Immunology/Inflammation
Read More about this categoryShow Less
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.
Research Areas
- 5-Lipoxygenase(17)
- Apoptosis(889)
- Cyclic GMP-AMP Synthase(7)
- TLR(137)
- Papain(1)
- PGDS(1)
- PGE synthase(26)
- SIKs(13)
- IκB/IKK(71)
- AP-1(15)
- KEAP1-Nrf2(62)
- NOD1(1)
- NF-κB(331)
- Interleukin Related(354)
- 15-lipoxygenase(2)
- Others(10)
- Aryl Hydrocarbon Receptor(43)
- CD73(17)
- Complement System(83)
- Galectin(14)
- IFNAR(70)
- NO Synthase(106)
- NOD-like Receptor (NLR)(75)
- STING(125)
- Reactive Oxygen Species(551)
- FKBP(17)
- eNOS(4)
- iNOS(29)
- nNOS(20)
- Glutathione(54)
- Adaptive Immunity(210)
- Allergy(118)
- Arthritis(34)
- Autoimmunity(181)
- Gastric Disease(94)
- Immunosuppressants(38)
- Immunotherapeutics(4)
- Innate Immunity(566)
- Pulmonary Diseases(109)
- Reactive Nitrogen Species(50)
- Specialized Pro-Resolving Mediators(49)
- Reactive Sulfur Species(28)
- BCL6(9)
- CD20(15)
- CD22(2)
- CD28(9)
- PSMA(15)
- FAP(26)
- Nuclear Factor of activated T Cells (NFAT)(2)
- Glycoprotein VI(2)
- Tim3(6)
- Hapten(1)
- Nectin-4(3)
- DOCK(4)
- MHC(15)
- Transmembrane Glycoprotein(48)
- TREM receptor(13)
- Inflammation or Immune System Disease(2)
- Musculoskeletal and Skin Disease(1)
- Fc Receptor (FcR)(16)
- IKZF Family(5)
- C-type Lectin-like Receptors (CTLRs)(13)
- Asialoglycoprotein Receptor (ASGPR)(3)
- Human leukocyte immunoglobulin (Ig)-like receptors (LILR)(1)
Products Related to Immunology/Inflammation(4922)
- GC73627HDAC/JAK/BRD4-IN-1CAS: 2755325-84-7Purity: >95.00%
HDAC/JAK/BRD4-IN-1(compuesto 25ap) es un potente inhibidor triple HDAC/JAK/BRD4.
- GC73631FPR1 antagonist 1Purity: >95.00%
FPR1 antagonist 1 (compuesto 24a) es un antagonista del receptor de péptido formi1 (FPR1) con una IC50 de 25 nM.
- GC73634Cu(II)-ElesclomolCAS: 1224195-72-5Purity: >99.00%
Cu(II)-Elesclomol es un quelato 1:1 formado por iones Elesclomol y Cu (II) ions, que puede inducir la muerte por cobre y tiene actividad anticancerígena
- GC73647STING-IN-7CAS: 899947-07-0Purity: >98.00%
STING-IN-7 (compuesto 21) es un potente inhibidor de la picadura con una IC50 de 11,5 nM.
- GC73688Hydroxy-PP-MeCAS: 833481-77-9Purity: >99.00%
Hydroxy-PP-Me es un potente y específico inhibidor CBR1 con una IC50 de 759 nM. Droxy-ppme inhila la apoptosis indupor la retirada del suero.
- GC73730RL-6-Me-7-OHCAS: 2184-54-5Purity: >96.00%
RL-6-Me-7-OH es un hapten que activa las células MAIT humanas y de ratones (EC50=25µM).
- GC73773PLK1/BRD4-IN-5Purity: >99.00%
PLK1/BRD4-IN-5 (compuesto SC10) es un inhibiplk1 y BRD4 activos por vía oral con valores de IC50 de 0.3 nM y 60.8 nM, respectivamente.
