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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PARP1/2/6 Inhibitor
AZ9482 is a potent inhibitor of PARP1, PARP2, and PARP6, exhibiting IC50 values of 1 nM for both PARP1 and PARP2, and 640 nM for PARP6. This compound effectively disrupts the DNA repair pathway in cancer cells, making it a valuable tool for studying cellular response to DNA damage. AZ9482 is appropriate for applications in cancer research, particularly in the context of synthetic lethality and therapeutic resistance. -
PARP-1/2/7 Inhibitor
PARP7-IN-16 is a selective and orally bioavailable inhibitor of PARP-1, PARP-2, and PARP-7, exhibiting IC50 values of 0.94 nM, 0.87 nM, and 0.21 nM, respectively. This compound serves as a valuable research tool for investigating the roles of PARP enzymes in cellular processes and their implications in oncogenesis. It is particularly relevant for studies focusing on breast cancer and prostate cancer, providing insights into therapeutic strategies that target DNA repair mechanisms. -
PROTAC PARP1 Degrader
PROTAC PARP1 degrader-1 is a potent degrader targeting PARP1 through the PROTAC mechanism. This compound facilitates the activation of the cGAS/STING immune pathway, enhancing T cell-mediated cytotoxicity against tumor cells. Additionally, by inhibiting DNA damage repair, PROTAC PARP1 degrader-1 promotes the accumulation of cytosolic DNA fragments, making it a valuable tool for research in cancer immunotherapy and the study of DNA repair mechanisms. -
PARP Inhibitor
K-756 is a selective tankyrase (TNKS) inhibitor that effectively inhibits the ADP-ribosylation activity of TNKS1 and TNKS2, exhibiting IC50 values of 31 nM and 36 nM, respectively. This compound plays a significant role in the study of various cancer-related pathways and cellular processes influenced by tankyrase activity. K-756 is applicable in research focused on DNA repair mechanisms, cellular signaling, and the modulation of Wnt signaling pathways. -
PARP10/15 Inhibitor
PARP10/15-IN-1 is a selective inhibitor targeting both PARP10 and PARP15, exhibiting IC50 values of 160 nM and 370 nM, respectively. This compound serves as a valuable tool for cancer research, enabling the investigation of PARP10 and PARP15's roles in tumorigenesis and therapeutic resistance. Its dual inhibitory properties facilitate studies aimed at understanding the molecular mechanisms of cancer progression and the potential for targeted therapies. -
PARP10 Inhibitor
PARP10-IN-3 is a selective inhibitor of the mono-ADP-ribosyltransferase PARP10, exhibiting an IC50 of 480 nM against human PARP10. Additionally, it demonstrates significant inhibitory activity towards PARP2 and PARP15 with IC50 values of 1.7 μM. This compound serves as a valuable tool in research applications targeting the role of PARP enzymes in cellular processes and their implications in various diseases, including cancer. -
PARP1/2 Inhibitor
Simmiparib is a potent and orally active inhibitor of PARP1 and PARP2, demonstrating IC50 values of 1.75 nM and 0.22 nM, respectively. This compound effectively induces the accumulation of DNA double-strand breaks and triggers G2/M phase arrest in homologous recombination repair-deficient cells, leading to apoptosis. Simmiparib exhibits significant antitumor activity in various cancer models, including xenografts in nude mice, making it a valuable tool for cancer research and therapeutic development. -
PARP-1 Inhibitor
PARP1-IN-5 dihydrochloride is a potent and selective inhibitor of PARP-1, with an IC50 of 14.7 nM. This compound exhibits low toxicity and is suitable for oral administration. PARP1-IN-5 dihydrochloride is primarily utilized in cancer research to investigate the role of PARP-1 in tumorigenesis and therapy resistance. -
PARP7 Inhibitor
PARP7-IN-17 is a potent PARP7 inhibitor with an IC50 of 4.5 nM, demonstrating effective oral bioavailability. This compound exhibits significant antitumor activity, making it a valuable tool for research into cancer therapeutics and the biological role of PARP7 in tumorigenesis. Its selective inhibition of PARP7 may aid in the development of targeted cancer treatments. -
