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Results for "

macrophages

" in MCE Product Catalog:

119

Inhibitors & Agonists

1

Biochemical Assay Reagents

4

Peptides

43

Natural
Products

1

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas
  • HY-W039897
    Methyl α-D-mannopyranoside

    Others Inflammation/Immunology
    Methyl α-D-mannopyranoside could target macrophages in anti-tuberculosis inhalation therapy.
  • HY-N2620
    Rutaevin

    Reactive Oxygen Species Inflammation/Immunology
    Rutaevin is isolated from the fruits of Euodia rutaecarpa. Rutaevin inhibits NO production in LPS-induced RAW 264.7 macrophages.
  • HY-Y0520
    Itaconic acid

    Endogenous Metabolite Inflammation/Immunology
    Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors.
  • HY-117432
    JC-171

    NOD-like Receptor (NLR) Inflammation/Immunology
    JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages.
  • HY-N2053
    Physalin L

    NO Synthase
    Physalin L inhibits LPS-induced NO production in macrophages with the average inhibitory rate of 70.97%. Anti-inflammatory activity.
  • HY-N8129
    Rhaponticin 6′′-O-gallate

    Others Others
    Rhaponticin 6′′-O-gallate is a stilbene glucoside gallate that can be found in rhizome of Rheum undulatum L. Rhaponticin 6′′-O-gallate inhibits nitric oxide production in lipopolysaccharide-activated macrophages.
  • HY-125527
    Resolvin D1

    RvD1

    Endogenous Metabolite Inflammation/Immunology
    Resolvin D1 (RvD1), an endogenous pro-resolving mediator of inflammation, is derived from omega-3 docosahexaenoic acid during the resolution phase of acute inflammation. Resolvin D1 blocks proinflammatory neutrophil migration by regulating actin polymerization, reduces TNF-α–mediated inflammation in macrophages, and enhances phagocytosis of apoptotic cells by macrophages.
  • HY-P1076
    CALP2

    Calcium Channel Phosphodiesterase (PDE) Inflammation/Immunology
    CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.
  • HY-P1076A
    CALP2 TFA

    Calcium Channel Phosphodiesterase (PDE) Inflammation/Immunology
    CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.
  • HY-125531
    Dactylorhin A

    Others Others
    Dactylorhin A, a succinate derivative ester, is isolated from rhizomes of Gymnadenia conopsea. Dactylorhin A exhibits moderate inhibitory effects on NO production effects in RAW 264.7 macrophage cells.
  • HY-136979
    RBN012759

    PARP Cancer Inflammation/Immunology
    RBN012759 is a potent, selective and orally active inhibitor of PARP14, with an IC50 of <3 nM. RBN012759 displays 300-fold selectivity over the monoPARPs and 1000-fold selectivity over the polyPARPs. RBN012759 decreases pro-tumor macrophage function and elicits inflammatory responses in tumor explants.
  • HY-126114
    Lupeol acetate

    Others Inflammation/Immunology
    Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
  • HY-N0569
    Madecassic acid

    NO Synthase COX TNF Receptor Interleukin Related Inflammation/Immunology
    Madecassic acid is isolated from Centella asiatica (Umbelliferae). Madecassic acid has anti-inflammatory properties caused by iNOS, COX-2, TNF-alpha, IL-1beta, and IL-6 inhibition via the downregulation of NF-κB activation in RAW 264.7 macrophage cells.
  • HY-107426
    Verrucarin A

    Muconomycin A

    Apoptosis Reactive Oxygen Species Cancer
    Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53.
  • HY-15701B
    ADH-503

    (Z)-Leukadherin-1 choline

    Complement System Cancer
    ADH-503 ((Z)-Leukadherin-1 choline) is an orally active and allosteric CD11b agonist. ADH-503 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
  • HY-15701A
    (Z)-Leukadherin-1

    ADH-503 free base

    Complement System Cancer
    (Z)-Leukadherin-1 (ADH-503 free base) is an orally active and allosteric CD11b agonist. (Z)-Leukadherin-1 leads to the repolarization of tumor-associated macrophages, reduction in the number of tumor-infiltrating immunosuppressive myeloid cells, and enhances dendritic cell responses.
  • HY-103697
    Gardiquimod

    Toll-like Receptor (TLR) HIV Cancer Infection
    Gardiquimod, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod specifically activates TLR7 when used at concentrations below 10 μM.
  • HY-W001174
    2,5-Dihydroxyacetophenone

    ERK NF-κB Inflammation/Immunology
    2,5-Dihydroxyacetophenone, isolated from Rehmanniae Radix Preparata, inhibits the production of inflammatory mediators in activated macrophages by blocking the ERK1/2 and NF-κB signaling pathways.
  • HY-103697A
    Gardiquimod diTFA

