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Catalog No.
Product Name
Application
Product Information
Citations
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PD-L1/HDAC Inhibitor
PD-L1/HDAC-IN-1 is a dual inhibitor targeting PD-L1, HDAC2, and HDAC3, with IC50 values of 88.10 nM, 27.98 nM, and 14.47 nM, respectively. This compound effectively disrupts the PD-1/PD-L1 interaction and demonstrates minimal cytotoxicity in MCF-7 cells (IC50=19.34 μM). PD-L1/HDAC-IN-1 enhances the expression of PD-L1 and CXCL10, thereby facilitating an anti-tumor immune response through increased T-cell recruitment into the tumor microenvironment (TME). Its unique mechanism positions it as a valuable tool for research in cancer immunotherapy. -
COX-2/HDAC Inhibitor
Andrographidine E is an inhibitor of cyclooxygenase-2 (COX-2) and histone deacetylases (HDAC), with an IC50 of 19 μM for COX-2 and a strong affinity for HDAC1 and HDAC3. This compound selectively binds to macrophages, suggesting its potential as an immunotargeting agent. Andrographidine E is valuable for research applications focused on inflammation and immune modulation. -
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. -
PD-1/PD-L1 Interaction Inhibitor
PD-1/PD-L1-IN 3 is a macrocyclic peptide that acts as a selective inhibitor of the PD-1/PD-L1 and CD80/PD-L1 interactions. By binding to PD-L1, it effectively disrupts the binding of PD-L1 to PD-1 and CD80, exhibiting IC50 values of 5.60 nM and 7.04 nM, respectively. This compound is valuable for research in various fields, particularly in cancer immunotherapy and the study of infectious diseases. -
COX-1/cAMP Phosphodiesterase Inhibitor
Triflusal is a dual inhibitor of Cyclooxygenase-1 (COX-1) and cAMP phosphodiesterase, which penetrates the blood-brain barrier. It effectively inhibits platelet aggregation, nuclear factor kappa B (NF-κB) activation, inducible nitric oxide synthase (iNOS) activity, and prostaglandin synthesis in ischemic tissues. Additionally, Triflusal enhances neutrophil nitric oxide production, endothelial nitric oxide synthase (eNOS) expression, and constitutive nitric oxide synthase (cNOS) activity. This compound is valuable for investigating thromboembolic and ischemic diseases of the cardiovascular and cerebrovascular systems, as well as Alzheimer's disease pathology. -
nNOS Inhibitor
NXN-188 is a selective nNOS inhibitor that also acts as an agonist for the 5HT-1B/1D receptors. This compound exhibits potential in modulating neurogenic inflammation and is particularly relevant in research focused on migraine pathophysiology and treatment strategies. Its dual action supports investigations into the intricate mechanisms underlying headache disorders. -
COX Inhibitor
Pentagamavunon-1 (PGV-1) is a COX-2 inhibitor that modulates multiple molecular pathways to induce apoptosis. This Curcumin analog exhibits notable oral bioactivity and suppresses key angiogenic factors, including vascular endothelial growth factor (VEGF). Additionally, PGV-1 inhibits NF-κB activation, highlighting its potential in cancer research and therapeutic applications targeting inflammation and tumor progression. -
CD47-SIRPα axis Inhibitor
DMUP is a potent inhibitor of the CD47-SIRPα axis. This compound promotes apoptosis and enhances macrophage phagocytosis in A549 lung cancer cells, while also reducing the expression of CD47 and SIRPα proteins. DMUP demonstrates significant antitumor activity, making it a valuable tool for research in cancer immunotherapy and macrophage biology. -
PD-1/PD-L1 Inhibitor
PD-1/PD-L1-IN-10 is a potent orally active inhibitor of the PD-1/PD-L1 interaction, with an IC50 value of 2.7 nM. This compound exhibits significant anticancer efficacy by blocking the immune checkpoint pathway, thereby enhancing T-cell activation and promoting anti-tumor responses. PD-1/PD-L1-IN-10 is valuable for research in immunotherapy and cancer treatment studies. -
EGFR/HER2/CDK9/COX-2 Inhibitor
