Catalog No.
Product Name
Application
Product Information
Citations
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PPAR agonist
Lobeglitazone is a novel thiazolidinedione-class compound and an orally active dual agonist of peroxisome proliferator-activated receptors (PPARs), with EC₅₀ values of 137.4 nM for PPARγ and 546.3 nM for PPARα. In addition to its metabolic effects, Lobeglitazone functions as an inhibitor of multiple pro-inflammatory and pro-fibrotic signaling pathways, including ERK, JNK, Smad, and NF-κB. Lobeglitazone exhibits a broad range of pharmacological activities, including anti-inflammatory, anti-diabetic, anti-fibrotic, and anti-atherosclerotic effects. These properties make it a promising candidate for therapeutic research in metabolic syndrome, type 2 diabetes, cardiovascular disease, and fibrosis-related conditions. - Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue that exhibits potent anti-inflammatory activity. It exerts its effects by blocking mitogen-activated protein kinase (MAPK) signaling and inhibiting the nuclear translocation of the NF-κB subunit p65, thereby suppressing key inflammatory pathways. Additionally, compound 5a27 reduces neutrophil infiltration and the production of pro-inflammatory cytokines. In vivo, it significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI), highlighting its potential as a therapeutic candidate for inflammatory and respiratory disorders.
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CD38 inhibitor
RBN013209 is an orally active, small molecule inhibitor of CD38, exhibiting potent inhibitory activity with an IC₅₀ ranging from 0.01 to 0.1 μM against human CD38. It effectively blocks the enzymatic conversion of extracellular NAD⁺ to ADPR and cADPR in both tumor cells and peripheral blood mononuclear cells (PBMCs), thereby modulating the tumor microenvironment. Beyond its direct antitumor potential, RBN013209 also enhances the efficacy of immunotherapies. It preserves the naïve and central memory phenotypes of CAR-T cells, while reducing the expression of activation markers and exhaustion-associated inhibitory receptors. These properties position RBN013209 as a promising agent for both tumor research and the development of combination strategies to improve CAR-T cell persistence and function. -
RAS inhibitor
RMC-7977 is an orally bioavailable, triple-complex RAS inhibitor that functions by simultaneously binding to cyclophilin A (CypA; K_d = 195 nM) and KRAS^G12V (K_d = 292 μM), facilitating the formation of a stable inhibitory complex. It exhibits broad-spectrum activity against RAS isoforms—including KRAS, NRAS, and HRAS—across both wild-type and mutant variants. RMC-7977 suppresses key oncogenic signaling pathways by inhibiting the phosphorylation of ERK, CRAF, and RSK, while promoting apoptosis through enhanced PARP cleavage. This dual mechanism results in significant tumor regression and reduced acquired resistance in KRAS^G12C-driven cancer models. It also shows favorable tolerability across a range of RAS-mutant tumor models, positioning it as a promising therapeutic candidate for RAS-driven malignancies. -
KRAS-G12C(ON) Inhibitor
Elironrasib is an orally active, covalent inhibitor specifically targeting the active GTP-bound form of KRAS^G12C (KRAS^G12C(ON)). It uniquely functions by forming a stable tri-complex with KRAS^G12C(ON) and cyclophilin A (CypA) within tumor cells, leading to steric hindrance that blocks the interaction between KRAS and its downstream effectors. This mechanism effectively suppresses RAS-mediated signaling, particularly the ERK pathway. Elironrasib induces apoptosis in KRAS^G12C-mutant H358 non-small cell lung cancer cells and demonstrates potent antiproliferative activity across KRAS^G12C-mutant cell lines, with a median IC₅₀ of 0.11 nM. Its high specificity and novel mechanism make it a promising therapeutic candidate for cancers driven by KRAS^G12C mutations. - Lysophosphatidylcholines (LPCs) are orally active lysolipids and key components of oxidized low-density lipoprotein (oxLDL). They are bioactive molecules known to induce cellular injury, promote the production of pro-inflammatory cytokines such as interleukin-1β (IL-1β), and trigger apoptosis. LPCs play a significant role in the pathophysiology of various inflammatory conditions and have been implicated in the progression of sepsis by amplifying inflammatory responses. Due to these properties, LPCs are actively studied in the context of inflammation, cardiovascular disease, and sepsis-related research.