    Toll-like Receptor (TLR) HIV Cancer Infection
    Gardiquimod diTFA, an imidazoquinoline analog, is a TLR7/8 agonist. Gardiquimod diTFA could inhibit HIV-1 infection of macrophages and activated peripheral blood mononuclear cells (PBMCs). Gardiquimod diTFA specifically activates TLR7 when used at concentrations below 10 μM.
  • HY-N8160
    Dehydrocurdione

    Keap1-Nrf2 Reactive Oxygen Species Inflammation/Immunology
    Dehydrocurdione, a zedoary-derived sesquiterpene, induces heme oxygenase (HO)-1, an antioxidative enzyme, in RAW 264.7 macrophages. Dehydrocurdione interacts with Keap1, resulting in Nrf2 translocation followed by activation of the HO-1 E2 enhancer. Dehydrocurdione suppresses lipopolysaccharide-induced NO release, a marker of inflammation. Anti-inflammatory activity.
  • HY-131040
    NLRP3-IN-NBC6

    NOD-like Receptor (NLR) Inflammation/Immunology
    NLRP3-IN-NBC6 is a potent, selective NLRP3 inflammasome inhibitor (IC50= 574 nM) that acts independently of Ca 2+. NLRP3-IN-NBC6 inhibits Nigericin (HY-127019)-induced inflammasome activation in THP-1 cells and Imiquimod (HY-B0180)-induced IL-1β release from LPS-primed bone marrow-derived macrophages (BMDMs).
  • HY-13682B
    Mifamurtide sodium

    MTP-PE sodium; L-MTP-PE sodium; CGP 19835 sodium

    Others Cancer Inflammation/Immunology
    Mifamurtide sodium (MTP-PE sodium), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide sodium, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide sodium has the potential for osteosarcoma research.
  • HY-13682
    Mifamurtide

    MTP-PE; L-MTP-PE; CGP 19835

    Others Cancer Inflammation/Immunology
    Mifamurtide (MTP-PE), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide has the potential for osteosarcoma research.
  • HY-15509A
    Semapimod tetrahydrochloride

    CNI-1493; CPSI-2364 tetrahydrochloride

    TNF Receptor Interleukin Related p38 MAPK Inflammation/Immunology
    Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.
  • HY-13682C
    Mifamurtide TFA

    MTP-PE TFA; L-MTP-PE TFA; CGP 19835 TFA

    Others Cancer Inflammation/Immunology
    Mifamurtide TFA (MTP-PE TFA), an analog of the muramyl dipeptide (MDP), is a nonspecific immunomodulator by stimulating the immune response activating macrophages and monocytes. Mifamurtide TFA, an orphan drug, is a specific ligand of NOD2 used as an insulin sensitizer. Mifamurtide TFA has the potential for osteosarcoma research.
  • HY-N3595
    Cleomiscosin A

    TNF Receptor Inflammation/Immunology
    Cleomiscosin A is a coumarino-lignoid from branch of Macaranga adenantha. Cleomiscosin A is active against TNF-alpha secretion of the mouse peritoneal macrophages.
  • HY-123986
    CTPI-2

    Mitochondrial Metabolism Cancer Inflammation/Immunology
    CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis, preventing the evolution to steatohepatitis, reducing inflammatory macrophage infiltration in the liver and adipose tissue, and starkly mitigating obesity induced by a high-fat diet. Antitumor activity.
  • HY-N3196
    Neotuberostemonine

    Others Infection Inflammation/Immunology
    Neotuberostemonine, one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, attenuates bleomycin-induced pulmonary fibrosis by suppressing the recruitment and activation of macrophages.
  • HY-P0240
    Tuftsin

    Endogenous Metabolite Inflammation/Immunology
    Tuftsin is a tetrapeptide. Tuftsin is a macrophage/microglial activator.
  • HY-109014
    Tenofovir exalidex

    CMX-157

    HIV HBV Nucleoside Antimetabolite/Analog Infection
    Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV.
  • HY-N2556
    Tirucallol

    Others Inflammation/Immunology
    Tirucallol, a tetracyclic triterpene, is isolated from Euphorbia lacteal latex. Tirucallol has topical anti-inflammatory effect. Tirucallol can suppress ear edema in the mouse model and inhibit nitrite production in lipopolysaccharide-stimulated macrophages.
  • HY-N0589
    Dehydrodiisoeugenol

