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Catalog No.
Product Name
Application
Product Information
Citations
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HDAC Inhibitor
HDAC-IN-71 is a potent histone deacetylase (HDAC) inhibitor that exhibits IC50 values of 12.6 nM for HDAC1, 14.1 nM for HDAC2, 20 nM for HDAC3, 3 nM for HDAC6, and 72 nM for HDAC10. This compound effectively induces apoptosis, making it a valuable tool in cancer research. Its selective inhibition of multiple HDAC isoforms can aid in elucidating the role of histone modification in tumor progression and therapeutic response. -
HDAC6 Inhibitor
C1A is an inhibitor of class I and II histone deacetylases (HDACs) as well as sirtuins, demonstrating an IC50 of 479 nM specifically for HDAC6. This compound promotes sustained acetylation of HDAC6 substrates, including α-tubulin and HSP90, contributing to its potent anticancer properties. C1A has been shown to effectively induce apoptosis in various cancer cell lines, making it a valuable tool for research in cancer biology and therapeutic development. -
LSD1/HDAC Inhibitor
LSD1/HDAC-IN-2 is a potent inhibitor of lysine-specific demethylase 1 (LSD1) and several histone deacetylases (HDAC1, HDAC2, HDAC3, HDAC6, and HDAC8), with IC50 values ranging from 1.0 to 39.0 nM. This compound demonstrates significant biological activity by inhibiting the proliferation of colorectal cancer cells, inducing apoptosis, and causing G2/M cell cycle arrest. Additionally, LSD1/HDAC-IN-2 reduces cell migration and displays antitumor efficacy in mouse models, making it a valuable tool for cancer research and therapeutic development. -
HDAC Inhibitor
HDAC-IN-42 is a potent and selective inhibitor of histone deacetylases (HDACs), displaying IC50 values of 0.19 µM for HDAC1 and 4.98 µM for HDAC6. This compound demonstrates significant anticancer and anti-proliferative effects, inducing apoptosis and causing cell cycle arrest in the G2/M phase. HDAC-IN-42 is valuable for research applications focused on cancer biology and the modulation of gene expression through epigenetic mechanisms. -
Top/HDAC Dual Inhibitor
Top/HDAC-IN-2 is a dual inhibitor targeting topoisomerase and histone deacetylases (HDACs). This compound demonstrates significant antitumor activity and effectively induces apoptosis in cancer cells. Its ability to concurrently interfere with these critical pathways makes it a valuable tool for researchers investigating cancer therapeutics and cell death mechanisms. -
FLT3/HDAC Inhibitor
HDAC-IN-63 is a dual inhibitor targeting both FLT3 and HDAC, with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1. It demonstrates potent inhibition of MV4-11 cell proliferation, with an IC50 of 92 nM, and effectively induces apoptosis while arresting the cell cycle in MV4-11 cells. This compound serves as a valuable research tool for the study of acute myeloid leukemia (AML) and the exploration of novel therapeutic strategies. -
HDAC4 Inhibitor
HDAC4-IN-1 is a selective inhibitor of histone deacetylase 4 (HDAC4), demonstrating an IC50 of 0.077 μM. This compound has been shown to enhance caspase-mediated apoptosis, highlighting its potential in anticancer applications. HDAC4-IN-1 is a valuable tool for research into drug combinations aimed at increasing the efficacy of cancer therapies. -
HDAC6 Inhibitor
HDAC6-IN-45 is a selective inhibitor of histone deacetylase 6 (HDAC6), demonstrating an IC50 of 15.2 nM. This compound has been shown to promote neurotrophic effects by enhancing the expression of GAP43 and Beta-3 tubulin, while also activating the Nrf2 signaling pathway. Further research applications include its ability to mitigate H2O2-induced reactive oxygen species production, inhibit apoptosis in PC12 cells, and confer neuroprotective effects in SCOP-induced zebrafish models of Alzheimer's disease. Additionally, HDAC6-IN-45 exhibits antioxidant properties and possesses favorable blood-brain barrier permeability. -
Topo II/ HDAC Inhibitor
Topo II/HDAC-IN-2 is a potent dual inhibitor targeting topoisomerase II (Topo II) and histone deacetylases (HDAC). This compound is known to induce apoptosis in various cancer cell lines, making it a valuable tool for investigating the mechanisms of tumorigenesis and potential therapeutic interventions. Research applications include studies on cancer biology, drug development, and the modulation of epigenetic regulators. -
NF-κB p65 Inhibitor, Apoptosis Inducer