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STING PROTAC degrader
Anti-inflammatory agent 70 (N-Me-SP23) is a PROTAC-based degrader targeting the STING (stimulator of interferon genes) protein, a key regulator of innate immune and inflammatory responses. By promoting STING degradation, N-Me-SP23 effectively inhibits the STING signaling pathway, leading to reduced downstream inflammatory cytokine production. This compound exhibits notable anti-inflammatory activity and holds potential for therapeutic research in STING-associated autoimmune and inflammatory disorders. -
COX-1/HDAC/Tyrosinase Inhibitor
Gnetol is a bioactive phenolic compound isolated from the root of *Gnetum montanum* with diverse pharmacological properties. It potently inhibits cyclooxygenase-1 (COX-1) with an IC₅₀ of 0.78 μM and exhibits histone deacetylase (HDAC) inhibitory activity. Gnetol is also a strong tyrosinase inhibitor, with an IC₅₀ of 4.5 μM against murine tyrosinase, leading to suppression of melanin biosynthesis. In addition to its antioxidant, antiproliferative, anticancer, and hepatoprotective effects, Gnetol modulates metabolic enzymes in a concentration-dependent manner, including α-amylase, α-glucosidase, and adipogenesis pathways, making it a promising candidate for research in oncology, dermatology, and metabolic disorders. -
NF-κB p65 Inhibitor
Licochalcone D is a naturally occurring flavonoid primarily found in the root of *Glycyrrhiza uralensis* (Chinese licorice). It functions as a potent and orally active inhibitor of the NF-κB p65 subunit, a key regulator of inflammation and cancer-related signaling pathways. Licochalcone D exhibits broad pharmacological properties, including antioxidant, anti-inflammatory, and anticancer activities, making it a promising candidate for research in inflammation-related diseases and oncology. -
PDE6D/IKZF1/IKZF3/CK1α Degrader
FPFT-2216 is a “molecular glue” degrader that facilitates the proteasomal degradation of multiple target proteins, including phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1) and Aiolos (IKZF3), as well as casein kinase 1α (CK1α). By promoting selective ubiquitination through E3 ligase recruitment, FPFT-2216 modulates key regulatory pathways and holds promise for research in oncology and inflammatory diseases. -
PROTAC NCOA4 degrader
PROTAC NCOA4 Degrader-1 (Compound V3) is a highly potent PROTAC targeting NCOA4, with a DC₅₀ of 3 nM in HeLa cells. It functions as a ferroptosis inhibitor by reducing NCOA4 levels and lowering intracellular ferrous iron (Fe²⁺) concentrations. PROTAC NCOA4 Degrader-1 has demonstrated protective effects in a CCl₄-induced acute liver injury model, making it a valuable tool for studying ferroptosis and liver disease therapeutics. -
PROTAC CRBN Degrader
CRBN-6-5-5-VHL is a potent and selective VHL-based PROTAC degrader targeting cereblon (CRBN), with a DC₅₀ of 1.5 nM. It selectively degrades CRBN without affecting neo-substrates IKZF1 and IKZF3. -
FKBP12F36V Degrader
dTAG-47 is a heterobifunctional degrader that selectively targets FKBP12^F36V-tagged proteins for degradation. By binding FKBP12^F36V, which acts as a degradation tag (dTAG), dTAG-47 enables conditional and selective protein degradation. It is a valuable tool for studying protein function in models such as basal-like breast cancer (BBC). -
PROTAC CDK4/6 Degrader
BSJ-03-204 triTFA is a potent and selective PROTAC degrader targeting CDK4/6, constructed using ligands for cereblon and CDK. Based on Palbociclib, it exhibits IC₅₀ values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1. BSJ-03-204 triTFA does not induce IKZF1/3 degradation and shows anti-cancer activity, making it a valuable tool for cell cycle and oncology research. -
FKBP12F36V degrader
dTAGV-1 TFA is a potent and selective degrader of FKBP12^F36V-tagged fusion proteins. It enables efficient in vivo degradation of FKBP12^F36V-Nluc, making it a valuable tool for conditional protein degradation studies in live models. -