CDK9-IN-41 is a potent inhibitor of CDK9, EGFR, HER2, and COX-2, exhibiting IC50 values of 192.81 nM, 254.03 nM, 238.81 nM, and 775 nM respectively. This compound demonstrates significant antitumor activity across various cancer cell lines, including leukemia, colon, melanoma, ovarian, and breast cancer. It serves as a valuable tool for exploring the role of these kinases in cancer biology and therapeutic applications. -
SIK Inhibitor
YKL-05-093 is a selective SIK (Salt-Induced Kinase) inhibitor, demonstrating a binding affinity (Kd) of 7.1 nM for SIK2. This compound effectively reduces the phosphorylation levels of HDAC4, HDAC5, and CRTC2, while inhibiting SOST expression and stimulating RANKL expression both in vitro and in vivo. YKL-05-093 is suitable for research applications focusing on bone diseases and related signaling pathways. -
PRMT5 Inhibitor
PRMT5-IN-53 is a potent, orally bioavailable inhibitor of PRMT5, exhibiting pIC50 values of ≥ 9.7 against both human and mouse PRMT5. It demonstrates high affinity for the PRMT5:MEP50 complex with a KD of 11.3 pM. This compound effectively inhibits PRMT5 in the intestines of murine models, leading to a significant reduction in the number and size of polyps while minimizing systemic hematological toxicity. PRMT5-IN-53 is particularly valuable for research in colorectal cancer, especially in the context of familial adenomatous polyposis (FAP). -
Nrf2 Activator/ROS Inhibitor
L-Cystine disodium monohydrate primarily functions as an Nrf2 activator and ROS inhibitor. It elevates Nrf2 protein expression and activates the Nrf2 transcription factor, leading to reduced reactive oxygen species (ROS) generation and protection against apoptosis caused by oxidants and Doxorubicin. Additionally, when combined with L-theanine, it enhances the production of antigen-specific IgG by increasing glutathione levels and promoting T helper 2-mediated responses in mice. This compound is valuable for research into cystinuria and the molecular mechanisms underlying kidney stone formation. -
Nrf2 Inhibitor
Nrf2-IN-4 is a potent Nrf2 inhibitor that induces ferroptosis through the inhibition of the Nrf2 pathway. By disrupting iron homeostasis and facilitating ferritin degradation, Nrf2-IN-4 triggers ferroptotic cell death. Additionally, it promotes lysosome activation by enhancing iron-dependent reactive oxygen species (ROS) production and acidification. Due to its significant antitumor efficacy, Nrf2-IN-4 is a valuable tool for studying breast cancer and exploring therapeutic strategies targeting the Nrf2 pathway. -
Nrf2 Activator/ROS Inhibitor
L-Cystine is an effective Nrf2 activator and reactive oxygen species (ROS) inhibitor. This extracellular form of L-Cysteine elevates Nrf2 protein expression and facilitates its transcriptional activity, thereby reducing ROS generation and providing protection against oxidant- or Doxorubicin-induced apoptosis. Additionally, L-Cystine has been shown to enhance antigen-specific IgG production and T helper 2 mediated responses through increased glutathione levels in murine models. This makes L-Cystine a valuable reagent for research in cystinuria and kidney stone formation. -
Nox2 Inhibitor
gp91 ds-tat is a specific inhibitor of NADPH oxidase 2 (Nox2), effectively blocking the production of superoxide generated by this enzyme. This bioactive peptide has demonstrated the ability to reduce reactive oxygen species (ROS), lipid peroxidation, and iron levels induced by high glucose conditions. Additionally, gp91 ds-tat inhibits homocysteine-induced activation of NLRP3 inflammasomes and restores the activity of lysosomal TRPML1 channels. Research applications include studies on Alzheimer's disease, glomerular inflammation, and cardiovascular disease, with implications for improving cerebrovascular and cognitive functions in APP/PS1 mouse models. -
Endogenous Metabolite; Nrf2 Activator; ROS Inhibitor
