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Catalog No.
Product Name
Application
Product Information
Citations
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Calcineurin inhibitor
Cyclosporine is a calcineurin phosphatase pathway inhibitor, used as an immunosuppressant drug to prevent rejection in organ transplantation. -
EGFR inhibitor
AV-412 (MP412) is an EGFR inhibitor with IC50s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFRL858R, EGFRT790M, EGFRL858R/T790M and ErbB2, respectively. -
elastogenesis inhibitor
L-Ascorbic acid (L-Ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid inhibits selectively Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid is also a collagen deposition enhancer and an elastogenesis inhibitor. -
NFAT5 inhibitor
KRN2 (bromide) is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM. -
IFN-α and IFNAR interaction inhibitor
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM). -
Arginase inhibitor
nor-NOHA acetate is a specific and reversible arginase inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia. -
tubulin polymerisation inhibitor
Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulin polymerisation inhibitor with IC50 of 10-100 nM in cancer cell lines; with potent cytotoxic and vascular disrupting activity in vitro and in vivo. -
cyclophilin inhibitor
Alisporivir (DEB-025; Debio-025) is a cyclophilin inhibitor molecule with potent anti-hepatitis C virus (HCV) activity. -
COX-2 inhibitor
Etoricoxib D4 (MK-0663 D4) is a deuterium labeled Etoricoxib. Etoricoxib is a non steroidal anti-inflammatory agent, acting as a selective and orally active COX-2 inhibitor, with IC50s of 1.1 μM and 116 μM for COX-2 and COX-1 in human whole blood. -
COX-2 Specific Inhibitor
SC-236 is a selective inhibitor of cyclooxygenase-2 (COX-2) with an IC50 of 10 nM and also acts as a PPARγ agonist. It effectively suppresses activator protein-1 (AP-1) through the inhibition of c-Jun NH2-terminal kinase, demonstrating significant anti-inflammatory effects. SC-236 has been shown to reduce ERK phosphorylation in murine models, highlighting its potential for investigating inflammatory pathways and therapeutic interventions. -
Arginase Inhibitor
Nor-NOHA dihydrochloride is a selective and reversible inhibitor of arginase, particularly impacting the activity of ARG2 under hypoxic conditions. This compound has been shown to induce apoptosis in ARG2-expressing cells and demonstrates anti-leukemic properties. Nor-NOHA dihydrochloride is useful for research applications related to endothelial dysfunction, immunosuppression, and metabolic studies. -
COX-2 Inhibitor
Humulone, a prenylated phloroglucinol derivative, is a selective inhibitor of cyclooxygenase-2 (COX-2). It demonstrates significant anti-inflammatory properties and serves as a positive modulator of GABAA receptors at low micromolar concentrations. Additionally, Humulone is known to inhibit bone resorption and exhibits antioxidant, anti-angiogenic, and pro-apoptotic activities, making it valuable for various research applications in inflammation and cancer studies. -
PD-L1 Inhibitor
PD-L1-IN-1 is a potent inhibitor targeting programmed cell death ligand 1 (PD-L1) with an IC50 of 115 nM. It effectively disrupts the PD-L1 and PD-1 interaction, enhancing antitumor immune responses in co-cultures of PD-L1 expressing cancer cells and peripheral blood mononuclear cells. Additionally, PD-L1-IN-1 demonstrates low cytotoxicity towards healthy cells, making it a valuable tool for immunological research and therapeutic applications in cancer treatment. -
COX-2 Inhibitor
DuP-697 is a potent, irreversible, and selective inhibitor of cyclooxygenase-2 (COX-2), exhibiting an IC50 of 10 nM for human COX-2 and 800 nM for COX-1. This compound demonstrates significant antiproliferative effects on HT29 colorectal cancer cells with an IC50 of 42.8 nM, as well as antiangiogenic and pro-apoptotic activities. By inhibiting prostaglandin synthesis, DuP-697 offers potential applications in studies related to inflammation, cancer, and fever reduction. -
Keap1-Nrf2 PPI Inhibitor
Tricetin is a competitive inhibitor of the Keap1-Nrf2 protein-protein interaction (PPI). This compound exhibits neuroprotective effects by activating the Nrf2/HO-1 signaling pathway, which mitigates 6-OHDA-induced neurotoxicity in models of Parkinson's disease. Its mechanism of action helps to prevent apoptosis through mitochondrial pathways, making it a valuable reagent for research into neurodegenerative diseases and oxidative stress response. -
ADAM-17 Inhibitor
ZLDI-8 is an inhibitor of the metalloproteinase enzyme ADAM-17, targeting the cleavage of Notch protein. This compound effectively reduces the expression of proteins associated with pro-survival pathways and epithelial-mesenchymal transition (EMT). Additionally, ZLDI-8 functions as a competitive and irreversible inhibitor of the tyrosine phosphatase Lyp, exhibiting an IC50 of 31.6 μM and a Ki of 26.22 μM. Notably, ZLDI-8 demonstrates potent growth inhibition of MHCC97-H cells with an IC50 of 5.32 μM, making it valuable for research into cellular signaling and cancer biology. -
MALT1 Inhibitor