    NF-κB COX Bacterial Infection Inflammation/Immunology
    Dehydrodiisoeugenol is isolated from Myristica fragrans Houtt, shows anti-inflammatory and anti-bacterial actions. Dehydrodiisoeugenol inhibits LPS- stimulated NF-κB activation and cyclooxygenase (COX)-2 gene expression in murine macrophages.
  • HY-110095
    (±)-CPSI-1306

    Others Metabolic Disease Inflammation/Immunology
    (±)-CPSI-1306 is an orally available antagonist of macrophage migration inhibitory factor (MIF).
  • HY-N3552
    Catalposide

    NF-κB Inflammation/Immunology
    Catalposide, an iridoid glycoside that could be isolated from Catalpa ovate G. Don (Bignoniaceae), inhibits TNF-α, IL-1β, and IL-6 productions and NF-κB (p65) activation in lipopolysaccharide-activated RAW 264.7 macrophages.
  • HY-16692
    ISO-1

    MIF Antagonist

    Others Inflammation/Immunology
    ISO-1 is a macrophage migration inhibitory factor (MIF) antagonist with an IC50 of 7 μM.
  • HY-N9394
    (+)-Norlirioferine

    Others Others
    (+)-Norlirioferine is an alkaloid compound. (+)-Norlirioferine inhibits the cell growth of macrophages and VERO cells.
  • HY-N7422
    Kauran-16,17-diol

    ent-Kauran-16β,17-diol

    Apoptosis Cancer Inflammation/Immunology
    Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC50 of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages.
  • HY-101716
    RP-54745

    Interleukin Related Inflammation/Immunology
    RP-54745 is an inhibitor of macrophage stimulation and interleukin-1 production, and a potential antirheumatic compound.
  • HY-N2008
    Luteolin 5-O-glucoside

    NO Synthase Reactive Oxygen Species Inflammation/Immunology
    Luteolin 5-O-glucoside, a major flavonoidfrom Cirsium maackii, possesses anti-inflammatory activity. Luteolin 5-O-glucoside inhibits LPS-induced NO production and t-BHP-induced ROS generation. Luteolin 5-O-glucoside suppresses the expression of iNOS and COX-2 in macrophages.
  • HY-117282
    JG-98

    HSP Apoptosis Cancer
    JG-98, an allosteric heat shock protein 70 (Hsp70) inhibitor, which binds tightly to a conserved site on Hsp70 and disrupts the Hsp70-Bag3 interaction. JG-98 shows anti-cancer activities affecting both cancer cells and tumor-associated macrophages.
  • HY-136239
    Beclomethasone 17-propionate

    Beclomethasone-17-monopropionate; 17-BMP

    Glucocorticoid Receptor Drug Metabolite Inflammation/Immunology
    Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages.
  • HY-110247
    TRAF-STOP inhibitor 6877002

    TNF Receptor NF-κB Inflammation/Immunology Cardiovascular Disease
    TRAF-STOP inhibitor 6877002, is a selective inhibitor of CD40-TRAF6 interaction, compound VII, shows inhibition of NF-κB activation in RAW cells, extracted from patent WO2014033122A1. TRAF-STOP 6877002 prevents the progression of established atherosclerosis in mice, reduces leukocyte recruitment and reduces macrophage activation; reduces macrophage proliferation in atherosclerotic plaques.
  • HY-110063
    4-IPP

    4-Iodo-6-phenylpyrimidine

    Others Metabolic Disease
    4-IPP (4-Iodo-6-phenylpyrimidine) is a specific suicide substrate and irreversible inhibitor of macrophage migration inhibitory factor (MIF).
  • HY-129151
    Ganoderic acid C1

    Others Inflammation/Immunology
    Ganoderic acid C1, a natural compound that could be isolated from G. lucidum, suppresses TNF-α production by murine macrophages (RAW 264.7 cells).
  • HY-13743
    Roquinimex

    Linomide; FCF89; ABR212616

    TNF Receptor Inflammation/Immunology
    Roquinimex (Linomide; PNU212616; ABR212616) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity; inhibits angiogenesis and reduces the secretion of TNF alpha.
  • HY-112622
    GSK3186899

    DDD-853651

    Parasite Cancer
    GSK3186899 (DDD-853651) is an inhibitor of cdc-2-related kinase 12 (CRK12), with an EC50 of 1.4 μM for L. donovani in an intra-macrophage assay.
  • HY-128578
    KPLH1130

    PDHK Metabolic Disease Inflammation/Immunology
    KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice.
  • HY-W010104
    L-Methionine sulfoxide

    H-Met(O)-OH

    Endogenous Metabolite Metabolic Disease
    L-Methionine sulfoxide (H-Met(O)-OH), a metabolite of Methionine, induces M1/classical macrophage polarization, and modulates oxidative stress and purinergic signaling parameters.
  • HY-103017
    JH-X-119-01 hydrochloride

