Catalog No.
Product Name
Application
Product Information
Citations
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HDAC1/HDAC2 inhibitor
BRD2492 (compound 6d) is a potent and selective inhibitor of histone deacetylases HDAC1 and HDAC2, with IC₅₀ values of 13.2 nM and 77.2 nM, respectively. It exhibits over 100-fold selectivity for HDAC1/2 compared to HDAC3 and HDAC6. BRD2492 effectively inhibits the proliferation of breast cancer cell lines, with IC₅₀ values of 1.01 μM for T-47D cells and 11.13 μM for MCF-7 cells, highlighting its potential as a targeted epigenetic therapeutic in breast cancer research. -
HDAC8 inhibitor
1-Naphthohydroxamic acid (Compound 2) is a potent and selective inhibitor of histone deacetylase 8 (HDAC8), with an IC₅₀ of 14 μM. It demonstrates high selectivity for HDAC8 over other HDAC isoforms, showing minimal activity against class I HDAC1 and class II HDAC6 (IC₅₀ > 100 μM). Unlike broad-spectrum HDAC inhibitors, 1-Naphthohydroxamic acid does not increase global histone H4 acetylation or reduce total intracellular HDAC activity, but it effectively induces tubulin acetylation. This selective profile makes it a valuable tool for studying HDAC8-specific functions. -
HDAC inhibitor
YSR734 (Compound 21) is a covalent histone deacetylase (HDAC) inhibitor with IC₅₀ values of 110 nM, 154 nM, and 143 nM for HDAC1, HDAC2, and HDAC3, respectively. It induces apoptosis in leukemia cells and promotes myoblast differentiation, making it a valuable compound for both cancer research and studies related to muscle regeneration. YSR734 is particularly relevant in the investigation of therapeutic strategies for Duchenne muscular dystrophy. -
HDAC6 inhibitor
PB131 is a highly selective and brain-permeable histone deacetylase 6 (HDAC6) inhibitor, exhibiting strong binding affinity with an IC₅₀ of 1.8 nM. It possesses potent anti-inflammatory activity and is particularly suited for research in inflammation-related disorders, including neuroinflammation, due to its effective central nervous system penetration and HDAC6 specificity. -
HDAC2/HDAC3 inhibitor
MI-192 is a selective inhibitor of histone deacetylases HDAC2 and HDAC3, with IC₅₀ values of 30 nM and 16 nM, respectively. It demonstrates high selectivity for HDAC2/3 over other HDAC isoforms. MI-192 induces apoptosis in myeloid leukemia cells and exhibits both anticancer and neuroprotective activities, making it a valuable compound for research in oncology and neurodegenerative diseases. -
HDAC inhibitor
Pivanex (AN-9) is an orally active histone deacetylase (HDAC) inhibitor derived from butyric acid. It downregulates BCR-ABL protein expression and promotes apoptosis, contributing to its antitumor effects. In addition, Pivanex exhibits antimetastatic and antiangiogenic properties, making it a promising candidate for research in hematologic malignancies and solid tumors. -
HDAC inhibitor
BRD4884 is a potent histone deacetylase (HDAC) inhibitor that selectively targets class I HDACs. It exhibits IC₅₀ values of 29 nM for HDAC1, 62 nM for HDAC2, and 1.09 µM for HDAC3. Its differential potency across HDAC isoforms makes BRD4884 a valuable tool for investigating HDAC1/2-mediated epigenetic regulation and their roles in disease pathogenesis. -
HDAC inhibitor
FNDR-20123 is a first-in-class, orally active histone deacetylase (HDAC) inhibitor developed for antimalarial therapy. It demonstrates potent inhibitory activity against both Plasmodium and human HDACs, with IC₅₀ values of 31 nM and 3 nM, respectively. FNDR-20123 effectively targets multiple stages of *Plasmodium falciparum*, with IC₅₀ values of 41 nM for the asexual blood stage and 190 nM for male gametocytes. It inhibits HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8 with IC₅₀ values of 25, 29, 2, 11, and 282 nM, respectively, and also exhibits nanomolar-level inhibition of Class III HDAC isoforms. FNDR-20123 shows a favorable safety profile, supporting its potential as a novel antimalarial agent targeting epigenetic regulation. -
HDAC inhibitor
Pomiferin (NSC 5113) is a natural compound that functions as a dual inhibitor of histone deacetylases (HDACs) and the mammalian target of rapamycin (mTOR). It exhibits an IC₅₀ of 1.05 μM for HDAC inhibition and an IC₅₀ of 6.2 μM for mTOR. With its dual-targeting activity, Pomiferin holds potential for anticancer research, particularly in pathways involving epigenetic regulation and cell growth signaling. -
HDAC inhibitor
m-Carboxycinnamic acid bishydroxamide is a potent histone deacetylase (HDAC) inhibitor, demonstrating in vitro ID₅₀ values of 10 nM for HDAC1 and 70 nM for HDAC3. It effectively induces apoptosis and suppresses tumor growth, making it a promising candidate for epigenetic cancer therapy and research focused on HDAC1/3-regulated pathways. -
HDAC6 inhibitor
HPB is a selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 31 nM. It demonstrates over 30-fold selectivity for HDAC6 compared to HDAC1, making it a valuable tool for studying HDAC6-specific biological functions and a promising candidate for the development of targeted therapies in diseases involving HDAC6 dysregulation.
