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.
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Application
Product Information
Citations
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EZH2 Inhibitor
MC3629 is a selective inhibitor of the histone methyltransferase EZH2, demonstrating significant anti-tumor activity. It effectively inhibits the proliferation and self-renewal of SHH MB cancer cells while also inducing apoptosis. MC3629 serves as a valuable tool for investigating drug resistance mechanisms and the aggressiveness of tumors in cancer research. -
SMYD2 Inhibitor
(R)-BAY-598 is a potent inhibitor of the protein-lysine methyltransferase SMYD2, exhibiting an IC50 value of 1.7 μM. This compound selectively interferes with SMYD2 activity, making it a valuable tool for studying the role of lysine methylation in various biological processes. It is applicable in research focused on cancer biology and epigenetic regulation, facilitating the understanding of disease mechanisms and the development of potential therapeutic strategies. -
SMYD2 Inhibitor
EPZ032597 is a selective, noncompetitive inhibitor of SMYD2, exhibiting an IC50 value of 16 nM. This compound is relevant for research into pancreatic ductal adenocarcinoma, targeting the modulation of epigenetic regulation involved in cancer progression. Its specificity for SMYD2 makes it a valuable tool for investigating the enzyme's role in tumor biology and potential therapeutic strategies. -
Histone Methyltransferases Inhibitor
TM2-115 is a potent inhibitor of histone methyltransferases in malaria parasites. By targeting these essential enzymes, TM2-115 leads to rapid and irreversible lethality in the parasites. This compound is crucial for studies aimed at understanding the epigenetic regulation of malaria and provides valuable insights into potential therapeutic strategies for combatting malaria infections. -
SMYD2 Inhibitor
EPZ033294 is a potent inhibitor of SMYD2, exhibiting an IC50 value of 3.9 nM. SMYD2 is a histone methyltransferase responsible for the methylation of lysine residues, notably converting BTF3 to BTF3me1. This compound effectively prevents the methylation process, as demonstrated by a concentration-dependent inhibitory effect observed in 293T cells. EPZ033294 is valuable for research applications focused on epigenetic regulation and the role of SMYD2 in various cellular processes. -
PRMT5 Inhibitor
PRMT5-IN-37 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), a key enzyme involved in epigenetic regulation and gene expression. This compound exhibits significant biological activity in blocking PRMT5 function, resulting in the inhibition of cellular proliferation in various cancer models. PRMT5-IN-37 is particularly useful for research applications focused on cancer biology and the development of targeted therapies. -
SETD7 Inhibitor
(S)-PFI-2 hydrochloride selectively inhibits the lysine methyltransferase SETD7, demonstrating approximately 500-fold higher potency compared to its (R) enantiomer. This compound operates via a unique mechanism that alters the catalytic functionality of SETD7, influencing the binding dynamics with substrate peptides and cofactor interactions. Its targeted inhibition positions (S)-PFI-2 as a valuable tool for investigating SETD7's role in various biological processes, including epigenetic regulation and cellular signaling pathways. This compound is particularly relevant for research applications focused on methylation dynamics and related therapeutics. -
Histone Methyltransferase Inhibitor
UNC2327 is an allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3), effectively disrupting its enzymatic activity. This compound plays a significant role in regulating histone methylation, thus influencing gene expression and chromatin dynamics. UNC2327 is utilized in research applications focused on epigenetic modifications and the functional study of PRMT3 in various biological contexts. -
EZH2/PRC2 Inhibitor
NPD13668 is an inhibitor of EZH2, targeting the polycomb repressive complex 2 (PRC2) to modulate gene silencing. This compound effectively disrupts EZH2 activity, leading to the reactivation of silenced H3K27me3 target genes and subsequent depletion of the H3K27me3 modification. NPD13668 is applicable in studies focused on prostate and ovarian cancer, providing insights into epigenetic regulation and potential therapeutic strategies. -
EZH2 Inhibitor
EZH2-IN-7 is a potent inhibitor of Enhancer of Zeste Homolog 2 (EZH2), targeting the enzyme involved in histone methylation. This compound effectively reduces the abnormal levels of H3K27 methylation associated with EZH2 overexpression and mutations, which contribute to the progression of various cancers, including breast cancer, prostate cancer, and leukemia. EZH2-IN-7 serves as a valuable tool for cancer research, particularly in understanding the role of EZH2 in tumor development and exploring potential therapeutic strategies. -