    IRAK Infection
    JH-X-119-01 hydrochloride is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 hydrochloride ameliorates LPS-induced sepsis in mice.
  • HY-N0268
    Irisflorentin

    NO Synthase Inflammation/Immunology
    Irisflorentin, a naturally occurring isoflavone, is an abundant active constituent in Rhizoma Belamcandae. Irisflorentin markedly reduces the transcriptional and translational levels of inducible nitric oxide synthase (iNOS) as well as the production of NO. Anti-inflammatory activity.
  • HY-N1487
    Oleanonic acid

    3-Oxooleanolic acid

    HIV Cancer
    Oleanonic acid (3-Oxooleanolic acid) is a triterpenoid, inhibits infection by HIV-1 in in vitro infected PBMC, naturally infected PBMC and monocyte/macrophages with EC50 of 22.7 mM, 24.6 mM and 57.4 mM, respectively.
  • HY-123601
    DHQZ 36

    Parasite Infection
    DHQZ 36 is a potent inhibitor of retrograde trafficking. DHQZ 36 inhibits Leishmania amazonensis infection in macrophages with an EC50 of 13.63 μM. DHQZ 36 has potent anti-parasite activity.
  • HY-16668
    Tyrphostin A1

    Tyrphostin 1; AG9

    Interleukin Related Inflammation/Immunology
    Tyrphostin A1(AG9) inhibits CD40L-stimulated IL-12 production in macrophage cultures and antigen-induced generation of Th1 cells.
  • HY-113134
    25-Hydroxycholesterol

    Endogenous Metabolite Inflammation/Immunology
    25-Hydroxycholesterol is a metabolite of cholesterol that is produced and secreted by macrophages in response to Toll-like receptor (TLR) activation. 25-hydroxycholesterol is a potent (EC50≈65 nM) and selective suppressor of IgA production by B cells.
  • HY-114492
    GSK547

    GSK'547

    RIP kinase Cancer
    GSK547 (GSK'547) is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIPK1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
  • HY-N0608
    Myrislignan

    NF-κB Inflammation/Immunology
    Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
  • HY-N6777
    Penicillic acid

    Caspase Bacterial Apoptosis Antibiotic Cancer Infection
    Penicillic acid is a polyketide mycotoxin produced by several species of Aspergillus and Penicillium. Penicillic acid exhibits cytotoxicity in rat alveolar macrophages (AM) in vitro. Penicillic acid inhibits Fas ligand-induced apoptosis by blocking self-processing of caspase-8.
  • HY-N7699A
    D-Trimannuronic acid

    TNF Receptor Inflammation/Immunology Neurological Disease
    D-Trimannuronic acid, an alginate oligomer is extracted from seaweed. D-Trimannuronic acid can induce TNF‐α secretion by mouse macrophage cell lines. D-Trimannuronic acid can be used for the research of pain and vascular dementia.
  • HY-N6893
    Ergolide

    NF-κB Inflammation/Immunology
    Ergolide is a sesquiterpene lactone isolated from the dried flowers of Inula Britannica. Ergolide inhibits inducible nitric oxide synthase and cyclo-oxygenase-2 expression in RAW 264.7 macrophages through the inactivation of NF-κB.
  • HY-106409
    Tefinostat

    CHR-2845

    HDAC Cancer
    Tefinostat (CHR-2845) is a monocyte/macrophage-targeted pan HDAC inhibitor, cleaved into active acid CHR-2847 by the intracellular esterase human carboxylesterase-1 (hCE-1). Anti-monocytoid lineage leukaemias activity.
  • HY-114492A
    (Rac)-GSK547

    RIP kinase Cancer
    (Rac)-GSK547 is the racemate of GSK547. GSK547 is a highly selective and potent inhibitor of receptor-interacting serine/threonine protein kinase 1 (RIP1), inhibits macrophage-mediated adaptive immune tolerance in pancreatic cancer.
  • HY-17009
    Iguratimod

    T614

    COX Inflammation/Immunology
    Iguratimod is an antirheumatic agent, acts as an inhibitor of COX-2, with an IC50 of 20 μM (7.7 μg/mL), but shows no effect on COX-1. Iguratimod also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.
  • HY-112885B
    nor-NOHA monoacetate

    Nω-Hydroxy-nor-L-arginine monoacetate

    Arginase Metabolic Disease
    nor-NOHA (Nω-Hydroxy-nor-L-arginine) monoacetate is a potent and selective arginase inhibitor. nor-NOHA monoacetate inhibits rat liver arginase with a Ki of 0.5 µM.
  • HY-109082
    Cevidoplenib