PROTAC CDK4 Degrader
BSJ-04-132 is a potent and selective Ribociclib-based PROTAC degrader targeting CDK4, constructed using ligands for cereblon and CDK. It exhibits IC₅₀ values of 50.6 nM for CDK4/D1 and 30 nM for CDK6/D1, while sparing CDK6 and IKZF1/3 from degradation. BSJ-04-132 demonstrates anti-cancer activity and is a valuable tool for cell cycle and oncology research. -
PROTAC CDK4/6 Degrader
BSJ-03-204 is a potent and selective PROTAC degrader targeting CDK4 and CDK6, constructed by linking Palbociclib to a cereblon ligand. It exhibits IC₅₀ values of 26.9 nM for CDK4/D1 and 10.4 nM for CDK6/D1, without inducing degradation of IKZF1 or IKZF3. BSJ-03-204 demonstrates strong anti-cancer activity and is a valuable tool for cell cycle and oncology research. -
FKBP12F36V degrader
dTAG-13 is a PROTAC-based heterobifunctional degrader that selectively targets FKBP12^F36V fused in-frame to a protein of interest. By engaging both FKBP12^F36V and the cereblon (CRBN) E3 ligase, dTAG-13 induces efficient and selective degradation of FKBP12^F36V-tagged proteins, making it a valuable tool for conditional protein knockdown studies. -
Anti-inflammatory Agent
Balanophonin is an anti-inflammatory agent that effectively inhibits microglial activation and subsequent neurodegeneration. This compound plays a crucial role in preventing activated microglia-induced apoptosis, making it a valuable tool for research in neuroinflammation and neurodegenerative disorders. Its applications extend to investigations of inflammatory pathways and potential cancer therapies. -
Anti-inflammatory Agent
Siegeskaurolic acid is an orally active anti-inflammatory agent that targets multiple inflammatory pathways. It effectively inhibits the production of nitric oxide (NO), prostaglandin E2 (PGE2), and tumor necrosis factor-alpha (TNF-alpha), along with the activation of nuclear factor-kappaB (NF-kB). This compound is valuable for research applications focused on inflammation and associated disease models. -
Anti-inflammatory Agent
Berkeleyacetal C is a meroterpenoid compound that acts as an anti-inflammatory agent by inhibiting the NF-κB, ERK1/2, and IRF3 signaling pathways. It effectively reduces the expression of inducible nitric oxide synthase (iNOS) and subsequent nitric oxide production in macrophages. Additionally, Berkeleyacetal C suppresses the expression and secretion of key pro-inflammatory cytokines and chemokines, including TNF-α, IL-6, IL-1β, MIP-1α, and MCP-1, while also inhibiting neutrophil activation and reactive oxygen species (ROS) production. This compound is valuable for research into inflammatory disorders. -
SIK1/2 Inhibitor
SIK2-IN-4 is a highly selective inhibitor of SIK1 and SIK2, exhibiting IC50 values of 0.143 μM and 0.076 μM, respectively. By targeting SIK1/2, SIK2-IN-4 reduces the phosphorylation of transcription coactivator 3 (CRTC3), thereby modulating cAMP response element binding protein (CREB)-dependent transcriptional activity. This compound demonstrates inhibitory effects on pro-inflammatory cytokines such as TNF, IL-12/23 p40, and IL-23, while promoting the expression of the anti-inflammatory cytokine IL-10. SIK2-IN-4 is a valuable tool for investigating intestinal inflammation and other chronic inflammatory conditions. -
Anti-inflammatory Agent
β-Bisabolol is a potent anti-inflammatory agent primarily acting through the inhibition of nitric oxide (NO) and pro-inflammatory cytokines such as TNF-α, IL-6, and IL-8 in LPS-stimulated macrophages and fibroblast cells. Its ability to decrease prostaglandin E2 (pGE2) production further underscores its anti-inflammatory properties. This compound is valuable for research on various inflammatory conditions, offering insights into therapeutic approaches for managing inflammation-related diseases. -
Anti-inflammatory Agent