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HDAC6 inhibitor
SelSA is a selective and orally active histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 56.9 nM. It also inhibits ERK1/2 phosphorylation, contributing to its anticancer effects. SelSA suppresses the proliferation of breast cancer and hepatocellular carcinoma cells with IC₅₀ values ranging from 0.58 to 2.6 μM, inhibits migration and invasion of Huh7 cells, and induces apoptosis. In vivo, SelSA demonstrates significant antitumor activity, supporting its potential as a therapeutic agent for solid tumors. -
HDAC inhibitor
KH16 is a potent histone deacetylase (HDAC) inhibitor with low nanomolar activity, selectively targeting class I HDACs—HDAC1, HDAC2, and HDAC3—with IC₅₀ values ranging from 6 to 34 nM. It effectively induces apoptosis and exhibits broad-spectrum antitumor activity across cancer cells with diverse gene expression profiles, making it a promising candidate for epigenetic cancer therapy research. -
NF-κB p65 Inhibitor
Licochalcone D is a naturally occurring flavonoid primarily found in the root of *Glycyrrhiza uralensis* (Chinese licorice). It functions as a potent and orally active inhibitor of the NF-κB p65 subunit, a key regulator of inflammation and cancer-related signaling pathways. Licochalcone D exhibits broad pharmacological properties, including antioxidant, anti-inflammatory, and anticancer activities, making it a promising candidate for research in inflammation-related diseases and oncology. -
HDAC11 inhibitor
PB94 is a selective inhibitor of histone deacetylase 11 (HDAC11), with an IC₅₀ of 108 nM. It can be radiolabeled as [¹¹C]-PB94 for positron emission tomography (PET) imaging, enabling in vivo assessment of brain uptake and metabolic properties. PB94 has demonstrated efficacy in alleviating neuropathic pain in mouse models and holds potential as a research tool for investigating HDAC11-related mechanisms in neurological disorders. -
HDAC6 inhibitor
AES-350 is a potent and orally bioavailable histone deacetylase 6 (HDAC6) inhibitor, with an IC₅₀ of 0.0244 μM and a Kᵢ of 0.035 μM. It also exhibits inhibitory activity against HDAC3 and HDAC8, with IC₅₀ values of 0.187 μM and 0.245 μM, respectively. AES-350 induces apoptosis in acute myeloid leukemia (AML) cells through HDAC inhibition, making it a promising compound for AML research and the development of epigenetic-based cancer therapies. -
HDAC6 inhibitor
ITF 3756 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6). In vitro, it effectively reduces the expression of PD-L1 on human monocytes and CD8⁺ T cells, suggesting immunomodulatory potential. ITF 3756 also exhibits antitumor activity, making it a promising candidate for cancer immunotherapy and epigenetic modulation research. -
HDAC inhibitor
HL23 is a histone deacetylase (HDAC) inhibitor with demonstrated efficacy against hepatocellular carcinoma (HCC). It enhances acetylation at the TXNIP promoter, leading to upregulation of TXNIP expression and modulation of potassium channel activity, ultimately inducing TXNIP-dependent potassium deprivation. HL23 effectively suppresses HCC progression and metastasis, and exhibits a synergistic antitumor effect when combined with Sorafenib, outperforming the combination of Sorafenib and Vorinostat in preclinical models. -
POLA1-HDAC11 Inhibitor
GEM144 is a potent and orally bioavailable dual inhibitor of DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It promotes p53 acetylation, induces p21 activation, and triggers G1/S cell cycle arrest followed by apoptosis. GEM144 exhibits significant antitumor efficacy in human orthotopic malignant pleural mesothelioma xenograft models, highlighting its potential as a targeted therapeutic agent for aggressive thoracic malignancies. -
HDAC inhibitor
F-SAHA is a histone deacetylase inhibitor (HDACi) structurally derived from suberoylanilide hydroxamic acid (SAHA). Its fluorine-18 (^18F) labeled derivative enables non-invasive imaging of HDAC expression and activity, making F-SAHA a valuable tool for tumor imaging research and the assessment of epigenetic modulation in vivo. -
POLA1/HDAC 11 Inhibitor
MIR002 is a potent, orally bioavailable dual inhibitor targeting DNA polymerase α (POLA1) and histone deacetylase 11 (HDAC11). It induces p53 acetylation, upregulates p21 expression, and triggers G1/S cell cycle arrest followed by apoptosis. MIR002 demonstrates significant antitumor efficacy in vivo, highlighting its potential as a therapeutic agent for cancers driven by POLA1 and HDAC11 dysregulation. -
