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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
RelB inhibitor
RS47 is a potent and specific inhibitor of the non-canonical NF-κB signaling pathway, acting by disrupting the binding of RelB to its target DNA with a Kd of 1.1 μM. It effectively inhibits the growth of colorectal cancer (CRC) cells and B lymphomas, making it a valuable research tool for studying and potentially targeting cancers driven by hyperactive non-canonical NF-κB signaling. -
Osteoclast formation inhibitor
ABD56 is a bioactive compound that inhibits osteoclast formation and induces osteoclast apoptosis. Its mechanism of action involves suppression of the NFκB and ERK signaling pathways, making it a promising candidate for research in bone metabolism and osteolytic diseases. -
Endoplasmic Reticulum Stress Inhibitor
Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an inhibitor of endoplasmic reticulum (ER) stress that significantly downregulates pro-apoptotic molecules, including caspase-3 and caspase-12. Additionally, it suppresses ERK signaling, contributing to its cytoprotective and anti-apoptotic effects. -
NF-κB inhibitor
Asperulosidic Acid (ASPA) is a bioactive iridoid glycoside isolated from the herb Hedyotis diffusa Willd., exhibiting anti-tumor, antioxidant, and anti-inflammatory properties. Its anti-inflammatory effects are associated with the downregulation of proinflammatory cytokines such as TNF-α and IL-6, mediated through inhibition of the NF-κB and MAPK signaling pathways. -
NF-κB/FAK/MAPK inhibitor
Keracyanin chloride is an orally active anthocyanin compound with potent antioxidant, anti-inflammatory, and hypoglycemic properties. It exerts its biological effects by inhibiting the NF-κB/FAK/MAPK signaling pathways, which are central to inflammation, cell adhesion, and metabolic regulation. -
ACAT inhibitor
Enniatin B1 is a mycotoxin produced by Fusarium species, known for its diverse bioactivities. It functions as a moderate inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC₅₀ of 73 μM in assays using rat liver microsomes, implicating a role in lipid metabolism modulation. Enniatin B1 is capable of crossing the blood-brain barrier, suggesting potential effects on central nervous system function. It also decreases the activation of ERK1/2 (p44/p42 MAPK) and moderately inhibits TNF-α-induced NF-κB activation, indicating anti-inflammatory and cell signaling modulatory properties. -
PDE4/NF-κB inhibitor
Sappanone A is an orally active homoisoflavone isolated from Caesalpinia sappan L., exhibiting notable anti-inflammatory and antioxidant properties. It functions as an inhibitor of phosphodiesterase 4 (PDE4) and NF-κB, key regulators of inflammatory signaling. Additionally, Sappanone A activates the Nrf2 pathway, leading to increased expression of the cytoprotective enzyme heme oxygenase-1 (HO-1). Sappanone A also inhibits RANKL-induced osteoclastogenesis, suggesting potential benefits in bone metabolism disorders. With its multifaceted bioactivity, Sappanone A holds significant promise for research in inflammation-related diseases, cardiovascular conditions, and bone health. -
NF-kB inhibitor
EF24 is a synthetic curcumin analogue and a potent NF-κB inhibitor with demonstrated oral bioavailability and strong antitumor activity. It exerts its anticancer effects, particularly in oral squamous cell carcinoma (OSCC), through deactivation of the MAPK/ERK signaling pathway. EF24 is effective against various cancer cell lines, with GI₅₀ values of 0.7 μM in melanoma and 0.8 μM in breast cancer cells. In MDA-MB-231 (breast cancer) and DU-145 (prostate cancer) cells, EF24 induces cell cycle arrest and apoptosis, accompanied by increased activation of caspase-3 and caspase-9. It also reduces the phosphorylation of MEK1 and ERK, further contributing to its pro-apoptotic and anti-proliferative effects. These properties make EF24 a promising compound for cancer therapy research. -
Microglial inhibitor
Inflachromene is a microglial inhibitor that exerts anti-inflammatory effects by directly binding to high mobility group box proteins HMGB1 and HMGB2. Through this interaction, it effectively downregulates the proinflammatory activities of HMGB proteins, leading to reduced microglial activation and neuronal damage. Inflachromene holds promise as a therapeutic candidate for the treatment of neuroinflammatory disorders, including neurodegenerative diseases and central nervous system injuries. -
