Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
MLLT1 PROTAC Degrader
PROTAC MLLT1 Degrader-1 is a targeted PROTAC degrader that specifically interacts with MLLT1. This compound effectively inhibits proliferation and viability of acute myeloid leukemia (AML) cells, while also suppressing tumor growth in human AML xenograft models. PROTAC MLLT1 Degrader-1 can be utilized for research focused on MLL-rearranged AML, enabling studies on its oncogene transcriptional regulation and potential therapeutic applications. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
PROTAC BRAF-V600E Degrader
PROTAC BRAF-V600E Degrader-2 is a highly selective degrader targeting the BRAF-V600E mutant, with dissociation constants (Kd) of 14.4 nM and 9.5 nM for BRAF and BRAF-V600E, respectively. This compound effectively induces degradation of the BRAF-V600E kinase domain without impacting wild-type BRAF. Its potent biological activity makes it a valuable tool for research applications focused on melanoma cell growth inhibition and the study of BRAF-related signaling pathways. -
pan-KRAS PROTAC Degrader
MCB-36 is a VHL-recruiting pan-KRAS PROTAC degrader that targets various KRAS mutants, including G12D, G12C, G12V, and wild-type forms, with an exceptionally high binding affinity (Kd ≈ 1 pM). This compound effectively lowers p-ERK levels, promoting apoptosis in KRAS-driven cancer cells while showing minimal impact on HRAS and NRAS protein levels. MCB-36 is particularly useful for investigating colorectal and lung cancers, as it demonstrates efficacy against KRASG12C inhibitor-resistant tumors and aids in remodeling the tumor immune microenvironment. -
DHFR-TS PROTAC Degrader
BION106 is a dihydrofolate reductase-thymidylate synthase (DHFR-TS) PROTAC degrader that effectively targets and degrades DHFR-TS. It demonstrates potent antimalarial activity against Plasmodium falciparum, with a Ki value of 2.68 nM and selective toxicity of 0.2 μM in parasite cells, while showing significantly reduced toxicity (>100 μM and 44.2 μM) in mammalian cells. BION106 is valuable for research on antimalarial therapies and the mechanisms underlying parasite survival. -
PROTAC DHFR Degrader
PROTAC DHFR Degrader-1 is a selective PROTAC degrader that targets the dihydrofolate reductase-thymidylate synthase (DHFR-TS) complex of Plasmodium falciparum, exhibiting a Ki of 2.01 nM. This compound specifically degrades the parasite's DHFR without affecting human DHFR, effectively inhibiting the growth of Plasmodium falciparum. PROTAC DHFR Degrader-1 is suitable for research focused on malaria and the molecular mechanisms related to Plasmodium falciparum.
