Catalog No.
Product Name
Application
Product Information
Citations
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BRD4 Inhibitor
ARV-825 is a hetero-bifunctional molecule that is composed of a BRD4 binding moiety joined to an E3 ligase cereblon binding moiety using proteolysis targeting chimera (PROTAC) technology.- Aidan L Forberg, .et al. , Ann Hematol, 2024, Jan;103(1):199-209 PMID: 37792064
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BET bromodomain Inhibitor
CPI203 is a novel potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM (BRD4 α-screen assay).- Derenzini E, .et al. , Cell Rep, 2018, Aug 21;24(8):2155-2166 PMID: 30134175
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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.- Junichi Yamamoto, .et al. , Sci Rep, 2026, Feb 5;16:7375 PMID: 41639146
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CBP/p300 bromodomain inhibitor
SGC-CBP30 is a potent and selective inhibitor of CREBBP (CBP) and EP300; which are general transcriptional co-activators.- Kevin Bohm, .et al. , Arch Pharm (Weinheim), 2023, Jul;356(7):e2200661 PMID: 37196427
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BET inhibitor
PFI-1 is a BET bromodomain inhibitor that exhibits inhibitory activity at BRD2 and BRD4.- Lisa-Maria Winter, .et al. , Sci Rep, 2023, Jul 26;13(1):12061 PMID: 37495707
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BET Bromodomain Inhibitor
GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4.- Momeny M, .et al. , Anticancer Drugs, 2018, Nov;29(10):1011-1020 PMID: 30096128
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CBP/beta-catenin antagonist
PRI-724 is the second-generation, potent and specific inhibitor of CBP/β-Catenin complex, and a modulator of the β-Catenin dependent canonical Wnt signaling pathway in cancer stem cells.
- Paul Mark Medina, .et al. , Transl Oncol, 2021, Jan;14(1):100940 PMID: 33221682
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BRD4 inhibitor
JQ-1 carboxylic acid is a highly potent, selective and cell-permeable BRD4 inhibitor with IC50s of 77 nM and 33 nM for BRD4(1) and BRD4(2), respectively.- Rahel Fitzel, .et al. , Neoplasia, 2023, Jul;41:100902 PMID: 37148657
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p300/CBP inhibitor
C646 is a selective p300/CREB-binding protein (CBP) inhibitor (Ki = 400 nM).- Thibaud Reyser, .et al. , Pharmaceutics, 2023, Oct 10;15(10):2440 PMID: 37896200
- Zhifeng Zhang, .et al. , PLoS One, 2017, 12(10): e0186900 PMID: 29049411
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BET Inhibitor
(+)-JQ1 is a potent, high affinity, selective BET bromodomain inhibitor.- Yoshimi Yasukawa, .et al. , Cancer Science, 2026, 117(7): 1894-1906 PMID: 42070972
- Stephanie Tanis, .et al. , Proc Natl Acad Sci U S A, 2026, Apr 14;123(15):e2517498123 PMID: 41945432
- Yuichiro Hara, .et al. , bioRxiv, 2025, Dec 05
- Jiang Zhou, .et al. , Neoplasia, 2025, Oct:68:101223 PMID: 40850308
- Kei Taga, .et al. , Microbiol Immunol, 2024, Mar;68(3):90-99 PMID: 38244193
- Deeksha Sharma, .et al. , Breast Cancer Res, 2023, Nov 15;25(1):144 PMID: 37968653
- Adriana K Alexander, .et al. , Nat Commun, 2023, Mar 29;14(1):1753 PMID: 36990976
- Haruki Kitamura, .et al. , Biochem Biophys Res Commun, 2023, Jan 22;641:139-147 PMID: 36527748
- Gerald Thiel, .et al. , Pharmaceuticals (Basel), 2022, Jul 10;15(7):846 PMID: 35890145
- Selase D Deletsu, .et al. , Biochem Biophys Res Commun, 2021, Aug 27;567:106-111 PMID: 34146904
- Cole Schonhofer, .et al. , Biochem Pharmacol, 2021, Apr;186:114462 PMID: 33577894
- Nandini Verma, .et al. , Sci Adv, 2020, 6 : eaba8968 PMID: 32937365
- Kuo MT, .et al. , Transl Oncol, 2020, 13(2):355-364 PMID: 31887630
- Rao Z, .et al. , J Immunol, 2019, Aug 15;203(4):1031-1043 PMID: 31300512
- A Carrer, .et al. , Cancer Discov, 2019, Jan 9. pii: CD-18-0567 PMID: 30626590
- Clocchiatti A, .et al. , J Clin Invest, 2018, Dec 3;128(12):5531-5548 PMID: 30395538
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BET inhibitor
GSK1324726A (I-BET726) is a novel, potent, and selective small molecule inhibitor of BET proteins with high affinity to BRD2 (IC50= 41 nM), BRD3 (IC50= 31 nM), and BRD4 (IC50= 22 nM).- Zhengjun Liu, .et al. , Cell Death Dis, 2020, May 5;11(5):318 PMID: 32371868
- BRD7-IN-1 free base, a modified derivative of BI7273 (BRD7/9 inhibitor), binds to a VHL ligand via a linker to form a PROTAC VZ185 (VZ185 against BRD7/9 with DC50s of 4.5 and 1.8 nM, respectively).
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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. -
BRD inhibitor
L-45 is the first potent, selective, and cell-active p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor with a Kd of 126±15 nM. - SMARCA-BD ligand 1 for Protac is a compound that binds to the BAF ATPase subunits SMARCA2, and used for degrading SMARCA2, based on PROTAC.
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BET bromodomain inhibitor
PROTAC BET-binding moiety 2 is an inhibitor of BET bromodomain. -
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. - Tz-Thalidomide is a tetrazine-tagged thalidomide derivative that functions as a ligand for E3 ligases. It exhibits binding affinity for BRD4, with IC₅₀ values of 46.25 μM for BRD4-1 and 62.55 μM for BRD4-2. As a click chemistry reagent, Tz-Thalidomide contains a tetrazine moiety capable of undergoing inverse electron demand Diels–Alder (iEDDA) reactions with trans-cyclooctene (TCO)-containing molecules, enabling bioorthogonal labeling and conjugation applications.
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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. - NICE-01 (AP1867-PEG2-JQ1; AP-PEG2-JQ1) is a bifunctional compound designed to induce nuclear import of cytosolic proteins. It functions by binding proteins in distinct cellular compartments and leveraging nuclear-localized BRD4 as a “carrier” to facilitate co-import and nuclear retention of cytosolic cargoes.