PARP7 Inhibitor
PARP7-IN-22 is a potent PARP7 inhibitor with an IC50 of 0.6 nM. This compound is orally active and enhances type I interferon signaling in vitro, facilitating T cell infiltration into tumor tissues and significantly inhibiting tumor growth. PARP7-IN-22 is of particular interest for research in cancer immunotherapy, providing valuable insights into therapeutic strategies that target immune responses in oncology. -
PARP Inhibitor
PARP7-IN-16 free base is a selective, orally active inhibitor of PARP-1, PARP-2, and PARP-7, exhibiting IC50 values of 0.94 nM, 0.87 nM, and 0.21 nM, respectively. This compound is valuable for investigating the role of PARP enzymes in DNA repair mechanisms and is particularly relevant in studies focused on breast and prostate cancer. Researchers can utilize PARP7-IN-16 free base to explore therapeutic strategies targeting these types of malignancies. -
PARP1 Inhibitor
PARP1-IN-11 is a selective inhibitor of the poly(ADP-ribose) polymerase 1 (PARP1) enzyme, demonstrating a potent inhibitory activity with an IC50 value of 0.082 µM. This compound exhibits complete inhibition of PARP2 and significantly inhibits the activity of PARP3, as well as tankyrases TNKS1 and TNKS2. PARP1-IN-11 is valuable for research applications focused on DNA repair mechanisms, cancer therapeutics, and the study of cellular responses to genotoxic stress. -
PARP14 PROTAC Degrader
RBN012811 is a selective PROTAC degrader that targets PARP14, facilitating its degradation through a ternary complex with cereblon by binding at the NAD+ site. With an IC50 of 10 nM, RBN012811 efficiently reduces endogenous PARP14 levels in various cell lines and primary human macrophages. This reduction is associated with decreased IL-10 production and IFN-β mRNA, alongside an increase in phosphorylated STAT1, thereby enhancing inflammatory signaling and inhibiting interferon-induced ADPr condensate formation. RBN012811 also influences viral replication dynamics, promoting HSV1 replication while diminishing VSV replication, making it valuable for research in cancer biology and viral infections. -
PARP1 Inhibitor
PARP1-IN-33 is a potent inhibitor of PARP1, exhibiting an IC50 of 0.41 nM. This compound demonstrates significant cytoprotective effects on retinal cells, with an EC50 of 0.02 nM in inhibiting MTS activity in H2O2-induced human retinal pigment epithelial cells. PARP1-IN-33 is valuable for research applications aimed at understanding retinal oxidative stress and developing therapeutic strategies for retinal diseases. -
PARP-1 Inhibitor
A-620223 is a potent inhibitor of PARP-1, exhibiting a Ki of 8 nM and an EC50 of 3 nM in whole cell assays. This compound demonstrates significant in vivo efficacy in murine models, particularly in the B16F10 melanoma model when used in combination with Temozolomide and in the MX-1 breast xenograft model with Cisplatin. A-620223 is suitable for research applications focusing on melanoma and breast cancer therapy. -
PARP Inhibitor
Saruparib is a potent and selective PARP inhibitor, primarily targeting PARP1 with an IC50 value of 3 nM and PARP2 with an IC50 of 1400 nM. This orally active compound demonstrates significant anti-proliferative effects and is particularly effective in inhibiting the growth of cells exhibiting deficiencies in DNA repair mechanisms. Saruparib is commonly utilized in research focused on cancer treatment strategies, particularly in the context of homologous recombination repair-deficient tumors. -
PARP1 Inhibitor
Fluzoparib is a highly potent oral inhibitor of PARP1, demonstrating an IC50 of 1.46 ± 0.72 nM in cell-free enzymatic assays. This compound selectively targets homologous recombination repair (HR)-deficient cells while sensitizing both HR-deficient and HR-proficient cells to cytotoxic agents. With favorable pharmacokinetic properties in vivo, Fluzoparib is an important reagent for studying BRCA1/2-mutant relapsed ovarian cancer and related therapeutic strategies. -
