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PDE4 Inhibitor
PDE4-IN-15 is a selective inhibitor of phosphodiesterase 4 (PDE4) with an IC50 value of 0.17 μM. This compound demonstrates notable anti-TNF-α activity, exhibiting an EC50 of 0.19 μM, which is significant for inflammatory research. Additionally, PDE4-IN-15 shows good skin permeability, making it suitable for studies involving topical administration and localized therapeutic applications. -
PDE Inhibitor
Theophylline sodium glycinate is a potent phosphodiesterase (PDE) inhibitor with significant effects on airway smooth muscle relaxation. It acts primarily by inhibiting PDE3, which contributes to its anti-inflammatory properties through the upregulation of IL-10 and the inhibition of NF-κB translocation into the nucleus. Additionally, Theophylline sodium glycinate has been shown to induce apoptosis. This reagent is valuable for research applications related to asthma and chronic obstructive pulmonary disease (COPD). -
PDE-4 Inhibitor
Apremilast-d5 is a deuterated analog of Apremilast, a potent inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. This compound effectively reduces TNF-α release in response to lipopolysaccharide (LPS) stimulation, exhibiting an IC50 of 104 nM. Apremilast-d5 is valuable for research applications related to inflammatory diseases and the modulation of immune responses. -
Phosphodiesterase (PDE) Inhibitor
CDC801 is a potent inhibitor of phosphodiesterase 4 (PDE4) and tumor necrosis factor-α (TNF-α), with IC50 values of 1.1 μM and 2.5 μM, respectively. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into conditions associated with elevated TNF-α levels, such as autoimmune diseases and chronic inflammatory disorders. CDC801 is suitable for exploring the therapeutic potential of PDE4 inhibition and its effects on inflammatory pathways. -
PDE Inhibitor
Theophylline monohydrate is a potent phosphodiesterase (PDE) inhibitor that primarily targets PDE3, promoting relaxation of airway smooth muscle. This compound exhibits anti-inflammatory properties by increasing interleukin-10 (IL-10) levels and inhibiting the nuclear translocation of NF-κB. Additionally, Theophylline monohydrate is known to induce apoptosis in certain cell types. It is widely utilized in research related to asthma and chronic obstructive pulmonary disease (COPD). -
Chloride Channel Inhibitor
Shikonin is a potent inhibitor of the TMEM16A chloride channel, exhibiting an IC50 value of 6.5 μM. This compound functions as a specific inhibitor of pyruvate kinase M2 (PKM2) and also modulates inflammatory pathways by inhibiting TNF-α and NF-κB activation. In addition, Shikonin decreases exosome secretion by impairing glycolytic processes and effectively inhibits AIM2 inflammasome activation. Its diverse activities make it a valuable reagent for investigating cellular signaling and inflammatory responses in research applications. -
MAO-A/B Inhibitor
1,4-Naphthoquinone serves as a potent inhibitor targeting monoamine oxidase A and B (MAO-A/B) with competitive inhibition of MAO-B (Ki=1.4 μM) and non-competitive inhibition of MAO-A (Ki=7.7 μM). This compound exhibits broad-spectrum biological activity, inhibiting various DNA polymerases alongside notable anti-tumor, anti-inflammatory, and antibacterial properties. Its mechanism includes the induction of oxidative stress, glutathione (GSH) depletion, suppression of DNA synthesis, and blockage of NF-κB nuclear translocation. 1,4-Naphthoquinone is applicable in research involving melanoma and colon cancer cell growth, endothelial cell function, and models of lipopolysaccharide (LPS)-induced inflammation. -
HDAC/NAMPT Inhibitor
HDAC/NAMPT-IN-1 is a potent dual inhibitor of histone deacetylases (HDAC) and nicotinamide adenine dinucleotide (NAD+) biosynthesis enzyme NAMPT, exhibiting IC50 values ranging from 0.72 to 37081 nM for HDAC and 1618 nM for NAMPT. This compound demonstrates significant potential in modulating cellular acetylation levels and metabolic processes associated with cancer and neurodegenerative diseases. Its application in research can facilitate studies on epigenetic regulation and NAD+ metabolism, contributing to a deeper understanding of cellular mechanisms and therapeutic strategies. -
CYP51/HDAC Inhibitor
