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Catalog No.
Product Name
Application
Product Information
Citations
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HDAC Inhibitor
Purinostat mesylate is a selective inhibitor of histone deacetylases (HDACs), effectively targeting class I and class IIb HDACs with IC50 values ranging from 0.81 to 11.5 nM. This compound induces apoptosis and influences the cell cycle in LAMA84 and 188 BL-2 cell lines, demonstrating potent anti-leukemic effects in vivo. Purinostat mesylate serves as a valuable tool for researching lymphoblastic leukemia and its therapeutic potential. -
JAK2/STAT3/NF-κB Inhibitor
Reticuline acts as a JAK2/STAT3 and NF-κB signaling pathway inhibitor, displaying notable anti-inflammatory properties. It effectively downregulates the mRNA expression of pro-inflammatory cytokines such as TNF-α and IL-6 while also reducing the phosphorylation levels of JAK2 and STAT3. Additionally, Reticuline demonstrates potential cardiovascular effects, making it a valuable tool for research in inflammation and cardiovascular studies. -
JAK/STAT and NF-κB Inhibitor
JAK-IN-23 is a potent dual inhibitor of the JAK/STAT and NF-κB signaling pathways, targeting JAK1, JAK2, and JAK3 with IC50 values of 8.9 nM, 15 nM, and 46.2 nM, respectively. This compound effectively modulates the expression of interferon-stimulated genes (ISG) and inhibits NF-κB activation, exhibiting IC50 values of 3.3 nM and 150.7 nM, respectively. JAK-IN-23 demonstrates significant anti-inflammatory properties by reducing the release of various pro-inflammatory cytokines. Its applications include research into inflammatory bowel disease (IBD) and other related inflammatory conditions. -
IRAK4/IRAK1 Inhibitor
IRAK4 modulator-2 is a selective inhibitor of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) and IRAK1, exhibiting IC50 values of 0.005 μM and 0.97 μM, respectively. This compound effectively disrupts IRAK-mediated signaling pathways, including JAK-STAT and NF-κB pathways, leading to a reduction in pro-inflammatory cytokine production, such as IL-1 and TNF. IRAK4 modulator-2 demonstrates potential for use in research focusing on autoimmune and inflammatory diseases, including rheumatoid arthritis, psoriasis, and inflammatory bowel disease. -
Cathepsin L/JAK Inhibitor
Dual Cathepsin L/JAK-IN-1 is a dual inhibitor targeting Cathepsin L (CTSL) and Janus kinases (JAK), exhibiting IC50 values of 0.68 μM for CTSL, 337.1 nM for JAK1, 5.251 nM for JAK2, 27.29 nM for JAK3, and 172.6 nM for TYK2. This compound effectively inhibits the activation of key signaling pathways, including MAPK, NF-κB, and JAK/STAT, thereby providing substantial anti-inflammatory effects. Dual Cathepsin L/JAK-IN-1 is useful for investigating mechanisms underlying acute lung injury (ALI) and other inflammatory conditions. -
IKKβ/JAK2 Inhibitor
EC-70124 is an orally active multikinase inhibitor that targets IKKβ and JAK2. By blocking IkB phosphorylation and the activation of STAT3 (Tyr705), EC-70124 inhibits NF-κB nuclear translocation and impedes STAT3 transcriptional activity. This compound has demonstrated the ability to reduce tumor growth and diminish cancer stem cell populations in prostate cancer cells and xenograft models, making it a valuable tool for research in prostate cancer. -
IKKε/TBK-1 Inhibitor
MRT67307 dihydrochloride is a potent inhibitor of IKKε and TBK-1, demonstrating IC50 values of 160 nM and 19 nM, respectively. Additionally, this compound inhibits ULK1 and ULK2 with IC50s of 45 nM and 38 nM, respectively. MRT67307 dihydrochloride plays a significant role in blocking autophagy in cellular environments, making it a valuable tool for studies involving inflammation and autophagic processes. -
