32 is a PROTAC degrader that targets SMARCA2 and SMARCA4 proteins. It demonstrates effective degradation of these proteins in A549 cells, achieving DC50 values below 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. This compound is suitable for research applications focusing on the regulation of chromatin remodeling and its implications in various cancers. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-16 (compound I-337) is a potent PROTAC degrader designed to selectively target and degrade SMARCA2 and SMARCA4 proteins. It demonstrates significant biological activity in A549 cells, achieving DC50 values of less than 100 nM and over 90% maximum degradation rate (Dmax%) after 24 hours of treatment. This compound is valuable for research applications focused on understanding the role of SMARCA2 and SMARCA4 in tumor biology and for exploring targeted protein degradation strategies. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-12 is a molecule specifically designed to induce degradation of the SMARCA2 protein. This PROTAC exhibits potent biological activity, effectively degrading SMARCA2 proteins in A549 cells with a DC50 value of less than 100 nM and achieving over 90% maximum degradation after 24 hours of treatment. This reagent is suitable for research applications focusing on targeted protein degradation and the functional analysis of SMARCA2 in cancer biology. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-35 is an efficient degrader targeting the SMARCA2 and SMARCA4 proteins, demonstrating a DC50 of less than 2.5 nM. This compound promotes the ubiquitination and subsequent degradation of the target proteins via the recruitment of E3 ligases. Its potent biological activity makes it valuable for research applications focused on epigenetics and cancer biology, particularly in studies targeting the modulation of chromatin remodeling complexes. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-14 is a targeted protein degradation compound designed to selectively degrade the SMARCA2 protein. Demonstrating a DC50 value of less than 100 nM, it achieves maximum degradation rates exceeding 90% in A549 cells following a 24-hour treatment. This reagent serves as a valuable tool for research applications focused on elucidating the role of SMARCA2 in various biological processes and therapeutic contexts. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4 degrader-41 is a potent degrader targeting the SMARCA2 and SMARCA4 proteins, exhibiting DC50 and IC50 values both below 0.1 μM. This compound facilitates the selective degradation of these ATP-dependent chromatin remodelers, making it a valuable tool for studying SMARCA2/4-related or SMARCA2/4-deficient cancers. Its application in cancer research can aid in elucidating the role of these proteins in tumorigenesis and therapeutic resistance. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-7 is a selective protein degrader that targets SMARCA2 and SMARCA4 proteins. Demonstrating effective degradation in A549 cells, it achieves DC50 values of less than 100 nM and results in more than 90% degradation after 24 hours of treatment. This compound serves as a valuable tool for investigating the roles of SMARCA2 and SMARCA4 in cancer biology and other research applications involving epigenetic regulation. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-22 is a targeted protein degradation reagent designed to selectively degrade SMARCA2 and SMARCA4 proteins. This compound effectively reduces SMARCA2 and SMARCA4 levels in A549 cells, achieving DC50 values of less than 100 nM and exceeding 90% maximum degradation rate after 24 hours of treatment. It is a valuable tool for research into the role of these proteins in various biological processes and disease states. -
BRD9 PROTAC Degrader
PROTAC BRD9 Degrader-8 is a selective BRD9 PROTAC degrader that operates through targeted protein degradation, exhibiting a DC50 of 16 pM. This compound effectively induces cell cycle arrest in the G1 phase and promotes apoptosis, making it a valuable tool for studies focused on acute myeloid leukemia and diffuse large B-cell lymphoma. Its mechanism provides a unique approach to modulating BRD9 levels in therapeutic research. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-15 is a targeted PROTAC that selectively degrades the SMARCA2 protein. Demonstrating a DC50 value of less than 100 nM, this compound achieves over 90% maximum degradation (Dmax%) within 24 hours in A549 cells. Its ability to modulate SMARCA2 levels makes it a valuable tool for research exploring the role of this protein in cancer biology and epigenetic regulation. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-23 is a targeted proteolysis-targeting chimera (PROTAC) designed to degrade SMARCA2 and SMARCA4 proteins. This compound effectively induces degradation of both targets in A549 cells, exhibiting a DC50 of less than 100 nM and achieving a maximum degradation rate exceeding 90% after 24 hours of treatment. It is suitable for use in studies aimed at understanding the functional roles of SWI/SNF chromatin remodeling complexes in cancer and other disease models. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-10 is a targeted protein degrader that specifically engages and promotes the degradation of SMARCA2. This compound demonstrates effective degradation of SMARCA2 proteins in A549 cells, achieving a DC50 value of less than 100 nM and a maximum degradation rate exceeding 90% after 24 hours of treatment. It serves as a valuable tool for research applications focused on elucidating the biological roles of SMARCA2 and its implications in cancer biology and therapeutics. -
SMARCA2 PROTAC degrader
PROTAC SMARCA2 degrader-6 (compound I-427) is a PROTAC agent specifically designed to target and induce the degradation of SMARCA2 proteins. This compound effectively degrades SMARCA2 in A549 cells, achieving a DC50 value of less than 100 nM and demonstrating a maximum degradation rate exceeding 90% within 24 hours of treatment. It serves as a powerful tool for investigating the role of SMARCA2 in various biological processes and potential therapeutic applications in cancer research. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-3 is a potent SMARCA2/4 degrader that utilizes the VH032-NH2 framework for targeted protein degradation. It exhibits a degradation potency (DC50) of less than 100 nM in MV4-11 cells, facilitating the selective depletion of SMARCA2 and SMARCA4 proteins. This compound is valuable for research applications involving chromatin remodeling and cancer biology, providing insights into the functional roles of these proteins in various cellular contexts. -
SMARCA2/4 PROTAC degrader
PROTAC SMARCA2/4-degrader-1 is a PROTAC degrader specifically designed to target SMARCA2 and SMARCA4 proteins. It effectively degrades these proteins in A549 cells, exhibiting a DC50 of less than 100 nM and achieving over 90% degradation after 24 hours of treatment. This compound is suitable for research applications focused on understanding the role of SMARCA2 and SMARCA4 in various biological processes and disease models.