CYP51/HDAC-IN-1 is a potent dual inhibitor of CYP51 and HDAC, demonstrating significant biological activity in combating virulence factors as well as down-regulating resistance-associated genes. This compound shows promising therapeutic potential for treating tropical candidiasis and cryptococcal meningitis, making it a valuable tool for research in antifungal therapies. -
HDAC1/MAO-B Inhibitor
HDAC1/MAO-B-IN-1 is a selective inhibitor targeting both HDAC1 and MAO-B, exhibiting IC50 values of 21.4 nM and 99.0 nM, respectively. This compound effectively crosses the blood-brain barrier, making it a valuable tool for studying neurological disorders. Its potential applications include research into Alzheimer's disease and related pathologies, facilitating the exploration of epigenetic modifications and monoamine metabolism in the brain. -
Dual HDAC/HSP90 Inhibitor
HDAC/HSP90-IN-1 is a potent dual inhibitor targeting both histone deacetylases (HDAC) with an IC50 of 194 nM and heat shock protein 90 (HSP90), specifically HSP90α with an IC50 of 153 nM. This compound induces the expression of HSP70, downregulates HSP90 client proteins, and facilitates the acetylation of α-tubulin and histone H3 in cancer cells. Additionally, HDAC/HSP90-IN-1 effectively reduces PD-L1 expression in interferon-gamma treated H1975 cells, making it a valuable tool for cancer research, particularly in lung and colon malignancies. -
sEH/HDAC6 inhibitor
sEH/HDAC6-IN-1 is a selective, orally active dual inhibitor of soluble epoxide hydrolase (sEH) and histone deacetylase 6 (HDAC6), exhibiting IC50 values of 2 nM for human sEH, 0.72 nM for murine sEH, and 5 nM for HDAC6. This compound demonstrates notable analgesic and anti-inflammatory properties, making it a valuable tool for research into pain management and inflammatory disorders. The ability to simultaneously target these two enzymes provides insights into their roles in various biological processes. -
sEH/HDAC6 Inhibitor
sEH/HDAC6-IN-2 is a potent dual inhibitor targeting soluble epoxide hydrolase (sEH) and histone deacetylase 6 (HDAC6), demonstrating IC50 values of 0.9 nM for human sEH, 46.8 nM for mouse sEH, and 8 nM for HDAC6. This compound is significant for investigating inflammatory pain mechanisms and related biological pathways, potentially aiding in the development of novel analgesics. Its dual activity positions it as a valuable tool in research focused on neuroinflammation and pain management. -
HDAC/PDE5 Inhibitor
CM-414 is a potent dual inhibitor of phosphodiesterase 5 (PDE5) and histone deacetylases (HDACs), exhibiting IC50 values of 60 nM for PDE5 and ranging from 91 nM to 490 nM for various HDAC isoforms, including HDAC6 and HDAC1. This compound effectively reduces levels of amyloid-beta (Aβ) and phosphorylated tau (pTau) in Tg2576 mouse models, making it a valuable tool for Alzheimer's disease research. Its ability to penetrate the blood-brain barrier enhances its potential for studying neurodegenerative disorders and therapeutic interventions. -
Dual HDAC/HSP90 Inhibitor
HDAC/HSP90-IN-2 is a dual inhibitor of histone deacetylases (HDAC) and heat shock protein 90 (HSP90), exhibiting an IC50 of 360 nM for HDAC and 77 nM for HSP90α. This compound effectively induces HSP70 expression, downregulates client proteins associated with HSP90, and enhances the acetylation of α-tubulin and histone H3 in cancer cells. Additionally, HDAC/HSP90-IN-2 reduces PD-L1 expression in H1975 cells treated with IFN-γ. Its applications are particularly relevant in cancer research, including studies focused on lung and colon cancer. -
HDAC/Hsp90 Inhibitor
HDAC/HSP90-IN-3 is a potent dual inhibitor targeting fungal Hsp90 and histone deacetylases (HDAC) with IC50 values of 0.83 μM and 0.91 μM, respectively. This compound demonstrates significant antifungal activity against azole-resistant Candida albicans. Additionally, HDAC/HSP90-IN-3 effectively suppresses key virulence factors and down-regulates drug-resistant genes such as ERG11 and CDR1, making it valuable for research in antifungal resistance and pathogenicity. -
HDAC6/HSP90 Inhibitor
HDAC6/HSP90-IN-1 is a potent dual inhibitor targeting both HDAC6 and HSP90, demonstrating IC50 values of 4.3 nM and 46.8 nM, respectively. This compound effectively down-regulates PD-L1 expression in INF-γ treated H1975 lung cancer cells, contributing to its potential in cancer therapy. Additionally, HDAC6/HSP90-IN-1 has shown promising efficacy in inhibiting tumor growth in human H1975 xenograft mice models, making it a valuable tool for cancer research. -