HDAC1 and HDAC2 inhibitor
KPZ560 is a potent inhibitor of histone deacetylases HDAC1 and HDAC2, with IC₅₀ values of 12 nM and 68 nM, respectively. It has been shown to enhance dendritic spine density in granule neurons of mice, indicating potential neurotrophic effects. Additionally, KPZ560 inhibits the proliferation of MCF breast cancer cells, supporting its potential application in both neurobiological and oncological research. -
HDAC6 inhibitor
MPI_5a is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), with an IC₅₀ of 36 nM. It exhibits minimal activity against other HDAC isoforms, demonstrating high isoform selectivity. In cellular assays, MPI_5a effectively inhibits acylated tubulin accumulation with an IC₅₀ of 210 nM, highlighting its utility in modulating HDAC6-dependent processes for potential therapeutic applications. -
HDAC6 inhibitor
QTX125 is a potent and highly selective inhibitor of histone deacetylase 6 (HDAC6), demonstrating excellent specificity over other HDAC isoforms. It exhibits significant antitumor activity through selective inhibition of HDAC6-mediated pathways. Both the salt and free base forms of QTX125 display comparable biological activity at equivalent molar concentrations, ensuring consistent pharmacological effects across different formulations. -
VDR agonist
Triciferol is a multifunctional small molecule that acts as both a vitamin D receptor (VDR) agonist and a histone deacetylase (HDAC) antagonist. It binds directly to VDR with an IC₅₀ of 87 nM and exhibits 1,25-dihydroxyvitamin D₃ (1,25D)-like potency in activating multiple VDR target genes. In addition to its transcriptional effects, Triciferol induces significant tubulin hyperacetylation and enhances histone acetylation, contributing to its antiproliferative and cytotoxic activities. This dual mechanism highlights its potential as a therapeutic agent in cancer and epigenetic modulation. -
HDAC3/8 PROTAC degrader
YX968 is a potent and selective PROTAC degrader targeting histone deacetylases HDAC3 and HDAC8, with DC₅₀ values of 1.7 nM and 6.8 nM, respectively. By inducing degradation of these epigenetic regulators, YX968 promotes apoptosis and exhibits significant antitumor activity, representing a promising therapeutic strategy for cancers driven by aberrant HDAC3/8 activity. -
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. -
HDAC Degrader
JPS016 is a benzamide-based PROTAC that recruits the Von Hippel-Lindau (VHL) E3 ligase to selectively degrade class I histone deacetylases (HDACs). It is a potent degrader of HDAC1/2, leading to broad transcriptional changes and enhanced apoptosis in HCT116 cells, supporting its application in epigenetic and cancer research. -
NF-κB Inhibitor
Micheliolide is a sesquiterpene lactone that functions as an NF-κB inhibitor. It exhibits significant anti-cancer and anti-inflammatory properties by attenuating high glucose-induced NF-κB activation and reducing the expression of inflammatory mediators such as MCP-1, TGF-β1, and FN in mouse mesangial cells. Additionally, Micheliolide inhibits LPS-induced NF-κB activation and the PI3K/Akt/p70S6K pathways, making it a valuable tool for studying inflammatory disease models, including colitis-associated cancer and rheumatic arthritis. -
Fluorometric HDAC Substrate
Boc-Lys(Ac)-AMC is a cell-permeable fluorometric substrate for histone deacetylases (HDACs). When cleaved by HDAC enzymes, it releases a fluorescent signal with excitation and emission maxima at 355 nm and 460 nm, respectively. This compound is valuable for studying HDAC activity in various biological contexts and can be utilized in high-throughput screening assays to evaluate enzyme inhibitors. -
NF-κB Inhibitor
Aristolochic acid A is a potent NF-κB inhibitor derived from the plant extracts of Aristolochia and Asarum species. This compound effectively diminishes the activities of activator protein 1 (AP-1) and NF-κB, making it a valuable tool for studying signaling pathways related to inflammation and cancer. Additionally, Aristolochic acid A has been shown to downregulate BLCAP gene expression in human cell lines, highlighting its potential for investigating gene regulation mechanisms. -
Endogenous Metabolite