PARP14 Inhibitor
RBN012759 is a potent and selective inhibitor of PARP14, exhibiting an IC50 of less than 3 nM. It demonstrates 300-fold selectivity for monoPARPs and 1000-fold selectivity for polyPARPs. RBN012759 has been shown to diminish pro-tumor macrophage activity and trigger inflammatory responses in tumor explants, making it a valuable tool for research in cancer biology and immune modulation. -
PARP Inhibitor
Basroparib is a selective inhibitor of tankyrase (TNKS1/TNKS2) with IC50 values of 29.94 nM and 3.68 nM, respectively, and exhibits limited activity against PARP1 (IC50 > 10 μM). This compound stabilizes AXIN1/2 proteins and effectively disrupts the Wnt/β-catenin signaling pathway, leading to inhibition of tumor cell proliferation and induction of apoptosis. Basroparib is particularly relevant for research in colorectal cancer (CRC) models bearing KRAS mutations, such as G12V/G12D, and demonstrates potential to overcome resistance to MEK inhibitors, providing synergistic antitumor effects. -
PARP Inhibitor
Benzamide is a potent inhibitor of poly(ADP-ribose) polymerase (PARP), demonstrating significant neuroprotective effects. It has been shown to protect against neurotoxicity induced by glutamate and methamphetamine in vitro. In vivo studies indicate that Benzamide can mitigate methamphetamine-induced dopamine depletions in mice without acute effects on striatal dopamine metabolism or body temperature regulation. Its dual role in neuroprotection and PARP inhibition makes it a valuable tool in neuropharmacology research. -
PARP10 Inhibitor
OUL232 is a potent inhibitor of poly(ADP-ribose) polymerase 10 (PARP10) and other mono-ADP-ribosyl transferases including PARP7, PARP11, PARP12, PARP14, and PARP15. With an IC50 of 7.8 nM, OUL232 represents the most effective PARP10 inhibitor characterized to date and is the first reported inhibitor targeting PARP12. This compound is valuable for studying the biological roles of PARP10 and PARP12 in cellular processes and may facilitate research into therapeutic strategies involving these targets. -
CBP/EP300 Inhibitor
CBP/EP300 bromodomain receptor-IN-1 is a selective inhibitor of the CBP/EP300 bromodomain. This compound demonstrates high-affinity binding to bromodomain-containing proteins at nanomolar concentrations. Its primary application lies in research focused on epigenetic regulation and oncogenesis, making it a valuable tool for studying gene expression modulation and therapeutic interventions in cancer biology. -
BRD4/CBP/p300 Inhibitor
CBP/p300/BRD4 ligand-1 is a small-molecule inhibitor that specifically targets the bromodomain and extraterminal (BET) family members BRD4, as well as the acetyltransferases CBP and p300. This compound functions by competitively binding to the functional domains of these proteins, preserving critical interactions. CBP/p300/BRD4 ligand-1 is suitable for the development of dual-target PROTAC degraders, making it valuable for research in prostate cancer and various other malignancies. -
EP300/CBP HAT Inhibitor
CBP/p300-IN-17 is a potent inhibitor of the EP300 and CBP histone acetyltransferases (HATs), exhibiting IC50 values of 0.18 µM and 0.69 µM for EP300 and LK2 H3K27, respectively. This compound demonstrates significant biological activity in modifying histone acetylation, making it valuable for research in epigenetics, cancer biology, and transcriptional regulation. Its selective inhibition of EP300 and CBP provides a critical tool for investigating their roles in various cellular processes and disease states. -
P300 HAT Inhibitor
P300-IN-6 is an orally bioavailable inhibitor targeting the histone acetyltransferase p300 HAT domain, exhibiting a human IC50 of 7 nM. This compound effectively suppresses c-Myc expression and reduces acetylation levels of histones H3K18 and H3K27, leading to inhibition of cancer cell proliferation. P300-IN-6 demonstrates significant antitumor activity in xenograft mouse models, making it a valuable tool for investigating therapeutic strategies in multiple myeloma research. -