PRMT5 Inhibitor
PRMT5-IN-49 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound exhibits significant antitumor activity by disrupting PRMT5-mediated methylation processes, which are critical for oncogenic signaling and cell proliferation. PRMT5-IN-49 is instrumental in cancer research and the investigation of epigenetic regulatory mechanisms in various malignancies. -
Histone Methyltransferase Inhibitor
PRMT5-IN-11 is a selective inhibitor of the protein methyltransferase complex PRMT5:MEP50, designed to disrupt histone methylation. With its structure-dependent activity in the (sub)micromolar range, this compound serves as a valuable tool for studying epigenetic regulation. It is ideally suited for research applications involving cancer biology and chromatin modifications. -
PRMT5 Inhibitor
PRMT5-IN-50 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting oral activity and favorable metabolic stability. This compound effectively inhibits symmetric dimethylarginine (SDMA) methylation in both MTAP-deleted and MTAP-wild type HCT116 cell lines, with IC50 values of 1.0 nM and 536 nM, respectively. Additionally, PRMT5-IN-50 demonstrates robust anti-proliferative effects, showing IC50 values of 19 nM and 1620 nM for tumor cell growth inhibition. In vivo studies indicate that PRMT5-IN-50 significantly suppresses tumor growth in mouse models, supporting its potential utility in cancer research. -
PRMT1 Inhibitor
PRMT1-IN-1 is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), which plays a crucial role in regulating gene expression and cellular signaling through arginine methylation. This compound exhibits potent inhibitory activity against PRMT1 and has applications in cancer research and investigations into epigenetic modulation. Its ability to selectively target PRMT1 makes it a valuable tool for elucidating the biological functions of this enzyme in various cellular processes. -
Histone Methyltransferase Inhibitor
PRMT5-IN-10 is a selective inhibitor of the protein methyltransferase complex PRMT5:MEP50. It demonstrates structure-dependent inhibition, affecting its ability to catalyze the methylation of histones. This compound is useful in investigating the role of PRMT5 in various biological processes, including gene expression regulation and epigenetic modifications, making it a valuable tool for research in cancer biology and epigenetics. -
PRMT5 inhibitor
PRMT5-IN-33 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating a competitive binding mechanism with an IC50 of 10.9 nM. This compound effectively induces apoptosis and inhibits the proliferation of Z-138 and MOLM-13 cell lines, highlighting its potential as a therapeutic agent. PRMT5-IN-33 exhibits significant antitumor activity, making it a valuable tool for cancer research and drug development. -
SMYD3 Inhibitor
EPZ028862 is a selective inhibitor of SMYD3, a histone methyltransferase involved in the regulation of gene expression. By targeting SMYD3, EPZ028862 disrupts cellular proliferation and oncogenic signaling pathways, demonstrating significant potential in cancer research applications. Its specificity makes it a valuable tool for studying the role of SMYD3 in tumor biology and for exploring therapeutic strategies against various cancers. -
Histone Methyltransferase Inhibitor
GSK2807 is a potent and selective histone methyltransferase inhibitor that competitively inhibits SAM binding to SMYD3, with a Ki value of 14 nM. This compound is valuable for cancer research, as it effectively prevents the methylation of MEKK2, thereby potentially influencing cell proliferation and tumor progression. GSK2807 is a promising tool for studying the role of SMYD3 in cancer biology and for evaluating therapeutic strategies targeting histone methylation. -
PRMT5 Inhibitor
PRMT5-IN-21 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5), a crucial enzyme involved in the regulation of gene expression and cellular signaling. This compound effectively suppresses PRMT5 activity, leading to alterations in histone and non-histone protein methylation. PRMT5-IN-21 is valuable for research applications aimed at investigating the role of PRMT5 in various biological processes, including cancer progression and cellular differentiation. -
PRMT5 Inhibitor
PRMT5-IN-36-d3 is a deuterated derivative of the PRMT5 inhibitor PRMT5-IN-36. This compound serves as an orally bioavailable inhibitor of protein arginine methyltransferase 5 (PRMT5), a target of interest in cancer research. PRMT5-IN-36-d3 is utilized to study the role of PRMT5 in tumorigenesis and its potential as a therapeutic target in various malignancies. -