Ergothioneine is an endogenous metabolite that acts as a potent antioxidant. It functions primarily as a specific inhibitor of p38 MAPK and Akt, which are critical signaling pathways involved in cellular stress responses. Ergothioneine is utilized in research focused on neuroprotection, cell apoptosis, and oxidative stress, making it a valuable compound for investigations into cellular resilience and health. -
VUBI1 Analogue
VUBI1 analogue-1 is an analogue of VUBI1, functioning as a selective activator of the SOS1 pathway with a Kd of 44 nM. This compound is valuable for studying SOS1 activation mechanisms and provides a basis for the synthesis of (4S)-PROTAC SOS1 degrader-1. Its applications include investigations into targeted degradation and modulation of cellular pathways involving SOS1, offering insights into cellular signaling and potential therapeutic strategies. -
TBK1 Degrader
PROTAC TBK1 Degrader-2 is a targeted protein degrader designed to selectively degrade the serine/threonine kinase TANK-binding kinase 1 (TBK1) with a DC50 of 15 nM and Kd of 4.6 nM, exhibiting a maximum efficiency of 96%. Additionally, this compound also influences IkB kinase IKKε, demonstrating an IC50 of 8.7 nM, and displays a low selectivity over TBK1 with an IC50 of 1.3 nM. This reagent is suitable for investigating TBK1-related signaling pathways and potential therapeutic applications in various diseases. -
PROTAC IRAK Degrader
Zomiradomide is an orally bioavailable PROTAC degrader targeting IRAK4, with a DC50 of 6 nM, which effectively inhibits the NF-κB signaling pathway. In addition to its suppression of IRAK4, Zomiradomide functions as a molecular glue, facilitating the degradation of Ikaros with a DC50 of 1 nM and consequently activating the type I IFN signaling pathway. This dual action positions Zomiradomide as a valuable tool in research focused on immune modulation and inflammatory responses. -
STAT3/NF-κB Inhibitor
Triacetylresveratrol is an acetylated analog of Resveratrol that functions as an inhibitor of STAT3 and NF-κB signaling pathways. It effectively reduces the phosphorylation levels of STAT3 and NF-κB in a dose- and time-dependent manner in PANC-1 and BxPC-3 cancer cell lines. Its promising anticancer activity makes it a valuable tool for research in cancer biology and therapeutic development. -
HDAC Inhibitor
HC-Toxin is a potent histone deacetylase (HDAC) inhibitor with an IC50 of 30 nM. This cyclic tetrapeptide effectively induces apoptosis in tumor cells, demonstrating significant anticancer activity. Its mechanism of action makes it valuable for research in cancer therapy and the modulation of gene expression. -
PDE Inhibitor
Theophylline, a potent phosphodiesterase (PDE) inhibitor, primarily targets PDE3, leading to relaxation of airway smooth muscle and enhanced bronchodilation. This compound also functions as an adenosine receptor antagonist and exhibits anti-inflammatory properties by elevating IL-10 levels and inhibiting NF-κB translocation into the nucleus. Additionally, Theophylline has been shown to induce apoptosis in certain cell types. Its applications are particularly relevant in the research of asthma and chronic obstructive pulmonary disease (COPD). -
TNF Receptor Inhibitor
Muscone, a TNF receptor inhibitor, is derived from the traditional Chinese medicine musk. It effectively inhibits NF-κB signaling and NLRP3 inflammasome activation, resulting in a significant reduction of inflammatory cytokines such as IL-1β, TNF-α, and IL-6. This compound is valuable in research focused on inflammation, cardiac function restoration, and improving survival rates in various pathological conditions. -
Apoptosis Inducer
Sanguinarine chloride is a benzophenanthridine alkaloid that functions as an apoptosis inducer primarily through the generation of reactive oxygen species (ROS). This compound is known to activate key signaling pathways, specifically JNK and NF-κB, facilitating programmed cell death. Sanguinarine chloride is widely utilized in cancer research and studies investigating apoptotic mechanisms. -
Anti-asthmatic Agent
Verproside, a catalpol derivative iridoid glycoside isolated from the genus Pseudolysimachion, represses TNF-α -induced MUC5AC expression by inhibiting NF-κB activation via the IKK/IκB signaling cascade. Verproside has potent anti-inflammatory, antioxidant, antinociceptive and anti-asthmatic activities. Verproside has the potential for the study of chronic obstructive pulmonary disease (COPD). -