HAT Inhibitor
SYY-B085-1 is a histone acetyltransferase (HAT) inhibitor with specific activity against various HAT enzymes. This compound plays a critical role in the regulation of gene expression and cellular processes by modulating acetylation levels on histones. SYY-B085-1 is utilized in research to explore the effects of HAT inhibition in cancer biology and epigenetic regulation. Its unique mechanism offers valuable insights for studies focused on transcriptional modulation and potential therapeutic interventions. -
p300/CBP HAT Inhibitor
CBP/p300-IN-19 is a potent inhibitor of the histone acetyltransferase (HAT) activity of p300 and CBP, exhibiting IC50 values of 1.4 µM and 2.2 µM, respectively, while showing limited inhibition of PCAF and Myst3 (>100 µM). This compound demonstrates significant anti-tumor activity, making it valuable for research into cancer biology and epigenetic regulation. Its ability to selectively target p300/CBP HAT provides a useful tool for investigating the role of acetylation in various cellular processes and disease states. -
EP300/CBP Inhibitor
EP300/CBP-IN-1 is a highly selective inhibitor targeting the EP300 and CBP bromodomain proteins, exhibiting IC50 values of 2.3 nM and 2.1 nM for CBP and EP300, respectively. This compound demonstrates significant anti-proliferative effects on CWR22RV1 prostate cancer cells, making it a valuable tool for research in cancer biology and epigenetic regulation. Its application extends towards elucidating the roles of EP300 and CBP in various cellular processes and disease states. -
HAT Inhibitor
DS-9300 is a selective inhibitor of the EP300/CBP histone acetyltransferases (HATs) with a potent IC50 value of 28 nM. This compound demonstrates significant anticancer activity and is applicable in prostate cancer research, providing valuable insights into the mechanisms of acetylation in tumorigenesis. DS-9300 serves as a critical tool for studying the role of HATs in cancer progression and therapeutic resistance. -
CBP/p300 Inhibitor
CBP/p300 Ligand 3 is a selective inhibitor targeting the CBP/p300 proteins, which function as histone acetyltransferases (HATs). By binding to specific domains within CBP/p300, this compound effectively inhibits their enzymatic activity and modulates interactions with transcription factors. This inhibition alters chromatin structure and gene expression, making CBP/p300 Ligand 3 a valuable tool for studying the role of CBP/p300 in various biological processes, including cancer progression and neurodegenerative diseases, where dysregulation of CBP/p300 is implicated. -
HAT Inhibitor
NSC 694623 is a potent inhibitor of histone acetyltransferases (HATs), with an IC50 value of 15.9 μM for recombinant p300/CBP-associated factor (PCAF). This compound exhibits antiproliferative effects on various cancer cell lines, making it a valuable tool for cancer research. Its capacity to modulate histone acetylation offers potential insights into epigenetic regulation and therapeutic strategies in oncology. -
CBP/p300 Inhibitor
PU141 is a selective inhibitor of the histone acetyltransferases CBP and p300. This compound induces cellular histone hypoacetylation, leading to significant inhibition of cell growth in various neoplastic cell lines derived from multiple tissue types. PU141 is primarily utilized in cancer research to explore mechanisms of transcriptional regulation and therapeutic interventions. -
p300/CBP HAT Inhibitor
CBP/p300-IN-19 hydrochloride is a selective inhibitor of the histone acetyltransferases (HAT) p300 and CBP, exhibiting IC50 values of 1.4 µM and 2.2 µM, respectively. It demonstrates significant antitumor activity, making it a valuable tool for cancer research. This compound can be applied in studies investigating the roles of acetylation in gene regulation and cell proliferation, as well as in the development of targeted therapies. -
PROTAC p300/CBP Degrader