IKKε Inhibitor
IKKε-IN-1 is a selective inhibitor of IKKε, a key enzyme involved in the NF-κB signaling pathway. This compound effectively reduces cell viability, inhibits colony formation, and diminishes cell migration in various cancer cell lines. Additionally, IKKε-IN-1 induces autophagy, illustrating its potential as a research tool in the study of multiple cancer types, including colorectal, hepatocellular, bladder, breast, lung, and cervical cancers. -
Carnitine Palmitoyltransferase I Upregulator, Peroxisome Proliferator-Activated Receptor α Upregulator, Nuclear Factor Erythroid 2-Related Factor 2 Activator, Nuclear Factor-Kappa B Inhibitor, Nuclear Factor Kappa B Kinase Subunit Beta Inhibitor, Sterol Regulatory Element-Binding Protein 1 Downregulator, Acetyl-CoA Carboxylase Downregulator, Acyl-CoA:Cholesterol Acyl Transferase 1 Inhibitor, Acyl-CoA:Cholesterol Acyl Transferase 2 Inhibitor
Esculeogenin A is a potent upregulator of Carnitine Palmitoyltransferase I and Peroxisome Proliferator-Activated Receptor α, while also acting as an activator of Nuclear Factor Erythroid 2-Related Factor 2. This compound exhibits key biological activities, including hepatoprotective, hypolipidemic, and antioxidant effects. Esculeogenin A modulates essential molecular targets such as SREBP1, NF-κB, and ACAT1/ACAT2, leading to enhanced hepatic fatty acid oxidation and diminished inflammation. It is applicable in research focused on nonalcoholic fatty liver disease, atherosclerosis, and hyperlipidemia, showcasing its potential to improve liver function and mitigate the risk of associated metabolic disorders. -
COX-2 Inhibitor/PPAR-γ Activator
Zaltoprofen sulfoxide is a selective COX-2 inhibitor with an IC50 of 45.38 nM, as well as a PPAR-γ activator. This compound effectively inhibits NF-κB and MAPK inflammatory signaling pathways, making it a valuable tool in the study of inflammation and acute lung injury models. It is particularly relevant for research focused on LPS-induced acute lung injury. -
TrxR1 Inhibitor
Aurothioglucose is a potent inhibitor of thioredoxin reductase 1 (TrxR1), exhibiting an IC50 value of 65 nM. This compound effectively inhibits the DNA binding activity of NF-κB in vitro, highlighting its role in modulating key transcriptional pathways. Additionally, Aurothioglucose demonstrates anti-HIV and anti-rheumatic properties, making it a valuable reagent for research in infectious diseases and autoimmune disorders. -
ROS Inhibitor
Isodeoxyelephantopin is a sesquiterpene lactone with a primary mechanism as a reactive oxygen species (ROS) inhibitor. It demonstrates significant biological activity by inducing ROS generation and suppressing NF-κB activation, thereby contributing to its anticancer properties. Additionally, Isodeoxyelephantopin modulates long non-coding RNA (LncRNA) expression, making it a valuable reagent for breast cancer research and related fields. -
IKKβ Inhibitor
IKKβ-IN-7 is a selective inhibitor of IKKβ, exhibiting an IC50 value of 9.44 μM. This compound induces DNA damage, S-phase cell cycle arrest, and apoptosis, while also promoting reactive oxygen species accumulation and loss of mitochondrial membrane potential. By inhibiting the phosphorylation of p65 and IκBα, IKKβ-IN-7 effectively restricts p65 nuclear translocation and modulates NF-κB-regulated gene expression. This agent demonstrates significant antitumor activity in xenograft models, particularly in colorectal cancer, while exhibiting low cytotoxicity in normal cells. IKKβ-IN-7 serves as a valuable tool for research in the field of colorectal cancer. -
HDAC1/HDAC2 Inhibitor