    Syk Inflammation/Immunology
    Cevidoplenib is an orally available inhibitor of spleen tyrosine kinase (Syk), with potential anti-inflammatory and immunomodulating activities.
  • HY-N0608A
    (Rac)-Myrislignan

    NF-κB Inflammation/Immunology
    (Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
  • HY-N0223
    Epibetulinic acid

    NO Synthase Prostaglandin Receptor Inflammation/Immunology Endocrinology
    Epibetulinic acid exhibits potent inhibitory effects on NO and prostaglandin E2 (PGE2) production in mouse macrophages (RAW 264.7) stimulated with bacterial endotoxin with IC50s of 0.7 and 0.6 μM, respectively. Anti-inflammatory activity.
  • HY-121356
    Carebastine

    Histamine Receptor Cancer Endocrinology
    Carebastine is the active metabolite of Ebastine. Carebastine is a histamine H1 receptor antagonist. Carebastine inhibits VEGF-induced HUVEC and HPAEC proliferation, migration and angiogenesis in a dose-dependent manner. Carebastine suppresses the expression of macrophage migration inhibitory factor.
  • HY-N4233
    Bisabolangelone

    p38 MAPK Inflammation/Immunology
    Bisabolangelone, a sesquiterpene derivative, is isolated from the roots of Osterici Radix. Bisabolangelone possesses anti-inflammatory properties, which inhibits LPS-stimulated inflammation through the blocking of NF-kappaB and MAPK pathways in macrophages. Bisabolangelone has anti-ulcer activities.
  • HY-128776
    Antitumor agent-19

    Others Cancer
    Antitumor agent-19 is an antitomor agent targeting tumor-associated macrophages (TAMs) to serve as an effective TAMs modulator. The EC50 values of Antitumor agent-19 in the RAW 264.7 cells and the BMDM cells are 17.18 μM and 18.87 μM, respectively.
  • HY-125827
    13-Methylberberine chloride

    13-Methylberberinium chloride

    Others Cancer Metabolic Disease
    13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS.
  • HY-N9000
    Loganic acid 6′-O-β-D-glucoside

    Others Inflammation/Immunology
    Loganic acid 6′-O-β-D-glucoside, a iridoidal glucoside, is isolated from the whole plant of Gentiana rhodantha (Gentianaceae). Loganic acid 6′-O-β-D-glucoside inhibits LPS-induced NO and TNF-α production in macrophage RAW264.7 cells.
  • HY-N2149A
    Tomatidine hydrochloride

    NF-κB JNK Autophagy Inflammation/Immunology Cardiovascular Disease
    Tomatidine hydrochloride acts as an anti-inflammatory agent by blocking NF-κB and JNK signaling. Tomatidine hydrochloride activates autophagy either in mammal cells or C elegans.
  • HY-100382
    FPTQ

    mGluR Others
    FPTQ is potent mGluR1 antagonist with IC50 values of 6 nM and 1.4 nM for human and mouse mGluR1 respectively. FPTQ has anti-oxidant and anti-inflammatory effects in vitro and in vivo.
  • HY-B0335
    Tolfenamic Acid

    GEA 6414

    COX Inflammation/Immunology Cancer
    Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
  • HY-115661
    Bisdionin C

    Bacterial Infection
    Bisdionin C is a potent GH18 chitinases inhibitor, with an IC50 of 0.2 μM for A. fumigatus ChiB1 (AfChiB1). Bisdionin C inhibits HCHT (human macrophage chitotriosidase) and acidic mammalian chitinase (AMCase) with IC50s of 8.3 and 3.4 μM, respectively.
  • HY-N2350
    Cynaropicrin

    MMP NF-κB TNF Receptor Cancer
    Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
  • HY-B0944
    Pidotimod

    Bacterial Inflammation/Immunology
    Pidotimod is an orally active dipeptide immunostimulant with immunomodulatory properties on the adaptive and the innate immune responses. Pidotimod increases macrophage activity and humoral immune functions. Pidotimod can be used for the research of chronic bronchitis, chronic obstructive pulmonary disease (COPD), bronchiectasis, and chronic idiopathic urticaria,et al.
  • HY-126390
    (E/Z)-BCI

    NSC 150117

    Phosphatase Apoptosis Cancer Inflammation/Immunology
    (E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway.
  • HY-113649
    AKB-6899

    HIF/HIF Prolyl-Hydroxylase Cancer
    AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects.
  • HY-13982
    JSH-23

    NF-κB Cancer Metabolic Disease Inflammation/Immunology
    JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
  • HY-110084
    BTZO-1