HDAC/PDE5 Inhibitor
CM-545 is a dual inhibitor targeting both histone deacetylases (HDACs) and phosphodiesterase 5 (PDE5). With pIC50 values of 7.47 for PDE5, 6.65 for HDAC1, 6.14 for HDAC2, 6.55 for HDAC3, and 6.84 for HDAC6, CM-545 demonstrates potent inhibitory activity. This compound has applications in cancer research and therapeutic interventions related to neurodegenerative diseases and cardiovascular conditions, owing to its modulation of histone acetylation and cyclic nucleotide signaling pathways. -
IDO Inhibitor
IDO1 and HDAC1 Inhibitor (Compound 10) is a dual-target inhibitor that effectively inhibits indoleamine 2,3-dioxygenase 1 (IDO1) and histone deacetylase 1 (HDAC1) with IC50 values of 69.0 nM and 66.5 nM, respectively. This compound demonstrates significant biological activity in modulating immune responses and epigenetic regulation. It is suitable for use in cancer research, immunotherapy studies, and investigations into the mechanistic roles of IDO1 and HDAC1 in various biological processes. -
MAO A/HDAC Inhibitor
MAO A/HDAC-IN-1 is a dual inhibitor targeting monoamine oxidase A (MAO A) and histone deacetylases (HDAC). This compound exhibits significant biological activity in glioma research, facilitating studies on tumor biology and epigenetic modifications. Additionally, MAO A/HDAC-IN-1 features an alkyne group that enables copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a valuable tool for click chemistry applications in investigating cellular processes. -
Hsp90 Inhibitor
PU24FCl is a selective inhibitor of the heat shock protein 90 (Hsp90). This compound demonstrates significant anti-cancer activity, promoting tumor regression by disrupting chaperone activity critical for the stability and function of multiple oncogenic clients. Notably, PU24FCl selectively accumulates in tumor tissues while being rapidly eliminated from normal tissues, enhancing its therapeutic potential in cancer research applications. -
MAO-B Inhibitor
Desmethoxyyangonin is a selective inhibitor of monoamine oxidase B (MAO-B), with an IC50 value of 0.123 µM. This kavalactone, derived from the Piper methysticum plant, exhibits notable anti-inflammatory properties through the inhibition of Jak2/STAT3 and IKK signaling pathways. Additionally, Desmethoxyyangonin plays a role in inducing CYP3A23 expression and contributes to skeletal muscle relaxation, making it a valuable tool for research in neuropharmacology and inflammation. -
PDE IV Inhibitor/A1AR Antagonist
Doxofylline is an orally active phosphodiesterase IV (PDE IV) inhibitor and adenosine A1 receptor (A1AR) antagonist. It exhibits anti-inflammatory properties by reducing mitochondrial reactive oxygen species (ROS) production and modulating various cellular pathways, including the NLRP3-TXNIP inflammasome activation. This compound is valuable for research related to respiratory diseases such as asthma, chronic obstructive pulmonary disease (COPD), and bronchospasm. -
PDE Inhibitor
Flavoxate hydrochloride is a competitive inhibitor of phosphodiesterase (PDE), providing significant antispasmodic effects through its action as a muscarinic acetylcholine receptor (mAChR) antagonist. In addition to its PDE inhibition, it exhibits moderate calcium antagonistic properties and local anesthetic effects. Flavoxate hydrochloride is utilized in research focused on overactive bladder (OAB) and related lower urinary tract infections, contributing to a better understanding of these conditions and potential therapeutic approaches. -
PDE5 Inhibitor
Vardenafil hydrochloride trihydrate is a selective and orally active phosphodiesterase-5 (PDE5) inhibitor, exhibiting an IC50 of 0.7 nM. It also demonstrates inhibitory effects on PDE1 and PDE6 with IC50 values of 180 nM and 11 nM, respectively, while showing minimal activity against PDE3 and PDE4 (IC50s >1000 nM). By competitively inhibiting the hydrolysis of cyclic guanosine monophosphate (cGMP), Vardenafil hydrochloride trihydrate elevates cGMP levels. This compound is primarily utilized in research related to erectile dysfunction as well as conditions such as hepatitis and diabetes. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride hydrochloride is a non-steroidal anti-inflammatory agent and an antagonist of the H1-histamine receptor. It selectively inhibits phosphodiesterase activities, including PDE3, PDE4, and PDE5, with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. This compound is valuable for research applications focused on respiratory diseases, highlighting its potential in therapeutic investigations and the modulation of inflammatory responses. -