MRLB-223 is a selective inhibitor of HDAC1 and HDAC2, demonstrating potent activity against tumor cells. It induces histone hyperacetylation and activates the intrinsic apoptotic pathway, leading to tumor cell apoptosis and degradation of Bcr-Abl in a caspase-dependent manner. Notably, MRLB-223 mediates p53-independent cell death in Bcr-Abl-expressing myeloid cells and shows efficacy in animal models of Eμ-myc lymphoma. This compound is valuable for research focusing on the mechanisms of lymphomagenesis and therapeutic strategies for Eμ-myc lymphoma. -
GADD45β/MKK7 Inhibitor
DTP3 TFA is a highly selective inhibitor of GADD45β/MKK7, targeting a critical pathway involved in cell survival in cancer cells downstream of the NF-κB signaling cascade. This compound exert biological activity by disrupting the function of the GADD45β/MKK7 module, influencing cellular responses to DNA damage and stress. DTP3 TFA serves as a valuable tool in cancer research, particularly in studies investigating the mechanisms of cell survival and the potential for therapeutic interventions in malignancies associated with aberrant NF-κB activity. -
Inflammation Inhibitor
Resolvin D5 is an anti-inflammatory agent primarily targeting the GPR32 receptor, effectively modulating inflammation responses. It alleviates Paclitaxel-induced mechanical allodynia and inflammatory pain in male mice through mechanisms that do not involve TRPV1 or TRPA1 channels. Resolvin D5 reduces LPS-induced ERK phosphorylation and NF-κB nuclear translocation while downregulating pro-inflammatory mediators, inhibiting Th17 differentiation, and promoting regulatory T cell differentiation. This compound is particularly relevant for research on chemotherapy-induced peripheral neuropathy, inflammatory pain, and rheumatoid arthritis. -
NF-κB&ERK1/2 Inhibitor
OP-1118 is a potent dual inhibitor of NF-κB and ERK1/2, targeting critical signaling pathways involved in inflammation and cell survival. This compound demonstrates significant anti-inflammatory, cytoprotective, anti-apoptotic, and antibacterial activities by inhibiting the phosphorylation of NF-κB and ERK1/2, leading to a reduction in pro-inflammatory cytokine expression. In preclinical models of Clostridium difficile infection, OP-1118 effectively mitigates toxin-induced intestinal inflammation, cellular damage, and apoptosis, with its protective effects possibly reversible by PMA. This makes OP-1118 a valuable reagent for research into inflammatory conditions and therapeutic interventions. -
Syk Inhibitor, NF-κB p65 Inhibitor, TGF-β1/Smad Signaling Inhibitor
Flavanomarein is a potent inhibitor of Syk and NF-κB p65, as well as a modulator of TGF-β1/Smad signaling pathways. This compound exhibits cytoprotective, anti-inflammatory, and antioxidant activities, enhancing AKT phosphorylation while regulating key proteins such as PKC-δ, P85α, PKC-β1, Sirt1, Bcl-2, and ICAD. Flavanomarein also inhibits the nuclear translocation of NF-κB p65 and modulates epithelial-mesenchymal transition (EMT) markers, promoting proliferation in HK-2 cells and protecting neuronal cells from 6-OHDA-induced neurotoxicity. This compound is valuable for research on Parkinson's disease and diabetic nephropathy. -
NF-κB Inhibitor/TRP Modulator
Cannabitwinol is a selective NF-κB inhibitor and thermosensitive TRP modulator. It effectively inhibits TNFα-induced NF-κB-driven transcription and IL-8 release, exhibiting notable anti-inflammatory and antioxidant properties. Cannabitwinol selectively activates cold-activated TRP channels, such as TRPA1 (EC50 = 3.0 μM), while antagonizing TRPM8 (IC50 = 3.9 μM), with minimal interaction with heat-activated TRP channels like TRPV1 and TRPV2. This compound is applicable in research focused on inflammatory skin diseases, cold allodynia, and hyperalgesia. -