QC-182 is a potent PROTAC degrader targeting p300/CBP, facilitating the degradation of these proteins. It effectively reduces p300 protein levels in SK-HEP-1 cells, with a DC50 of 93 nM. Additionally, QC-182 demonstrates significant growth inhibition in SK-HEP-1 and JHH7 cell lines, with IC50 values of 0.733 μM and 0.477 μM, respectively. This reagent is valuable for research focused on hepatocellular carcinoma (HCC). -
CBP HAT Inhibitor
NiCur is a potent and selective inhibitor of CBP histone acetyltransferase (HAT) with an IC50 value of 0.35 μM. By targeting CBP HAT activity, NiCur effectively downregulates p53 activation in response to genotoxic stress. This compound is suitable for mechanistic studies, allowing researchers to investigate pathways involving histone acetylation without altering the expression of target proteins. -
HAT Inhibitor
SYY-B029-2 is a potent inhibitor of histone acetyltransferases (HATs), exhibiting an IC50 of 1.4 nM. This compound demonstrates significant anti-proliferative effects on human mantle cell lymphoma (MCL) cell line MAVER-1 and human castration-resistant prostate cancer cell line LNCaP clone FGC, with IC50 values of 15 nM and 13 nM, respectively. SYY-B029-2 serves as a valuable tool for research into epigenetic regulation and cancer therapy. -
P300/CBP Inhibitor
Pocenbrodib is a potent inhibitor of the P300/CBP transcriptional coactivators. By blocking the function of these coactivators, Pocenbrodib effectively inhibits the acetylation of both histone and non-histone proteins, impacting gene expression regulation. This compound is particularly valuable for research into castration-resistant prostate cancer and other cancer types that are associated with dysregulated acetylation processes. -
p300/CBP Inhibitor
CBP/p300-IN-5 is a potent inhibitor of p300/CBP histone acetyltransferase, demonstrating an IC50 value of 18.8 nM. This compound serves as a valuable tool for studying the role of histone acetylation in gene regulation and various biological processes. Its application is significant in cancer research and therapeutic development, where modulation of acetylation pathways is of interest. -
p300/CBP HAT Inhibitor
B026 is a selective and potent inhibitor of the p300/CBP histone acetyltransferase (HAT) with IC50 values of 1.8 nM for p300 and 9.5 nM for CBP. This compound exhibits significant anticancer activity against androgen receptor-positive (AR+) prostate cancer cell lines, making it a valuable tool for research in cancer biology and epigenetic regulation. Its oral bioavailability enables easy administration for in vivo studies targeting p300/CBP-mediated pathways. -
CBP/p300 Inhibitor
CBP/p300-IN-20 is a selective inhibitor of the p300/CBP transcriptional coactivators, displaying a high potency with a pIC50 of 10.1 for p300. This compound is useful in cancer research, providing insights into the role of p300/CBP in oncogenic transcriptional regulation and potential therapeutic interventions. Its specificity towards p300 allows for targeted studies in related signaling pathways and tumor biology. -
CBP/EP300 Inhibitor
CBP/p300-IN-14 is a highly potent inhibitor of CBP/EP300, a lysine acetyltransferase, with an IC50 of 3.3 nM. This compound is utilized to study the role of CBP/EP300 in various biological processes, including transcriptional regulation and cellular signaling pathways. Its application is critical in research focused on cancer, metabolic disorders, and other diseases where histone acetylation plays a significant role. -
EP300/CBP HAT Inhibitor
CBP/p300-IN-18 is a potent inhibitor of the EP300 and CBP histone acetyltransferases (HATs), exhibiting IC50 values of 0.056 µM and 0.46 µM for EP300 and LK2 H3K27, respectively. This compound serves as a valuable tool for investigating the role of histone acetylation in various biological processes and disease states. It is particularly useful in studies focused on chromatin remodeling, gene expression, and potential therapeutic applications in cancer and other disorders associated with dysregulated acetylation. -