HDAC11 inhibitor
Elevenostat (JB3-22) is a selective histone deacetylase 11 (HDAC11) inhibitor with an IC₅₀ of 0.235 µM. It exhibits antitumor activity by inducing apoptosis in multiple myeloma cells and shows potential as a therapeutic agent in hematologic malignancies. Additionally, Elevenostat has been shown to inhibit the maturation of mouse oocytes, suggesting a role for HDAC11 in reproductive biology and offering a tool for studying epigenetic regulation in oocyte development. -
HDAC6/HDAC10/LTA4H Inhibitor
Bufexamac is a nonsteroidal anti-inflammatory drug (NSAID) that functions as a dual inhibitor of class IIb histone deacetylases—HDAC6 and HDAC10—as well as leukotriene A4 hydrolase (LTA4H). It exhibits binding affinities (K\_d) of 0.53 µM for HDAC6 and 0.22 µM for HDAC10. Through its dual inhibitory activity, Bufexamac combines epigenetic modulation with anti-inflammatory effects, making it a valuable compound for research in inflammation, immune regulation, and HDAC-related pathologies. -
HDAC6 inhibitor
TYA-018 is an orally active, potent, and highly selective inhibitor of histone deacetylase 6 (HDAC6). In preclinical studies, TYA-018 demonstrates cardioprotective effects by preserving heart function in mice. Additionally, it enhances systemic energetics by upregulating the expression of genes involved in fatty acid metabolism, protein turnover, and oxidative phosphorylation, highlighting its potential in both cardiovascular and metabolic disease research. -
Snail/HDAC inhibitor
CYD19 is a potent dual-target inhibitor that simultaneously disrupts Snail and HDAC1 activity. It exhibits an IC₅₀ of 0.405 μM against HDAC1 and binds Snail with a K\_d of 0.18 μM. In HCT-116 colorectal cancer cells, CYD19 increases histone H4 acetylation and downregulates Snail protein expression, leading to the induction of apoptosis. This dual mechanism positions CYD19 as a promising therapeutic candidate for targeting epithelial–mesenchymal transition (EMT) and epigenetic dysregulation in cancer. -
CoreDAC Inhibitor
TNG260 is a selective and orally bioavailable inhibitor of histone deacetylase 1 (HDAC1) and the CoREST transcriptional corepressor complex. It exhibits approximately 10-fold selectivity for HDAC1 over HDAC3 and 500-fold selectivity for the CoREST complex compared to other HDAC-containing complexes such as NuRD and Sin3. TNG260 modulates the tumor immune microenvironment by reducing immunosuppressive neutrophil infiltration, enhancing effector T cell recruitment, and reversing anti-PD-1 resistance associated with STK11 mutations through inhibition of the CoREST–HDAC1 axis. In preclinical models, TNG260 induces durable tumor regression when combined with α-PD-1 therapy in MC38 tumor-bearing mice harboring STK11 mutations, while demonstrating reduced hematologic toxicity compared to non-selective HDAC inhibitors. -
phospholipase A2/HDAC2 inhibitor
Rhamnetin is a naturally occurring flavonoid and quercetin derivative found in *Coriandrum sativum*. It functions as an inhibitor of secretory phospholipase A₂ and histone deacetylase 2 (HDAC2), contributing to its broad pharmacological profile. Rhamnetin exhibits notable antitumor, antioxidant, and anti-inflammatory activities, making it a promising compound for research in cancer, oxidative stress-related conditions, and inflammatory diseases. -
HDAC10 inhibitor
DKFZ-748 is a selective histone deacetylase 10 (HDAC10) inhibitor with a pIC₅₀ of 7.66, corresponding to an IC₅₀ of approximately 22 nM. It exhibits antitumor activity, making it a valuable tool for studying HDAC10-mediated biological processes and a promising candidate for the development of targeted cancer therapies. -
HDAC6 inhibitor
KA2507 is a potent, orally active, and highly selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 2.5 nM. It exhibits strong antitumor activity and immunomodulatory effects in preclinical models, making it a promising candidate for cancer therapy, particularly in tumors where HDAC6 plays a key role in tumor progression and immune evasion. -
GRK5 inhibitor
KR-39038 is a potent and orally bioavailable inhibitor of G protein-coupled receptor kinase 5 (GRK5), with an IC₅₀ of 0.02 μM. It effectively suppresses angiotensin II–induced cellular hypertrophy by inhibiting the HDAC5 signaling pathway in neonatal cardiomyocytes. KR-39038 exhibits strong anti-hypertrophic activity and improves cardiac function in preclinical models, making it a promising candidate for research in heart failure and related cardiovascular diseases. -