NF-κB Inhibitor
Bengamide B is a potent inhibitor of NF-κB with an IC50 of 85 nM. This compound effectively reduces LPS-induced expression of pro-inflammatory cytokines, including TNF-α, IL-6, and MCP-1, demonstrating significant anti-inflammatory activity. Additionally, Bengamide B displays antitumor efficacy, with an IC50 of 2 nM against HCT-116 colorectal cancer cells, making it a valuable reagent for research in inflammation and oncology. -
SEAP Inhibitor
Cycloepoxydon is a potent inhibitor of secreted alkaline phosphatase (SEAP) expression, targeting both NF-κB and AP-1 signaling pathways. It effectively reduces PMA-induced SEAP expression with IC50 values ranging from 1-2 μg/mL (4.2-8.4 μM) for NF-κB and 3-5 μg/mL (12.6-21 μM) for AP-1. This compound is valuable for research applications involving inflammation, cancer biology, and signal transduction studies. -
NF-κB Inhibitor
2,4,5-Trimethoxybenzoic acid is an NF-κB inhibitor with notable anti-inflammatory properties. This compound, derived from purple perilla extracts, effectively inhibits LPS-induced inflammatory responses by blocking the activation of NF-κB and STAT signaling pathways. It has been shown to suppress M1 macrophage phenotype-mediated inflammation, making it a valuable tool for research into diabetes and related inflammatory conditions. -
IKKε/TBK-1 Inhibitor
MRT67307 hydrochloride is a selective inhibitor of IKKε and TBK-1, exhibiting IC50 values of 160 nM and 19 nM, respectively. Additionally, it inhibits ULK1 and ULK2 with IC50s of 45 nM and 38 nM, respectively. This compound is employed in research to study autophagy regulation and related cellular processes. It is particularly useful in investigations of inflammatory signaling pathways and cancer biology. -
HDAC Inhibitor
HDAC-IN-37 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.0551 μM for HDAC1, 1.24 μM for HDAC3, 0.948 μM for HDAC8, and 34.2 μM for HDAC6. This compound effectively increases histone acetylation through a slow-off binding mechanism. Additionally, HDAC-IN-37 disrupts the transition from the G1 phase to the S phase of the cell cycle and promotes early apoptosis in various cell types, making it a valuable tool for research in cancer biology and therapeutic development. -
c-Met/HDAC Inhibitor
c-Met/HDAC-IN-3 is a dual inhibitor targeting c-Met and histone deacetylase 1 (HDAC1), exhibiting IC50 values of 12.50 nM and 26.97 nM, respectively. This compound demonstrates significant biological activity by inducing apoptosis and causing cell cycle arrest at the G2/M phase. c-Met/HDAC-IN-3 serves as a valuable tool for research in cancer biology and therapeutic development, particularly in studies focused on synergistic inhibition of oncogenic pathways. -
HDAC6 Inhibitor
HDAC6-IN-4 is a potent and selective inhibitor of histone deacetylase 6 (HDAC6), exhibiting an IC50 value of 23 nM. This compound promotes apoptosis in cancer cells and demonstrates significant antitumor efficacy while exhibiting minimal toxicity. HDAC6-IN-4 is valuable for research in cancer biology, particularly in studies focused on epigenetic regulation and therapeutic development. -
HDAC Inhibitor
HDAC-IN-31 is a selective and orally active histone deacetylase (HDAC) inhibitor, exhibiting IC50 values of 84.90 nM for HDAC1, 168.0 nM for HDAC2, 442.7 nM for HDAC3, and greater than 10,000 nM for HDAC8. This compound induces apoptosis and triggers G2/M phase cell cycle arrest, demonstrating significant antitumor efficacy. HDAC-IN-31 is applicable in research focused on diffuse large B-cell lymphoma and other cancer studies. -
Topoisomerase/HDAC Inhibitor
