Catalog No.
Product Name
Application
Product Information
Citations
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PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-2 is a proteolysis-targeting chimera (PROTAC) that selectively targets BRD4 and Cereblon. With an IC50 of 14.2 nM against the BRD4 BD1 domain, this compound effectively induces proteasomal degradation of BRD4. It is valuable for research applications investigating the role of BRD4 in transcription regulation, cancer biology, and other diseases associated with aberrant gene expression. -
PROTAC BRD4BD1L94V Degrader
XY-06-007 is a selective and potent bump-and-hole (B&H) PROTAC that degrades BRD4BD1L94V. It exhibits a degradation concentration (DC50) of 10 nM at 6 hours, effectively targeting BRD4BD1L94V without degrading off-target proteins. With favorable pharmacokinetic properties, XY-06-007 is suitable for in vivo studies and serves as a valuable tool for research into BRD4-related pathways and therapeutic applications. -
SMARCA2 PROTAC Degrader
SMD-3236 is a SMARCA2 PROTAC degrader that effectively induces the degradation of the SMARCA2 protein through proteasome- and ubiquitin-dependent mechanisms, achieving a DC50 of 0.5 nM and Dmax of 98%. It demonstrates an IC50 of 42.2 nM against human SMARCA2, providing significant growth inhibition in SMARCA4-deficient cancer cells. SMD-3236 has shown profound and sustained depletion of SMARCA2 in tumor tissues and suppresses tumor growth in relevant xenograft models. This reagent is valuable for research focusing on SMARCA4-deficient cancers, including melanoma, non-small cell lung cancer, and acute myeloid leukemia. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-10 is a proteolysis-targeting chimera (PROTAC) designed to selectively degrade the BRD4 protein via recruitment of the von Hippel-Lindau (VHL) E3 ligase. This compound exhibits significant biological activity in degrading BRD4 in PC3 prostate cancer cells, demonstrating effective DC50 values of 1.3 nM when conjugated with STEAP1 antibodies and 18 nM with CLL1 antibodies. This reagent is valuable for studying the role of BRD4 in cancer biology and exploring targeted degradation strategies in therapeutic applications. -
BRD9 degrader
PROTAC BRD9 Degrader-6 is a highly effective degrader targeting BRD9, exhibiting an IC50 of 0.13 nM. This compound selectively induces proteolysis of BRD9, facilitating the study of diseases associated with the BAF complex. It is a valuable tool for researchers investigating the role of BRD9 in various biological contexts and its potential therapeutic applications. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-18 is a dual-target PROTAC degrader that selectively degrades the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF complex. It exhibits potent degradation activity with DC50 values of less than 100 nM in A549 cells for SMARCA2 and MV411 cells for SMARCA4. This reagent is useful for investigating the functional roles of SMARCA2 and SMARCA4 in cellular processes and may provide new insights into therapeutic strategies targeting chromatin remodeling in cancer research. -
BRD PROTAC Degrader
PROTAC BRD4 Degrader-26 is a photo-regulated PROTAC designed to selectively degrade BRD4 through a photocleavable linker. This compound achieves an impressive 80% degradation of BRD4 at a concentration of 1 μM, demonstrating significant potency. The degradation process can be controlled by UV light, allowing for precise temporal regulation of BRD4 levels. It is an essential tool for researchers investigating the role of BRD4 in various biological pathways and its potential as a therapeutic target. -
SMARCA2 Degrader
PROTAC SMARCA2/4-degrader-10 targets the selective degradation of SMARCA2, exhibiting a DC50 value of less than 100 nM. This compound serves as a valuable tool in cancer research, facilitating studies on tumor biology and the therapeutic potential of targeting the BRG1/BRM-associated factor complex. The design incorporates a ligand linked to a VHL ligand, enhancing the efficacy of the degrader in cellular environments. -
PROTAC BRD3 Degrader
PROTAC BRD3 Degrader-1 is a potent and selective proteolysis-targeting chimera (PROTAC) designed to degrade BRD3. Its mechanism involves the targeted degradation of BRD3, leading to the downregulation of H3K18ac while sparing BRD2 and BRD4. This compound demonstrates significant efficacy in reducing intraocular inflammation in the experimental autoimmune uveitis mouse model and inhibits pro-inflammatory responses in microglial cells, making it a valuable tool for uveitis research. -
SMARCA2/4 Molecular Glue Degrader
SMARCA2/4 degrader-1 is a molecular glue degrader specifically targeting SMARCA2 and SMARCA4, exhibiting a DC50 value of 2.2 nM for SMARCA4. This compound functions by covalently bridging CUL4DCAF16 and CRL1FBXO22, leading to the efficient degradation of SMARCA2 and SMARCA4 proteins. It is utilized in research to understand the roles of these proteins in various biological processes and disease states, particularly in cancer biology and epigenetic regulation. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-21 is a targeted protein degradation compound that selectively degrades the SMARCA2 protein through the ubiquitin-proteasome system. It demonstrates potent biological activity with a DC50 value of 10-50 nM in A549 cells and exhibits even greater efficacy in MV411 cells, achieving a DC50 of less than 1 nM for SMARCA2 while showing limited degradation of SMARCA4 (DC50 >100 nM). This compound is useful for investigating the functional roles of SMARCA2 in cancer biology and therapeutic development. -
