Immunology/Inflammation
The immune and inflammation-related pathway including the Toll-like receptors pathway, the B cell receptor signaling pathway, the T cell receptor signaling pathway, etc.
Toll-like receptors (TLRs) play a central role in host cell recognition and responses to microbial pathogens. TLR4 initially recruits TIRAP and MyD88. MyD88 then recruits IRAKs, TRAF6, and the TAK1 complex, leading to early-stage activation of NF-κB and MAP kinases [1]. TLR4 is endocytosed and delivered to intracellular vesicles and forms a complex with TRAM and TRIF, which then recruits TRAF3 and the protein kinases TBK1 and IKKi. TBK1 and IKKi catalyze the phosphorylation of IRF3, leading to the expression of type I IFN [2].
BCR signaling is initiated through ligation of mIg under conditions that induce phosphorylation of the ITAMs in CD79, leading to the activation of Syk. Once Syk is activated, the BCR signal is transmitted via a series of proteins associated with the adaptor protein B-cell linker (Blnk, SLP-65). Blnk binds CD79a via non-ITAM tyrosines and is phosphorylated by Syk. Phospho-Blnk acts as a scaffold for the assembly of the other components, including Bruton’s tyrosine kinase (Btk), Vav 1, and phospholipase C-gamma 2 (PLCγ2) [3]. Following the assembly of the BCR-signalosome, GRB2 binds and activates the Ras-guanine exchange factor SOS, which in turn activates the small GTPase RAS. The original RAS signal is transmitted and amplified through the mitogen-activated protein kinase (MAPK) pathway, which including the serine/threonine-specific protein kinase RAF followed by MEK and extracellular signal related kinases ERK 1 and 2 [4]. After stimulation of BCR, CD19 is phosphorylated by Lyn. Phosphorylated CD19 activates PI3K by binding to the p85 subunit of PI3K and produce phosphatidylinositol-3,4,5-trisphosphate (PIP3) from PIP2, and PIP3 transmits signals downstream [5].
Central process of T cells responding to specific antigens is the binding of the T-cell receptor (TCR) to specific peptides bound to the major histocompatibility complex which expressed on antigen-presenting cells (APCs). Once TCR connected with its ligand, the ζ-chain–associated protein kinase 70 molecules (Zap-70) are recruited to the TCR-CD3 site and activated, resulting in an initiation of several signaling cascades. Once stimulation, Zap-70 forms complexes with several molecules including SLP-76; and a sequential protein kinase cascade is initiated, consisting of MAP kinase kinase kinase (MAP3K), MAP kinase kinase (MAPKK), and MAP kinase (MAPK) [6]. Two MAPK kinases, MKK4 and MKK7, have been reported to be the primary activators of JNK. MKK3, MKK4, and MKK6 are activators of P38 MAP kinase [7]. MAP kinase pathways are major pathways induced by TCR stimulation, and they play a key role in T-cell responses.
Phosphoinositide 3-kinase (PI3K) binds to the cytosolic domain of CD28, leading to conversion of PIP2 to PIP3, activation of PKB (Akt) and phosphoinositide-dependent kinase 1 (PDK1), and subsequent signaling transduction [8].
References
[1] Kawai T, Akira S. The role of pattern-recognition receptors in innate immunity: update on Toll-like receptors[J]. Nature immunology, 2010, 11(5): 373-384.
[2] Kawai T, Akira S. Toll-like receptors and their crosstalk with other innate receptors in infection and immunity[J]. Immunity, 2011, 34(5): 637-650.
[3] Packard T A, Cambier J C. B lymphocyte antigen receptor signaling: initiation, amplification, and regulation[J]. F1000Prime Rep, 2013, 5(40.10): 12703.
[4] Zhong Y, Byrd J C, Dubovsky J A. The B-cell receptor pathway: a critical component of healthy and malignant immune biology[C]//Seminars in hematology. WB Saunders, 2014, 51(3): 206-218.
[5] Baba Y, Matsumoto M, Kurosaki T. Calcium signaling in B cells: regulation of cytosolic Ca 2+ increase and its sensor molecules, STIM1 and STIM2[J]. Molecular immunology, 2014, 62(2): 339-343.
[6] Adachi K, Davis M M. T-cell receptor ligation induces distinct signaling pathways in naive vs. antigen-experienced T cells[J]. Proceedings of the National Academy of Sciences, 2011, 108(4): 1549-1554.
[7] Rincón M, Flavell R A, Davis R A. The Jnk and P38 MAP kinase signaling pathways in T cell–mediated immune responses[J]. Free Radical Biology and Medicine, 2000, 28(9): 1328-1337.