Carbonic Anhydrase Inhibitor
Fluorometholone acetate is a synthetic glucocorticoid corticosteroid that functions as a potent inhibitor of carbonic anhydrase (CA). It displays inhibition with IC50 values of 2.18 μM for human carbonic anhydrase I (hCA-I) and 17.5 μM for human carbonic anhydrase II (hCA-II). This compound exhibits significant anti-inflammatory properties, making it valuable for research in external ocular inflammation and related therapeutic applications. -
PDE Inhibitor
Pentoxifylline is a non-selective phosphodiesterase (PDE) inhibitor with significant haemorheological properties. It exhibits immune modulation, anti-inflammatory, anti-fibrinolytic, and anti-proliferative activities, making it a valuable tool in biomedical research. Pentoxifylline is particularly applicable in studies of peripheral vascular disease, cerebrovascular disease, and other conditions associated with impaired regional microcirculation. -
HMG-CoA Reductase (HMGCR) Inhibitor
Pravastatin is a competitive inhibitor of HMG-CoA reductase (HMGCR), playing a critical role in the regulation of cholesterol biosynthesis. With an IC50 value of 5.6 μM, it effectively reduces cholesterol levels and is commonly utilized in cardiovascular research. This compound is valuable for studies investigating lipid metabolism and the pharmacological modulation of cholesterol levels in various biological systems. -
PDE5 Inhibitor
Vardenafil hydrochloride is a selective phosphodiesterase-5 (PDE5) inhibitor, exhibiting an IC50 of 0.7 nM. This compound demonstrates moderate inhibition of PDE1 and PDE6, with IC50 values of 180 nM and 11 nM, respectively, while showing minimal activity against PDE3 and PDE4. By competitively inhibiting the hydrolysis of cyclic guanosine monophosphate (cGMP), Vardenafil hydrochloride effectively elevates cGMP levels. It serves as a valuable tool in research related to erectile dysfunction, hepatitis, and diabetes. -
CYP3A4 Inhibitor
Escholtzine perchlorate is a potent CYP3A4 inhibitor derived from the alkaloid Eschscholzia californica. This compound demonstrates significant biological activity, with an IC50 value for CYP3A4 of 13.4 μM and an EC50 value for the 5-HT1A receptor of 11 μM. Escholtzine perchlorate is primarily utilized in research focused on anxiety and depression, offering valuable insights into pharmacological mechanisms related to these conditions. -
5-HT6R/MAO-B Inhibitor
5-HT6R/MAO-B modulator 1 is a selective antagonist of the 5-HT6 receptor with Gs signaling activity and serves as an irreversible inhibitor of monoamine oxidase B (MAO-B). This compound demonstrates glioprotective effects and has the capability to reverse memory deficits induced by scopolamine. Additionally, it features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions, making it a versatile tool for chemical biology applications. -
Hsp90 Inhibitor
Conglobatin is a macrolide dilactone that functions as an Hsp90 inhibitor. It selectively binds to the N-terminal domain of Hsp90, effectively disrupting the Hsp90-Cdc37 complex formation. This compound demonstrates significant apoptotic activity in human breast cancer cells and esophageal squamous cell carcinoma cells, and it exhibits notable antitumor efficacy in vivo, making it a potential candidate for cancer research applications. -
Enpp/Carbonic Anhydrase Inhibitor
Enpp/Carbonic anhydrase-IN-2 is a potent inhibitor of ecto-nucleotide pyrophosphatase/phosphodiesterase (Enpp) and carbonic anhydrases, exhibiting IC50 values of 1.13 µM for NPP1, 1.07 µM for NPP2, 0.74 µM for NPP3, 0.33 µM for CA-IX, and 0.68 µM for CA-XII. This compound demonstrates significant antiproliferative effects on cancer cells while maintaining low cytotoxicity toward normal cell lines. Additionally, Enpp/Carbonic anhydrase-IN-2 has been shown to induce apoptosis, making it a valuable tool for cancer biology research and therapeutic development. -