    Apoptosis Cardiovascular Disease
    BTZO-1 binds to Macrophage migration inhibitory factor (MIF) with a Kd value of 68.6 nM, and its binding requires the N-terminal Pro1. BTZO-1 can activate antioxidant response element (ARE)-mediated gene expression and suppress oxidative stress-induced cardiomyocyte apoptosis in vitro.
  • HY-N2106
    Dehydroevodiamine

    NF-κB COX PGE synthase NO Synthase Inflammation/Immunology
    Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
  • HY-B0557
    Bisacodyl

    Others Metabolic Disease
    Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE2 by direct activation of colon macrophages. PGE2 acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.
  • HY-113446
    Leukotriene C4

    Endogenous Metabolite Inflammation/Immunology Cardiovascular Disease
    Leukotriene C4 is the parent cysteinyl leukotriene produced by the LTC4 synthase catalyzed conjugation of glutathione to LTA4. Leukotriene C4 is produced by neutrophils, macrophages, mast cells, and by transcellular metabolism in platelets. Leukotriene C4 is one of the constituents of slow-reacting substance of anaphylaxis (SRS-A) and exhibits potent smooth muscle contracting activity.
  • HY-P1119
    WRW4

    Others Neurological Disease
    WRW4, a specific formyl peptide receptor-like 1 (FPRL1) antagonist, inhibits WKYMVm binding to FPRL1 with an IC50 of 0.23 μM. WRW4 specifically inhibits the increase in intracellular calcium by the FPRL1 agonists MMK-1, amyloid beta42 (Abeta42) peptide, and F peptide.
  • HY-131180
    BMS-986235

    LAR-1219

    Others Cardiovascular Disease
    BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure.
  • HY-129113
    α-​Chaconine

    COX Inflammation/Immunology
    α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
  • HY-114180
    RU.521

    RU320521

    Cyclic GMP-AMP Synthase Metabolic Disease
    RU.521 (RU320521) is a potent and selective cyclic GMP-AMP synthase (cGAS) inhibitor and inhibits cGAS-mediated interferon upregulation. RU.521 suppresses dsDNA-activated reporter activity with an IC50 of 700 nM. RU.521 reduces constitutive expression of interferon in macrophages from a mouse model of Aicardi-Goutières syndrome (AGS).
  • HY-15507
    VGX-1027

    GIT 27

    Interleukin Related TNF Receptor Metabolic Disease Inflammation/Immunology
    VGX-1027 is an orally active isoxazole compound that exhibits various immunomodulatory properties. VGX-1027 targets macrophages, reducing the production of the proinflammatory mediators TNF-α, IL-1β, IL-10. VGX-1027 has antidiabetogenic effects by limiting cytokine-mediated immunoinflammatory events.
  • HY-14648
    Dexamethasone

    Hexadecadrol; Prednisolone F

    Glucocorticoid Receptor SARS-CoV Autophagy Complement System Mitophagy Bacterial Antibiotic Cancer Infection Endocrinology Inflammation/Immunology
    Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
  • HY-105268
    AzddMeC

    CS-92

    HIV Reverse Transcriptase Nucleoside Antimetabolite/Analog Infection
    AzddMeC (CS-92) is an antiviral nucleoside analogue and a potent potent, selective and orally active HIV-1 reverse transcriptase and HIV-1 replication inhibitor. In HIV-1-infected human PBM cells and HIV-1-infected human macrophages, the EC50 values of AzddMeC are 9 nM and 6 nM, respectively.
  • HY-N2535
    Coniferaldehyde

    Ferulaldehyde

    Apoptosis Inflammation/Immunology
    Coniferaldehyde (Ferulaldehyde) is an effective inducer of heme oxygenase-1 (HO-1). Coniferaldehyde exerts anti-inflammatory properties in response to LPS. Coniferaldehyde inhibits LPS-induced apoptosis through the PKCα/β II/Nrf-2/HO-1 dependent pathway in RAW264.7 macrophage cells.
  • HY-15652
    Freselestat

    ONO-6818; ONO-PO-736

    Elastase Inflammation/Immunology
    Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.
  • HY-P1439A
    RS 09 TFA

    Toll-like Receptor (TLR) Inflammation/Immunology
    RS 09 TFA is a TLR4 agonist. RS 09 TFA promotes NF-κB nuclear translocation and induces inflammatory cytokine secretion in RAW264.7 macrophages in vitro. RS 09 TFA acts as an adjuvant in vivo; RS 09 TFA enhances X-15 specific antibody serum concentrations, when administered with X-15-KLH in mice.
  • HY-N4137
    Tormentic acid

