Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
PCAF inhibitor
L-Moses (L-45) dihydrochloride is the first potent, selective, and cell-permeable inhibitor of the p300/CBP-associated factor (PCAF) bromodomain, with a Kd of 126 nM. -
BET inhibitor
JQ1-TCO (JQ1-trans-cyclooctene) is a derivative of JQ1, a BET inhibitor, modified for click chemistry applications. It serves as a molecular probe for in vitro and in vivo studies. - Artepillin C is an orally active compound that functions as a CREB/CRTC2 inhibitor and a covalent TRPA1 agonist (EC50 = 1.8 μM). It suppresses CREB/CRTC2-mediated gene transcription and downregulates BMAL1 expression, thereby modulating glucose and lipid metabolism. Additionally, Artepillin C activates TRPA1 channels, eliciting spicy taste signals. It exhibits antitumor activity by inhibiting cell proliferation and inducing necroptosis, improves insulin resistance, and reduces hepatic lipid synthesis. Artepillin C is applicable for research into metabolic syndrome, tumor prevention and treatment, and inflammation.
- Ganodermanontriol, a sterol isolated from *Ganoderma lucidum*, exerts anti-inflammatory effects in tert-butyl hydroperoxide (t-BHP)-damaged hepatic cells by upregulating heme oxygenase-1 (HO-1) expression. It demonstrates hepatoprotective activity.
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L-Moses Control
D-Moses (D-45), the enantiomer of L-Moses (L-45), is an inactive control compound for L-Moses, a potent and selective inhibitor of the p300/CBP-associated factor (PCAF) bromodomain (Brd). Unlike L-Moses, D-Moses exhibits no observable binding to PCAF Brd, making it suitable for use as a negative control in studies involving L-Moses. -
SPIN1 inhibitor
MS31 is a potent, highly selective fragment-like inhibitor of the methyllysine reader protein spindlin 1 (SPIN1). It strongly inhibits SPIN1 interactions with H3K4me3, with IC50 values of 77 nM (AlphaLISA) and 243 nM (FP). MS31 selectively binds to Tudor domain II of SPIN1 with a Kd of 91 nM and potently blocks binding of trimethyllysine-containing peptides to SPIN1. It exhibits no toxicity toward nontumorigenic cells. -
SP140 Inhibitor
GSK761 is a selective inhibitor of speckled 140 kDa (SP140) protein, with an IC50 of 77.79 nM. It suppresses monocyte-to-inflammatory macrophage differentiation and lipopolysaccharide (LPS)-induced inflammatory activation. Additionally, GSK761 promotes the production of CD206+ regulatory macrophages by inhibiting SP140. -
ATAD2 bromodomain inhibitor
AZ13824374 is a highly potent and selective ATAD2 bromodomain inhibitor, demonstrating cellular target engagement and antiproliferative activity in various breast cancer models. It inhibits ATAD2 with pIC50 values of 8.2 in the ATAD2 FRET assay and 6.2 in the ATAD2 NanoBRET assay. -
BET inhibitor
Amredobresib (BI894999) is an orally active BET inhibitor that potently blocks the binding of BRD4-BD1 and BRD4-BD2 bromodomains to acetylated histones, with IC50 values of 5 nM and 41 nM, respectively. It demonstrates anticancer activity against acute myeloid leukemia (AML) and NUT carcinoma. -
BET/BRD4 bromodomain inhibitor
AZD5153 is a bivalent, selective, and orally active BET/BRD4 bromodomain inhibitor with an IC50 of 5 nM for full-length BRD4 (FL-BRD4). It simultaneously binds both bromodomains of BRD4, enhancing its inhibitory potency. AZD5153 is applicable for research into cancers, including acute myeloid leukemia, multiple myeloma, and diffuse large B-cell lymphoma. -
BET family bromodomain inhibitor
NHWD-870 is a potent, orally active, and selective BET family bromodomain inhibitor, specifically targeting BRD2, BRD3, BRD4 (IC50 = 2.7 nM), and BRDT. It exhibits strong tumor-suppressive effects, enhances tumor apoptosis, inhibits tumor proliferation, and disrupts cancer cell-macrophage interactions. -
Menin-MLL inhibitor
BMF-219 (Menin-MLL inhibitor 21) is a specific, irreversible inhibitor of the Menin-MLL interaction, suitable for research into autoimmune diseases, heteroimmune diseases, cancer, and other menin-MLL-dependent conditions.
