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Catalog No.
Product Name
Application
Product Information
Citations
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PLK1/BRD4 Inhibitor
PLK1/BRD4-IN-5 is a potent inhibitor targeting both PLK1 and BRD4, exhibiting IC50 values of 0.3 nM and 60.8 nM, respectively. This compound effectively induces cell cycle arrest in the S phase and promotes apoptosis in MV4-11 cells in a dose-dependent manner. PLK1/BRD4-IN-5 is a valuable tool for cancer research, facilitating studies on mechanisms of tumorigenesis and therapeutic responses. -
p300/CBP Inhibitor
DCH36_06 is a selective inhibitor of the p300/CBP acetyltransferases, exhibiting IC50 values of 0.6 μM for p300 and 3.2 μM for CBP. This compound induces hypoacetylation of histone H3 at lysine 18 (H3K18) in leukemic cells, contributing to its anti-tumor properties. DCH36_06 is useful for investigating the role of p300/CBP in transcriptional regulation and potential therapeutic applications in cancer research. -
BRD4 Inhibitor
BRD4-IN-41 is a selective BRD4 inhibitor that targets the acetyl-lysine binding site with an IC50 of 34 nM. In addition to inhibiting BRD4, it also affects multiple kinases, including JAK2, FLT3, and NTRK3, with IC50 values ranging from 0.9 nM to 43 nM. This compound downregulates c-MYC, lowers phosphorylated STAT3 levels, and induces G1 cell cycle arrest and apoptosis, demonstrating significant anti-cancer activity. BRD4-IN-41 is particularly relevant for research on hematological malignancies such as multiple myeloma and acute myeloid leukemia. -
HDAC/JAK/BRD4 Inhibitor
HDAC/JAK/BRD4-IN-1 is a potent inhibitor targeting histone deacetylases (HDAC), Janus kinases (JAK), and bromodomain-containing protein 4 (BRD4). This compound demonstrates significant anti-proliferative effects and promotes apoptosis in MDA-MB-231 breast cancer cells. Additionally, HDAC/JAK/BRD4-IN-1 exhibits promising anticancer activity in vivo, making it a valuable tool for research in cancer therapeutics and the study of epigenetic and signaling pathways. -
CBP Inhibitor
DC-CPin711 is a potent and selective inhibitor of the CREB-binding protein (CBP) bromodomain, demonstrating an IC50 of 0.0626 μM. This compound effectively induces apoptosis and arrests the cell cycle at the G1 phase, making it a valuable tool for research into cellular proliferation and death pathways. Its specificity for CBP enhances its utility in investigating the role of bromodomain-containing proteins in various biological processes and diseases. -
BRD4 Inhibitor
BRD4 Inhibitor-18 is a potent inhibitor of the Bromodomain-containing protein 4 (BRD4), exhibiting an IC50 value of 110 nM. This compound features a hydrophobic acetylcyclopentanyl side chain and significantly reduces the proliferation of MV-4-11 leukemia cells, which are characterized by high BRD4 expression. In addition, BRD4 Inhibitor-18 promotes apoptosis and induces G0/G1 cell cycle arrest, making it a valuable tool for research into cancer therapeutics and cell cycle regulation. -
CDK6/BRD4 Inhibitor
BC13 is a selective inhibitor of CDK6 and BRD4, demonstrating IC50 values of 234 nM and 36 nM, respectively. This compound exhibits notable antiproliferative effects, facilitating cell apoptosis and inducing DNA damage in various cell lines. Additionally, BC13 has been shown to elevate reactive oxygen species (ROS) levels, making it a valuable tool for research in cancer biology and therapeutic development targeting cell cycle regulation. -
BRD2/BRD4 Inhibitor
KB-0118 is a selective inhibitor of the bromodomains BRD2 and BRD4, exhibiting Kd values of 36.7 μM and 47.4 μM, respectively. This orally active compound effectively inhibits the production of pro-inflammatory cytokines, such as TNF, IL-1β, and IL-23a, and selectively reduces Th17 cell differentiation. The compound modulates Th17-driven inflammatory processes through the epigenetic suppression of BRD4, leading to decreased expression of STAT3 and other target genes. KB-0118 demonstrates potential therapeutic benefits in models of inflammatory bowel disease (IBD). -