SMARCA2/4 Inhibitor
SMARCA2-IN-8 is a selective inhibitor of the SWI/SNF chromatin remodeling complexes SMARCA2 and SMARCA4, exhibiting potent activity with IC50 values of 5 nM and 6 nM, respectively. This compound effectively inhibits the proliferation of SMARCA2-mutated cancer cells, specifically SKMEL5, with an AAC50 of 5 nM and downregulates SMARCA2-dependent KRT80 gene expression at an AAC50 of 10 nM. SMARCA2-IN-8 demonstrates substantial antitumor efficacy and favorable pharmacokinetic properties in preclinical mouse models, making it a valuable tool for investigating chromatin remodeling in cancer research. -
BRD4 PROTAC Degrader
BRD4 degrader-6 is a dimeric PROTAC degrader targeting the BRD4 protein, demonstrating a DC50 of less than 0.1 μM. This compound facilitates the ubiquitination and subsequent degradation of BRD4, contributing to its anticancer properties. It serves as a valuable tool for studying BRD4-related pathways and potential therapeutic strategies in cancer research. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-6, a targeted degrader of SMARCA2 and SMARCA4, employs a proteolysis-targeting chimeric approach to facilitate the degradation of these proteins. This compound demonstrates significant potential in cancer research by selectively lowering SMARCA2/4 levels, thereby disrupting oncogenic signaling pathways. Its unique structure includes a ligand for SMARCA2/4 and a VHL ligand to promote ubiquitination and subsequent proteasomal degradation, making it a valuable tool for elucidating the role of these proteins in tumor biology. -
E3 ligase ligand
(S,R,S)-AHPC-Me-amide-C9-acid is an E3 ligase ligand-linker conjugate designed for targeted protein degradation applications. This reagent facilitates the synthesis of PROTAC SMARCA2 degrader-31, enabling investigations into the modulation of protein levels via the ubiquitin-proteasome system. Its unique structure enhances selectivity and efficacy in the degradation of specific target proteins, making it a valuable tool in chemical biology and therapeutic research. -
PROTAC BRD4/BRD2 Degrader
PROTAC BRD2/BRD4 degrader-1 is an effective PROTAC targeting the BET proteins BRD4 and BRD2 with high selectivity. This compound facilitates the rapid and reversible degradation of BRD4 and BRD2, while sparing BRD3, making it a powerful tool for research into solid tumors. Its composition includes a BET inhibitor, a linker, and thalidomide, which targets cereblon (CRBN) and cullin 4A. This degrader demonstrates potential in cancer therapeutics with a minimal cytotoxic effect on cells. -
BRD4 PROTAC Degrader
BRD-SF2 is a BRD4-targeted PROTAC degrader that facilitates the selective degradation of the BRD4 protein. With a DC50 of 17.2 μM, it utilizes a VHL ligand and a specific linker to induce proteasomal degradation. This compound is valuable for research applications in cancer biology and epigenetics, providing insights into the role of BRD4 in transcriptional regulation and cellular processes. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4 degrader-36 is a selective dual degrader targeting SMARCA2 and SMARCA4, demonstrating DC50 values of 0.22 nM and 0.85 nM, respectively. This compound exhibits significant anti-cell proliferation activity, making it a valuable tool for research in cancer biology and epigenetic regulation. It employs a unique mechanism of action involving targeted protein degradation, which can provide insights into the functional roles of SMARCA2 and SMARCA4 in various cellular processes. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-17 is an innovative PROTAC degrader designed to target the catalytic subunits SMARCA2 and SMARCA4 of the SWI/SNF chromatin remodeling complex. This compound effectively induces the degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, exhibiting DC50 values of less than 100 nM for both targets. It presents a valuable tool for research studies focused on the modulation of chromatin dynamics and cancer biology. -
SMARCA2/SMARCA4 PROTAC degrader
PROTAC SMARCA2/4 degrader-39 is a selective degrader that targets the SMARCA2 (BRM) and SMARCA4 (BRG1) proteins through the PROTAC mechanism. This compound exhibits significant efficacy in promoting the degradation of these chromatin remodeling proteins, which is crucial in various oncological contexts, particularly non-small cell lung cancer and colorectal cancer. Researchers may find this degrader valuable for studying the molecular mechanisms underlying tumor growth and developing innovative therapeutic strategies. -
BRD4 Degrader
EN884 is a selective degrader of BRD4, functioning through a SKP1- and proteasome-dependent mechanism. This compound facilitates targeted protein degradation and is applicable in synthetic proteolysis targeting chimeras (PROTACs) research. EN884 is valuable for investigating the role of BRD4 in various biological processes and disease contexts. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-29 (Compound I-279) is a selective degrader aimed at the catalytic subunits of the SWI/SNF chromatin remodeling complexes, SMARCA2 and SMARCA4. This compound effectively induces the degradation of SMARCA2 in A549 cells and SMARCA4 in MV411 cells, achieving a degradation concentration (DC50) of less than 100 nM for both targets. It is designed for use in research focused on chromatin regulation, epigenetic modifications, and related therapeutic applications. -
