Epigenetics
Epigenetics research delves into the molecular mechanisms that control gene expression and cellular traits without altering the underlying DNA sequence. One crucial aspect of this field is the role of small molecules, which act as powerful regulators of epigenetic modifications. These small compounds, typically comprising a few dozen to a few hundred atoms, have emerged as essential tools in understanding and manipulating the epigenome.
- DNA Methylation Inhibitors: Small molecules like 5-azacytidine and 5-aza-2'-deoxycytidine are DNA methyltransferase inhibitors. They block the addition of methyl groups to DNA, leading to DNA demethylation. This can reactivate silenced genes, potentially offering therapeutic avenues for conditions like cancer.
- HDAC inhibitors: HDACs remove acetyl groups from histone proteins, contributing to gene repression. Small molecule HDAC inhibitors, such as Vorinostat and Romidepsin, can reverse this process by increasing histone acetylation, allowing genes to be more accessible for transcription. These inhibitors are being explored for cancer therapy and other conditions.
- Histone Methyltransferase Inhibitors: Small molecules like GSK126 inhibit specific histone methyltransferases, affecting histone methylation patterns. This can alter gene expression, making them promising candidates for cancer and other diseases with epigenetic dysregulation.
- RNA Modulators: Small molecules can also target non-coding RNAs involved in epigenetic regulation. For instance, small molecules called small interfering RNAs (siRNAs) can be designed to target and degrade specific long non-coding RNAs, influencing gene expression.
- Epigenetic Reader Domain Inhibitors: These small molecules target proteins that recognize and bind to specific epigenetic marks. Examples include inhibitors of bromodomain-containing proteins (BET inhibitors), which can disrupt gene regulation by interfering with protein-DNA interactions.
Small molecules in epigenetics research not only provide insights into the fundamental biology of gene regulation but also hold immense promise for developing novel therapeutics. Their ability to selectively modulate specific epigenetic marks and pathways has led to ongoing clinical trials and drug development efforts for various diseases, including cancer, neurological disorders, and inflammatory conditions. Understanding and harnessing the power of these small molecules is at the forefront of modern epigenetics research, offering new hope for precision medicine and targeted therapies.
3 key components involved in the regulation of epigenetic modifications
Epigenetics Writer
Epigenetics writers are enzymes responsible for adding chemical marks or modifications to DNA or histone proteins. These marks include DNA methylation (addition of methyl groups to DNA) and histone modifications (such as acetylation, methylation, phosphorylation, etc.).
Epigenetics Reader
Function: Epigenetics readers are proteins that can recognize and bind to specific epigenetic marks on DNA or histones. These reader proteins interpret the epigenetic code and facilitate downstream cellular processes, such as gene activation or repression.
Epigenetics Eraser
Function: Epigenetics erasers are enzymes responsible for removing or reversing epigenetic marks on DNA or histones. This process allows for the dynamic regulation of gene expression and the resetting of epigenetic states during various stages of development and in response to environmental changes.
Catalog No.
Product Name
Application
Product Information
Citations
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Sirtuin Substrate
Ac-QPKK(Ac)-AMC is a fluorogenic substrate specifically designed for sirtuin enzymes, facilitating the study of sirtuin-mediated deacetylation processes. This reagent enables the quantitative analysis of sirtuin activity, making it a valuable tool for investigating the role of sirtuins in various biological processes and disease states, including aging and metabolic disorders. Researchers can leverage Ac-QPKK(Ac)-AMC to explore sirtuin function in high-throughput screening assays and in-depth mechanistic studies. -
SIRT1 Inhibitor
ZINC08792229 is a potent inhibitor of SIRT1, a nicotinamide adenine dinucleotide (NAD+)-dependent deacetylase playing a crucial role in cellular regulation. This compound exhibits significant biological activity that may contribute to research on SIRT1-related diseases, including aging, diabetes, and cancer. It serves as a valuable tool for exploring the therapeutic potential of targeting SIRT1 in various pathological conditions. -
SIRT1/SIRT2 Inhibitor
Aristoforin, a hypericin derivative, selectively inhibits SIRT1 and SIRT2, resulting in G1 phase cell cycle arrest. This compound also scavenges hydroxyl free radicals and demonstrates protective effects against Fe2+-induced DNA breakage. Aristoforin is valuable for research in the context of breast cancer and colon adenocarcinoma studies. -
SIRT6 Modulator