    Others Inflammation/Immunology Cardiovascular Disease
    Tormentic acid, a triterpene isolated from Rosa rugosa, exerts anti-inflammatory, antihyperlipidemic, and anti-atherogenic properties.
  • HY-N3204
    Neoechinulin A

    Apoptosis Neurological Disease
    Neoechinulin A is an isoprenyl indole alkaloid that exhibits scavenging, neurotrophic factor-like, and anti-apoptotic activities. Neoechinulin A induces memory improvements and antidepressant-like effects in mice.
  • HY-N3977
    Grifolic acid

    GPR120 Inflammation/Immunology
    Grifolic acid is a phenolic compound that is first extracted from the mushroom Albatrellus confluens. Grifolic acid acts as an agonist of the free fatty acid receptor (FFAR4/GPR120).
  • HY-134463
    NHWD-870

    Epigenetic Reader Domain Apoptosis Cancer
    NHWD-870 is a potent, orally active and selective BET family bromodomain inhibitor and only binds bromodomains of BRD2, BRD3, BRD4 (IC50=2.7 nM), and BRDT. NHWD-870 has potent tumor suppressive efficacies and suppresses cancer cell-macrophage interaction. NHWD-870 increases tumor apoptosis and inhibits tumor proliferation.
  • HY-15652A
    Freselestat quarterhydrate

    ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate

    Elastase Inflammation/Immunology
    Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity.
  • HY-N0222
    Avicularin

    Others Cancer Inflammation/Immunology
    Avicularin is a bio-active flavonoid from plants, anti-inflammatory, anti-allergic, anti-oxidant, hepatoprotective, and anti-tumor activities. Avicularin exhibits anti-inflammatory activity through the suppression of ERK signaling pathway in LPS-stimulated RAW 264.7 macrophage cells. Avicularin ameliorates human hepatocellular carcinoma via the regulation of NF κB (p65), COX 2 and PPAR γ activities.
  • HY-106634
    Mitoguazone

    Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG

    HIV Apoptosis Cancer Infection
    Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.
  • HY-130484
    2,3-Dehydro-3,4-dihydro ivermectin

    Parasite
    2,3-Dehydro-3,4-dihydro ivermectin is an analog of ivermectin (HY-15310) and an anthelmintic. 2,3-Dehydro-3,4-dihydro ivermectin has activity against L. amazonensis promastigotes and amastigotes (IC50s=13.8 and 3.6 µM, respectively) without inducing cytotoxicity to macrophages (IC50= 65.5 µM).
  • HY-N6727
    Gliotoxin

    Aspergillin

    Apoptosis PKA NF-κB Bacterial Fungal Antibiotic Infection Inflammation/Immunology
    Gliotoxin is a secondary metabolite, the most abundant mycotoxin secreted by A. fumigatus, inhibits the phagocytosis of macrophages and the immune functions of other immune cells . Gliotoxin inhibits inducible NF-κB activity by preventing IκB degradation, which consequently induces host-cell apoptosis. Gliotoxin activates PKA and increases intracellular cAMP concentration; modulates actin cytoskeleton rearrangement to facilitate A. fumigatus internalization into lung epithelial cells.
  • HY-B0335S
    Tolfenamic Acid-D4

    COX Inflammation/Immunology Cancer
    Tolfenamic Acid-D4 (GEA 6414-D4) is the deuterium labeled Tolfenamic Acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
  • HY-18054
    BVT 2733

    Others Inflammation/Immunology
    BVT 2733 is a potent, selective, and orally active non-steroidal 11β-hydroxydehydrogenase 1 (11β-HSD1) inhibitor. BVT 2733 is potently against the mouse enzyme (IC50=96 nM) over the human enzyme (IC50=3341 nM). BVT 2733 has the potential for the study of arthritis and obesity related disease.
  • HY-14743B
    Golotimod hydrochloride

    SCV 07 hydrochloride; Gamma-D-glutamyl-L-tryptophan hydrochloride

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod hydrochloride (SCV 07 hydrochloride), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod hydrochloride (SCV 07 hydrochloride) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod hydrochloride (SCV 07 hydrochloride) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-128598
    MD2-TLR4-IN-1

    Toll-like Receptor (TLR) Cancer Inflammation/Immunology
    MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
  • HY-W018643
    Ferulic acid methyl ester

    Methyl ferulate

    p38 MAPK Autophagy Inflammation/Immunology Neurological Disease Cancer
    Ferulic acid methyl ester (Methyl ferulate) is a derivative of ferulic acid, isolated from Stemona tuberosa, with anti-inflammatory and antioxidant properties. Ferulic acid methyl ester is a cell membrane and brain permeable compound, shows free radical scavenging ability, used in the research of neurodegenerative disorders. Ferulic acid methyl ester inhibits COX-2 expression, blocks p-p38 and p-JNK in primary bone marrow derived-macrophages.
  • HY-14743
    Golotimod