BRD4 PROTAC Degrader
RAJQ14 is a PROTAC degrader that selectively targets BRD4, facilitating its degradation through the ubiquitination-independent pathway. By binding to the 19S proteasome cap subunits RPN1, RPN10, RPN13, and USP14, RAJQ14 recruits BRD4 to the proteasome, promoting proteolytic degradation. This compound is an invaluable tool for cancer research, enabling studies of the mechanisms underlying BRD4 modulation and its role in tumor biology. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-28 is a selective PROTAC agent that targets SMARCA2, effectively inducing its degradation with a DC50 of 3 nM in HiBiT A549 cells. This compound utilizes a bifunctional mechanism, linking a ligand for SMARCA2 with an E3 ligase ligand, facilitating targeted protein degradation. It serves as a potent tool for research applications aimed at studying SMARCA2's role in cellular processes and its potential implications in cancer therapeutics. -
SMARCA2/4 PROTAC Degrader
PROTAC SMARCA2/4-degrader-19 is designed to target the catalytic subunits of the SWI/SNF complex, specifically SMARCA2 and SMARCA4. This potent degrader effectively leads to the degradation of SMARCA2 in MV411 and A549 cells with a DC50 of less than 100 nM, as well as SMARCA4 in MV411 with a similar DC50. It serves as a valuable tool for researching the functional roles of these proteins in cancer biology and therapeutic development. -
Molecular Glue BRD4 Degrader
BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue that selectively targets BRD4 for degradation by inducing a ternary complex with RNF126, an E3 ligase. This compound effectively promotes the degradation of both the long and short isoforms of BRD4 within cellular contexts. It serves as a valuable tool for investigating the roles of BRD4 in various biological processes and disease states, particularly in cancer research and therapeutic development. -
BAZ2A/B PROTAC Degrader
dBAZ2 is a novel PROTAC degrader targeting BAZ2A and BAZ2B, demonstrating DC50 values of 180 nM and 250 nM, respectively. This compound facilitates the ubiquitination and subsequent proteasomal degradation of BAZ2A and BAZ2B, making it a valuable tool for studying their biological roles. dBAZ2 is suitable for research applications in cancer biology, epigenetics, and the exploration of targeted protein degradation mechanisms. -
SMARCA2 PROTAC Degrader
PROTAC SMARCA2 degrader-26 is a specific degrader targeting the SMARCA2 protein. This compound exhibits potent activity, inducing a degradation of 94% for SMARCA2 and 57% for SMARCA4 in VCaP cells. Additionally, PROTAC SMARCA2 degrader-26 demonstrates significant antiproliferative effects, making it a valuable tool for research applications aimed at investigating the roles of SMARCA proteins in cancer and other diseases. -
SMARCA2 Inhibitor
SMARCA2-IN-2 is a specific inhibitor of SMARCA2, demonstrating an IC50 range of 101-500 µM. This compound is relevant for investigations into cancer biology, as it provides insights into the role of SMARCA2 in tumorigenesis. Its ability to selectively modulate SMARCA2 activity makes it a valuable tool for understanding epigenetic regulation in cancer research. -
SMARCA2/4 Degrader
PROTAC SMARCA2/4-degrader-31 is a targeted degradative agent designed to induce proteolytic degradation of the catalytic subunits SMARCA2 and SMARCA4 within the SWI/SNF chromatin remodeling complex. This compound demonstrates effective degradation of SMARCA2 in A549 cells with a DC50 of less than 100 nM and SMARCA4 in MV411 cells, also with a DC50 below 100 nM. It is a valuable tool for studying the functional roles of these proteins in cancer biology and epigenetic regulation. -
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. -
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. -
BAZ2B PROTAC Degrader
dBAZ2B is a selective BAZ2B PROTAC degrader with a DC50 of 19 nM. This compound effectively promotes the degradation of the BAZ2B protein, facilitating investigations into protein homeostasis and targeted protein degradation mechanisms. It serves as a valuable tool for research in cellular signaling pathways and potential therapeutic applications in cancer and other diseases. -
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. -
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. -
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 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. -
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. -
BET PROTAC Degrader
PROTAC BET Degrader-16 is a potent BET PROTAC degrader specifically targeting BRD4 with a DC50 of 0.31 nM, displaying a strong selectivity for BRD4 over other BET family proteins. This compound facilitates the degradation of BRD2, BRD3, and BRD4 through the ubiquitin-proteasome system, utilizing CRBN E3 ligase recruitment. Research applications include the induction of cell cycle arrest and promotion of apoptosis, demonstrating anti-tumor effects particularly in acute myeloid leukemia. -
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. -
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. -
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. -
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. -
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. -
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.