MDL 201112 is a carbocyclic nucleoside functioning as an anti-inflammatory agent. It effectively reduces TNF-α production and inhibits the expression of MHC class II Ia+ antigens. This compound is valuable for research applications focused on inflammation and immunology, providing insights into the mechanisms underlying these biological processes. -
Anti-inflammatory Agent
Delmitide (RDP58) is an orally active d-isomer decapeptide that functions as a potent anti-inflammatory agent. It effectively inhibits the production of pro-inflammatory cytokines such as TNF-α, IFN-γ, and interleukin (IL)-12, while also up-regulating heme oxygenase 1 activity. Delmitide is valuable for research applications focused on ulcerative colitis and other inflammatory conditions. -
Anti-inflammatory Agent
Asperflavin is an anti-inflammatory agent derived from the marine fungus Eurotium amstelodami. It effectively inhibits the production of nitric oxide (NO), prostaglandin E2 (PGE2), and proinflammatory cytokines, along with downregulating the expression of inducible nitric oxide synthase (iNOS) in LPS-treated RAW 264.7 cells. Asperflavin serves as a valuable tool in the investigation of inflammatory diseases and their mechanisms. -
Anti-inflammatory Agent
TNF-α-IN-15 is a selective inhibitor of tumor necrosis factor-alpha (TNF-α), a key pro-inflammatory cytokine involved in various inflammatory processes. By decreasing TNF-α levels in the bloodstream, TNF-α-IN-15 exhibits significant anti-inflammatory activity. This compound is valuable for research applications investigating inflammatory diseases and may provide insights into therapeutic strategies targeting TNF-α-mediated pathways. -
Anti-Inflammatory Compound
Gnetifolin E is a derivative of resveratrol trimer, derived from Gnetum brunonianum. It exhibits significant anti-inflammatory activity by inhibiting tumor necrosis factor-alpha (TNF-α). Gnetifolin E is utilized in research focused on inflammatory diseases and could serve as a potential lead compound for therapeutic development. -
Anti-inflammatory Agent
Anti-inflammatory agent 105 targets the inhibition of TNF-α synthesis and release, demonstrating a potent biological activity with an IC50 of 0.124 nM in the human macrophage cell line U937. This compound is valuable for research applications focused on understanding inflammation-related pathways and the development of therapeutic strategies against inflammatory diseases. -
TNFα/IL-2 Inhibitor
Immuno modulator-1 is a potent inhibitor of TNFα and IL-2, displaying IC50 values of 4.7 nM and 26 nM, respectively, in human peripheral blood mononuclear cells (hPBMC). This compound is valuable for investigating immune response modulation and inflammatory pathways. Additionally, Immuno modulator-1 demonstrates a hERG potassium channel blocking effect, exhibiting a 20% inhibitory percentage at a concentration of 3 μM, making it relevant for studies involving cardiac safety profiles. -
TLR7 Agonist
SMU-L11-R is a selective TLR7 agonist that demonstrates an EC50 of 0.012 μM for human TLR7. This compound specifically activates TLR7, recruits MyD88, and initiates the MAPK/NF-κB signaling pathways, resulting in the secretion of pro-inflammatory cytokines such as TNF-α, IL-1β, and IL-6 in both mouse and human peripheral blood mononuclear cells. Additionally, SMU-L11-R promotes M1-like macrophage polarization and exhibits synergistic anti-tumor effects in combination with PD-L1 inhibitors through the upregulation of CD8+ T cells, making it a valuable tool for research in colorectal cancer. -
Anti-inflammatory Agent
Sinulatumolin C is an anti-inflammatory agent that exhibits significant inhibition of tumor necrosis factor-alpha (TNF-α), with an IC50 value of 2.6 μM. This compound is valuable for research applications focused on understanding inflammatory pathways and exploring potential therapeutic strategies for inflammatory diseases. Its efficacy in modulating TNF-α makes it a useful tool in the study of immune responses and related biological processes. -