Sulfonylurea Herbicide, Photosynthetic System Inhibitor, Acetolactate Synthase (ALS) Inhibitor, Branched-chain Amino Acids (BCAAs) Inhibitor
Nicosulfuron is a selective sulfonylurea herbicide that acts as an inhibitor of acetolactate synthase (ALS) within the photosynthetic system. It effectively disrupts the synthesis of branched-chain amino acids (BCAAs), which is beneficial for maize cultivation by enhancing adaptability through glycolysis and the tricarboxylic acid cycle. Additionally, Nicosulfuron demonstrates antifungal properties and its degradation is dependent on glucose concentration when interacting with Plectosphaerella cucumerina AR1 in a planktonic environment. This compound is widely used in agricultural research for studying herbicide efficacy and metabolic pathways. -
FAAH/MAGL Inhibitor
1-Monomyristin serves as a dual inhibitor of fatty acid amide hydrolase (FAAH) and monoacylglycerol lipase (MAGL), with IC50 values of 18 μM and 32 μM, respectively. It effectively inhibits the hydrolysis of 2-oleoylglycerol via MAGL, exhibiting antibacterial and antifungal activities against pathogens such as Staphylococcus aureus, Aggregatibacter actinomycetemcomitans, and Candida albicans. Additionally, 1-Monomyristin demonstrates lethality to brine shrimp and shows marginal cytotoxicity against prostate cancer cells. This reagent is suitable for research focused on bacterial and fungal infections, as well as various cancer types, including renal cancer, prostate adenocarcinoma, and pancreatic cancer. -
Fungal CYP51 Inhibitor
VT-1598 is an orally active and selective inhibitor of fungal cytochrome P450 51 (CYP51). It exhibits potent antifungal activity against Candida auris, making it a valuable tool for research into fungal infections. Additionally, VT-1598 contains an alkyne group, allowing it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) for click chemistry applications, facilitating the study of various biological interactions. -
Bacterial Inhibitor
5,6-Dihydroxyindole is a bacterial inhibitor known for its broad-spectrum antibacterial, antifungal, antiviral, and antiparasitic activities. As a precursor in melanin synthesis, it exhibits cytotoxic properties, demonstrating significant toxicity against a variety of pathogenic organisms. This compound is valuable for research applications focused on antimicrobial resistance and the development of novel therapeutic agents. -
MAO Inhibitor
Phenelzine sulfate is an irreversible, orally active monoamine oxidase (MAO-A and MAO-B) inhibitor, primarily utilized as an antidepressant agent. It enhances levels of neurotransmitters, including serotonin, norepinephrine, and dopamine, while inhibiting GABA transaminase and primary amine oxidase, and sequestering reactive aldehydes. Additionally, Phenelzine sulfate suppresses oxidative stress and lipogenesis and inhibits LSD1 (Ki: 5.6 μM). Its applications extend across research into neurological, metabolic, and oncological diseases, particularly in the context of depression, anxiety disorders, stroke, spinal cord injury, traumatic brain injury, multiple sclerosis, Parkinson's disease, Alzheimer's disease, inflammatory pain, obesity, and prostate cancer. -
EGFR/HER2/DHFR Inhibitor
EGFR/HER2/DHFR-IN-1 is a selective inhibitor targeting the epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and dihydrofolate reductase (DHFR). This compound demonstrates potent antitumor efficacy, with IC50 values of 0.153 μM for EGFR, 0.108 μM for HER2, and 0.291 μM for DHFR. EGFR/HER2/DHFR-IN-1 effectively arrests the cell cycle at the G1/S phase and promotes apoptosis in MCF-7 breast cancer cells, making it a valuable reagent for cancer research and therapeutic development. -
DHFR Inhibitor
DHFR-IN-4 is a potent inhibitor of dihydrofolate reductase (DHFR) with an IC50 value of 123 nM. In addition to its primary activity, DHFR-IN-4 exhibits inhibitory effects on epidermal growth factor receptor (EGFR) and HER2, with IC50 values of 246 nM and 357 nM, respectively. This compound demonstrates significant cytotoxic potency across a broad spectrum of cancer cell lines, making it a valuable tool for cancer research and drug development. -
HSP90/EGFR Inhibitor