EZH2 Inhibitor
EZH2-IN-19 is a potent inhibitor of enhancer of zeste homolog 2 (EZH2) with an IC50 value of 0.32 nM. This compound is primarily utilized in cancer research to investigate the epigenetic regulation of gene expression mediated by EZH2. Its specific inhibition of EZH2 makes it a valuable tool for studying various malignancies associated with dysregulated histone methylation. -
DOT1L Inhibitor
EPZ-4777 is a selective inhibitor of DOT1L, targeting the methylation of histone H3 at lysine 79 (H3K79) in cancer cells. This compound effectively blocks the expression of genes associated with leukemia and selectively induces cell death in translocated cells, making it a valuable tool in cancer research. Its specificity for DOT1L-related pathways positions EPZ-4777 as a significant reagent for studying leukemogenesis and potential therapeutic interventions. -
PRMT5 Inhibitor
PRMT5-IN-53 is a potent, orally bioavailable inhibitor of PRMT5, exhibiting pIC50 values of ≥ 9.7 against both human and mouse PRMT5. It demonstrates high affinity for the PRMT5:MEP50 complex with a KD of 11.3 pM. This compound effectively inhibits PRMT5 in the intestines of murine models, leading to a significant reduction in the number and size of polyps while minimizing systemic hematological toxicity. PRMT5-IN-53 is particularly valuable for research in colorectal cancer, especially in the context of familial adenomatous polyposis (FAP). -
EZH2 Inhibitor
SKLB-03220 is a selective covalent inhibitor of EZH2, exhibiting an IC50 of 1.72 nM for EZH2MUT. This compound demonstrates minimal activity against other histone methyltransferases and kinases, ensuring its specificity. SKLB-03220 has shown significant potency in ovarian cancer cell lines, inducing apoptotic processes, and effectively inhibits tumor growth in the PA-1 xenograft model. It is an important tool for research focused on ovarian cancer pathways and treatments. -
PRMT5 Inhibitor
PRMT5-IN-51 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). It exhibits potent antiproliferative activity in various cancer cell lines, making it a valuable tool for investigating the role of PRMT5 in tumorigenesis. This compound is useful for research applications focused on understanding the molecular mechanisms of cancer and the therapeutic potential of PRMT5 inhibition. -
G9a Inhibitor
G9a-IN-2 is a potent inhibitor of the histone methyltransferase G9a, exhibiting an IC50 of 0.024 μM. This compound effectively reduces levels of H3K9me2 and promotes the mRNA expression of γ-globin. G9a-IN-2 holds potential for therapeutic applications in ameliorating sickle cell disease (SCD) through its modulation of epigenetic mechanisms. -
EZH2 Inhibitor
YM281 is a potent inhibitor of the EZH2 enzyme, a key component of the polycomb repressive complex involved in histone methylation. This compound effectively induces apoptosis and causes cell cycle arrest at the G0/G1 phase, demonstrating significant antitumor activity in vivo. YM281 holds promise for research applications focused on lymphoma and may contribute to the development of targeted therapies in epigenetic regulation studies. -
PRMT5 Inhibitor
PRMT5-IN-28 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound targets the enzyme responsible for the arginine methylation of various proteins, which plays a crucial role in gene expression regulation, mRNA splicing, and cellular signaling pathways. Inhibition of PRMT5 has been shown to impede cancer cell proliferation and promote apoptosis, making it valuable for research applications in cancer biology and therapeutic development. Additionally, targeting PRMT5 may provide insights into mechanisms of immune evasion in tumors. -
PRMT5 Inhibitor
PRMT5-IN-52 is a potent non-nucleoside inhibitor of Protein Arginine Methyltransferase 5 (PRMT5), demonstrating an inhibitory rate of 20.2% at a concentration of 10 μM. This compound exhibits significant antitumor activity, making it a valuable tool for research in various cancer types, including lung, prostate, and colorectal carcinoma. It provides a promising avenue for investigating the role of PRMT5 in cancer biology and therapeutic development. -
G9a Inhibitor
CSV0C018875 is a quinoline-based inhibitor targeting the G9a protein (EHMT2). This compound demonstrates reduced cytotoxicity compared to other G9a inhibitors, making it a valuable tool for studies related to epigenetic regulation. Its selective inhibition of G9a can facilitate research into the roles of histone methylation in gene expression and various diseases, providing insights into potential therapeutic strategies. -
PRMT5 Inhibitor