SGR-1505 is a small molecule inhibitor targeting MALT1, effectively modulating the NF-κB signaling pathway. This compound demonstrates significant anti-proliferative and antitumor activities by inhibiting MALT1 enzymatic activity, leading to alterations in cell cycle progression, DNA damage response, and apoptosis-related gene expression in in vivo tumor models. SGR-1505 exhibits both tumorostatic and regressive effects in activated B cell-like diffuse large B cell lymphoma (ABC-DLBCL) xenograft models. It is a valuable tool for research into activated B-cell-like diffuse large B-cell lymphoma, non-Hodgkin B-cell lymphomas, chronic lymphocytic leukemia, and mature B cell neoplasms. -
COX Inhibitor
Metamizole sodium is a potent cyclooxygenase (COX) inhibitor that exhibits significant anti-inflammatory, analgesic, and antipyretic properties. This compound not only inhibits cell proliferation but also promotes apoptosis in various cell types. Additionally, Metamizole sodium serves as a spasmolytic agent, making it a valuable tool for research applications aimed at pain relief and the study of inflammatory processes. Its multifunctional activities contribute to its utility in diverse areas of biomedical research. -
iNOS Inhibitor
1400W is a selective inhibitor of inducible nitric-oxide synthase (iNOS) with a Kd value of ≤ 7 nM, demonstrating slow and tight binding characteristics. This compound effectively inhibits iNOS induction in microglial cells, leading to reduced nitric oxide production, which in turn helps alleviate oxidative stress and neuronal apoptosis in the rat cerebral cortex. 1400W's ability to ameliorate spatial memory dysfunction associated with acute hypobaric hypoxia-reoxygenation makes it a valuable tool for research in neuroprotection and neurodegenerative disease studies. -
pan-SIK/PAK2/3 Inhibitor
MRIA9 is an ATP-competitive inhibitor targeting pan Salt-Inducible kinases (SIK) as well as PAK2 and PAK3. It exhibits potent biological activity with IC50 values of 516 nM for SIK1, 180 nM for SIK2, and 127 nM for SIK3. MRIA9 is suitable for applications in signaling pathway research and the study of various cellular processes influenced by SIK and PAK kinases. -
GCK/MAP4K2 Inhibitor
TL4-12 is a selective inhibitor of MAP4K2 and GCK, demonstrating a dose-dependent ability to downregulate IKZF1 and BCL-6. This compound effectively inhibits cell proliferation in multiple myeloma with an IC50 of 37 nM, and it also induces apoptosis in cancerous cells. TL4-12 holds potential for overcoming resistance to immunomodulatory agents in the treatment of multiple myeloma. -
PTPN2/1 Dual Inhibitor
PTPN2/1-IN-4 is a potent dual inhibitor of PTPN1 and PTPN2, exhibiting IC50 values of 12.8 nM and 5.8 nM, respectively. This compound effectively modulates the IFNγ-JAK-STAT signaling pathway, resulting in enhanced CD8+ T-cell infiltration into tumors. PTPN2/1-IN-4 demonstrates significant anticancer activity, inhibiting tumor growth both as a standalone treatment and in combination with anti-PD-1 antibodies in B16-OVA syngeneic mouse models, making it a valuable tool for cancer research. -
JAK2 Inhibitor
Tkip is a selective inhibitor of JAK2, targeting the JAK2 autophosphorylation site. It effectively inhibits JAK2 autophosphorylation and the phosphorylation of the IFN-γ receptor subunit IFNGR-1, thereby reducing the antiviral effects of IFN-γ and downregulating MHC Class I molecule expression. Tkip is a valuable tool for investigating the IFN-γ signaling pathway and its implications in various biological processes. -
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. -
FKBP51-Hsp90 Interaction Inhibitor
FKBP51-Hsp90-IN-1 is a selective inhibitor targeting the FKBP51-Hsp90 protein-protein interaction, exhibiting an IC50 value of 0.1 μM against FKBP51. This compound is valuable for research into stress-related diseases, Alzheimer's disease, and various metabolic disorders, owing to its ability to modulate protein interactions critical for cellular stress responses and stability. Its specificity makes it a potent tool for elucidating the role of FKBP51 in disease mechanisms. -
FKBP51-Hsp90 Inhibitor
FKBP51-Hsp90-IN-2 is a selective inhibitor of the FKBP51-Hsp90 protein-protein interaction, demonstrating IC50 values of 0.4 µM for FKBP51 and 5 µM for FKBP52. This compound has been shown to enhance cellular energy metabolism and promote neurite growth. Its efficacy makes FKBP51-Hsp90-IN-2 a valuable tool in research focused on neurodegenerative diseases and cancer. -
KRAS(Q61H) Inhibitor
RM-046 is a selective inhibitor targeting the KRAS(Q61H) mutant, functioning through the formation of a ternary complex with cyclophilin A. This compound non-covalently binds to activated KRASQ61H, obstructing effector binding and thereby inhibiting downstream signal transduction pathways. RM-046 has demonstrated efficacy in suppressing ERK phosphorylation, stalling cancer cell proliferation, and promoting anti-tumor activity, including tumor regression in preclinical xenograft studies. It serves as a valuable tool for investigating KRASQ61H-associated malignancies. -
FAP Inhibitor