BD2-selective BET Inhibitor
BET-IN-23 is a BD2-selective BET inhibitor with a reported IC50 of 2.9 nM. This compound exhibits anticancer properties, effectively inhibiting the proliferation of acute myeloid leukemia (AML) cell lines by inducing G0/G1 cell cycle arrest and apoptosis in vitro. BET-IN-23 serves as a valuable tool for research in cancer biology, specifically in the study of leukemia and other malignancies involving BET protein dysregulation. -
CBP Bromodomain Inhibitor
Ischemin is a selective inhibitor of the CBP bromodomain, effectively disrupting the interaction between p53 and CBP, consequently reducing transcriptional activity. With an IC50 value of 5 µM, Ischemin demonstrates the ability to inhibit p53-induced p21 activation. Additionally, it has been shown to protect against apoptosis in ischemic cardiomyocytes. This reagent is valuable for investigating mechanisms involved in cardiovascular diseases, particularly myocardial ischemia. -
PARP1/BRD4 Inhibitor
PARP1/BRD4-IN-1 is a selective inhibitor targeting both PARP1 and BRD4, demonstrating IC50 values of 49 nM and 202 nM, respectively. This compound effectively represses the expression and activity of these proteins, leading to synergistic inhibition of malignant pancreatic cancer cell growth. PARP1/BRD4-IN-1 is a valuable tool for exploring therapeutic strategies in cancer research, particularly in the context of PARP and BRD4 signaling pathways. -
BRD4 Inhibitor
BET-IN-20 is a selective BRD4 bromodomain inhibitor with an IC50 of 1.9 nM. This compound demonstrates significant anticancer activity by inducing apoptosis in acute myeloid leukemia (AML) cells and effectively arresting the cell cycle in the G0/G1 phase. Additionally, BET-IN-20 inhibits c-Myc and CDK6, while enhancing PARP cleavage, making it a valuable tool for cancer research and therapeutic development. -
PARP1/BRD4 Inhibitor
PARP1/BRD4-IN-2 is a selective inhibitor of PARP1 and BRD4, demonstrating IC50 values of 197 nM and 238 nM, respectively. This compound effectively impedes DNA damage repair mechanisms, inhibits the G0/G1 cell cycle transition, and induces apoptotic cell death. PARP1/BRD4-IN-2 has shown significant anti-tumor efficacy in the MDA-MB-468 xenograft mouse model, making it a valuable tool for research in triple-negative breast cancer (TNBC). -
Dual PLK1/BET Inhibitor
WNY0824 is a dual inhibitor targeting Polo-like kinase 1 (PLK1) and the Bromodomain and Extra-Terminal (BET) protein family. It demonstrates potent inhibitory activity, with IC50 values of 22 nmol/L for PLK1 and varying efficacy against BRD2, BRD3, BRD4, and BRDT. WNY0824 induces cell cycle arrest and apoptosis by disrupting AR- and MYC-mediated transcriptional processes, making it valuable for research in cancer biology. Furthermore, it has shown effectiveness in inhibiting tumor growth in Enzalutamide-resistant castration-resistant prostate cancer (CRPC) xenograft models, highlighting its potential in overcoming treatment resistance. -
BET binding to histones inhibitor
(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome. -
BET inhibitor
(Rac)-BAY1238097 is a BET inhibitor, with an IC50 of 1.02 μM for BRD4. Used in cancer research. -
BET inhibitor
CPI-0610 carboxylic acid is a potent bromodomain and extra-terminal (BET) protein inhibitor. CPI-0610 carboxylic acid has the potential in the therapy of multiple myeloma. -
BET/BRD4 bromodomain inhibitor
AZD5153 6-Hydroxy-2-naphthoic acid is the 6-Hydroxy-2-naphthoic acid of AZD5153. AZD5153 is a potent, selective, and orally available BET/BRD4 bromodomain inhibitor; disrupts BRD4 with an IC50 of 1.7 nM. -
BET bromodomain inhibitor
Molibresib besylate (GSK 525762C; I-BET 762 besylate) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM. -
SMARCA4/SMARCA2 ATPase inhibitor
FHD-286 is a selective, orally active inhibitor of the SMARCA4/SMARCA2 (BRG1/BRM) ATPase. It holds potential for research into BAF (BRG1/BRM-associated factor)-related disorders, including acute myeloid leukemia. -
p300/CBP inhibitor
