Catalog No.
Product Name
Application
Product Information
Citations
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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. -
SMARCA2 Degrader
ACBI2 is a potent VHL PROTAC designed for the targeted degradation of SMARCA2. With an EC50 of 7 nM and a DC50 of 1 nM in RKO cells, ACBI2 selectively modulates SMARCA2 levels, making it a valuable tool for studying SMARCA2-related pathways. This compound is particularly relevant in lung cancer research, facilitating investigations into therapeutic strategies targeting SMARCA2 degradation. -
PROTAC BRD4 Degrader
GAL-02-221 is a PROTAC designed to target and degrade BRD4 through ligands that recruit von Hippel-Lindau (VHL) E3 ligase. This compound effectively promotes the degradation of BRD4 in both HER2-positive and negative breast cancer cell lines, demonstrating potential utility in the study of tumor biology and therapeutic approaches. Its ability to selectively eliminate BRD4 highlights its relevance in cancer research and provides a valuable tool for investigating mechanisms of oncogenesis and treatment resistance. -
PROTAC CBP/P300 Degrader
PROTAC CBP/P300 Degrader-1 is a highly effective PROTAC designed to selectively degrade the CBP and p300 proteins. This compound exhibits significant potency in reducing cell viability across various cancer cell lines, making it a valuable tool for research in cancer biology and therapeutic development. Its ability to modulate the activity of these key transcription coactivators facilitates investigations into oncogenic pathways and potential treatment strategies. -
SMARCA2 PROTAC Degrader
YD23 is a selective SMARCA2 PROTAC degrader with DC50 values of 64 nM and 297 nM in H1792 and H1975 cell lines, respectively. This reagent induces the degradation of SMARCA2, exhibiting synthetic lethality towards SMARCA4-deficient cells and selectively inhibiting growth in SMARCA4 mutant lung cancer cells. YD23 also reduces chromatin accessibility in SMARCA4 deficient cells, impacting genes associated with cell cycle and growth regulation. It is a valuable tool for researching non-small cell lung cancer (NSCLC) and evaluating tumor growth in SMARCA4-mutant xenograft models. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-8 is a proteolysis-targeting chimera (PROTAC) that engages both von Hippel-Lindau (VHL) and BRD4, exhibiting IC50 values of 1.1 nM for BRD4 BD1 and 1.4 nM for BRD4 BD2. This compound effectively promotes the degradation of BRD4 protein in PC3 prostate cancer cells, making it a valuable tool for research into BRD4-related signaling pathways and cancer therapeutics. Its high potency highlights its potential use in studying mechanisms of protein regulation and developing novel cancer treatments. -
PROTAC BRD Degrader
β-NF-JQ1 is a PROTAC that targets bromodomain-containing (BRD) proteins by leveraging β-NF as a ligand for the Aryl Hydrocarbon Receptor (AhR) E3 ligase. This compound facilitates the degradation of BRD proteins through the recruitment of AhR, leading to effective protein knockdown. β-NF-JQ1 demonstrates significant anticancer activity, making it a valuable tool for research in cancer biology and the development of targeted therapeutic strategies. -
CBP/p300 PROTAC Degrader
CBPD-268 is a highly potent CBP/p300 PROTAC degrader, exhibiting a DC50 value of ≤ 0.03 nM. This compound effectively induces degradation of CBP/p300 and demonstrates significant inhibition of cell growth, showcasing its antitumor potential. CBPD-268 is particularly relevant for research into androgen receptor-positive prostate cancer, facilitating studies on novel therapeutic strategies. -
PROTACs
PROTAC BRD9 Degrader-4 is a bifunctional degrader targeting BRD9 through the proteolysis-targeting chimera (PROTAC) mechanism. It effectively induces degradation of BRD9, thereby altering oncogenic pathways associated with various cancers. This compound is utilized in cancer research to study the therapeutic potential of BRD9 modulation and the implications of targeted degradation in tumor biology. -
BRD42/BRD4 Degrader
IBG1 is a molecular glue degrader that selectively targets BRD2 and BRD4, exhibiting a degradation capability with a DC50 of 0.15 nM. Notably, IBG1 does not significantly impact the paralogue BRD3. This compound effectively inhibits the growth of cancer cells and is a valuable tool for research focused on tumor biology and therapeutic strategies. -
SMARCA2 PROTAC degrader
SMD-3040 is a selective SMARCA2 PROTAC degrader with a DC50 of 12 nM and a maximal degradation efficiency of 91%. This compound effectively inhibits tumor cell proliferation, demonstrating significant antitumor activity. SMD-3040 is particularly useful in studies related to various tumors, including melanoma. -
PROTAC BRD4 Degrader
PROTAC BET Degrader-10 is a selective degrader targeting the BET protein BRD4 through a PROTAC mechanism, featuring a DC50 of 49 nM. This compound utilizes ligands for Cereblon and BRD4, promoting the ubiquitination and subsequent degradation of BRD4. It serves as a valuable tool for investigating the role of BRD4 in various biological processes and cancer-related research applications. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-1 is a novel PROTAC that utilizes ligands for both Cereblon and BRD4, exhibiting an IC50 of 41.8 nM against the BRD4 bromodomain 1 (BD1). This compound promotes the degradation of BRD4 protein, leading to a significant decrease in c-Myc expression. It is designed for research applications aimed at understanding the role of BRD4 in transcriptional regulation and its implications in various cancers. -
PROTAC BRD4 Degrader
KB02-JQ1 is a selective PROTAC BRD4 degrader that functions as a molecular glue, specifically targeting BRD4 while sparing BRD2 and BRD3. This compound induces BRD4 degradation by covalently modifying the E3 ligase DCAF16, thereby enhancing the stability and duration of protein degradation in biological systems. Its unique design, which incorporates JQ1 linked to the ubiquitin E3 ligase ligand KB02, facilitates targeted modulation of gene expression, making it a valuable tool for research in cancer biology and therapeutic development. -
BRD4 Degrader
PROTAC BRD4 Degrader-6 is a potent small-molecule degrader that targets BRD4, exhibiting an IC50 value of 2.7 nM for the BRD4 BD1 domain. This compound effectively degrades BRD4 protein and leads to the downregulation of c-Myc expression. In vitro studies demonstrate its capacity to inhibit proliferation and induce apoptosis in the pancreatic cancer cell line BxPC3, making it a valuable tool for research in human pancreatic cancer biology. -
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. -
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.