Wighteone, a prenylated isoflavone, acts as an HSP90 and EGFR inhibitor, specifically targeting the EGFR L858R/T790M mutations. This compound effectively reduces HSP90 expression, inhibits EGF-induced phosphorylation of EGFR, and disrupts downstream signaling through ERK and AKT pathways. Wighteone demonstrates significant biological activity by inducing cell cycle redistribution, inhibiting proliferation, and triggering apoptosis in various cancer cell lines. It is relevant for research on HER2-positive breast cancer, leukemia, non-small cell lung cancer with specific mutations, and also displays antifungal properties. -
PPAR Inhibitor
AZ0108 is a selective inhibitor of poly(ADP-ribose) polymerases (PARPs), including PARP1, PARP2, PARP3, PARP6, TNKS1, and TNKS2. It displays potent inhibitory activity with IC50 values of <0.03 μM for PARP1 and PARP2, and exhibits significant biological effects such as preventing centrosome clustering with an EC50 of 0.053 μM. Additionally, AZ0108 demonstrates cytotoxicity in OCI-LY-19 cells, with a GI50 value of 0.017 μM, and shows favorable pharmacokinetic properties in rat and mouse models, making it a valuable tool for cellular and molecular biology research focused on DNA repair and cancer therapeutic studies. -
Poly(ADP-ribose) Synthetase Inhibitor
2-Methylquinazolin-4-ol is a potent competitive inhibitor of poly(ADP-ribose) synthetase, exhibiting a Ki value of 1.1 μM. Additionally, it functions as an inhibitor of mammalian aspartate transcarbamylase (ATCase) with an IC50 of 0.20 mM. This compound has significant applications in research focused on cellular stress responses, DNA repair mechanisms, and metabolic regulation. -
PPAR-1 Inhibitor
AZD-9574-acid is a selective PPAR-1 inhibitor that serves as a crucial building block for the development of PROTAC molecules. Its inhibition of PPAR-1 demonstrates significant potential in the regulation of metabolic pathways and inflammatory responses. This compound is essential for researchers exploring targeted protein degradation and its applications in therapeutic development. -
MAO Inhibitor
Tranylcypromine-d5 hydrochloride is a deuterium-labeled derivative of the irreversible, nonselective monoamine oxidase (MAO) inhibitor, Tranylcypromine. It exhibits potent antidepressant activity by inhibiting MAO, thereby increasing levels of neurotransmitters such as serotonin and norepinephrine in the brain. Additionally, this compound has been identified as a lysine-specific demethylase 1 (LSD1) inhibitor, demonstrating efficacy in reducing lesion growth and alleviating generalized hyperalgesia in mouse models of induced endometriosis. It serves as a valuable tool in neurological and pain research applications. -
HSP90/LSD1 Inhibitor
HSP90/LSD1-IN-1 is a dual inhibitor targeting HSP90 and LSD1, effectively disrupting their interaction and function. This compound demonstrates significant antiproliferative activity in prostate cancer cell lines, exhibiting GI50 values of 0.24 μM for PC-3 and 0.30 μM for DU145. It is a valuable tool for research into therapeutic strategies against prostate cancer and the role of chaperone proteins and histone demethylases in tumor biology. -
CYP17A1/HDAC6 Inhibitor
CYP17A1/HDAC6-IN-1 is a dual inhibitor targeting both CYP17A1 and HDAC6, exhibiting IC50 values of 0.284 μM and 0.6015 μM, respectively. This compound demonstrates significant anti-tumor activity, making it a valuable tool for research in cancer biology. Its ability to simultaneously inhibit these targets suggests potential applications in therapeutic strategies against malignancies driven by steroidogenesis and histone deacetylation. -
LSD1/HDAC6/MAO-A Inhibitor
LSD1/HDAC6-IN-2 is a potent inhibitor targeting LSD1, HDAC6, and MAO-A, with IC50 values of 5 nM, 11 nM, and 5 nM, respectively. It demonstrates significant inhibitory effects on the growth of multiple myeloma cell lines, including MM.1S, MM.1R, and RPMI-8226. This compound is suitable for research applications focused on acute myeloid leukemia and lymphoma, providing insights into potential therapeutic mechanisms. -
HDAC11 Inhibitor
TD034 is a selective, reversible, and noncovalent inhibitor of HDAC11, exhibiting an IC50 value of 5.1 nM and a Ki of 1.5 nM. This compound specifically targets HDAC11 without affecting other histone deacetylases or sirtuins, and it inhibits the defatty acylation of the substrate SHMT2. Additionally, TD034 reduces the levels of YAP1 through its action on HDAC11. This reagent is suitable for investigating the role of HDAC11 in lung cancer research.