BR103354 is a selective inhibitor of fibroblast activation protein (FAP) with an IC50 of 14 nM against human FAP. It effectively restores levels of phosphorylated ERK and Glut1, reduces non-fasting blood glucose concentrations, and enhances glucose tolerance, while also decreasing hepatic triglyceride content. This compound demonstrates potential in alleviating hepatic steatosis and fibrosis, making it a valuable tool for research into type 2 diabetes and non-alcoholic steatohepatitis. -
PIKfyve Inhibitor
AS2677131 is a potent and orally active inhibitor of PIKfyve, targeting the PIKfyve-c-Rel signaling pathway. It effectively inhibits the production of pro-inflammatory cytokines, including IL-12p40, IL-6, and IL-1β, by selectively blocking the DNA-binding activity of c-Rel to their respective promoters. Additionally, AS2677131 reduces MHC class II expression on B cells. This compound is valuable for research in the fields of inflammation and immunology, particularly in studies related to arthritis. -
IL-23 Inhibitor
IL-23 cyclic peptide inhibitor 105 targets the interleukin-23 (IL-23) pathway, serving as a specific inhibitor of this pro-inflammatory cytokine. It exhibits significant potential in modulating inflammatory responses associated with disorders such as inflammatory bowel disease (IBD). This compound is a valuable tool for researchers investigating the role of IL-23 in various inflammatory conditions and developing therapeutic strategies targeting IL-23 signaling. -
IL-17 Inhibitor
IL-17-IN-4 is a potent IL-17 inhibitor with an IC50 of less than 0.1 μM, making it a valuable tool for investigating the role of IL-17 in inflammatory diseases. This compound can facilitate research aimed at understanding the mechanisms of inflammation and the therapeutic potential of IL-17 modulation in conditions such as rheumatoid arthritis and psoriasis. Its high potency enables effective studies of IL-17 signaling pathways in various biological contexts. -
IL-1β Secretion Inhibitor
K-832 is an orally active inhibitor of IL-1β secretion, targeting the interleukin-1 pathway. This compound demonstrates significant biological activity by reducing inflammatory responses associated with autoimmune disorders. K-832 is applicable in the research of rheumatoid arthritis and other conditions linked to elevated IL-1β levels, making it a valuable tool for studying inflammation and immune response modulation. -
Keap1-Nrf2 Inhibitor
Keap1-Nrf2-IN-25 is a potent inhibitor of the Keap1-Nrf2 interaction, exhibiting an IC50 of 0.55 μM and a binding affinity (Kd) of 0.50 μM. This compound effectively activates the Nrf2 pathway, leading to the reduction of reactive oxygen species (ROS) and pro-inflammatory cytokines such as IL-1β and IL-6. Keap1-Nrf2-IN-25 has demonstrated protective effects in models of colitis, particularly against DSS-induced inflammation, making it a valuable tool for research in oxidative stress and inflammatory diseases. -
IL-1 Inhibitor
E5090 is an orally active inhibitor of IL-1 generation, acting through its conversion in vivo to the active deacetylated form, DA-E5090. This compound exhibits significant anti-inflammatory properties, making it valuable for studies related to inflammation and immune response modulation. E5090 is useful in various immunology research applications, particularly in understanding the role of IL-1 in disease states. -
IL-17A Inhibitor
Acetyl zingerone is an IL-17A inhibitor that exhibits potent anti-inflammatory and antioxidant activities. This compound plays a crucial role in protecting melanocytes from DNA damage by inhibiting matrix metalloproteinases and downregulating IL-17A target gene expression. Acetyl zingerone is valuable for research focused on inflammatory skin conditions and mechanisms of cellular protection. -
Inflammatory Cytokine Inhibitor
JTE-607 free base is a selective inhibitor of inflammatory cytokine synthesis, targeting the Cleavage and Polyadenylation Specificity Factor 3 (CPSF3). This compound effectively reduces the production of key inflammatory cytokines, including TNF-α, IL-1β, IL-6, IL-8, and IL-10, in LPS-stimulated human peripheral blood mononuclear cells (PBMCs), achieving IC50 values of 11, 5.9, 8.8, 7.3, and 9.1 nM, respectively. JTE-607 free base demonstrates potential utility in research aimed at understanding and mitigating inflammatory responses, particularly in the context of endotoxin shock. -
IL-1/β-transferase Inhibitor
Pentenocin B is an IL-1/β-transferase inhibitor that selectively targets the interleukin-1 signaling pathway. This compound exhibits weak inhibitory activity against IL-1 and β-transferase, which are crucial in mediating inflammatory responses. Pentenocin B is useful for research applications focused on inflammation and related signaling mechanisms. -
IL-2 secretion inhibitor
BC12-4 is a potent inhibitor of interleukin-2 (IL-2) secretion, primarily acting on immune cell signaling pathways. This compound exhibits immunomodulatory activity, making it valuable in the study of cytokine regulation and immune responses. BC12-4 is suitable for research applications focused on autoimmune diseases, transplantation, and cancer immunotherapy.