NEO2734 (EP31670) is an orally active dual inhibitor of p300/CBP and BET bromodomains, with IC₅₀ values of <30 nM for both targets. It is effective in both SPOP-mutant and wild-type prostate cancer models. -
SMARCA4/SMARCA2 ATPase Inhibitor
FHT-1015 is a selective allosteric inhibitor of SMARCA4 (BRG1) and SMARCA2 (BRM), with IC₅₀ values of 4 nM and 5 nM, respectively. It binds to an allosteric site, inducing conformational changes that inhibit the ATPase activity of BRG1/BRM. FHT-1015 disrupts tumor cell growth and migration and is applicable in research on uveal melanoma and hematologic malignancies. -
ATAD2 bromodomain inhibitor
GSK8814 is a potent and selective chemical probe and inhibitor of the ATAD2 bromodomain, with an IC₅₀ of 0.059 μM, a pK\_d of 8.1, and a pK\_i of 8.9 in BROMOscan. It binds to ATAD2 and BRD4 BD1 with pIC₅₀ values of 7.3 and 4.6, respectively, demonstrating over 500-fold selectivity for ATAD2. GSK8814 is suitable for research in cancers associated with ATAD2 bromodomain activity. -
Menin inhibitor
BN-104 (BNM-1192) is an orally active and selective brain-penetrant menin inhibitor that disrupts the menin-MLL interaction, leading to degradation of the menin protein. It exhibits antitumor activity and is applicable in cancer research, including studies on acute myeloid leukemia. BN-104 is a weak hERG inhibitor, with an IC₅₀ greater than 100 μM. -
Menin inhibitor
Enzomenib is an inhibitor of menin, a protein encoded by the multiple endocrine neoplasia (MEN) gene. It disrupts the interaction between menin and mixed lineage leukemia (MLL) fusion proteins and is applicable in the study of hematological malignancies. -
BET/EP300 inhibitor
XP-524 is a potent dual inhibitor of BET and EP300, exhibiting strong antitumor activity in vivo. It prevents KRAS-induced neoplastic transformation and prolongs survival in two transgenic mouse models of aggressive pancreatic ductal adenocarcinoma (PDAC). XP-524 also enhances self-peptide presentation and promotes tumor infiltration by cytotoxic T lymphocytes, supporting its potential for PDAC research. -
CBP/p300 inhibitor
CBP/p300-IN-8 is a potent inhibitor of the CBP/p300 family of bromodomains, with an IC₅₀ of 0.01–0.1 µM for CBP. It also inhibits BRD4 activity with significantly lower potency (IC₅₀ = 1–1000 µM). -
p300/CBP inhibitor
CBP/p300-IN-12 is a potent and selective covalent inhibitor of the histone acetyltransferases p300 and CBP, with an IC₅₀ of 166 nM for p300. It reduces H3K27Ac levels in PC-3 cells with an EC₅₀ of 37 nM and forms a covalent adduct with cysteine residue C1450. -
BRD4/NAMPT inhibitor
BRD4/NAMPT-IN-1 (Compound A2) is a dual inhibitor of NAMPT and BRD4, with IC₅₀ values of 35 nM and 58 nM, respectively. It suppresses the growth and migration of hepatocellular carcinoma cells and induces apoptosis. In the HCCLM3 xenograft mouse model, BRD4/NAMPT-IN-1 exhibits potent anticancer activity without apparent toxicity. -
BET BD1 inhibitor
LT052 is a highly selective BET BD1 inhibitor with an IC₅₀ of 87.7 nM. It demonstrates nanomolar potency against BRD4 BD1 and exhibits 138-fold selectivity over BRD4 BD2 (IC₅₀ = 12.130 μM). LT052 possesses anti-inflammatory activity and is applicable in acute gout arthritis research. -
BRD4 inhibitor
BRD4 Inhibitor-30 (Compound 1) is a BRD4 inhibitor with an IC₅₀ value of 415 nM. -
menin-MLL interaction inhibitor
Menin-MLL Inhibitor 20 is an irreversible inhibitor of the menin-MLL interaction with demonstrated antitumor activity. It is referenced as Intermediate 6 in patent WO2020142557A1. -
BRD4/CK2 inhibitor
BRD4/CK2-IN-1 is the first highly potent and orally active dual inhibitor of BRD4 and casein kinase 2 (CK2), with IC₅₀ values of 180 nM and 230 nM, respectively. It exhibits strong anticancer activity with minimal toxicity, and induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC) cells. -
KIX-KID interaction inhibitor
Naphthol AS-E is a potent, cell-permeable inhibitor of the KIX-KID interaction. It binds directly to the KIX domain of CBP with a Kd of 8.6 μM and inhibits the interaction between the KIX domain and the KID domain of CREB with an IC₅₀ of 2.26 μM. Naphthol AS-E is applicable in cancer research.