N-Desmethyldauricine is an inhibitor of NF-κB p65 with significant apoptotic effects. It effectively reduces p65 protein expression, induces apoptosis, and arrests the cell cycle at the G0/G1 phase. Additionally, N-Desmethyldauricine attenuates intercellular adhesion and inhibits the growth of 3D spheroids derived from triple-negative breast cancer. This compound is useful for research involving triple-negative breast cancer dynamics and therapeutic strategies. -
FLT3/HDAC Inhibitor
FLT3/HDAC-IN-3 is a dual inhibitor targeting FLT3 and HDAC, with a potent inhibitory effect on FLT3 (IC50 = 14 nM) and HDAC isoforms, including HDAC1 (IC50 = 27 nM) and HDAC6 (IC50 = 20 nM). This compound demonstrates selective inhibition, exhibiting reduced activity against HDAC8 and no activity toward HDAC4. FLT3/HDAC-IN-3 has shown anti-proliferative effects across various hematological malignancy cell lines and demonstrates efficacy in the Jeko-1 xenograft model without significant toxicity. It is suitable for research focused on hematological malignancies and the role of dual inhibition in therapeutic strategies. -
HDAC Inhibitor
HDAC-IN-81 is a potent HDAC1 inhibitor, demonstrating an IC50 value of 4.5 nM. This compound exhibits significant anti-cancer activity by effectively inhibiting cell proliferation and inducing apoptosis in cancer cells. It serves as a valuable tool for research applications in cancer biology and epigenetic regulation. -
HDAC Inhibitor
Valproic acid magnesium is an orally active histone deacetylase (HDAC) inhibitor that exhibits an IC50 range of 0.5 to 2 mM, specifically inhibiting HDAC1 with an IC50 of 400 μM while promoting the proteasomal degradation of HDAC2. This compound activates Notch1 signaling and demonstrates anti-proliferative effects in small cell lung cancer (SCLC) cells. Valproic acid magnesium has diverse therapeutic applications, including the treatment of epilepsy, bipolar disorder, metabolic diseases, HIV infection, and the prevention of migraine headaches. -
HDAC Inhibitor
Nanatinostat TFA is a potent, orally active inhibitor of class I histone deacetylases (HDACs), with IC50 values of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. It demonstrates reduced activity against HDAC5 and HDAC6, with IC50 values of 200 nM and 2100 nM, respectively. Nanatinostat TFA effectively induces apoptosis in myeloma cells and exhibits significant anticancer properties against various malignancies, including advanced solid tumors and colorectal cancer. Its selective inhibition of HDACs positions it as a valuable compound for cancer research and therapeutic development. -
PI3K/HDAC Inhibitor
Fimepinostat mesylate is a potent dual inhibitor targeting class I phosphoinositide 3-kinases (PI3Ks) and histone deacetylases (HDACs). It exhibits IC50 values of 19 nM for PI3Kα, 54 nM for PI3Kβ, 39 nM for PI3Kδ, and 1.7 nM for HDAC1, 5.0 nM for HDAC2, 1.8 nM for HDAC3, and 2.8 nM for HDAC10. This compound is valuable for research applications focusing on cancer biology, epigenetic regulation, and cellular signaling pathways. -
HDAC Inhibitor
MC2625 is a potent histone deacetylase (HDAC) inhibitor, specifically targeting HDAC3 and HDAC6 with IC50 values of 80 nM and 11 nM, respectively. This compound effectively increases levels of acetylated histone H3 and acetylated tubulin, promoting apoptosis in cancer stem cells (CSCs) and inhibiting their growth. MC2625 serves as a valuable tool for research focused on cancer therapeutics and the role of epigenetics in tumor biology. -
HDAC Inhibitor, Topoisomerase I Inhibitor
WJ35435 is a dual-target HDAC and topoisomerase I inhibitor that exerts anticancer activity by inducing DNA damage and promoting cell cycle arrest at the G1 and G2 phases, ultimately leading to apoptosis. This compound enhances histone H3 acetylation and phosphorylation, along with α-tubulin acetylation and the formation of γ-H2AX, thereby effectively demonstrating its anti-HDAC properties. WJ35435 holds potential for advancing research in cancer therapeutics. -
NF-κB Inhibitor
15-Deoxy-Δ12,14-prostaglandin A1 is a potent inhibitor of NF-κB signaling, functioning through the modulation of inflammatory pathways. It has been shown to induce apoptosis and effectively inhibit TNF-α-induced upregulation of adhesion molecules on endothelial cells, thereby preventing monocyte arrest. This compound is valuable for research in inflammation, cardiovascular diseases, and apoptosis studies. -
HDAC Inhibitor