Top/HDAC-IN-1 is a dual inhibitor targeting both topoisomerase and histone deacetylases (HDACs), demonstrating IC50 values of 18 nM for HDAC1, 230 nM for HDAC2, 790 nM for HDAC3, 87 nM for HDAC6, and 5250 nM for HDAC8. This compound exhibits significant antitumor activity against HCT116 cells, with an IC50 of 180 nM, effectively inducing apoptosis and promoting G2 cell cycle arrest. Top/HDAC-IN-1 serves as a valuable tool in cancer research, particularly for studies involving epigenetic modulation and cell proliferation. -
mTOR/HDAC6 Inhibitor
mTOR/HDAC6-IN-1 is a potent dual inhibitor targeting mTOR and HDAC6, exhibiting IC50 values of 133.7 nM and 56 nM, respectively. This compound is known to induce significant autophagy and apoptosis while suppressing cell migration. It holds potential for research applications in triple-negative breast cancer (TNBC) studies, offering insights into the interplay between these critical pathways in cancer progression. -
HDAC Inhibitor
HDAC-IN-59 is a potent inhibitor of histone deacetylases (HDACs), demonstrating significant biological activity in cancer research. This compound promotes the generation of reactive oxygen species (ROS), leading to DNA damage and the induction of apoptosis via the mitochondria-related pathway. Additionally, HDAC-IN-59 effectively disrupts the cell cycle at the G2/M phase, making it a valuable tool for studying the mechanisms of cell growth regulation and apoptosis in various cancer models. -
S100P Inhibitor
5-Methyl cromolyn disodium is a selective inhibitor of the S100P protein, targeting its interaction with the receptor for advanced glycation end-products (RAGE). It effectively suppresses NF-κB activity and cell proliferation while enhancing Gemcitabine-induced apoptosis. In preclinical mouse models, 5-Methyl cromolyn disodium demonstrates significant anti-tumor effects by reducing growth and metastasis of pancreatic ductal adenocarcinoma (PDAC), ultimately extending survival. This compound serves as a valuable tool for investigating pancreatic cancer mechanisms and potential therapeutic approaches. -
JAK/HDAC Inhibitor
JAK/HDAC-IN-2 is a dual-target inhibitor of Janus kinase (JAK) and histone deacetylase (HDAC), specifically inhibiting HDAC3/6 and JAK1/2 with nanomolar potency. This compound demonstrates proapoptotic activity by inhibiting histone deacetylation and STAT3 phosphorylation, contributing to its mechanism of action. JAK/HDAC-IN-2 exhibits significant antiproliferative effects in various hematological malignancies and solid tumors, making it a valuable tool for cancer research and therapeutic studies. -
c-Met/HDAC Inhibitor
c-Met/HDAC-IN-2 is a highly potent dual inhibitor targeting c-Met and histone deacetylases (HDACs), exhibiting IC50 values of 18.49 nM for HDAC1 and 5.40 nM for c-Met. This compound demonstrates significant antiproliferative effects against various cancer cell lines, notably inducing G2/M-phase cell cycle arrest and apoptosis in HCT-116 cells. c-Met/HDAC-IN-2 is a valuable tool for investigating mechanisms of anti-cancer resistance and exploring therapeutic strategies in oncology research. -
HDAC inhibitor
HDAC-IN-67 is a potent inhibitor of histone deacetylases HDAC1 and HDAC6, demonstrating IC50 values of 22 nM and 8 nM, respectively. This compound effectively inhibits cell proliferation and induces apoptosis in various cancer cell lines. Its significant antitumor activity makes HDAC-IN-67 a valuable tool for cancer research and a potential candidate for therapeutic development. -
PIM-1/HDAC Inhibitor
PIM-1/HDAC-IN-1 is a selective inhibitor of PIM-1 as well as histone deacetylases HDAC 1 and HDAC 6, exhibiting an IC50 of 343.87 nM for PIM-1 and 63.65 nM and 62.39 nM for HDAC 1 and HDAC 6, respectively. This compound demonstrates significant apoptotic activity in MCF-7 cell lines, inducing pre-G1 apoptosis and causing cell cycle arrest at the G2/M phase. PIM-1/HDAC-IN-1 is a valuable tool for research on cancer biology and the regulation of cell proliferation and apoptosis. -