SIRT6 modulator-1 is a selective modulator of SIRT6, a key enzyme involved in regulating metabolic processes and DNA repair. This compound influences SIRT6 activity, enhancing its role in chromatin dynamics and cellular stress responses. SIRT6 modulator-1 has potential applications in research focused on aging, metabolic disorders, and cancer by elucidating the pathways regulated by SIRT6. -
SIRT3 Inhibitor
SIRT3-IN-2 is a selective inhibitor of the SIRT3 enzyme, demonstrating a reduction of SIRT3 activity by 39% at a concentration of 200 µM. This compound is valuable for investigations into metabolic homeostasis and its implications in tumor suppression. SIRT3-IN-2 can be utilized in research aimed at understanding the regulatory roles of sirtuins in cellular metabolism and cancer biology. -
SIRT2 Inhibitor
SIRT2-IN-15 is a selective inhibitor of the SIRT2 deacetylase and deamyloacylase enzymes, demonstrating IC50 values of 7 μM and 37 μM, respectively. This compound modulates cellular acetylation states, making it a valuable tool for investigating the roles of SIRT2 in various biological processes, including neurodegenerative diseases, cancer metabolism, and aging. SIRT2-IN-15 can be utilized in research applications focusing on the molecular mechanisms of SIRT2-related pathways and potential therapeutic targets. -
SIRT1 Activator
3β,6α,12β-Dammar-E-20(22)-ene-3,6,12,25-tetraol is a potent SIRT1 activator that enhances SIRT1 activity significantly. This compound has demonstrated anti-tumor activity, making it a valuable tool for research in cancer biology and therapeutic interventions targeting SIRT1 modulation. Its role in promoting cellular metabolism and longevity pathways further supports its use in studies related to aging and metabolic disorders. -
SIRT2 Inhibitor
A2B57 is a selective inhibitor of SIRT2, exhibiting an IC50 value of 6.3 µM. This compound effectively modulates the activity of SIRT2, making it a valuable tool for exploring the role of this enzyme in various biological processes. Its application extends to studies in neurodegeneration, metabolism, and cellular stress responses, providing insights into SIRT2-related pathways. -
SIRT1/2/3 Inhibitor
SIRT-IN-6 is a pan-inhibitor targeting SIRT1, SIRT2, and SIRT3, with IC50 values exceeding 50 μM. This compound is valuable for studying its effects in metabolic, inflammatory, oncologic, and neurodegenerative disorders. Its broad inhibition profile makes it a suitable tool for elucidating the roles of sirtuins in various biological processes and disease states. -
SIRT2 Inhibitor
A1B11 is a selective inhibitor of Sirtuin 2 (SIRT2) with an IC50 value of 5.3 μM. This compound is primarily utilized in research focused on neurodegenerative diseases, where SIRT2 modulation plays a critical role in the underlying mechanisms of pathology. A1B11 provides a valuable tool for investigating the therapeutic potential of SIRT2 inhibition in various neurodegenerative conditions. -
SIRT1/3 Activator
Nicotinamide riboside (triflate) is a potent activator of the SIRT1 and SIRT3 pathways, functioning as an orally active precursor to NAD+. This compound significantly elevates NAD+ levels, thereby enhancing oxidative metabolism and providing protective effects against metabolic disturbances triggered by high-fat diets. Additionally, it has demonstrated neuroprotective properties, as evidenced by its ability to mitigate cognitive decline in transgenic mouse models of Alzheimer’s disease, making it valuable for research in metabolic health and neurodegenerative disorders. -
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. -
SIRT1/2 Inhibitor
Sirt1/2-IN-1 is a selective inhibitor of SIRT1 and SIRT2, exhibiting IC50 values of 1.81 and 2.10 µg/mL, respectively, while also inhibiting SIRT3 with an IC50 of 20.5 µg/mL. This compound induces hyperacetylation of α-tubulin, with an IC50 of 32.05 µg/mL, demonstrating its potential for modulating protein acetylation. Sirt1/2-IN-1 is particularly relevant in cancer research, showcasing significant anticancer activity that supports its use in investigating therapeutic strategies targeting sirtuin pathways. -
HDAC Inhibitor
HDAC-IN-54 is a potent histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 25 nM for human HDAC1, 66 nM for HDAC2, 6.5 nM for HDAC3, and 281 nM for HDAC6. This compound effectively induces acetylation of α-tubulin and histone H3, promoting cancer cell apoptosis, particularly in synergy with cisplatin. HDAC-IN-54 is relevant for research applications in head and neck cancer, ovarian cancer, and tongue squamous cell carcinoma. -
HDAC6 Degrader
HDAC6 degrader-5 functions as an HDAC6 degrader, demonstrating potent inhibitory and degradation capabilities with an IC50 of 4.95 nM and a DC50 of 0.96 nM. This compound effectively inhibits the release of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, while also preventing hepatocyte apoptosis. Additionally, HDAC6 degrader-5 shows anti-inflammatory effects in mouse models of acetaminophen-induced liver injury, making it a valuable tool for research on inflammatory diseases and liver pathologies. -
HDAC3 Degrader