    SCV 07; Gamma-D-glutamyl-L-tryptophan

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod (SCV-07), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod (SCV-07) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod (SCV-07) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-N0633
    Muscone

    Interleukin Related TNF Receptor NF-κB NOD-like Receptor (NLR) Inflammation/Immunology Cardiovascular Disease
    Muscone is the main active monomer of traditional Chinese medicine musk. Muscone inhibits NF-κB and NLRP3 inflammasome activation. Muscone remarkably decreases the levels of inflammatory cytokines (IL-1β, TNF-α and IL-6), and ultimately improves cardiac function and survival rate.
  • HY-14743A
    Golotimod TFA

    SCV 07 TFA; Gamma-D-glutamyl-L-tryptophan TFA

    Bacterial STAT Infection Inflammation/Immunology
    Golotimod TFA (SCV 07 TFA), an immunomodulating peptide with antimicrobial activity, significantly increases the efficacy of antituberculosis therapy, stimulates thymic and splenic cell proliferation, and improves macrophage function. Golotimod TFA (SCV 07 TFA) inhibits STAT3 signaling and modulates the duration and severity of oral mucositis in animal models that received radiation or a combination of radiation and Cisplatin. Golotimod TFA (SCV 07 TFA) is also a potential therapeutic for recurrent genital herpes simplex virus type 2 (HSV-2).
  • HY-15648F
    GSK-J4 hydrochloride

    Histone Demethylase Cancer
    GSK-J4 hydrochloride is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 hydrochloride inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK-J4 hydrochloride is a cell permeable prodrug of GSK-J1.
  • HY-19999A
    PF-CBP1 hydrochloride

    Epigenetic Reader Domain Histone Acetyltransferase Neurological Disease
    PF-CBP1 hydrochloride is a highly selective inhibitor of the CREB binding protein bromodomain (CBP BRD). PF-CBP1 inhibits CREBBP and EP300 bromodomains with IC50 of 125 nM and 363 nM respectively. PF-CBP1 hydrochloride reduces LPS-induced inflammatory cytokines expression (IL-1βIL-6 and IFN-β) in primary macrophages. PF-CBP1 hydrochloride also downregulates RGS4 expression cortical neurons and can be used for the research of neurological disorders, including epilepsy and parkinson's disease, et al.
  • HY-124958
    NDMC101

    NF-κB Dipeptidyl Peptidase Metabolic Disease Inflammation/Immunology
    NDMC101 is a potent osteoclastogenesis inhibitor and inhibits osteoclast differentiation via down-regulation of NFATc1-modulated gene expression. NDMC101 is similar to the DPP4 substrate and is a significant inhibitor of early T-cell activation via DPP4 inhibition. NDMC101can be used for study of bone disorders, such as rheumatoid arthritis, and synovial inflammation et al.
  • HY-15648B
    GSK-J4

    Histone Demethylase Apoptosis Cancer
    GSK-J4 is a potent dual inhibitor of H3K27me3/me2-demethylases JMJD3/KDM6B and UTX/KDM6A with IC50s of 8.6 and 6.6 μM, respectively. GSK-J4 inhibits LPS-induced TNF-α production in human primary macrophages with an IC50 of 9 μM. GSK J4 is a cell permeable prodrug of GSK-J1. GSK-J4 induces endoplasmic reticulum stress-related apoptosis.
  • HY-100401A
    Pactimibe sulfate

    CS-505

    Acyltransferase Cardiovascular Disease
    Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
  • HY-100401
    Pactimibe

    CS-505 free base

    Acyltransferase Cardiovascular Disease
    Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity.
  • HY-16961
    Sitravatinib

    MGCD516; MG-516

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib (MGCD516) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.
  • HY-16961A
    Sitravatinib malate

    MGCD516 malate; MG-516 malate

    VEGFR c-Kit FLT3 Discoidin Domain Receptor Trk Receptor Cancer Inflammation/Immunology
    Sitravatinib malate (MGCD516 malate) is an orally bioavailable receptor tyrosine kinase (RTK) inhibitor with IC50s of 1.5 nM, 2 nM, 2 nM, 5 nM, 6 nM, 6 nM, 8 nM, 0.5 nM, 29 nM, 5 nM, and 9 nM for Axl, MER, VEGFR3, VEGFR2, VEGFR1, KIT, FLT3, DDR2, DDR1, TRKA, TRKB, respectively. Sitravatinib malate shows potent single-agent antitumor efficacy and enhances the activity of PD-1 blockade through promoting an antitumor immune microenvironment.