FGFR/HDAC Inhibitor
HDAC-IN-50 is a potent dual inhibitor targeting FGFR and HDAC with IC50 values of 0.18 nM for FGFR1, 1.2 nM for FGFR2, 0.46 nM for FGFR3, 1.4 nM for FGFR4, and varying inhibitory effects on HDAC isoforms such as HDAC1 (1.3 nM), HDAC2 (1.6 nM), HDAC6 (2.6 nM), and HDAC8 (13 nM). This compound effectively induces apoptosis and causes cell cycle arrest at the G0/G1 phase. Additionally, HDAC-IN-50 decreases the expression of phosphorylated forms of FGFR1, ERK, and STAT3, indicating its potential applications in cancer research and therapy. -
Tubulin/HDAC Inhibitor
Tubulin/HDAC-IN-1 is a dual inhibitor targeting tubulin and histone deacetylase 8 (HDAC8) through CH/π interaction and hydrogen bonding, respectively. This compound effectively inhibits tubulin polymerization and selectively inhibits HDAC8 with an IC50 value of 150 nM. Tubulin/HDAC-IN-1 demonstrates cytotoxic effects against a range of human cancer cell lines, induces cell cycle arrest in the G2/M phase, and promotes apoptosis. It is a valuable reagent for research involving hematologic malignancies and solid tumors, including neuroblastoma and leukemia. -
HDAC6 Inhibitor
SAHA-OH is a selective inhibitor of histone deacetylase 6 (HDAC6) with an IC50 of 23 nM, demonstrating a 10- to 47-fold selectivity over HDAC isoforms 1, 2, 3, and 8. This compound exhibits notable anti-inflammatory properties and has been shown to reduce macrophage apoptosis. It is a valuable tool for research focused on the modulation of histone acetylation and the investigation of HDAC6's role in various inflammatory pathways. -
VEGFR-2/HDAC Dual Inhibitor
VEGFR2/HDAC1-IN-1 is a potent dual inhibitor of VEGFR-2 and HDAC, demonstrating IC50 values of 57.83 nM and 9.82 nM, respectively. This compound effectively arrests the cell cycle at the S and G2 phases, leading to apoptosis in HeLa cells. Additionally, VEGFR2/HDAC1-IN-1 exhibits significant anti-angiogenic properties, making it a valuable tool for research in cancer biology and targeted therapies. -
HDAC Inhibitor
HDAC-IN-34 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.022 μM for HDAC1 and 0.45 μM for HDAC6. This compound binds to DNA, leading to DNA damage and inducing apoptosis through the p53 signaling pathway. Additionally, HDAC-IN-34 exhibits significant anti-proliferative effects against HCT-116 colorectal cancer cells, with an IC50 of 1.41 μM, making it a valuable tool for cancer research and epigenetic studies. -
NF-κB Inhibitor
NF-κB-IN-5 is a potent inhibitor of nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) that acts by directly interacting with the NF-κB complex. This compound demonstrates significant antitumor activity across multiple human cancer cell lines, including HCT116, U87-MG, HepG2, BGC823, and PC9, with IC50 values ranging from 2.02 to 5.35 μM. NF-κB-IN-5 also promotes apoptosis in U87-MG cells and induces cell cycle arrest in the G0/G1 phase, positioning it as a valuable tool for cancer research and therapeutic development. -
HDAC/PSMD14 Inhibitor
HDAC/PSMD14-IN-1 is a dual-target inhibitor of HDAC1 and PSMD14, exhibiting IC50 values of 238.7 nM and 141.2 nM, respectively. This compound demonstrates significant cytotoxicity against esophageal squamous cell carcinoma (ESCC) cell lines, with IC50 values ranging from 30 to 250 nM. In addition to its ability to induce apoptosis, HDAC/PSMD14-IN-1 effectively reverses epithelial-mesenchymal transition (EMT) and shows promising anti-tumor activity in KYSE30 mouse xenograft models. It is a valuable tool for advancing research in esophageal cancer. -