Anti-inflammatory Agent
Kaempferol 3-O-(2G-glucosylrutinoside)-7-O-glucoside is a potent anti-inflammatory agent that targets key signaling pathways, including NF-κB, MAPK, and Akt. This compound significantly reduces the production of inflammatory mediators such as nitric oxide (NO) and prostaglandin E2 (PGE2) in LPS-induced RAW 264.7 macrophages. Additionally, it suppresses the secretion of pro-inflammatory cytokines, including TNF-α, IL-1β, and IL-6, making it valuable for research into inflammation and related disorders. -
Anti-inflammatory Agent
TNF-α-IN-12 is a potent inhibitor of tumor necrosis factor-alpha (TNF-α) with an IC50 value of 0.1 μM. This compound effectively reduces TNF-α levels in serum, demonstrating anti-inflammatory activity. It is suitable for research applications aimed at understanding inflammation-related diseases and evaluating potential therapeutic strategies targeting TNF-α signaling pathways. -
COX-1/2 Inhibitor
Cudraflavone B is a prenylated flavonoid that functions as a dual inhibitor of COX-1 and COX-2, demonstrating significant anti-inflammatory and anti-tumor activity. This compound inhibits the translocation of nuclear factor κB (NF-κB) in macrophages, leading to decreased tumor necrosis factor α (TNFα) gene expression and secretion. Additionally, Cudraflavone B induces the mitochondrial apoptotic pathway while activating MAPK signaling pathways, including p38 and ERK, and upregulating SIRT1 expression. These mechanisms contribute to its efficacy in attenuating the growth of human oral squamous cell carcinoma cells, making it a valuable tool for cancer research. -
Anti-TNFRSF17/CD3E Antibody
Gamgertamig is a humanized IgG4 bispecific antibody that simultaneously targets TNFRSF17 and CD3E. This antibody exhibits potent immunomodulatory activity by activating T cells in the presence of TNFRSF17-expressing cells, making it a valuable tool for enhancing anti-tumor immune responses. It is ideal for research applications in cancer immunotherapy and provides insights into T cell modulation and tumor microenvironment interactions. -
Anti-inflammatory Agent
rel-Cleroindicin F is an anti-inflammatory agent that targets the NF-κB signaling pathway. It effectively inhibits the production of nitric oxide (NO) and tumor necrosis factor-alpha (TNF-α) by downregulating NF-κB and its kinases in LPS-stimulated RAW 264.7 cells. This mechanism contributes to the suppression of inducible nitric oxide synthase expression, leading to decreased NO production. Rel-Cleroindicin F is valuable for research into inflammatory processes and potential therapeutic applications. -
Anti-inflammatory Agent
SKF 104351 is an orally active anti-inflammatory agent that functions by inhibiting the production of tumor necrosis factor-alpha (TNF-α). This compound plays a significant role in modulating inflammatory responses, making it valuable for research focused on chronic inflammatory diseases. Its ability to suppress cytokine production positions SKF 104351 as a crucial tool for studies aimed at understanding the mechanisms underlying inflammation and developing therapeutic interventions. -
Anti-inflammatory Agent
Arucadiol is a rosane-type diterpenoid known for its anti-inflammatory properties. It effectively inhibits the production of pro-inflammatory cytokines, specifically TNF-α, IL-1β, and IL-8, by 39.8%, 44.4%, and 34.5% respectively at a concentration of 5 μM. This compound functions by reducing the mRNA and protein expression of these inflammatory mediators, making it a valuable tool for research on inflammation-related cardiovascular conditions, such as atherosclerosis. Arucadiol can be naturally sourced from the roots of Salvia miltiorrhiza var. alba. -
Anti-Inflammatory Agent
