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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Catalog No.
Product Name
Application
Product Information
Citations
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EZH2 Inhibitor
EZH2-IN-14 is a highly selective inhibitor of EZH2, a histone methyltransferase, with an IC50 of 12 nM. By specifically targeting and inhibiting the methyltransferase activity of EZH2 within the PRC2 complex, EZH2-IN-14 effectively reduces levels of H3K27me3. This compound exhibits over 200-fold selectivity for EZH2 compared to the closely related EZH1, making it a valuable tool for research into epigenetic regulation and cancer biology. -
SETD2 Inhibitor
EZM0414 TFA is a potent and selective inhibitor of SETD2, exhibiting an IC50 of 18 nM in biochemical assays and 34 nM in cellular assays. This orally active reagent is suitable for investigating its effects on relapsed or refractory multiple myeloma and diffuse large B-cell lymphoma. EZM0414 TFA facilitates valuable research into the role of SETD2 in cancer biology and therapeutic development. -
SETD7 Inhibitor
PFI-2 hydrochloride is a potent and selective inhibitor of SET domain containing lysine methyltransferase 7 (SETD7). It exhibits significant inhibitory activity with an IC50 value of 2.0 nM, making it an essential tool for studying the role of SETD7 in various biological processes. PFI-2 hydrochloride is valuable for investigating mechanisms underlying chronic kidney disease and inflammation, particularly in the context of renal fibrosis research. -
SETDB1-TTD Inhibitor
SETDB1-TTD-IN-1 is a selective inhibitor targeting the tandem Tudor domain of the SET domain bifurcated protein 1 (SETDB1-TTD), exhibiting a binding affinity (Kd) of 88 nM. This compound enhances the methyltransferase activity of SETDB1, making it a valuable tool for investigating the biological roles and disease associations of SETDB1-TTD in epigenetic regulation and cellular processes. Researchers can utilize SETDB1-TTD-IN-1 to explore its implications in various biological contexts. -
PRMT5 Inhibitor
PF-06939999 is a potent, orally active inhibitor of protein arginine methyltransferase 5 (PRMT5), functioning as a S-adenosylmethionine (SAM) competitive antagonist. It effectively suppresses the expression of symmetric dimethylarginine (SDMA) protein, with an IC50 value of 1.1 nM in A427 cells. Due to its ability to inhibit PRMT5 activity, PF-06939999 demonstrates significant antitumor effects, making it valuable for cancer research focused on epigenetic regulation and methylation pathways. -
JMJD1C Inhibitor
JMJD1C-IN-1 is a selective inhibitor of JMJD1C with an IC50 of 0.59 μM and a Kd of 1.96 μM. This compound effectively disrupts the binding of JMJD1C to the H3K9me2 peptide substrate as demonstrated in the HTRF assay, showing an IC50 of 1.47 μM. JMJD1C-IN-1 enhances tumor immunotherapy research by impairing intratumoral regulatory T (Treg) cell fitness through the accumulation of H3K9me2, which downregulates PD1 expression, and by reducing STAT3 demethylation, thereby promoting STAT3 activation. Furthermore, it exhibits dose-dependent antitumor efficacy across various mouse cancer models, including fibrosarcoma, melanoma, lung cancer, hepatocellular carcinoma, and colorectal cancer. -
PRMT1 Inhibitor
Furamidine dihydrochloride is a selective inhibitor of protein arginine methyltransferase 1 (PRMT1), exhibiting an IC50 of 9.4 μM. This compound demonstrates significant selectivity for PRMT1 over PRMT5, PRMT6, and PRMT4, making it an essential tool for studying PRMT-related biological processes. In addition, Furamidine dihydrochloride inhibits tyrosyl-DNA phosphodiesterase 1 (TDP-1) competitively and reversibly, showing enhanced activity with duplex DNA substrates. Furthermore, it possesses antiparasitic properties, expanding its potential applications in chemical and biological research. -
SETD2 Inhibitor
EPZ-719 is a selective inhibitor of the SETD2 enzyme, exhibiting an IC50 value of 0.005 μM. This compound demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology and therapeutic development. EPZ-719 may be utilized to explore the role of SETD2 in tumorigenesis and to evaluate potential treatment strategies targeting this pathway. -
DOT1L Inhibitor
Dot1L-IN-4 is a potent inhibitor of the DOT1L enzyme, exhibiting an IC50 of 0.11 nM. It effectively disrupts the activity of the telomeric silencing 1-like protein, making it a valuable tool for research into epigenetic regulation and gene expression modulation. Its application extends to studies on leukemia and other cancer types where DOT1L is implicated, facilitating investigations into therapeutic approaches targeting this pathway. -