[8] Bashour K T, Gondarenko A, Chen H, et al. CD28 and CD3 have complementary roles in T-cell traction forces[J]. Proceedings of the National Academy of Sciences, 2014, 111(6): 2241-2246.
Targets for Immunology/Inflammation
- Cyclic GMP-AMP Synthase(1)
- Apoptosis(137)
- 5-Lipoxygenase(18)
- TLR(106)
- Papain(2)
- PGDS(1)
- PGE synthase(26)
- SIKs(10)
- IκB/IKK(83)
- AP-1(2)
- KEAP1-Nrf2(47)
- NOD1(1)
- NF-κB(265)
- Interleukin Related(129)
- 15-lipoxygenase(2)
- Others(10)
- Aryl Hydrocarbon Receptor(35)
- CD73(16)
- Complement System(46)
- Galectin(30)
- IFNAR(19)
- NO Synthase(78)
- NOD-like Receptor (NLR)(37)
- STING(84)
- Reactive Oxygen Species(434)
- FKBP(14)
- eNOS(4)
- iNOS(24)
- nNOS(21)
- Glutathione(37)
- Adaptive Immunity(144)
- Allergy(129)
- Arthritis(25)
- Autoimmunity(134)
- Gastric Disease(64)
- Immunosuppressants(27)
- Immunotherapeutics(3)
- Innate Immunity(411)
- Pulmonary Diseases(76)
- Reactive Nitrogen Species(43)
- Specialized Pro-Resolving Mediators(42)
- Reactive Sulfur Species(24)
Products for Immunology/Inflammation
- Cat.No. Product Name Information
- GC35412 Asperulosidic Acid Asperulosidic Acid (ASPA), a bioactive iridoid glycoside, is extracted from the herbs of Hedyotis diffusa Willd.
- GC42860 Aspochalasin D Aspochalasin D is a co-metabolite originally isolated from A.
- GC46886 Aspyrone A fungal metabolite with diverse biological activities
- GC31350 Astaxanthin Astaxanthin, the red dietary carotenoid, is an orally effective and potent antioxidant.
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GC68702
Astegolimab
Astegolimab (MSTT 1041A; RG 6149) is a human IgG2 monoclonal antibody that can block IL-33 signaling by targeting the IL-33 receptor ST2. Astegolimab has potential for use in research on chronic obstructive pulmonary disease (COPD).
- GC41640 Asterriquinol D dimethyl ether Asterriquinol D dimethyl ether is a fungal metabolite that has been found in A.
- GN10415 Astilbin
- GC42863 Asukamycin Asukamycin is polyketide isolated from the S.
- GC32457 Asymmetric dimethylarginine An endogenous NOS inhibitor
- GC46091 Aszonapyrone A A meroditerpene fungal metabolite with diverse biological activities
- GC39554 AT2 receptor agonist C21 An AT2 receptor agonist
- GC62334 AT791 AT791 is a potent and orally bioavailable TLR7 and TLR9 inhibitor.
- GC46887 Atazanavir-d6 An internal standard for the quantification of atazanavir
- GC12537 ATB-337 ATB-337 is a hybrid molecule of an H2S donor and the NSAID diclofenac.
- GC16245 ATB-343 hybrid molecule of an H2S donor and the NSAID indomethacin
- GC46892 ATRA-BA Hybrid A prodrug form of all-trans retinoic acid and butyric acid
- GN10627 Atractylenolide I
- GC48925 Aureonitol A fungal metabolite
- GC41490 Aureusimine B Aureusimine B, also known as phevalin, is a natural pyrazinone produced by certain fungi and by Staphylococcus spp., including S.
- GC46895 Aurintricarboxylic Acid (ammonium salt) A protein synthesis inhibitor with diverse biological activities
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GC40005
Aurodox
Aurodox is a polyketide antibiotic originally isolated from S.
- GC49646 Aurothioglucose (hydrate) A TrxR inhibitor
- GC42877 AUY954 AUY954 is an orally bioavailable and selective agonist of the sphingosine-1-phosphate receptor 1 (S1P1; EC50 = 1.2 nM for stimulating GTPγS binding to S1P1 in CHO cells).
- GC32486 AVE-3085 AVE-3085 is a potent endothelial nitric oxide synthase enhancer, used for cardiovascular disease treatment.
- GC42880 Avenanthramide-C methyl ester Avenanthramide-C methyl ester is an inhibitor of NF-κB activation that acts by blocking the phosphorylation of IKK and IκB (IC50 ~ 40 μM).
- GC45388 Averantin
- GC42881 Avermectin B1a aglycone Avermectin B1a aglycone is an aglycone form of the anthelmintic and insecticide avermectin B1a.