L-Cystine hydrochloride is an endogenous metabolite that serves as a potent Nrf2 activator and reactive oxygen species (ROS) inhibitor. It enhances Nrf2 protein expression, facilitating transcriptional responses that combat oxidative stress. Research indicates that L-Cystine hydrochloride reduces ROS generation and protects cells from apoptosis induced by oxidants or Doxorubicin. Additionally, its combination with L-theanine has been shown to boost antigen-specific IgG production by elevating glutathione levels and promoting T helper 2 (Th2) responses. This compound has significant potential for studying cystinuria and kidney stone formation. -
Nucleoside Reverse Transcriptase Inhibitor
Stavudine is an orally active nucleoside reverse transcriptase inhibitor (NRTI) that selectively targets HIV-1 and HIV-2. In addition to its antiviral properties, Stavudine inhibits mitochondrial DNA replication and has been shown to reduce NLRP3 inflammasome activation while modulating Amyloid-β autophagy. Furthermore, Stavudine is associated with the induction of apoptosis, making it a valuable tool for research in HIV treatment and cellular apoptosis mechanisms. -
COX Inhibitor
[8]-Shogaol is a potent inhibitor of cyclooxygenase (COX), specifically targeting COX-2 with an IC50 of 17.5 μM. This compound exhibits significant antiplatelet properties (IC50=5 μM) and demonstrates anti-cancer and anti-inflammatory activities. Additionally, [8]-Shogaol modulates key signaling pathways by inhibiting TAK1, IKK, and Akt, thereby influencing MAPK signaling and alleviating synovitis. Its unique pharmacological profile makes it a valuable reagent for research in cancer, inflammation, and cardiovascular diseases. -
COX Inhibitor
Diclofenac potassium is a potent nonselective inhibitor of cyclooxygenase (COX) enzymes, demonstrating IC50 values of 4 nM for human COX-1 and 1.3 nM for human COX-2 in CHO cells, along with 5.1 μM and 0.84 μM for ovine COX-1 and COX-2, respectively. This reagent exhibits significant anti-inflammatory properties and is particularly effective in inducing apoptosis in neural stem cells through the activation of the caspase cascade. It is widely used in research studies focusing on inflammatory pathways and neural stem cell biology. -
CXCR Inhibitor
Corydalmine, a CXCR inhibitor, demonstrates significant antifungal activity by inhibiting spore germination in various plant pathogenic and saprophytic fungi. Additionally, it serves as an oral analgesic agent, exhibiting potent analgesic effects. Corydalmine has been shown to alleviate Vincristine-induced neuropathic pain in murine models through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, making it a valuable tool for pain research and therapeutic applications. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-3 is a dual inhibitor targeting CYP51 and PD-L1, exhibiting potent antifungal activity with IC50 values of 0.205 μM and 0.039 μM, respectively. This compound induces early apoptosis in fungal cells by reducing levels of intracellular IL-2, NLRP3, and NF-κBp65 proteins. Additionally, CYP51/PD-L1-IN-3 causes mitochondrial damage and reactive oxygen species (ROS) accumulation, ultimately resulting in fungal lysis and cell death. This compound serves as a valuable tool for research in fungal infections and immune modulation. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-2 is a quinazoline compound that functions as a dual inhibitor of CYP51 and PD-L1, exhibiting IC50 values of 0.263 μM and 0.017 μM, respectively. It displays notable antifungal activity by triggering early apoptosis in fungal cells, leading to significant reductions in intracellular IL-2, NLRP3, and NF-κBp65 protein levels. Additionally, CYP51/PD-L1-IN-2 induces mitochondrial damage and reactive oxygen species (ROS) accumulation, culminating in fungal lysis and subsequent cell death. This compound is valuable for research exploring antifungal mechanisms and cancer immunotherapy. -
CYP51/PD-L1 Inhibitor