HDAC6 inhibitor
T-518 is an orally active, selective histone deacetylase 6 (HDAC6) inhibitor with an IC₅₀ of 36 nM for human HDAC6. It is capable of crossing the blood–brain barrier, making it suitable for central nervous system applications. T-518 is particularly useful in tauopathy research, where HDAC6 inhibition may modulate tau pathology and neurodegenerative processes. -
HDAC1 inhibitor
9-Hydroxyoctadecanoic acid (9-HSA) is a naturally derived inhibitor of histone deacetylase 1 (HDAC1), inhibiting approximately 66.4% of HDAC1 enzymatic activity at a concentration of 5 μM. It exhibits notable anticancer activity, likely through epigenetic modulation of gene expression, making it a promising compound for cancer research and therapeutic development targeting HDAC1-regulated pathways. -
HDAC6 inhibitor
SE-7552 is an orally active, highly selective histone deacetylase 6 (HDAC6) inhibitor, based on a 2-(difluoromethyl)-1,3,4-oxadiazole (DFMO) scaffold, with an IC₅₀ of 33 nM. As a non-hydroxamate HDAC6 inhibitor, SE-7552 demonstrates exceptional isoform selectivity, showing over 850-fold preference for HDAC6 compared to other HDAC isozymes. In preclinical studies, SE-7552 effectively inhibits multiple myeloma tumor growth in vivo and also exhibits anti-obesity effects in diet-induced obese mouse models, highlighting its therapeutic potential in both oncology and metabolic disease research. -
COX-1/HDAC/Tyrosinase Inhibitor
Gnetol is a bioactive phenolic compound isolated from the root of *Gnetum montanum* with diverse pharmacological properties. It potently inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 0.78 μM and exhibits histone deacetylase (HDAC) inhibitory activity. Gnetol is also a strong tyrosinase inhibitor, with an IC₅₀ of 4.5 μM against murine tyrosinase, leading to suppression of melanin biosynthesis. In addition to its antioxidant, antiproliferative, anticancer, and hepatoprotective effects, Gnetol modulates metabolic enzymes in a concentration-dependent manner, including α-amylase, α-glucosidase, and adipogenesis pathways, making it a promising candidate for research in oncology, dermatology, and metabolic disorders. -
HDAC inhibitor
Marein is a natural compound with multifaceted pharmacological properties, including HDAC inhibition with an IC₅₀ of 100 μM. It exerts neuroprotective effects by preserving mitochondrial function and activating the AMPK signaling pathway. In HepG2 cells, Marein improves high glucose–induced insulin resistance by enhancing glucose uptake via the CaMKK/AMPK/GLUT1 pathway, promoting glycogen synthesis through the IRS/Akt/GSK-3β pathway, and suppressing gluconeogenesis via the Akt/FoxO1 axis. Additionally, Marein possesses antioxidative, antihypertensive, antihyperlipidemic, and antidiabetic properties, making it a promising candidate for metabolic and neurodegenerative disease research. -
HDAC inhibitor
Crebinostat is a potent, broad-spectrum histone deacetylase (HDAC) inhibitor with IC₅₀ values of 0.7 nM (HDAC1), 1.0 nM (HDAC2), 2.0 nM (HDAC3), and 9.3 nM (HDAC6). It effectively induces acetylation of histone H3 and H4, and enhances the expression of Egr1, a cAMP response element-binding protein (CREB) target gene. In cultured neurons, Crebinostat increases the density of synapsin-1 puncta along dendrites, indicating enhanced synaptic connectivity. By modulating chromatin-mediated neuroplasticity, Crebinostat has been shown to improve memory performance in mice, supporting its potential for neuropsychiatric and cognitive disorder research. -
HDAC inhibitor
Bakkenolide A is a natural sesquiterpene lactone isolated from *Petasites tricholobus*. It exhibits anti-leukemic activity by modulating epigenetic and signaling pathways, specifically through inhibition of histone deacetylase 3 (HDAC3) and regulation of the PI3K/Akt signaling cascade. These combined effects contribute to its potential as a therapeutic agent in leukemia research. -
HDAC8 inhibitor
NCC-149 is a selective inhibitor of histone deacetylase 8 (HDAC8), making it a valuable tool for studying HDAC8-specific functions. It has shown utility in promoting neural differentiation, and is particularly useful in research focused on neurodevelopmental processes and potential therapeutic strategies for neurological disorders involving epigenetic dysregulation. -