CBP/p300 Inhibitor
CBP/p300-IN-21 is a selective inhibitor of the CBP/p300 transcriptional co-activators, exhibiting IC50 values of 0.07 μM for p300 and 1.755 μM for CBP. This compound effectively reduces the acetylation level of histone H3 at lysine 18 (H3K18Ac), implicating a potential role in modulating gene expression. Furthermore, CBP/p300-IN-21 has demonstrated efficacy in inhibiting the growth of 4T1 tumors in murine models, highlighting its relevance in cancer research and therapeutic applications. -
CBP/p300 Inhibitor
CBP/p300-IN-15 is a potent inhibitor of the CBP/p300 coactivators, exhibiting IC50 values of 2.50 nM for p300 and 28.0 nM for CBP. This compound demonstrates significant biological activity in ovarian cancer cell lines, with EC50 values of 0.865 μM for OVCAR-3 and 2.71 μM for A2780. CBP/p300-IN-15 is a valuable tool for investigating the role of CBP/p300 in ovarian cancer research and could provide insights into therapeutic strategies targeting these coactivators. -
Ep300/CREBBP Inhibitor
Ep300/CREBBP-IN-3 is a potent inhibitor of the Ep300 and CREBBP enzymes, demonstrating IC50 values of 0.056 μM and 0.095 μM, respectively. This compound is primarily utilized in cancer research, facilitating investigations into the role of histone acetylation in tumor progression and therapy resistance. Its ability to selectively inhibit these acetyltransferases makes it a valuable tool for understanding the epigenetic regulation of gene expression in oncology. -
BRD4/CBP/p300 PROTAC Degrader
PROTAC CBP/p300/BRD4 Degrader-1 is a dual-target PROTAC degrader that specifically targets BRD4, CBP, and p300, achieving DC50 values of 8.8 pM, 6.55 nM, and 1.05 nM, respectively. This compound promotes CRBN- and proteasome-mediated degradation of BRD4 and CBP/p300, leading to the downregulation of c-Myc and acetyl-H3K27, and inducing apoptosis. It exhibits significant antiproliferative and antitumor effects, demonstrated by tumor growth inhibition in xenograft models. PROTAC CBP/p300/BRD4 Degrader-1 is a valuable tool for research focused on prostate and colorectal cancer. -
HAT Inhibitor
PU139 is a potent pan-histone acetyltransferase (HAT) inhibitor that specifically targets Gcn5, p300/CBP-associated factor (PCAF), CREB-binding protein (CBP), and p300. This compound demonstrates inhibitory activity with IC50 values of 8.39 μM, 9.74 μM, 2.49 μM, and 5.35 μM for each respective HAT. PU139 is valuable for research applications exploring histone acetylation and its roles in gene regulation, cellular signaling, and cancer biology. -
EP300/CBP Inhibitor
CPI-1612 is a potent, orally active inhibitor of EP300/CREB-binding protein (CBP) histone acetyltransferase, exhibiting an IC50 of 8.1 nM for EP300 HAT. This compound demonstrates significant anticancer activity, making it a valuable tool for cancer research. Its ability to modulate acetylation pathways enables investigations into epigenetic regulation and therapeutic strategies targeting malignancies. -
KDM2B Inhibitor
KDM2B-IN-3 is a selective inhibitor of the histone demethylase KDM2B, designed to modulate epigenetic regulation. By inhibiting KDM2B, this compound can alter histone methylation patterns, making it a valuable tool for cancer research and investigations into epigenetic modifications. Its potential applications include studying the role of KDM2B in tumorigenesis and evaluating therapeutic strategies targeting epigenetic regulators. -
LSD1 Inhibitor
Pulrodemstat (hydrochloride) is a potent and selective reversible inhibitor of lysine-specific demethylase-1 (LSD1), exhibiting an IC50 value of 0.25 nM. This compound demonstrates minimal enzymatic inhibition of LSD2, MAO-A, and MAO-B, making it a highly specific agent. Pulrodemstat (hydrochloride) promotes differentiation in acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells, showcasing significant anticancer activity. It serves as a valuable tool for research in cancer biology and therapeutic development.