CYP51/PD-L1-IN-1 is a dual inhibitor targeting both CYP51 and PD-L1, exhibiting an IC50 of 0.884 μM for CYP51 and 0.083 μM for PD-L1. This quinazoline compound demonstrates notable antifungal activity by inducing early apoptosis in fungal cells while significantly reducing intracellular levels of IL-2, NLRP3, and NF-κBp65. Additionally, CYP51/PD-L1-IN-1 contributes to mitochondrial damage and reactive oxygen species (ROS) accumulation, ultimately leading to fungal lysis and cell death. This compound is valuable for research focused on antifungal therapies and immune modulation. -
CXCR Inhibitor
Corydalmine hydrochloride is a potent CXCR inhibitor that demonstrates significant biological activity by inhibiting spore germination in certain plant pathogenic and saprophytic fungi. Additionally, it exhibits notable analgesic properties, effectively alleviating Vincristine-induced neuropathic pain in murine models. This effect is mediated through the inhibition of the NF-κB-dependent CXCL1/CXCR2 signaling pathway, highlighting its potential applications in pain management research and fungal inhibition studies. -
COX Inhibitor
Indomethacin farnesil is a prodrug of indomethacin, primarily targeting cyclooxygenase (COX) enzymes. This potent, blood-brain barrier-permeable inhibitor exhibits nonselective activity against COX-1 and COX-2, with IC50 values of 18 nM and 26 nM, respectively. Indomethacin farnesil has been shown to disrupt autophagic flux by impairing lysosomal function, making it useful for investigating inflammatory pathways and autophagy-related processes in research applications. -
ULK1/ULK2 Inhibitor
SBP-5147 is a potent inhibitor of ULK1 and ULK2, exhibiting an IC50 of 2 nM for ULK1 and 53 nM for ULK2. This compound effectively inhibits the phosphorylation of Beclin-1 and Vps34, reduces autophagic flux, and downregulates the expression of key autophagy-related proteins ATG13 and ATG101. Additionally, SBP-5147 enhances MHC-I expression, induces caspase-dependent apoptosis, and decreases the viability of non-small cell lung cancer cells. Its mechanism of action makes SBP-5147 a valuable tool for research in non-small cell lung cancer and autophagy modulation. -
CATS Inhibitor
Z-Val-Val-Nle-diazomethylketone is a selective inhibitor of cathepsin S (CATS). This compound effectively reduces the IFNg-induced upregulation of MHCII molecules, specifically HLA-DR and Ii-p33/35, while promoting an increase in the Ii-p10 protein level. It is valuable for research into dermatological conditions such as psoriasis, atopic dermatitis, and actinic keratosis. -
mPGES-1/5-LOX Inhibitor
YS121 is a dual inhibitor targeting microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LOX), with IC50 values of 3.4 μM and 6.5 μM, respectively. It demonstrates specific, reversible binding to mPGES-1, indicated by a KD of 10-14 μM. YS121 reduces PGE2 production in IL-1β-stimulated A549 cells with an EC50 of 12 μM and activates PPAR-α and PPAR-γ, with EC50 values of 1 μM and 3.6 μM, respectively. Additionally, YS121 exhibits significant anti-inflammatory effects in human whole blood and in vivo, making it a valuable tool for pleurisy research. -
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. -
Nrf2 Inhibitor
Nrf2-IN-3 is a small-molecule inhibitor targeting Nrf2 by enhancing the production of reactive oxygen species (ROS). It specifically binds to KEAP1 mutants, restoring their ability to inhibit Nrf2 and facilitating proteasome-dependent degradation of Nrf2 in cells. This compound has shown potential in sensitizing KEAP1-mutated tumor cells to chemotherapeutic agents such as Cisplatin and Gefitinib, making it a valuable tool for research in cancer therapeutics and Nrf2-related signaling pathways. -
COX-2 Inhibitor
Hexahydrocurcumin is a selective, orally active inhibitor of cyclooxygenase-2 (COX-2), demonstrating significant potential in anti-inflammatory applications. As one of the primary metabolites of curcumin, it exhibits antioxidant and anticancer properties, making it relevant for research in various therapeutic areas. Its selectivity towards COX-2 over COX-1 highlights its potential for minimizing gastrointestinal side effects often associated with non-steroidal anti-inflammatory drugs (NSAIDs). -