HDAC Inhibitor
HDAC-IN-48 is a potent inhibitor of histone deacetylases (HDACs) that exhibits significant cytotoxicity, with a GI50 of approximately 20 nM. This hybrid molecule incorporates pharmacophores from SAHA and CETZOLE, effectively inducing ferroptosis while inhibiting HDAC activity. Additionally, HDAC-IN-48 features an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a valuable tool for click chemistry applications in chemical biology and therapeutic research. -
HDAC11 Inhibitor
HDAC11-IN-3 is a selective inhibitor of HDAC11, exhibiting an IC50 of 4.1 nM. This compound demonstrates potent anti-acute myeloid leukemia (AML) activity against U937 and OCI-AML2 cell lines with an IC50 of 10 μM. It effectively induces apoptosis, cell cycle arrest, and differentiation while upregulating iron transporters transferrin (TF) and transferrin receptor (TFRC). Additionally, HDAC11-IN-3 activates the p62-Keap1-Nrf2-HMOX1 pathway, resulting in elevated intracellular iron levels and subsequent ferroptosis in AML cells. This reagent is suited for studies investigating the molecular mechanisms of AML and can be utilized alone or in combination with other therapeutic agents like Cytarabine. -
LSD1 Inhibitor
Higenamine hydrochloride is a selective inhibitor of LSD1, with an IC50 value of 1.47 μM. This compound exhibits anti-inflammatory and antibacterial properties, and has been shown to attenuate IL-1β-induced apoptosis via the ROS-mediated PI3K/Akt signaling pathway. Additionally, Higenamine hydrochloride protects brain cells from oxygen deprivation and promotes bone formation in osteoporosis through the SMAD2/3 pathway. Its versatile applications make it suitable for research in cancer, inflammation, cardiorenal syndrome, and related diseases. -
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. -
Naa50 Inhibitor
Naa50-IN-1 is a potent inhibitor of N-alpha-acetyltransferase 50 (Naa50), exhibiting an IC50 of 7 nM against the human enzyme. This compound shows selectivity for related acetyltransferases, Naa10 and Naa60. Naa50-IN-1 interacts with the substrate-binding pocket of Naa50, with its binding affinity augmented by the presence of AcCoA, making it a valuable tool for investigating the biological roles of protein acetylation. Research applications include studies on gene regulation and enzyme activity related to Naa50 and its substrates. -
EZH2 Inhibitor
TDI-6118 is a potent inhibitor of the histone methyltransferase EZH2, known for its ability to penetrate the blood-brain barrier. This compound exhibits significant biological activity in targeting EZH2, making it a valuable tool for investigating central nervous system malignancies. Its application in research may contribute to a better understanding of the molecular mechanisms underlying various brain cancers. -
CARM1/HDAC2 inhibitor
CARM1/HDAC2-IN-1 is a dual inhibitor targeting both CARM1 and HDAC2, exhibiting IC50 values of 3.71 nM and 4.07 nM, respectively. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. CARM1/HDAC2-IN-1 is suitable for studies investigating the role of these epigenetic regulators in tumor biology and therapeutic strategies. -
DOT1L Inhibitor，PROTAC
DOT1L705 is a PROTAC degrader that selectively targets DOT1L, facilitating the recruitment of the VHL E3 ubiquitin ligase for proteasomal degradation of the protein. This leads to a significant reduction in H3K79 methylation levels, ultimately decreasing the viability of leukemia cells. DOT1L705 is particularly relevant for research focused on MLL-rearranged leukemia, making it a valuable tool for investigating the underlying mechanisms of disease progression. -
HuR Inhibitor
SRI-43265 is a selective inhibitor of human antigen R (HuR) dimerization, a crucial process impacting HuR's role in post-transcriptional regulation of target mRNAs. By disrupting HuR multimers, SRI-43265 demonstrates potential in studying cancer and inflammatory processes, where HuR's activity contributes to pathogenesis. This reagent is valuable for investigating the molecular mechanisms underlying these diseases and for exploring therapeutic strategies targeting HuR functions. -
HuR Inhibitor