Non-steroidal Anti-inflammatory Agent
Gaultherin is an orally active non-steroidal anti-inflammatory agent that selectively inhibits key inflammatory pathways, including NF-κB, MAPK, COX-2 (IC50 = 0.35 mg/mL), LOX (IC50 = 0.56 mg/mL), and HYAL (IC50 = 28.58 μg/mL). This compound demonstrates anti-inflammatory, antipyretic, and analgesic activities, making it suitable for research into inflammation-related conditions. Additionally, Gaultherin exhibits modest direct antioxidant capacity, particularly in cell-based models, while sparing COX-1, thus reducing the likelihood of gastrointestinal side effects commonly associated with traditional non-steroidal anti-inflammatory drugs. -
NF-κB Inhibitor
Sciadopitysin is a biflavonoid that serves as a potent NF-κB inhibitor. Its primary mechanism involves the inhibition of RANKL-induced osteoclastogenesis, contributing to the prevention of bone loss. By suppressing NF-κB activation and lowering the expression levels of c-Fos and NFATc1, Sciadopitysin demonstrates significant potential for research applications focused on bone metabolism and related disorders. -
Anti-inflammatory Agent
Darutoside is an orally active diterpene compound that functions primarily as an anti-inflammatory agent. It exhibits notable analgesic properties and enhances wound healing by inhibiting COX-2 expression and the migration of inflammatory cells. Additionally, Darutoside modulates macrophage polarization towards the M2 phenotype through NF-κB pathway inhibition, thereby reducing inflammation. This compound has been shown to significantly alleviate acute gouty arthritis by regulating metabolic networks involved in inflammatory responses. -
GR Agonist
Flumethasone is a highly selective and potent glucocorticoid receptor (GR) agonist. It effectively activates GR, leading to the inhibition of nuclear factor kappa B (NF-κB) and subsequent reduction of pro-inflammatory cytokine production, such as TNF-α and IL-1β. Additionally, Flumethasone upregulates anti-inflammatory gene expression, particularly IL-10, and modulates metabolic enzyme activity, including tyrosine aminotransferase. This compound is valuable for research into inflammatory diseases, cancer, and endocrine regulation. -
Bacterial Inhibitor
Ceftiofur is a cell wall synthesis inhibitor targeting bacterial penicillin-binding proteins (PBPs). It demonstrates bactericidal activity by interfering with the peptidoglycan synthesis in bacterial cell walls, resulting in cell lysis. Additionally, Ceftiofur exhibits anti-inflammatory properties by inhibiting the activation of NF-κB and MAPKs, which decreases the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6. This makes Ceftiofur a valuable reagent in research investigating bacterial infections and inflammation processes. -
Pro-apoptotic Compound
Dracorhodin perchlorate is a pro-apoptotic compound that targets multiple signaling pathways, inhibiting PI3K/Akt and NF-κB activation. This natural product derived from Dragon's blood upregulates p53 expression, activates caspases, and induces reactive oxygen species (ROS), leading to programmed cell death. It is also known to regulate TLR4, thereby promoting wound healing and offering therapeutic potential in diabetes management. Additionally, Dracorhodin perchlorate exhibits anti-tumor activity against various cancers, including prostate, breast, and cervical cancer, making it a valuable tool for cancer research. -
Insecticide
Azadirachtin is a triterpenoid compound with potent insecticidal properties. It induces apoptosis in insect cells via the mitochondrial pathway, acting through the modulation of the Bcl-2/Bax ratio and activation of Apaf-1 and caspase-3. Additionally, Azadirachtin has demonstrated anti-inflammatory effects by inhibiting the NF-κB signaling pathway, and exhibits a range of other biological activities, including anticancer and antimalarial effects. This compound is widely utilized in research applications focused on pest control and the study of apoptotic mechanisms. -
NF-κB Inhibitor
Cardamonin is a potent NF-κB inhibitor derived from cardamom. It exerts broad biological activity by targeting key signaling pathways, including mTOR, Akt, STAT3, Wnt/β-catenin, and COX-2. This compound has demonstrated significant anticancer, anti-inflammatory, antimicrobial, and antidiabetic properties, making it valuable for various research applications in cancer biology and inflammation studies.