AZ-PRMT5i-1 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating potent inhibitory activity while targeting MTAP-deficient cancers. This compound exhibits both in vitro and in vivo antitumor properties and shows cooperativity with methylthioadenosine (MTA). AZ-PRMT5i-1 is useful for research applications focused on the therapeutic potential of disrupting aberrant PRMT5 activity in cancer models. -
Histone Methyltransferase Inhibitor
PRMT6-IN-2 is a potent inhibitor of the histone methyltransferases PRMT6 and CARM1, exhibiting an IC50 value of 30 nM. This compound targets PRMT6, which is frequently overexpressed in various cancer cell types, and demonstrates promising potential for anticancer therapeutic development. Its dual inhibition mechanism makes PRMT6-IN-2 an important tool for investigating the role of arginine methylation in cancer progression. -
Histone Methyltransferase Inhibitor
(R)-BAY-6035 is a selective inhibitor of histone methyltransferase, specifically targeting the methylation of MAP3K2 by SMYD3. This compound exhibits nanomolar potency and offers high specificity against various kinases and protein lysine methyltransferases. It is suitable for research applications exploring gene regulation, epigenetic modifications, and signaling pathways related to cancer and other diseases. -
G9a/GLP Inhibitor
DS79932728 is a potent inhibitor of G9a and GLP, demonstrating IC50 values of 12.6 nM and 75.7 nM, respectively. This compound effectively induces the endogenous production of γ-globin, leading to elevated levels of fetal hemoglobin (HbF) and an increase in the proportion of F-reticulocytes. Its favorable oral absorption properties have been validated in cynomolgus monkey models, making it a valuable tool for research on hematological disorders and therapeutic strategies aimed at enhancing HbF synthesis. -
PRMT5 Inhibitor
PRMT5-IN-47 is a selective, orally bioavailable inhibitor of protein arginine methyltransferase 5 (PRMT5), exhibiting an IC50 of 15 nM. This compound demonstrates significant antiproliferative effects and is recognized for its potential anticancer activity. PRMT5-IN-47 serves as a valuable tool in cancer research, enabling studies on cellular proliferation and the therapeutic targeting of PRMT5 in various malignancies. -
SETD7 Inhibitor
DC-S238 is a highly selective inhibitor of the histone methyltransferase SETD7 (SETD7) with an IC50 of 4.88 μM. This compound is effective in modulating histone methylation and is valuable for investigating its role in cancer, diabetes, and inflammatory disease research. Its oral bioavailability and specificity make it a useful tool for elucidating the biological functions associated with SETD7. -
PRMT5 Inhibitor
PRMT5-IN-17 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5), a key enzyme involved in epigenetic regulation. This compound demonstrates significant anti-tumor activity, making it a promising candidate for cancer research. PRMT5's role in modulating gene expression through arginine methylation highlights the relevance of PRMT5-IN-17 in studies aimed at understanding cancer progression and developing novel therapeutic strategies. -
EZH2 Inhibitor
EZH2-IN-18 is a potent inhibitor of enhancer of zeste homologue 2 (EZH2) with an IC50 of 1.01 nM. This compound effectively inhibits cell proliferation and induces apoptosis in tumor cells. EZH2-IN-18 is utilized in research applications focusing on cancer biology and epigenetic regulation, making it a valuable tool for studies on EZH2-related pathways and therapeutic strategies. -
EZH2 Inhibitor
EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2), demonstrating significant anticancer activity. It acts competitively with the cofactor S-adenosylmethionine (SAM) and non-competitively with peptide or nucleosome substrates. This compound is instrumental in research applications focused on targeted cancer therapies and understanding the epigenetic regulation of gene expression. -
PRMT5 Inhibitor
PRMT5-IN-19 is a selective non-nucleoside inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating IC50 values of 23.9 nM in radioactive biochemical assays and 47 nM in AlphaLISA assays. This compound effectively occupies the SAM-binding pocket of PRMT5, inhibiting its methyltransferase activity with notable selectivity for PRMT5 over other PRMTs and protein lysine methyltransferases (PKMTs). PRMT5-IN-19 has been shown to inhibit cell proliferation through the induction of apoptosis, making it useful for research in cancer biology and therapeutic development. -
PRMT5-MTA complex Inhibitor
PRMT5-MTA-IN-8 is a potent inhibitor of the PRMT5-MTA complex, with an IC50 value of 4.4 nM. This compound effectively reduces the intracellular levels of symmetric dimethylarginine (SDMA) and inhibits the proliferation of MTAP-deficient cells. Research has demonstrated its antitumor activity, particularly in mouse models of triple-negative breast cancer, by promoting tumor cell apoptosis through PRMT5 inhibition. PRMT5-MTA-IN-8 is suitable for investigations into cancer biology and therapeutic strategies targeting PRMT5-related pathways. -