Sinulatumolin E is a terpenoid that functions as an anti-inflammatory agent, primarily through its ability to inhibit TNF-α, with an IC50 value of 3.6 μM. This compound exhibits notable anti-inflammatory activity, making it potentially useful for research in inflammation-related pathways and conditions. -
Anti-inflammatory Agent
Trigraecum is a flavonoid compound derived from Dracaena steudneri and Dalbergia cochinchinensis, functioning as an anti-inflammatory agent. It effectively inhibits lipopolysaccharide (LPS)-induced production of pro-inflammatory cytokines such as IL-1β, IL-2, GM-CSF, and TNF-α in human peripheral blood mononuclear cells. Trigraecum is valuable for studies focused on inflammatory diseases and the underlying mechanisms of immune response modulation. -
CD28 Inhibitor
CD28-IN-3 is a selective CD28 inhibitor that effectively interrupts the CD28-B7 interaction, with an IC50 of 7.80 μM and a Kd of 52.45 μM. This compound significantly suppresses the production of key proinflammatory cytokines, including IFN-γ, IL-2, and TNF-α. CD28-IN-3 is valuable for research focused on checkpoint-resistant cancers, providing insights into immune modulation and potential therapeutic strategies. -
Anti-inflammatory Agent
Anti-inflammatory agent 11 targets and inhibits key inflammatory processes by suppressing inducible nitric oxide synthase (iNOS) expression. This compound demonstrates significant antimycobacterial activity against Mycobacterium tuberculosis strains H37Rv and M299, with minimum inhibitory concentrations (MIC50) of 1.3 μM and 6.9 μM, respectively. Additionally, it effectively reduces the production of pro-inflammatory cytokines such as TNF-α and IL-1β. Anti-inflammatory agent 11 is suitable for research in tuberculosis and related inflammatory diseases. -
Anti-inflammatory Agent
Etiprednol dicloacetate is an anti-inflammatory agent that effectively inhibits eosinophil accumulation. This compound is valuable in the study of inflammatory airway diseases, including asthma, providing insights into potential therapeutic strategies. Its mechanism of action and biological activity render it a useful tool for researchers investigating respiratory inflammation. -
Anti-inflammatory Agent
Anti-inflammatory agent 41 is an effective inhibitor of lipopolysaccharide (LPS)-induced expression of pro-inflammatory cytokines IL-6 and TNF-α in J774A.1, THP-1, and LX-2 cells. This compound also inhibits the activation of the NF-κB signaling pathway. Its primary applications include investigating the mechanisms of inflammation and assessing potential therapeutic strategies in inflammation-related diseases. -
Anti-Cancer/Inflammatory Agent
Crocatin B is a natural compound derived from P. crocatum Ruiz & Pav that functions as an anti-cancer and anti-inflammatory agent. It exerts its anti-inflammatory effects by inhibiting the expression of TNF-α and ICAM-1. Additionally, Crocatin B demonstrates notable anti-tumor activity, making it a valuable reagent for research in cancer therapies and inflammation studies. -
Anti-inflammatory Agent
Anti-inflammatory agent 20 is a potent inhibitor of nitric oxide (NO) activity, demonstrating significant anti-inflammatory properties. This compound effectively suppresses lipopolysaccharide (LPS)-induced inflammation by inhibiting the activation of NF-κB and MAPK signaling pathways, leading to a reduction in pro-inflammatory cytokines such as IL-6, TNF-α, as well as the enzymes iNOS and COX-2. It serves as a valuable tool for research applications focused on inflammation and related signaling mechanisms. -
CD28 Inhibitor
CD28-IN-1 is a selective inhibitor of CD28 with a dissociation constant (KD) of 12.48 μM. It effectively disrupts the CD28-B7 interactions, leading to a significant reduction in CD28-mediated immune activation. This compound has been shown to suppress cytokine production, including IFN-γ, IL-2, and TNF-α, in primary human T cells when co-cultured with tumor spheroids and human epithelial tissues. CD28-IN-1 is suitable for research focused on tumor immunity and T cell modulation.