HDAC3 Degrader-2 is a selective degrader of histone deacetylase 3 (HDAC3), functioning through targeted degradation to inhibit the activation of the NLRP3 inflammasome. By facilitating the reduction of IL-1β maturation and caspase-1 activity, HDAC3 Degrader-2 demonstrates significant anti-inflammatory effects. This reagent is applicable in researching conditions such as endotoxin shock, colitis, and gouty arthritis, providing valuable insights into mechanisms of inflammation and therapeutic interventions. -
JAK/STAT Inhibitor
Phenylpyropene C is a JAK/STAT pathway inhibitor known to effectively inhibit interferon-gamma (IFN-γ) mediated expression of reporter genes, with an IC50 range of 5.4 to 10.8 μM. Additionally, it serves as an inhibitor of acyl-CoA, exhibiting an IC50 of 16.0 μM. This compound is valuable for research applications focusing on the modulation of immune responses and the exploration of cytokine signaling pathways. -
HDAC Inhibitor
2-Propylpent-4-ynoic acid, a histone deacetylase (HDAC) inhibitor, exhibits an IC50 of 0.5 mM against human HDAC. This compound induces P-glycoprotein function and has been associated with teratogenicity, fetal growth inhibition, and neurotoxicity. Notably, the S-enantiomer demonstrates more significant teratogenic effects compared to its R-enantiomer and other analogs. 2-Propylpent-4-ynoic acid is relevant in research focused on the mechanisms underlying colon cancer and neural tube defects, including exencephaly. -
Sirtuin-modulating Compound
Sirtuin Modulator 9 is a sirtuin-modulating compound that enhances cellular lifespan and promotes mitochondrial activity. This compound has potential applications in research related to aging, inflammation, and cancer. Investigators may utilize Sirtuin Modulator 9 to explore its therapeutic effects in age-related disorders and diseases associated with compromised mitochondrial function. -
AMPK/SIRT3/PGC-1α Modulator
MitoPBN is an AMPK/SIRT3/PGC-1α modulator that enhances mitochondrial function by acting as a reactive oxygen species scavenger. This compound promotes mitochondrial biogenesis through increased AMPK phosphorylation, restoration of SIRT3 expression, and upregulation of PGC-1α. MitoPBN is effective in regulating glucose metabolism, as it decreases blood glucose levels by inhibiting hepatic gluconeogenesis and enhancing glucose uptake, while also improving ATP production and maintaining mitochondrial membrane potential. Additionally, it can reduce apoptosis and enhance sperm motility and membrane integrity, making it a valuable reagent for research related to diabetes and metabolic disorders. -
Stable Isotope
SAH-13C10 is a stable isotope labeled derivative of S-Adenosylhomocysteine (SAH). As an important amino acid derivative, SAH plays a crucial role as a modulator in various metabolic pathways and serves as an intermediate in the synthesis of cysteine and adenosine. It functions as an inhibitor of the METTL3-METTL14 heterodimer complex, demonstrating an IC50 of 0.9 μM, making it valuable for research in epitranscriptomics and cellular metabolism studies. -
WDR5 Ligand
Dimethyl-F-OICR-9429-COOH is a potent ligand for the WD40 repeat domain protein 5 (WDR5), functioning as a critical component in the synthesis of proteolysis-targeting chimeras (PROTACs). Its specific binding to WDR5 facilitates the targeted degradation of associated proteins, making it a valuable tool in chemical biology research. This compound is instrumental in the exploration of protein interactions and the development of innovative therapeutic strategies. -
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. -
PARP-1 Inhibitor
L-2286 is a potent orally active inhibitor of PARP-1. This compound demonstrates significant biological activity by alleviating carotid artery remodeling, reducing oxidative stress and inflammation in spontaneously hypertensive rats, while also providing neuroprotective effects in the dorsal hippocampus. L-2286 is applicable in research focused on hypertension and its associated vascular and neurological complications. -
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. -
EGFR PARP Dual-targeting PROTAC Molecule
DP-C-4 is a Cereblon-based dual-targeting PROTAC molecule designed for the concurrent degradation of epidermal growth factor receptor (EGFR) and poly (ADP-ribose) polymerase (PARP). This compound demonstrates significant biological activity by promoting the targeted destruction of these proteins, which can be crucial in cancer research and therapeutic applications. DP-C-4 may facilitate studies investigating the interplay between EGFR and PARP pathways, potentially leading to new insights in oncology and the development of innovative treatment strategies. -
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. -
PROTAC Linkers
6-Hydroxy-1-(4-(2-hydroxyethyl)piperazin-1-yl)hexan-1-one serves as a key linker in the development of PROTAC molecules targeting METTL3. This compound is integral for facilitating the degradation of specific proteins, thereby enabling cellular pathway modulation and functional studies. Researchers can employ this linker to explore targeted protein degradation applications in various biological contexts. -
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.