ZM-32 is a potent inhibitor of human antigen R (HuR), a critical regulator of mRNA stability. By downregulating the expression of vascular endothelial growth factor A (VEGF-A) and matrix metalloproteinase 9 (MMP9), ZM-32 effectively inhibits angiogenesis in breast cancer. Demonstrating broad-spectrum anti-proliferative effects across various cancer cell lines, ZM-32 also shows significant antitumor efficacy in mouse models of the MDA-MB-231 breast cancer cell line. -
HuR-ARE Inhibitor
Azaphilone-9 (AZA-9) is a potent inhibitor of the HuR-ARE RNA interaction, demonstrating an IC50 value of 1.2 μM. By binding to the RNA-binding protein Hu antigen R (HuR), Azaphilone-9 disrupts the stabilization of various oncogenic mRNAs in tumor cells. This mechanism suggests that Azaphilone-9 may serve as a valuable tool for investigating cancer cell growth and progression in research applications targeting RNA-protein interactions. -
HuR Inhibitor
Okicenone is an inhibitor of Hu protein R (HuR), a key regulator of messenger RNA stability and translation. By disrupting HuR oligomerization and its RNA binding capabilities, Okicenone modulates HuR trafficking, influencing cytokine expression and T-cell activation. This compound is valuable in research focused on immune response modulation and the role of mRNA-binding proteins in cellular processes. -
METTL3 Inhibitor
METTL3-IN-1 is a potent METTL3 inhibitor designed to selectively inhibit the activity of the METTL3 methyltransferase. This compound demonstrates significant biological activity in modulating RNA methylation, making it a valuable tool for studying the role of METTL3 in various cellular processes. It is applicable in research areas such as epitranscriptomics and cancer biology, where understanding RNA modifications is crucial. -
METTL3 Inhibitor
METTL3-IN-2 is a selective inhibitor of the methyltransferase METTL3, exhibiting an IC50 value of 6.1 nM. This compound effectively inhibits cell proliferation in Caov3 ovarian cancer cells, providing a valuable tool for research into the regulation of RNA methylation and its implications in cancer biology. METTL3-IN-2 can be utilized in studies focused on understanding METTL3's role in tumor growth and the development of targeted cancer therapies. -
METTL3 Inhibitor
METTL3-IN-3 is a selective inhibitor of the methyltransferase METTL3, which plays a critical role in RNA m6A methylation. This compound demonstrates significant inhibition of METTL3 activity, thereby impacting the regulation of gene expression and RNA metabolism. METTL3-IN-3 is valuable for research applications focusing on epitranscriptomics, RNA modifications, and their implications in various biological processes and diseases. -
METTL3 Inhibitor
METTL3-IN-5 is a selective inhibitor of METTL3, a key enzyme involved in N6-methyladenosine (m6A) methylation. This compound demonstrates potent inhibitory effects on the growth of MOLM-13 cells, with an IC50 of less than 2 μM. While exhibiting minimal hERG inhibitory activity (IC50 >30 μM), METTL3-IN-5 is a valuable tool for researching acute myeloid leukemia (AML) and m6A-related biological processes. -
METTL3 Inhibitor
METTL3-IN-13 is a selective inhibitor of the methyltransferase METTL3. This compound exhibits significant biological activity by disrupting RNA methylation, which plays a critical role in various cancer types including hypopharyngeal squamous cell carcinoma and non-small cell lung cancer. It serves as a valuable tool for investigating the role of METTL3 in oncogenic processes and may assist in the development of targeted therapies. -
miR-155 Inhibitor
Cobomarsen sodium is a targeted miR-155 inhibitor that modulates various signaling pathways, including JAK/STAT, MAPK/ERK, and PI3K/AKT, contributing to the regulation of cell survival. This oligonucleotide is primarily employed in research focused on B-cell lymphoma, enabling insights into the molecular mechanisms of this malignancy and potential therapeutic strategies. -
miR-155 Inhibitor
Cobomarsen is an oligonucleotide inhibitor targeting miR-155. This compound modulates various signaling pathways associated with cell survival, including the JAK/STAT, MAPK/ERK, and PI3K/AKT pathways. Cobomarsen is primarily utilized in research focused on B-cell lymphoma, providing insights into miRNA-mediated gene regulation and potential therapeutic approaches. -
TET Inhibitor
TETi76 is a potent inhibitor of TET family enzymes, demonstrating IC50 values of 1.5 μM for TET1, 9.4 μM for TET2, and 8.8 μM for TET3. By competitively binding to the active site of these enzymes, TETi76 effectively decreases cytosine hydroxymethylation and inhibits the clonal growth of TET2 mutant cells both in vitro and in vivo, while sparing normal hematopoietic precursor cells. This selective activity makes TETi76 a valuable tool for investigating leukemia and studying TET-related pathways in cancer research. -