HDAC-IN-46 is a potent inhibitor of histone deacetylases (HDACs), demonstrating IC50 values of 0.21 μM for HDAC1 and 0.021 μM for HDAC6. In MDA-MB-231 cells, HDAC-IN-46 promotes the upregulation of phosphorylated p38 while downregulating Bcl-xL and cyclin D1, leading to significant G2 phase cell cycle arrest and apoptosis. This compound is valuable for research focused on triple-negative breast cancer (TNBC). -
NF-κB Inhibitor
Declopramide is a potent NF-κB inhibitor that exerts antitumor effects by inducing apoptosis in cancer cells. It has demonstrated efficacy in inhibiting the proliferation of HL60 and K562 cell lines, as well as reducing tumor growth in a mouse model of human brain astrocytoma (T24). Additionally, Declopramide functions as a chemosensitizer, making it a valuable tool for investigating therapeutic strategies in cancer research. -
HDAC Inhibitor
HDAC-IN-57 is a potent orally active inhibitor of histone deacetylases (HDACs), exhibiting IC50 values of 2.07 nM for HDAC1, 4.71 nM for HDAC2, 2.4 nM for HDAC6, and 107 nM for HDAC8. In addition, HDAC-IN-57 inhibits lysine-specific demethylase 1 (LSD1) with an IC50 of 1.34 µM. This compound induces apoptosis and demonstrates significant anti-tumor activity, making it a valuable tool for cancer research and therapeutic development targeting epigenetic regulation. -
TLR4/NF-κB Inhibitor
TLR4/NF-κB-IN-1 is a selective inhibitor of the TLR4/NF-κB signaling pathway, demonstrating significant anti-inflammatory properties. This compound exhibits the ability to penetrate the blood-brain barrier, making it suitable for studies involving neuroinflammation. In murine models, TLR4/NF-κB-IN-1 effectively reduces acute neuroinflammation induced by lipopolysaccharides (LPS) while downregulating the expression of TLR4, phosphorylated NF-κB, and phosphorylated IκB-α proteins, providing a valuable tool for researching neuroinflammatory processes and their therapeutic modulation. -
TLR4/MyD88/NF-κB Inhibitor
SjDX5-271 is a small peptide inhibitor targeting the TLR4/MyD88/NF-κB signaling pathway. It is known to induce cell polarization and mitigate hepatic inflammation, demonstrating protective effects against liver ischemia-reperfusion injury in mouse models. This compound is valuable for research in immunology and liver-related inflammation studies. -
TLR7/TLR9 Inhibitor
ODN 24888 is a guanine-modified inhibitory oligonucleotide (INH-ODN) that specifically targets TLR7 and TLR9 signaling pathways. It effectively inhibits interferon-alpha (IFN-α) secretion and NF-κB activation, while also reducing interleukin-6 (IL-6) release. ODN 24888 is valuable for studying immune and inflammatory responses and can be utilized as a vaccine adjuvant in various research applications. -
TLR Inhibitor
TIC10g is a dual inhibitor of toll-like receptors 7 and 9 (TLR7 and TLR9). It effectively decreases TNF-α release in mouse macrophages and human B lymphocytes, with IC50 values of 14.5 μM and 6.5 μM for TLR7, and 7.69 μM and 11.5 μM for TLR9, respectively. TIC10g also inhibits the activation of NF-κB and MAPK pathways, demonstrating potential as an anti-inflammatory agent in conditions such as systemic lupus erythematosus and rheumatoid arthritis. -
TLR4 Signaling Inhibitor
NCI126224 is a TLR4 signaling inhibitor that modulates immune responses by suppressing lipopolysaccharide (LPS)-induced production of key inflammatory mediators, including NF-κB, TNF-α, IL-1β, and nitric oxide. This compound demonstrates biological activity in the low nanomolar to low micromolar range, making it a valuable tool for research into inflammatory diseases and their mechanisms. Its ability to interfere with TLR4 signaling pathways positions NCI126224 as a significant reagent for exploring potential therapeutic strategies in inflammation-related studies. -
TLR4/NF-kB/MAPK Inhibitor
TLR4/NF-κB/MAPK-IN-1 is an inhibitor targeting the TLR4/NF-κB/MAPK signaling pathways. It exhibits significant anti-neuroinflammatory activity by suppressing the activation of these pathways, leading to reduced inflammatory responses. This compound is particularly useful for research applications focusing on neuroinflammation and related neurodegenerative diseases. -
TLR4/NF-κB Inhibitor
Ligusticum cycloprolactam is a potent TLR4/NF-κB inhibitor with significant anti-inflammatory properties. It has been shown to alleviate renal injury by effectively disrupting the TLR4/NF-κB signaling pathway in both in vivo and in vitro models. In studies, Ligusticum cycloprolactam reduces serum uric acid levels, diminishes tubular damage, and decreases inflammatory infiltration and interstitial collagen deposition, leading to improved renal function. This compound serves as a valuable reagent for research into hyperuricemic nephropathy. -
