Catalog No.
Product Name
Application
Product Information
Citations
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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. -
CECR2 inhibitor
NVS-CECR2-1 is a potent and selective non-BET family bromodomain (BRD) inhibitor targeting cat eye syndrome chromosome region, candidate 2 (CECR2). It binds CECR2 BRD with high affinity (IC50 = 47 nM; KD = 80 nM). NVS-CECR2-1 exhibits cytotoxic activity and induces apoptosis in various cancer cells through both CECR2-dependent and CECR2-independent mechanisms. -
ENL/AF9 YEATS domain inhibitor
SR-0813 is a potent and selective inhibitor of the ENL and AF9 YEATS domains. It exhibits IC50 and EC50 values of 25 nM and 205 nM, respectively, for the ENL YEATS domain, and 311 nM and 76 nM (CETSA) for the AF9 YEATS domain. SR-0813 binds MAP3K19 with significantly lower affinity (Kd = 3.5 μM) compared to ENL YEATS (Kd = 30 nM), demonstrating over 100-fold selectivity. It is suitable for research into acute leukemia. -
BPTF inhibitor
BPTF-IN-BZ1 is a highly potent BPTF inhibitor with a Kd of 6.3 nM. -
PBRM1 Bromodomain inhibitor
PBRM1-BD2-IN-8 (compound 34) is a potent inhibitor of the PBRM1 bromodomain, with a Kd of 4.4 μM and an IC50 of 0.16 μM for PBRM1-BD2, and a Kd of 25 μM for PBRM1-BD5. It exhibits anti-cancer activity. -
Menin-MLL Interaction Inhibitor
Ziftomenib (KO-539) is an orally active inhibitor of the menin–MLL (KMT2A) interaction, designed to disrupt oncogenic gene expression in MLL-rearranged cancers. It exhibits potent antitumor activity and is under investigation for the treatment of acute leukemias driven by MLL rearrangements or NPM1 mutations. Ziftomenib corresponds to compound 151 in patent WO2017161028A1. -
Menin-MLL Interaction Inhibitor
DSP5336 is an orally active small molecule inhibitor that targets the interaction between menin and MLL (mixed-lineage leukemia) proteins. By disrupting this protein–protein interaction, DSP5336 impairs leukemogenic gene expression programs driven by MLL rearrangements. It is currently undergoing clinical evaluation for the treatment of patients with relapsed or refractory acute leukemia, particularly those harboring MLL rearrangements. -
DK/PI3K/BRD4 Inhibitor
SRX3177 is a potent triple inhibitor targeting CDK4/6, PI3K, and BRD4, with IC50 values of <2.5 nM for CDK4, 3.3 nM for CDK6, 79 nM for PI3Kα, 83 nM for PI3Kδ, 3.18 μM for PI3Kγ, and 33 nM and 89 nM for BRD4 BD1 and BD2, respectively. It exhibits broad cytotoxic activity against cancer cells while sparing normal epithelial cells, highlighting its potential as a targeted cancer therapeutic with reduced toxicity. -
PROTAC BRD4 Degrader
PROTAC BRD4 Degrader-12 (compound 9c) is a bifunctional molecule designed to target and degrade the bromodomain-containing protein BRD4 by recruiting the von Hippel–Lindau (VHL) E3 ubiquitin ligase. It functions as a highly potent degrader, with a DC₅₀ of 0.39 nM and 0.24 nM when conjugated to STEAP1 and CLL1 antibodies, respectively, enabling targeted delivery and degradation of BRD4 in PC3 prostate cancer cells. -
PROTAC BRD4 degrader
dBET23 is a highly potent and selective PROTAC degrader targeting the bromodomain-containing protein BRD4. It exhibits a DC₅₀ of approximately 50 nM at 5 hours for the BRD4 bromodomain 1 (BRD4^BD1) protein, effectively promoting its ubiquitination and proteasomal degradation. dBET23 serves as a valuable chemical tool for studying BRD4-dependent transcriptional regulation and holds potential for therapeutic applications in BRD4-driven cancers. -
PROTAC BET degrader
SJ995973 is a highly potent PROTAC (proteolysis-targeting chimera) designed to selectively degrade bromodomain and extra-terminal domain (BET) family proteins, including BRD2, BRD3, and BRD4. By inducing targeted proteasomal degradation, SJ995973 enables efficient disruption of BET protein function, offering a powerful approach for investigating BET-related transcriptional regulation and for the development of novel anticancer therapies. -
FFAR3 agonist
AR420626 is a selective agonist of free fatty acid receptor 3 (FFAR3, also known as GPR41), with an IC₅₀ of 117 nM. It demonstrates anti-inflammatory, antitumor, and antidiabetic activities. AR420626 improves neurogenic diarrhea by modulating neural pathways mediated by nicotinic acetylcholine receptors (nAChRs). In cancer models, it suppresses the growth of HepG2 xenografts and inhibits hepatoma cell proliferation through apoptosis induction. Additionally, AR420626 mitigates allergic asthma and eczema and enhances glucose uptake by activating FFAR3-mediated Ca²⁺ signaling, offering potential therapeutic benefits in metabolic disorders such as diabetes. -
Protac smarca2 degrader
SMD-3040 formate is a potent and selective PROTAC degrader targeting SMARCA2, a core ATPase subunit of the SWI/SNF chromatin remodeling complex. It exhibits strong in vivo antitumor activity, making it a promising candidate for cancer research involving epigenetic regulation and synthetic lethality strategies. -
PROTAC CBP/p300 Degrader
CBPD-409 is an orally active PROTAC degrader targeting CBP/p300, with a DC₅₀ of 0.2–0.4 nM. It shows potent antiproliferative activity in AR⁺ prostate cancer cell lines (VCaP, LNCaP, 22Rv1) with IC₅₀ values of 1.2–2.0 nM and demonstrates significant antitumor efficacy. -
PROTAC CBP/p300 degrader
JET-209 is a potent PROTAC degrader targeting CBP and p300, with DC₅₀ values of 0.05 nM and 0.2 nM, respectively. It is composed of lenalidomide, a linker, and the bromodomain inhibitor GNE-207. JET-209 is a valuable tool for cancer research involving epigenetic regulation. -
BRD9 Degrader
FHD-609 is a PROTAC degrader and inhibitor of BRD9, a key component of the non-canonical BAF (ncBAF) chromatin remodeling complex. It is designed for studying cancers harboring mutations in BAF complex subunits. FHD-609 shows potential in adrenocortical carcinoma (ACC) treatment, particularly in combination with Telomelysin or INO5401.