- GC42882 Avermectin B1a monosaccharide Avermectin B1a monosaccharide is a macrolide anthelmintic and monosaccharide form of avermectin B1a.
- GC45984 Avilamycin A An antibiotic
- GC48511 Avrainvillamide A fungal metabolite
- GC42885 AX 048 The group IVA phospholipase A2 (PLA2), known as calcium-dependent cytosolic PLA2 (cPLA2), selectively releases arachidonic acid from membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes.
- GC35440 AX-024 AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM.
- GC19046 AX-024 hydrochloride AX-024 hydrochloride is an cytokine release inhibitor which can strongly inhibit the production of interleukin-6 (IL-6), tumor necrosis factor-α (TNFα), interferon-γ (IFN-γ), IL-10 and IL-17A.
- GC65283 AXC-715 trihydrochloride AXC-715 (T785) trihydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1.
- GC64938 AZD-7648 AZD-7648 is a potent, orally active, selective DNA-PK inhibitor with an IC50 of 0.6 nM. AZD-7648 induces apoptosis and shows antitumor activity.
- GC10135 AZD3264 IKK2 inhibitor
- GC62488 AZD8848 AZD8848 is a selective toll-like receptor 7 (TLR7) antedrug agonist which is developed for the research of asthma and allergic rhinitis.
- GC49057 Azelastine-13C-d3 (hydrochloride) An internal standard for the quantification of azelastine
- GC42891 azido-FTY720 FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine.
- GC46903 Azithromycin-d3 An internal standard for the quantification of azithromycin
- GC46904 Azoxystrobin A broad-spectrum fungicide
- GC60616 AZT triphosphate AZT triphosphate (3'-Azido-3'-deoxythymidine-5'-triphosphate) is a active triphosphate metabolite of Zidovudine (AZT).
- GC60617 AZT triphosphate TEA AZT triphosphate TEA (3'-Azido-3'-deoxythymidine-5'-triphosphate TEA) is a active triphosphate metabolite of Zidovudine (AZT).
- GC45795 Aztreonam-d6 An internal standard for the quantification of aztreonam
- GC39280 B022 B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor (Ki of 4.2 nM; IC50=15.1 nM).
- GC18580 B355252 A neuroprotective agent
- GC42895 Bacillosporin C Bacillosporin C is an oxaphenalenone dimer originally isolated from T.
- GC49793 Bacitracin A (technical grade) A polypeptide antibiotic
- GC46905 Bacitracin Complex A mixture of bacitracin polypeptides in complex with copper
- GC45938 Bacopaside X A triterpenoid saponin
- GC49302 Bactenecin (bovine) (trifluoroacetate salt) A cationic peptide
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GN10018
Baicalin
A flavonoid with diverse biological activities
- GC52344 Bak BH3 (72-87) (human) (trifluoroacetate salt) A Bak-derived peptide
- GC18126 Balsalazide anti-inflammatory drug
- GC35466 Balsalazide sodium hydrate Balsalazide sodium hydrate could suppress colitis-associated carcinogenesis through modulation of IL-6/STAT3 pathway.
- GC17574 BAPTA calcium chelator
- GC18313 BAR501 Impurity BAR501 impurity is an impurity found in the preparation of BAR501 that acts as an agonist of the G protein-coupled bile acid-activated receptor (GP-BAR1).
- GC66331 Basiliximab Basiliximab (CHI 621) is a recombinant chimeric murine/human IgG1 monoclonal anti-interleukin-2 receptor antibody. Basiliximab can be used for the research of renal transplantation.
- GC52476 Bax Inhibitor Peptide V5 (trifluoroacetate salt) A Bax inhibitor
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GC10345
Bay 11-7085
NK-κB activation inhibitor
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GC13035
Bay 11-7821
A selective and irreversible NF-κB inhibitor
- GC42897 BAY 61-3606 (hydrochloride) BAY 61-3606 is a cell-permeable, reversible inhibitor of spleen tyrosine kinase (Syk; Ki = 7.5 nM; IC50 = 10 nM).
- GC35474 Bay 65-1942 free base Bay 65-1942 free base is an ATP-competitive and selective IKKβ inhibitor.
- GC16303 Bay 65-1942 HCl salt
- GC35475 Bay 65-1942 R form Bay 65-1942 R form is the less active R-form of Bay 65-1942.
- GC60624 BAY-985 A dual inhibitor of TBK1 and IKKε
- GC12232 BAY-X 1005 BAY-X 1005 (BAY X 1005; DG-031) is an orally active and selective 5-lipoxygenase activating protein (FLAP) inhibitor.