NF-κB Inhibitor
NF-κB-IN-14 is an NF-κB inhibitor that effectively modulates inflammatory responses by significantly inhibiting nitric oxide production in LPS-stimulated macrophages, with an IC50 of 6.4 μM. This compound disrupts the TLR4-MyD88 protein interaction, leading to the suppression of the NF-κB signaling pathway. Additionally, NF-κB-IN-14 has demonstrated efficacy in reducing ear edema and inflammation in a mouse model of atopic dermatitis, highlighting its potential utility in inflammatory research. -
MyD88 Inhibitor
LM9 is a selective inhibitor of MyD88, a key adaptor protein in the Toll-like receptor (TLR) signaling pathway. By blocking the binding of TLR4 to MyD88, LM9 disrupts MyD88 homodimer formation and subsequent activation of the NF-κB signaling pathway. This compound demonstrates significant anti-inflammatory effects, mitigating atherosclerosis and fibrosis in models of obesity-induced cardiomyopathy. LM9 is valuable for research focused on understanding the mechanisms of inflammation, fibrosis, and cardiovascular diseases. -
TLR4/JNK/NF-κB Inhibitor
TLR4-IN-2 is an inhibitor targeting TLR4, JNK, and NF-κB pathways. It demonstrates anti-inflammatory properties by reducing nitric oxide production in LPS-stimulated RAW264.7 cells, with an IC50 of 23.2 µM. By inhibiting TLR4 expression and diminishing JNK phosphorylation, TLR4-IN-2 effectively suppresses NF-κB activation and the transcription of inflammation-related genes, leading to lower levels of iNOS, COX-2, and various inflammatory mediators. This compound shows potential for investigating therapeutic strategies in inflammatory diseases such as rheumatoid arthritis and other inflammatory disorders. -
NF-κB Inhibitor
Ergolide is a selective NF-κB/p65 and NLRP3 inhibitor that effectively disrupts the NF-κB signaling pathway and inhibits the nuclear translocation of p65. By irreversibly binding to the NACHT domain of NLRP3, Ergolie suppresses inflammasome assembly, significantly reducing the production of inflammatory mediators such as NO and PGE2. This compound promotes apoptosis in cancer cells, induces autophagy, and generates reactive oxygen species (ROS). Ergolide also enhances the therapeutic efficacy of vincristine and has been shown to alleviate acute lung injury in models of sepsis and inflammation, contributing to research in metastatic uveal melanoma, neurodegenerative diseases, and acute lymphoblastic leukemia. -
HDAC inhibitor
Droxinostat is a selective inhibitor of HDAC3, HDAC6, and HDAC8 that shows comparable inhibition of HDAC6 and HDAC8 with IC50 = 2.47 and 1.46 μmol/L, respectively. - Parthenolide ((-)-Parthenolide) is a sesquiterpene lactone which occurs naturally in the plant feverfew (Tanacetum parthenium).
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HDAC Inhibitor
Pyroxamide (NSC 696085) is a potent inhibitor of affinity-purified HDAC1 and causes the accumulation of acetylated core histones in MEL cells cultured with the agent. -
HDAC inhibitor
Sodium butyrate (NaB, Butanoic acid sodium salt), sodium salt of butyric acid, is a histone deacetylase inhibitor and competitively binds to the zinc sites of class I and II histone deacetylases (HDACs). -
HDAC inhibitor
Valproic acid sodium salt (Sodium Valproate) is an HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM, also inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. -
IKK2/IKK complex/IKK1 inhibitor
IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. -
HDAC inhibitor
Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM. -
HDAC inhibitor
Belinostat (PXD101; PX105684) is a potent HDAC inhibitor with an IC50 of 27 nM in HeLa cell extracts. -
NF-κB inhibitor
Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B is also a regulator of skeletal muscle mass. -
HDAC6 inhibitor
Tubastatin A is a potent HDAC6 inhibitor with an IC50 value of 15 nM. -
pan-HDAC inhibitor
Quisinostat dihydrochloride (JNJ-26481585 dihydrochloride) is an orally available, potent pan-HDAC inhibitor with IC50s of 0.11 nM, 0.33 nM, 0.64 nM, 0.46 nM, and 0.37 nM for HDAC1, HDAC2, HDAC4, HDAC10 and HDAC11, respectively. Quisinostat dihydrochloride has a broad spectrum antitumoral activity. -
NF-κB inhibitor
Cyclo(his-pro) (Cyclo(histidyl-proline)) is an orally active cyclic dipeptide structurally related to tyreotropin-releasing hormone. Cyclo(his-pro) could inhibit NF-κB nuclear accumulation.