KEAP1-NRF2 Inhibitor
Keap1-Nrf2-IN-14 is a potent inhibitor of the KEAP1-NRF2 interaction, exhibiting an IC50 value of 75 nM and a Kd of 24 nM for KEAP1. This compound promotes the expression of NRF2 target genes, resulting in enhanced antioxidant and anti-inflammatory responses. Keap1-Nrf2-IN-14 is valuable for investigating oxidative stress-related inflammation and exploring therapeutic strategies targeting the KEAP1-NRF2 signaling pathway. -
COX-2 Inhibitor
COX-2-IN-65 is a selective inhibitor of cyclooxygenase-2 (COX-2) with a reported IC50 of 10.24 μM. This compound exhibits antibacterial activity against Staphylococcus aureus and Escherichia coli, while also scavenging reactive oxygen species (ROS). COX-2-IN-65 is valuable for research applications focused on bacterial infections and inflammation pathways. -
ROS Inhibitor
Picrasidine A is a potent reactive oxygen species (ROS) inhibitor derived from the natural product Picrasma quassioides. This compound demonstrates the ability to inhibit UVB-induced ROS generation, making it a valuable tool for research in oxidative stress and related cellular responses. Its applications extend to studies investigating the protective effects against UV radiation and the underlying mechanisms of antioxidative pathways. -
PPARγ Inhibitor, heme oxygenase-1 Activator, Nrf2 Activator
PIISVYWK is a potent PPARγ inhibitor that also acts as an activator of heme oxygenase-1 (HO-1) and nuclear factor erythroid 2-related factor 2 (Nrf2). This compound effectively modulates the HO-1/Nrf2 signaling pathway, contributing to the reduction of oxidative stress and inflammation, while also exhibiting anti-obesity properties. PIISVYWK is suitable for research applications focused on obesity and related metabolic disorders. -
PGE2 Inhibitor
N1-Acetyl-5-methoxykynuramine hydrochloride is a potent inhibitor of prostaglandin E2 (PGE2) production, acting as an active metabolite of melatonin. This compound effectively scavenges reactive oxygen species and suppresses COX-2 expression in RAW 264.7 macrophages in a dose- and time-dependent manner. Additionally, in a mouse model of Parkinson's disease induced by MPTP, it diminishes lipid peroxidation in key brain regions. N1-Acetyl-5-methoxykynuramine hydrochloride is relevant for research focused on metabolic and neurological disorders. -
mTOR Inhibitor
RapaLink-1 is a third-generation bivalent inhibitor targeting the mechanistic target of rapamycin (mTOR). By combining Rapamycin with MLN0128 through an inert linker, RapaLink-1 demonstrates superior efficacy in inhibiting both wild-type and mutant forms of mTOR compared to other inhibitors. This compound effectively crosses the blood-brain barrier, promoting durable mTORC1 inhibition via FKBP12 binding. Additionally, RapaLink-1 exhibits anticancer properties and may play an antithrombotic role in antiphospholipid syndrome by enhancing autophagy. -
'Nrf2 Activator, ROS Inhibitor'
Ezetimibe ketone is a potent Nrf2 activator and reactive oxygen species (ROS) inhibitor. It effectively reduces H2O2-induced ROS production and mitigates apoptosis in renal tubular epithelial cells. This compound has significant implications for research on renal tubular injury and inflammation. -
mTOR Inhibitor/Autophagy Inducer
mTOR inhibitor-8 is a potent inhibitor of the mechanistic target of rapamycin (mTOR), functioning through the interaction with FKBP12. This compound effectively suppresses mTOR activity and induces autophagy in A549 human lung cancer cells. It is a valuable tool for studying mTOR signaling pathways and the role of autophagy in cancer research. -
FAP Inhibitor
FAPI-mFS is an irreversible inhibitor of fibroblast activation protein (FAP), which targets FAP's enzymatic activity to enhance cancer cell uptake and retention through covalent binding. This compound is particularly useful for cancer imaging and therapy when labeled with radioisotopes such as 68Ga or 177Lu. Additionally, FAPI-mFS serves as a valuable tool in the synthesis and research of radionuclide-drug conjugates (RDCs), facilitating advancements in targeted cancer treatments. -