EZH2 Inhibitor
DCE_254 is an EZH2 inhibitor with an IC50 value of 11 μM, demonstrating significant antiproliferative activity against lymphoma cell lines. It interferes with the SAM-mediated methyl transfer process, thereby inhibiting the development of hypermethylation-related cancers, with an IC50 of 10.3 μM. This compound is valuable for research into targeted therapies for cancers influenced by epigenetic modifications. -
EZH2 Inhibitor
EZH2-IN-5 is a highly potent inhibitor of the EZH2 enzyme, exhibiting IC50 values of 1.52 nM for wild-type EZH2 and 4.07 nM for the mutant variant Tyr641. This compound effectively interferes with the methyltransferase activity of EZH2, leading to a reduction in histone methylation. EZH2-IN-5 is utilized in research focused on cancer biology, particularly in hematological malignancies and solid tumors characterized by aberrant EZH2 activity. -
PRMT5 Inhibitor
PRMT5-IN-16 is a potent inhibitor of protein arginine methyltransferase 5 (PRMT5), which plays a crucial role in epigenetic regulation. This compound exhibits significant anti-tumor activity, making it a valuable tool for studying cancer biology and epigenetic modifications. PRMT5-IN-16 is suitable for research applications aimed at exploring the therapeutic potential of PRMT5 inhibition in various cancer models. -
Aurora-A Inhibitor
PHA-680626 is a selective inhibitor of Aurora-A kinase, disrupting its interaction with N-Myc. This compound effectively inhibits the kinase activities of both AURKA and Bcr-Abl, leading to the degradation of N-Myc. Additionally, PHA-680626 reduces phosphorylation levels of CrkL and histone H3. Its anti-proliferative and pro-apoptotic effects have been demonstrated in Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ hematopoietic stem cells, making it a valuable tool for research in cancer therapeutics. -
PRMT5 Inhibitor
PRMT5-MTA-IN-4 is a potent irreversible inhibitor of protein arginine methyltransferase 5 (PRMT5), demonstrating an IC50 of 8 nM. This compound effectively blocks arginine methylation, leading to the inhibition of ribosomal RNA processing and the expression of cell cycle-related proteins. PRMT5-MTA-IN-4 exhibits significant antiproliferative effects across various tumor cell lines, with an IC50 of 0.3 μM in DLD-1 cells. This reagent is an important tool for investigating hematological malignancies, including acute myeloid leukemia and diffuse large B-cell lymphoma. -
EZH2-EED interaction Inhibitor
DC-PRC2in-01 is a potent inhibitor of the EZH2-EED interaction, exhibiting an IC50 of 4.21 μM and a dissociation constant (Kd) of 4.56 μM. This compound disrupts the EZH2-EED complex, leading to degradation of PRC2 core components and a reduction in H3K27me3 levels. Consequently, DC-PRC2in-01 effectively inhibits PRC2-driven proliferation of lymphoma cells and induces cell cycle arrest. It is particularly valuable for studying PRC2-related malignancies, such as Diffuse Large B-cell Lymphoma (DLBCL) and follicular lymphoma (FL). -
G9a/GLP Inhibitor
Antitumor agent-101 is a selective covalent inhibitor of the lysine methyltransferases G9a and GLP, exhibiting IC50 values of 8.5 nM and 5.5 nM, respectively. This compound demonstrates significant antitumor efficacy in the PANC-1 xenograft model, making it a valuable tool for studying the role of G9a and GLP in cancer biology. Its mechanism of action provides insights into potential therapeutic strategies for targeting malignant cells through epigenetic modulation. -
PRMT5 inhibitor
PRMT5-IN-54 is a selective inhibitor of protein arginine methyltransferase 5 (PRMT5). This compound plays a critical role in modulating gene expression through arginine methylation. PRMT5-IN-54 is particularly useful for investigating its potential therapeutic effects in autoimmune diseases and other conditions where PRMT5 activity is implicated. By inhibiting PRMT5, this reagent may contribute to unraveling the molecular mechanisms underlying various pathological states. -
PRMT Inhibitor
GSK3368715 hydrochloride is a reversible, orally active inhibitor targeting type I protein arginine methyltransferases (PRMTs). It demonstrates potent inhibitory activity with IC50 values of 3.1 nM for PRMT1, 48 nM for PRMT3, 5.7 nM for PRMT6, and 1.7 nM for PRMT8, while exhibiting weaker activity against PRMT4 (IC50 1148 nM). This compound effectively induces changes in arginine methylation states, modifies exon usage, and exhibits significant anticancer effects, making it valuable for research in cancer biology and epigenetic regulation.