TET1 Inhibitor
NSC-311068 is a potent inhibitor of TET1, targeting the enzyme's transcriptional activity and its role in modifying 5-hydroxymethylcytosine (5hmC). This compound effectively reduces TET1 expression levels and attenuates global 5hmC levels. NSC-311068 demonstrates significant cytotoxicity in acute myeloid leukemia (AML) cells characterized by elevated TET1 expression, making it a valuable tool for studying TET1-related pathways and potential therapeutic approaches in AML. -
WDR5 Inhibitor
WDR5-IN-5 is a selective inhibitor targeting the WIN site of the WD repeat domain 5 (WDR5). This compound demonstrates significant anti-proliferative activity against various cancer cell lines and possesses favorable pharmacokinetic properties in murine models. With a high binding affinity to WDR5, the Ki value is recorded at less than 0.02 nM, making it a valuable tool for research into cancer biology and potential therapeutic applications. -
WDR5 Inhibitor
WDR5-IN-6 is a selective inhibitor of WDR5, acting primarily at the WBM site. This compound demonstrates significant anti-tumor activity by inhibiting cell proliferation in neuroblastoma cell lines. Additionally, WDR5-IN-6 exhibits notable synergy with OICR-9429, another WDR5 inhibitor that targets the WIN site. This compound is valuable for research applications focused on neuroblastoma and related oncological studies. -
WDR5 Inhibitor
WM-586 is a covalent inhibitor of WDR5, effectively disrupting the interaction between WDR5 and MYC with an IC50 value of 101 nM. This compound demonstrates significant potential in cancer research, particularly in the study of neuroblastoma, breast cancer, bladder cancer, and colorectal cancer. Its ability to target the WDR5-MYC complex makes it a valuable tool for exploring therapeutic strategies in various malignancies. -
WDR5-MYC Interaction Inhibitor
WM-662 is an inhibitor targeting the WDR5-MYC interaction, exhibiting an IC50 of 18 μM. This compound is particularly relevant for investigations into cancer biology, aging processes, and neurodegenerative disorders. Its ability to disrupt the WDR5-MYC interaction positions WM-662 as a valuable tool in studying dysregulated gene expression associated with these conditions. -
WDR5-MYC Interaction Inhibitor
Anticancer agent 126 is a specific inhibitor of the WDR5-MYC interaction, targeting the critical role of this complex in oncogenic signaling. This compound effectively disrupts the binding of WDR5 to MYC, leading to a reduction in MYC target gene expression. It is suitable for research applications focused on elucidating the mechanisms of cancer biology and developing therapeutic strategies against MYC-driven malignancies. -
WDR5 Inhibitor
WDR5-IN-7 is a potent inhibitor of WD repeat domain 5 (WDR5), utilizing a benzoxazepinone structure. This compound exhibits significant anti-cancer activity and is particularly useful in the study of various tumor models. WDR5-IN-7 serves as a valuable tool for elucidating the role of WDR5 in oncogenic processes and for exploring therapeutic strategies in cancer research. -
WDR5-MLL1 Inhibitor
DDO-2213 is a potent inhibitor of the WDR5-MLL1 complex, exhibiting an IC50 of 29 nM and a Kd value of 72.9 nM for WDR5. This compound selectively targets MLL histone methyltransferase activity, effectively inhibiting the proliferation of cells containing MLL translocations. DDO-2213 is a valuable tool for research focused on MLL fusion leukemia and its underlying mechanisms. -
WDR5-MLL1 Inhibitor
WDR5-0102 is a selective inhibitor of the WDR5-MLL1 complex, exhibiting a dissociation constant (Kd) of 4 μM and a competitive inhibition constant (Kdis) of 7 μM. This compound effectively suppresses the H3K4 methyltransferase activity of MLL1 without affecting other human methyltransferases, including SETD7 and several others such as G9a, EHMT1, SUV39H2, SETD8, PRMT3, and PRMT5. WDR5-0102 is a valuable tool for investigating the role of MLL1 in various biological processes and its implications in cancer research. -
MLL1-WDR5 PPI Inhibitor
DDO-2093 is a selective inhibitor of the MLL1-WDR5 protein-protein interaction, exhibiting a potent IC50 of 8.6 nM and a dissociation constant (Kd) of 11.6 nM. This compound demonstrates significant antitumor activity by selectively targeting and inhibiting the catalytic function of the MLL complex. DDO-2093 is useful in research focused on understanding MLL-related oncogenesis and potential therapeutic strategies in cancer treatment. -
