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Catalog No.
Product Name
Application
Product Information
Citations
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PCAF inhibitor
L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-permeable inhibitor of the p300/CBP-associated factor (PCAF) bromodomain, with a Kd of 126 nM. -
BET inhibitor
JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1, a BET inhibitor, modified for click chemistry applications. It serves as a molecular probe for in vitro and in vivo studies. -
SPIN1 inhibitor
MS31 is a potent, highly selective fragment-like inhibitor of the methyllysine reader protein spindlin 1 (SPIN1). It strongly inhibits SPIN1 interactions with H3K4me3, with IC50 values of 77 nM (AlphaLISA) and 243 nM (FP). MS31 selectively binds to Tudor domain II of SPIN1 with a Kd of 91 nM and potently blocks binding of trimethyllysine-containing peptides to SPIN1. It exhibits no toxicity toward nontumorigenic cells. -
SP140 Inhibitor
GSK761 is a selective inhibitor of speckled 140 kDa (SP140) protein, with an IC50 of 77.79 nM. It suppresses monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation. Additionally, GSK761 promotes the production of CD206+ regulatory macrophages by inhibiting SP140. -
ATAD2 bromodomain inhibitor
AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor, demonstrating cellular target engagement and antiproliferative activity in various breast cancer models. It inhibits ATAD2 with pIC50 values of 8.2 in the ATAD2 FRET assay and 6.2 in the ATAD2 NanoBRET assay. -
BET inhibitor
Amredobresib (BI894999) is an orally active BET inhibitor that potently blocks the binding of BRD4-BD1 and BRD4-BD2 bromodomains to acetylated histones, with IC50 values of 5 nM and 41 nM, respectively. It demonstrates anticancer activity against acute myeloid leukemia (AML) and NUT carcinoma. -
BET/BRD4 bromodomain inhibitor
AZD5153 is a bivalent, selective, and orally active BET/BRD4 bromodomain inhibitor with an IC50 of 5 nM for full-length BRD4 (FL-BRD4). It simultaneously binds both bromodomains of BRD4, enhancing its inhibitory potency. AZD5153 is applicable for research into cancers, including acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma. -
BET family bromodomain inhibitor
NHWD-870 is a potent, orally active, and selective BET family bromodomain inhibitor, specifically targeting BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. It exhibits strong tumor-suppressive effects, enhances tumor apoptosis, inhibits tumor proliferation, and disrupts cancer cell-macrophage interactions. -
Menin-MLL inhibitor
BMF-219 (Menin-MLL inhibitor 21) is a specific, irreversible inhibitor of the Menin-MLL interaction, suitable for research into autoimmune diseases, heteroimmune diseases, cancer, and other menin-MLL-dependent conditions. -
CECR2 inhibitor
NVS-CECR2-1 is a potent and selective non-BET family bromodomain (BRD) inhibitor targeting cat eye syndrome chromosome region, candidate 2 (CECR2). It binds CECR2 BRD with high affinity (IC50 = 47 nM; KD = 80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis in various cancer cells through both CECR2-dependent and CECR2-independent mechanisms. -
ENL/AF9 YEATS domain inhibitor
SR-0813 is a potent and selective inhibitor of the ENL and AF9 YEATS domains. It exhibits IC50 and EC50 values of 25 nM and 205 nM, respectively, for the ENL YEATS domain, and 311 nM and 76 nM (CETSA) for the AF9 YEATS domain. SR-0813 binds MAP3K19 with significantly lower affinity (Kd = 3.5 μM) compared to ENL YEATS (Kd = 30 nM), demonstrating over 100-fold selectivity. It is suitable for research into acute leukemia. -
BPTF inhibitor
BPTF-IN-BZ1 is a highly potent BPTF inhibitor with a Kd of 6.3 nM. -
PBRM1 Bromodomain inhibitor
PBRM1-BD2-IN-8 (compound 34) is a potent inhibitor of the PBRM1 bromodomain, with a Kd of 4.4 μM and an IC50 of 0.16 μM for PBRM1-BD2, and a Kd of 25 μM for PBRM1-BD5. It exhibits anti-cancer activity. -
Menin-MLL Interaction Inhibitor
Ziftomenib (KO-539) is an orally active inhibitor of the menin–MLL (KMT2A) interaction, designed to disrupt oncogenic gene expression in MLL-rearranged cancers. It exhibits potent antitumor activity and is under investigation for the treatment of acute leukemias driven by MLL rearrangements or NPM1 mutations. Ziftomenib corresponds to compound 151 in patent WO2017161028A1. -
Menin-MLL Interaction Inhibitor
DSP5336 is an orally active small molecule inhibitor that targets the interaction between menin and MLL (mixed-lineage leukemia) proteins. By disrupting this protein–protein interaction, DSP5336 impairs leukemogenic gene expression programs driven by MLL rearrangements. It is currently undergoing clinical evaluation for the treatment of patients with relapsed or refractory acute leukemia, particularly those harboring MLL rearrangements. -
DK/PI3K/BRD4 Inhibitor
SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of <2.5 nM for CDK4, 3.3 nM for CDK6, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, and 33 nM and 89 nM for BRD4 BD1 and BD2, respectively. It exhibits broad cytotoxic activity against cancer cells while sparing normal epithelial cells, highlighting its potential as a targeted cancer therapeutic with reduced toxicity. -
PI3K/BRD4 Inhibitor
PI3Kα-IN-28 is a potent dual-target inhibitor of PI3K and BRD4. This compound effectively suppresses cell proliferation in various cancer cell lines, including KYSE180 and KYSE450, while also inhibiting migration and colony formation. Additionally, PI3Kα-IN-28 induces G0/G1 phase cell cycle arrest and promotes cellular senescence by enhancing the proportion of senescent cells. Mechanistically, it decreases the levels of p-AKT and c-Myc, while activating the AMPK-p27 pathway, making it a valuable tool for cancer research, particularly in esophageal cancer studies. -
BET/HDAC Inhibitor
TW9 is a potent dual inhibitor that targets bromodomain and extraterminal (BET) proteins and histone deacetylases (HDAC) with KDs of 0.069 μM and 0.231 μM for BRD4(1) and BRD4(2), respectively, and an IC50 of 0.29 μM for HDAC1. This compound is a novel derivative of the BET inhibitor (+)-JQ1 and the class I HDAC inhibitor CI994. TW9 demonstrates significant anti-tumor activity in pancreatic ductal adenocarcinoma (PDAC) and enhances the efficacy of the chemotherapeutic agent Gemcitabine, making it a valuable tool for cancer research applications. -
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/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. -
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. -
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. -
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. -
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/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. -
EP300/CBP Inhibitor
DS17701585 is a selective inhibitor of EP300 and CBP, demonstrating IC50 values of 0.040 µM for CBP, 0.15 µM for EP300, 0.45 µM for H3K27, and 0.70 µM for SOX2. This compound is orally active and is primarily utilized in cancer research to explore the roles of histone acetyltransferases and related transcriptional regulators in tumorigenesis. Its specificity and potency make it a valuable tool for investigating the epigenetic mechanisms underlying various cancers.