- GC18487 BC-1215 BC-1215 is an inhibitor of F-box protein 3 (FBXO3; IC50 = 0.9 μg/mL for Il-1β release).
- GC41583 BCN-E-BCN BCN-E-BCN is a strained cycloalkyne probe for detecting proteins that have been sulfenylated, the first intermediate step in protein oxidation.
- GC35481 BCX 1470 BCX 1470 inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.
- GC35482 BCX 1470 methanesulfonate BCX 1470 methanesulfonate inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM), 3.4- and 200-fold better, respectively, than that of trypsin.
- GC46908 BE-24566B A fungal metabolite
- GC46910 Beauvericin A A cyclodepsipeptide with diverse biological activities
- GC49038 Benanomicin A A microbial metabolite with antifungal, fungicidal, and antiviral activities
- GC52468 Benanomicin B A microbial metabolite with antifungal, fungicidal, and antiviral activities
- GC49040 Benanomicin B (formate) A microbial metabolite with antifungal, fungicidal, and antiviral activities
- GC49042 Benastatin A A bacterial metabolite with diverse biological activities
- GC49043 Benastatin B A bacterial metabolite with diverse biological activities
- GC49044 Benastatin C A bacterial metabolite with diverse biological activities
- GC64354 Bendamustine Bendamustine (SDX-105 free base), a purine analogue, is a DNA cross-linking agent. Bendamustine activates DNA-damage stress response and apoptosis. Bendamustine has potent alkylating, anticancer and antimetabolite properties.
- GC34046 Bendazol Bendazol is a hypotensive drug which can also enhance NO synthase activity in renal glomeruli and collecting tubules.
- GC15949 Benfotiamine A lipid-soluble form of vitamin B1
- GC49836 Benoxaprofen Benoxaprofen (LRCL 3794) is a potent and long-acting anti-inflammatory and antipyretic compound.
- GC39346 Benralizumab Benralizumab (MEDI-563) is an interleukin-5 receptor α (IL-5Rα)-directed cytolytic monoclonal antibody that induces direct, rapid and nearly complete depletion of eosinophils via enhanced antibody-dependent cell-mediated cytotoxicity.
- GC35494 Benzoyloxypaeoniflorin Benzoyloxypaeoniflorin, isolated from the root of Paeonia suffruticosa, is a tyrosinase inhibitor against mushroom tyrosinase with IC50 of 0.453 mM.
- GC15058 Benzydamine HCl Benzydamine HCl is a locally-acting nonsteroidal anti-inflammatory drug with local anaesthetic and analgesic properties; selectively binds to prostaglandin synthetase and has notable in vitro antibacterial activity.
- GC60636 Benzyl butyl phthalate Benzyl butyl phthalate, a member of phthalic acid esters (PAEs), can trigger the migration and invasion of hemangioma (HA) cells via upregulation of Zeb1. Benzyl butyl phthalate activates aryl hydrocarbon receptor (AhR) in breast cancer cells to stimulate SPHK1/S1P/S1PR3 signaling and enhances formation of metastasis-initiating breast cancer stem cells (BCSCs).
- GN10443 Berbamine
- GN10358 Berbamine hydrochloride
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GN10221
Berberine
Berberine (Natural Yellow 18) is an alkaloid isolated from the Chinese herbal medicine Huanglian, as an antibiotic. Berberine (Natural Yellow 18) induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase.
- GC35497 Berberine chloride hydrate Berberine chloride hydrate (Natural Yellow 18 chloride hydrate) is an alkaloid that acts as an antibiotic. Berberine chloride hydrate induces reactive oxygen species (ROS) generation and inhibits DNA topoisomerase. Antineoplastic properties.
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GN10208
Berberine hydrochloride
Berberine hydrochloride is an isoquinoline alkaloid derived from the Ranunculaceae medicinal plant Coptis chinensis. It has various pharmacological activities such as anti-tumor, anti-inflammatory, and hypoglycemic activities.
- GN10523 Berberine Sulfate
- GC49387 Berberine-d6 (chloride) An internal standard for the quantification of berberine
- GC46098 Berkeleylactone E A macrolide antibiotic
- GC42925 Berteroin Berteroin is a sulforaphane analog found in cruciferous vegetables including Chinese cabbage, rucola salad leaves, and mustard oil.
- GC46922 Betamethasone 21-phosphate (sodium salt hydrate) A synthetic glucocorticoid
- GC52329 Betamethasone-d5 An internal standard for the quantification of betamethasone
- GC10480 Betulinic acid A plant triterpenoid similar to bile acids
- GC48504 Betulinic Aldehyde oxime A derivative of betulin