Catalog No.
Product Name
Application
Product Information
Citations
- 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.
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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. -
BRD4 degrader
PLX-3618 is a molecular glue that induces BRD4 degradation with a DC₅₀ of 12.2 nM. It promotes polyubiquitination and subsequent proteasomal degradation of BRD4 by recruiting the E3 ligase substrate receptor DCAF11. PLX-3618 inhibits the proliferation of various cancer cell lines, induces apoptosis in AML cells, and exhibits antitumor activity in AML mouse models. -
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. - 653-47 hydrochloride is a potentiator that significantly enhances the CREB (cAMP-response element-binding protein) inhibitory activity of 666-15. It also functions as a very weak CREB inhibitor on its own, with an IC₅₀ of 26.3 μM.
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ENL PROTAC Degrader
MS41 is a selective PROTAC degrader of eleven-nineteen leukemia (ENL), with DC₅₀ values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). MS41 effectively inhibits the proliferation of ENL-dependent leukemia cells, induces G1 phase cell cycle arrest, and promotes apoptosis. It reduces chromatin occupancy of the ENL-associated transcription elongation complex, thereby suppressing oncogenic gene expression and leukemia progression. -
CECR2/BPTF probe
TP-238 hydrochloride is a potent and selective dual probe for CECR2 and BPTF, with IC₅₀ values of 30 nM and 350 nM, respectively. It also inhibits BRD9 with a pIC₅₀ of 5.9 and shows minimal activity against a panel of 338 other kinases.
