Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-12 (compound 9c) is a bifunctional molecule designed to target and degrade the bromodomain-containing protein BRD4 by recruiting the von Hippel–Lindau (VHL) E3 ubiquitin ligase. It functions as a highly potent degrader, with a DC₅₀ of 0.39 nM and 0.24 nM when conjugated to STEAP1 and CLL1 antibodies, respectively, enabling targeted delivery and degradation of BRD4 in PC3 prostate cancer cells. -
PROTAC BRD4 degrader
dBET23 is a highly potent and selective PROTAC degrader targeting the bromodomain-containing protein BRD4. It exhibits a DC₅₀ of approximately 50 nM at 5 hours for the BRD4 bromodomain 1 (BRD4^BD1) protein, effectively promoting its ubiquitination and proteasomal degradation. dBET23 serves as a valuable chemical tool for studying BRD4-dependent transcriptional regulation and holds potential for therapeutic applications in BRD4-driven cancers. -
PROTAC BET degrader
SJ995973 is a highly potent PROTAC (proteolysis-targeting chimera) designed to selectively degrade bromodomain and extra-terminal domain (BET) family proteins, including BRD2, BRD3, and BRD4. By inducing targeted proteasomal degradation, SJ995973 enables efficient disruption of BET protein function, offering a powerful approach for investigating BET-related transcriptional regulation and for the development of novel anticancer therapies. -
FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
Protac smarca2 degrader
SMD-3040 formate is a potent and selective PROTAC degrader targeting SMARCA2, a core ATPase subunit of the SWI/SNF chromatin remodeling complex. It exhibits strong in vivo antitumor activity, making it a promising candidate for cancer research involving epigenetic regulation and synthetic lethality strategies. -
PROTAC CBP/p300 Degrader
CBPD-409 is an orally active PROTAC degrader targeting CBP/p300, with a DC₅₀ of 0.2–0.4 nM. It shows potent antiproliferative activity in AR⁺ prostate cancer cell lines (VCaP, LNCaP, 22Rv1) with IC₅₀ values of 1.2–2.0 nM and demonstrates significant antitumor efficacy. -
PROTAC CBP/p300 degrader
JET-209 is a potent PROTAC degrader targeting CBP and p300, with DC₅₀ values of 0.05 nM and 0.2 nM, respectively. It is composed of lenalidomide, a linker, and the bromodomain inhibitor GNE-207. JET-209 is a valuable tool for cancer research involving epigenetic regulation. -
BRD9 Degrader
FHD-609 is a PROTAC degrader and inhibitor of BRD9, a key component of the non-canonical BAF (ncBAF) chromatin remodeling complex. It is designed for studying cancers harboring mutations in BAF complex subunits. FHD-609 shows potential in adrenocortical carcinoma (ACC) treatment, particularly in combination with Telomelysin or INO5401. -
PROTAC p300/CBP Degrader
dCBP-1 is a potent and selective heterobifunctional PROTAC degrader of p300/CBP, utilizing a cereblon ligand for E3 ligase recruitment. It effectively eliminates oncogenic enhancer activity driving MYC expression and demonstrates strong cytotoxicity against multiple myeloma cells, making it a valuable tool for epigenetic and cancer research. -
PROTAC BRD4 Degrader
GNE-987 is a highly potent PROTAC degrader of BRD4, composed of a BET inhibitor, a von Hippel-Lindau (VHL) ligand, and a ten-methylene linker. It binds both BD1 and BD2 bromodomains of BRD4 with low nanomolar affinity (IC₅₀ = 4.7 and 4.4 nM) and induces BRD4 degradation with a DC₅₀ of 0.03 nM in EOL-1 AML cells. GNE-987 is also suitable for use in PROTAC–Antibody Conjugates (PAC), making it a valuable tool for targeted protein degradation and epigenetic cancer research. -
PROTAC SMARCA2/SMARCA4 degrader
AU-15330 is a PROTAC degrader targeting the SWI/SNF chromatin remodeling ATPase subunits SMARCA2 and SMARCA4. It effectively suppresses tumor growth in prostate cancer xenograft models and enhances the therapeutic efficacy of the AR antagonist enzalutamide. AU-15330 also induces remission in castration-resistant prostate cancer models, demonstrating strong antitumor activity with a favorable safety profile. -
SMARCA2/SMARCA4/PBRM1 Degrader
ACBI1 is a potent and cooperative PROTAC degrader targeting SMARCA2, SMARCA4, and PBRM1, with DC₅₀ values of 6 nM, 11 nM, and 32 nM, respectively. It exhibits strong anti-proliferative activity and induces apoptosis, making it a valuable tool for studying chromatin remodeling and cancer therapeutics. -
SMARCA2/SMARCA4/PBRM1 Degrader
AU-24118 is an orally bioavailable PROTAC degrader targeting the mSWI/SNF chromatin remodeling complex ATPases SMARCA2 and SMARCA4, as well as PBRM1. It offers a powerful approach for modulating epigenetic regulation and holds promise for the treatment of cancers driven by alterations in SWI/SNF complex components. -
PROTAC BRD9 Degrader
CFT8634 is an orally bioavailable PROTAC that targets the E3 ubiquitin ligase CRBN to degrade BRD9. This heterobifunctional molecule effectively inhibits the growth of tumor cells reliant on BRD9, making it a valuable tool for researching synovial sarcoma and SMARCB1-deficient solid tumors. CFT8634 facilitates targeted degradation through its unique binding properties, offering a strategic approach to investigate the role of BRD9 in SMARCB1-related cancers, including malignant rhabdoid tumors. -
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. -
GSPT1/BRD4 Degrader
DP-15 is a targeted degrader for GSPT1 and BRD4, demonstrating DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits potent anti-proliferative effects against acute myeloid leukemia (AML) and non-Hodgkin lymphoma (NHL) cells, with IC50 values in the nanomolar range. Additionally, DP-15 induces G1 phase cell cycle arrest and promotes apoptosis in MOLM13 cells. In vivo studies have shown its effective anti-leukemia activity in MOLM-13 xenograft mouse models, supporting its potential application in cancer research. -
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. -
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. -
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. -
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. -
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.