HDAC Inhibitor
1-Alaninechlamydocin is a cyclic tetrapeptide that functions as a potent histone deacetylase (HDAC) inhibitor with an IC50 of 6.4 nM. This compound effectively induces G2/M cell cycle arrest and promotes apoptosis in MIA PaCa-2 cells, making it a valuable tool for cancer research. Its activity in modulating epigenetic regulation highlights its potential applications in therapeutic development and studies of cellular differentiation and survival. -
HDAC Class I Inhibitor
HDAC-IN-27 is a selective inhibitor of Class I histone deacetylases (HDAC1-3) with an IC50 range of 0.43 to 3.01 nM. It demonstrates significant anti-proliferative and pro-apoptotic effects against acute myeloid leukemia (AML) cell lines by promoting histone acetylation, specifically AcHH3 and AcHH4. This compound is valuable for research into the mechanisms of AML and potential therapeutic applications in histone modification regulation. -
HDAC6 Inhibitor
Daphnegiravone D is an inhibitor of HDAC6, targeting histone deacetylation to modulate gene expression. This compound demonstrates significant anti-hepatocellular carcinoma activity by inducing apoptosis and selectively inhibiting the proliferation of liver cancer cells. Its mechanism involves the p38 and JNK MAPK signaling pathways, making it a valuable tool for research in cancer therapeutics and cellular signaling. -
HDAC1/6 Inhibitor
HDAC1/6-IN-1 is a potent inhibitor targeting HDAC1 and HDAC6, exhibiting IC50 values of 1.3 nM and 13 nM, respectively. This compound effectively inhibits the methylation and deacetylation of H3K9, leading to significant biological activity, including the induction of apoptosis in cancer cells, G0/G1 cell cycle arrest, and the inhibition of cell migration and invasion. It serves as a valuable tool in cancer research and the study of epigenetic regulation. -
c-Myc Inhibitor
EP12 is a selective c-Myc inhibitor that stabilizes c-Myc G-quadruplexes. This compound induces apoptosis and causes DNA damage in multiple myeloma cells, effectively inhibiting their growth. Additionally, EP12 disrupts the nuclear translocation of P65/P50 by interfering with the NF-κB signaling pathway, highlighting its potential in cancer research and therapeutic applications. -
IRAK4 Inhibitor
Emavusertib phosphate is a potent inhibitor of IRAK4, exhibiting an IC50 of 57 nM. This compound effectively disrupts NF-κB and MyD88 signaling pathways, leading to a significant reduction in pro-inflammatory cytokines such as IL-6 and IL-10. Emavusertib phosphate demonstrates both anti-inflammatory and anti-proliferative effects on cancer cells, promoting apoptosis and showcasing antitumor activity in preclinical mouse models. Its applications extend to investigating inflammatory diseases and cancer therapies. -
IRAK4 Inhibitor
Emavusertib maleate is a potent inhibitor of IRAK4, demonstrating an IC50 of 57 nM, and FLT3. This orally bioavailable compound inhibits NF-κB and MyD88 signaling pathways, effectively reducing the production of pro-inflammatory cytokines such as IL-6 and IL-10. Its anti-inflammatory and anti-proliferative properties make it a valuable tool for cancer research, promoting apoptosis in cancer cells and demonstrating antitumor activity in preclinical mouse models. -
NF-κB Inhibitor
Amorfrutin A is an NF-κB inhibitor that inhibits TNF-α-induced IκBα degradation, p65 nuclear translocation, and DNA-binding activity of the NF-κB complex. This compound promotes apoptosis in HeLa cells by enhancing the proteolytic activities of caspase-3 and PARP. Its mechanism suggests potential research applications in studying inflammation, cancer biology, and cell death pathways.