FAP Inhibitor
NOTA-FAPI is a fibroblast activation protein (FAP) inhibitor designed for targeted tumor imaging. This compound effectively binds to FAP, facilitating the visualization of tumors with high detection efficacy. NOTA-FAPI demonstrates superior imaging quality, making it a valuable tool for cancer research and diagnostic applications. -
Autotaxin Inhibitor
MHC02181 is a potent inhibitor of Autotaxin (ATX), demonstrating an IC50 value of 9.41 μM. By inhibiting ATX, it plays a critical role in modulating lysophosphatidic acid (LPA) production, which is involved in various physiological and pathological processes. This reagent is valuable for research applications focused on cancer progression, fibrosis, and other ATX-mediated diseases. -
Autotaxin Inhibitor
MHC00188 is an allosteric inhibitor of Autotaxin (ATX) with an IC50 of 2.53 μM. This compound modulates ATX activity, which plays a critical role in the production of lysophosphatidic acid (LPA), a signaling lipid involved in various physiological processes. MHC00188 is useful for research into cancer biology, inflammation, and other conditions related to aberrant LPA signaling. -
COX Inhibitor
Aspirin DL-lysine is a lysine-conjugated derivative of aspirin that functions primarily as a cyclooxygenase (COX) inhibitor. This compound effectively inhibits the synthesis of thromboxane A2 (TXA2) in platelets, leading to a reduction in platelet activation and aggregation. Aspirin DL-lysine is valuable for research applications focused on thrombin generation, particularly in clinical studies involving unstable angina pectoris. -
PI3K/Akt Inhibitor, MAPK Inhibitor, NF-κB Inhibitor, Nrf2/ARE Activator
JRN73958 is a potent inhibitor of the PI3K/Akt, MAPK, and NF-κB signaling pathways. This compound effectively reduces LPS/IFNγ-induced activation of these pathways, making it a valuable tool for investigating their roles in cancer biology, particularly in leukemia research. Additionally, JRN73958 acts as an Nrf2/ARE activator, further expanding its utility in studies related to oxidative stress and cell survival mechanisms. -
FKBP12 Inhibitor
WAY-380153 is an FKBP12 inhibitor that demonstrates moderate binding affinity for FKBP12, with a KD of 19 μM measured via isothermal titration calorimetry and 15 μM via nuclear magnetic resonance. This compound is relevant for research applications involving neurotrophy and neuroprotection, serving as a valuable tool for investigating conditions related to neuronal health and function. -
FKBP12 Inhibitor
ElteN378 is a selective inhibitor of FKBP12. This compound has demonstrated significant biological activity in the modulation of protein folding and signaling pathways. Research applications include investigations into neurodegenerative diseases such as Alzheimer's and Parkinson's, as well as studies on amyotrophic lateral sclerosis, proliferation disorders, and various cancer types. -
FKBP35 Inhibitor
D44 is a selective inhibitor of FKBP35, targeting the PPIase activity essential for Plasmodium survival. With IC50 values of 132 nM for Plasmodium falciparum and 125 nM for Plasmodium vivax, D44 demonstrates significant antiplasmodium activity. This compound is valuable for research applications focused on malaria and other infectious diseases, providing insights into potential therapeutic approaches. -
WNT7A Inhibitor/Photosensitizer
WNT7A-IN-1 sodium is a selective inhibitor of WNT7A that disrupts the interaction between WNT7A and its receptor FZD5, leading to enhanced expression of MHC-I. This reagent is known to significantly increase levels of MHC-I and phosphorylated p65 while decreasing active β-catenin expression. Additionally, WNT7A-IN-1 sodium acts as a photosensitizer in the green spectral region, making it suitable for applications in photodynamic therapy and immunological studies.