HDAC inhibitor
CM-1758 is a histone deacetylase (HDAC) inhibitor with demonstrated antitumor activity in vivo. In acute myeloid leukemia (AML) cells, CM-1758 induces the acetylation of non-histone proteins, suggesting a broader epigenetic and post-translational regulatory effect beyond chromatin remodeling. Its dual impact on tumor growth and protein acetylation supports its potential as a therapeutic agent in hematologic malignancies. -
HDAC6 inhibitor
MPT0G211 is a highly potent, orally bioavailable, and selective histone deacetylase 6 (HDAC6) inhibitor, with an IC₅₀ of 0.291 nM and over 1000-fold selectivity against other HDAC isoforms. It efficiently crosses the blood–brain barrier and demonstrates neuroprotective effects by reducing tau phosphorylation and improving cognitive function in Alzheimer's disease models. Additionally, MPT0G211 exhibits anti-metastatic and anticancer activities, making it a promising therapeutic candidate for both neurodegenerative disorders and oncology research. -
HDAC inhibitor
MPT0B390 is a potent arylsulfonamide-based histone deacetylase (HDAC) inhibitor that also functions as an inducer of tissue inhibitor of metalloproteinases 3 (TIMP3). It exhibits strong antitumor properties, including inhibition of tumor growth, metastasis, and angiogenesis. MPT0B390 shows significant antiproliferative activity against the human colon cancer cell line HCT116, with a GI₅₀ of 0.03 μM, highlighting its potential as a promising candidate for cancer therapy. -
class-IIa HDAC inhibitor
NT160 is a highly potent inhibitor of class IIa histone deacetylases (HDACs), with an IC₅₀ value of 0.046 μM. Due to its strong inhibitory activity and potential central nervous system (CNS) penetration, NT160 is a valuable compound for investigating the role of class IIa HDACs in CNS-related disorders, including neurodegenerative and neuropsychiatric diseases. -
DNA Methyltransferase Inhibitor
RSC133 is a dual epigenetic modulator that inhibits both histone deacetylases (HDACs) and DNA methyltransferases (DNMTs). It effectively enhances the reprogramming of human somatic cells into induced pluripotent stem cells (iPSCs) and supports the maintenance of pluripotency by promoting an undifferentiated state. RSC133 is a valuable tool for stem cell research and epigenetic reprogramming studies. -
HDAC inhibitor
Alteminostat (CKD-581) is a potent, broad-spectrum histone deacetylase (HDAC) inhibitor that targets both class I and class II HDAC isoforms. It promotes histone H3 and α-tubulin acetylation, indicating effective inhibition of nuclear and cytoplasmic HDAC activity. Alteminostat is being investigated for its therapeutic potential in hematologic malignancies, including lymphoma and multiple myeloma, and serves as a valuable tool in epigenetic cancer research. -
HDAC6 inhibitor
CG347B is a selective inhibitor of histone deacetylase 6 (HDAC6) and also serves as a structural scaffold in the synthesis of other metalloenzyme inhibitors. Due to its HDAC6 selectivity, CG347B is a valuable tool for research in oncology, immunology, and neurology, where HDAC6 plays key roles in regulating protein homeostasis, immune response, and neurodegenerative processes. -
HDAC inhibitor
MC1742 is a potent pan-HDAC inhibitor with broad activity across multiple HDAC isoforms, exhibiting IC₅₀ values of 0.1 μM (HDAC1), 0.11 μM (HDAC2), 0.02 μM (HDAC3), 0.007 μM (HDAC6), 0.61 μM (HDAC8), 0.04 μM (HDAC10), and 0.1 μM (HDAC11). It effectively increases acetylation of histone H3 and α-tubulin, markers of HDAC inhibition. MC1742 inhibits the growth of cancer stem cells (CSCs), and induces growth arrest, apoptosis, and differentiation, particularly in sarcoma CSC models, making it a promising candidate for targeting therapy-resistant cancer cell populations. -
HDAC1 inhibitor
SB-429201 is a potent and selective inhibitor of histone deacetylase 1 (HDAC1), with an IC₅₀ of approximately 1.5 μM. It exhibits at least a 20-fold selectivity for HDAC1 over other class I isoforms, including HDAC3 and HDAC8. SB-429201 serves as a valuable tool for studying HDAC1-specific functions and may have potential applications in epigenetic and cancer research. -
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.
