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Catalog No.
Product Name
Application
Product Information
Citations
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p300/CBP histone acetyltransferase inhibitor
P300/CBP-IN-3, a p300/CBP histone acetyltransferase inhibitor. -
BRD4-BD1 inhibitor
BRD4 Inhibitor-10 is a potent BRD4-BD1 inhibitor extracted from patent WO2015022332A1, Compound II-25, has an IC50 of 8 nM. -
Bromodomain inhibitor
Bromodomain IN-1 is a Bromodomain inhibitor extracted from patent WO2016069578A1, compound 4 . -
BRM/BRG1 ATP Inhibitor
BRM/BRG1 ATP Inhibitor-1 is an allosteric dual brahma homolog (BRM)/SWI/SNF related matrix associated actin dependent regulator of chromatin subfamily A member 2 (SMARCA2) and brahma related gene 1 (BRG1)/SMARCA4 ATPase activity inhibitor, both IC50s are below 0.005 ?M. -
BET bromodomain inhibitor
Bromodomain inhibitor-8 (Intermediate 21) is a BET bromodomain inhibitor for treating autoimmune and inflammatory diseases. -
BET bromodomain inhibitor
(+)-JQ1 PA is a clickable JQ1 for building PROTACs, which acts as a BET bromodomain inhibitor. -
Bromodomain inhibitor
BMS-986158 is an inhibitor of the bromodomain and extra-terminal (BET) proteins. -
MBT Domain (L3MBTL1) Inhibitor
UNC 926 is a methyl lysine reader domain inhibitor. -
BET inhibitor
OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM). -
BET bromodomain inhibitor
RVX-208 is a potent BET bromodomain inhibitor with IC50 of 0.510 uM for BD2, about 170-fold selectivity over BD1. - GSK 525768A is the enantiomer compound of GSK 525762A, which is a potent small molecule inhibitor that disrupt the function of the BET family of bromodomains (Brd2, Brd3, and Brd4); GSK 525768A has NO activity towards BET.
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BET bromodomain inhibitor
The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. -
KAT5 (Tip60), p300/PCAF inhibitor
Anacardic Acid is a potent inhibitor of p300 and p300/CBP-associated factor histone acetyltranferases. -
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. -
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.