PARP-1 Inhibitor
PARP-1-IN-32 is a potent inhibitor of poly(ADP-ribose) polymerase-1 (PARP-1). This compound is utilized in cancer research to investigate the mechanisms of DNA repair and cellular response to genotoxic stress. Its ability to selectively inhibit PARP-1 makes it a valuable tool for studying the role of this enzyme in tumor biology and therapeutic resistance. -
SIRT6 Inhibitor
SIRT6-IN-6 is a selective inhibitor of SIRT6, demonstrating a potent IC50 of 4.93 μM and a Ki of approximately 10 μM. This compound shows significant selectivity against other histone deacetylases, including SIRT1-3 and HDAC1-11. Research findings indicate that SIRT6-IN-6 effectively elevates the expression of the glucose transporter GLUT-1, which contributes to the reduction of blood glucose levels in mouse models of type 2 diabetes. This reagent is valuable for studies focused on the mechanistic pathways associated with type 2 diabetes and metabolic regulation. -
Sirtuin Inhibitor
MC3482 is a selective inhibitor of sirtuin 5 (SIRT5), known for its role in mitochondrial metabolism and deacylation processes. This compound effectively modulates SIRT5 activity, making it valuable for studies examining the implications of SIRT5 in cellular energy regulation and metabolic disorders. Its use in research can contribute to understanding SIRT5's role in various physiological and pathological conditions, including cancer and neurodegeneration. -
SIRT5 Inhibitor
MC3138 is a selective SIRT5 inhibitor, demonstrating notable antitumor activity in human pancreatic ductal adenocarcinoma (PDAC) cells, with IC50 values ranging from 25.4 to 236.9 μM. In preclinical studies, MC3138 enhances the efficacy of Gemcitabine, significantly inhibiting tumor growth in murine models. This compound is valuable for research into targeted cancer therapies and the modulation of metabolic pathways related to SIRT5 activity. -
SIRT5 Inhibitor
Et-29 is a potent inhibitor of SIRT5, with a reported Ki value of 40 nM, demonstrating selectivity for this target. By modulating the activity of SIRT5, Et-29 plays a significant role in the study of metabolic processes and post-translational modifications. This reagent is ideal for research applications focused on the regulation of cellular metabolism and potential therapeutic strategies in metabolic diseases. -
SIRT6 Inhibitor
SIRT6-IN-2 is a selective and competitive inhibitor of SIRT6, exhibiting an IC50 of 34 μM. This compound enhances the acetylation of H3K9 and promotes glucose uptake in cultured cells. Additionally, SIRT6-IN-2 demonstrates the ability to reduce T cell proliferation, showcasing its immunosuppressive properties and potential chemosensitizing effects. Research applications include the study of metabolic regulation and immune response modulation. -
SIRT Inhibitor
SIRT-IN-3 is a selective inhibitor of SIRT1 with an IC50 of 17 μM. It demonstrates approximately 4-fold selectivity over SIRT2 and 14-fold selectivity over SIRT3, exhibiting IC50 values of 74 μM and 235 μM, respectively, for these isoforms. This compound is valuable for research applications investigating the role of SIRT1 in cellular processes, including aging, metabolism, and gene regulation. -
SIRT5 Inhibitor
SIRT5 Inhibitor 3 is a potent and competitive inhibitor of SIRT5, exhibiting an IC50 value of 5.9 μM. This compound effectively inhibits the desuccinylation activity of SIRT5, making it a valuable tool for studying the enzyme's role in various biological processes. SIRT5 Inhibitor 3 is applicable in research focused on cancer and neurodegenerative diseases, providing insights into potential therapeutic strategies. -
SIRT1 Inhibitor
SIRT1-IN-4 is a selective SIRT1 inhibitor that demonstrates an IC50 of 10.04 μM. This compound is utilized in research focused on cancer biology, providing valuable insights into the role of SIRT1 in tumorigenesis and potential therapeutic approaches. Further studies may explore its utility in modulating cellular processes regulated by SIRT1. -
SIRT1 Inhibitor
(S)-Selisistat is a selective inhibitor of SIRT1, demonstrating an IC50 value of 98 nM. This compound effectively modulates the activity of the sirtuin family of proteins, which are implicated in various cellular processes, including metabolism and aging. (S)-Selisistat is valuable for research exploring the role of SIRT1 in age-related diseases and metabolic disorders, making it a crucial tool for investigating therapeutic strategies in these areas.