- GC73793PSMA binder-1CAS: 2170653-14-0Purity: >98.00%
PSMA binder-1 es un ligando para PSMA y puede ser usado para sintetizar Ac-PSMA-trillium.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC73601 | UCM-1336 | 1621535-90-7 | >99.00% | |
UCM-1336 es un potente inhibidor de la ICMT, con una IC50 de 2 μM. | ||||
| GC73627 | HDAC/JAK/BRD4-IN-1 | 2755325-84-7 | >95.00% | |
HDAC/JAK/BRD4-IN-1(compuesto 25ap) es un potente inhibidor triple HDAC/JAK/BRD4. | ||||
| GC73629 | FB49 | 3074495-82-9 | >98.50% | |
FB49 es un inhibidor altamente selectivo del athanogen 3 (BAG3) asociado con bcl-2, con un Ki de 45 μM. | ||||
| GC73630 | ZZM-1220 | - | >98.00% | |
ZZM-1220 es un inhibidor covalente de la histona lisina metltransferasa G9a/GLP con IC50s de 458 nM y 924 nM, respectivamente. | ||||
| GC73631 | FPR1 antagonist 1 | - | >95.00% | |
FPR1 antagonist 1 (compuesto 24a) es un antagonista del receptor de péptido formi1 (FPR1) con una IC50 de 25 nM. | ||||
| GC73632 | NSC 48160 | 6640-90-0 | >99.00% | |
NSC 48160 inhiel crecimiento de las células cancerosas del páncreas con IC50s de 84,3 μM para CPFAC-1 y 94,5 μM para BxPC-3. | ||||
| GC73634 | Cu(II)-Elesclomol | 1224195-72-5 | >99.00% | |
Cu(II)-Elesclomol es un quelato 1:1 formado por iones Elesclomol y Cu (II) ions, que puede inducir la muerte por cobre y tiene actividad anticancerígena | ||||
| GC73643 | NBI-961 | 2225902-98-5 | >99.00% | |
NBI-961 es un potente inhibidor de NEK2 que inhila la degradación proteasomal. | ||||
| GC73644 | NT-0796 | 2272917-13-0 | >99.00% | |
NT-0796 es un inhibidel inflammasoma NLRP3 activo por vía oral, selectivo y penetrpor el SNC. | ||||
| GC73647 | STING-IN-7 | 899947-07-0 | >98.00% | |
STING-IN-7 (compuesto 21) es un potente inhibidor de la picadura con una IC50 de 11,5 nM. | ||||
| GC73678 | RMC-4998 | 2642037-07-6 | >96.00% | |
RMC-4998 es un inhibidor activo oral dirigido al estado activo o ligado a GTP del mutante KRASG12C. | ||||
| GC73688 | Hydroxy-PP-Me | 833481-77-9 | >99.00% | |
Hydroxy-PP-Me es un potente y específico inhibidor CBR1 con una IC50 de 759 nM. Droxy-ppme inhila la apoptosis indupor la retirada del suero. | ||||
| GC73697 | STM3006 | 2499664-52-5 | >97.00% | |
STM3006 es un inhibidor de METTL3 altamente potente, selectivo y activo por vía oral (IC50: 5 nM). | ||||
| GC73702 | NSC 689534 | 907958-80-9 | >96.00% | |
NSC 689534 puede formar quelde cobre con Cu2+. | ||||
| GC73730 | RL-6-Me-7-OH | 2184-54-5 | >96.00% | |
RL-6-Me-7-OH es un hapten que activa las células MAIT humanas y de ratones (EC50=25µM). | ||||
| GC73740 | DCZ5418 | 2883709-99-5 | >99.00% | |
DCZ5418 es un inhibidor de TRIP13. | ||||
| GC73744 | JAB-2485 | 2899209-55-1 | >98.00% | |
JAB-2485 es un potente y selectivo inhibidor de la cinasa de Aurora a (AURKA), con una IC50 de 0,33 nM. | ||||
| GC73750 | GLPG3312 | 2340388-72-7 | >98.00% | |
GLPG3312 (compuesto 28) es un inhibidor selectivo de pan-SIK con valores de IC50 de 2.0 nM, 0.7 nM y 0.6 nM para SIK1, SIK2 y SIK3, respectivamente. | ||||
| GC73760 | Trilexium | 1983180-82-0 | >99.00% | |
Trilexium (TRX-E-009-1) es una tercera generación de benzopirano estructuralmente relacionado con TRX-E-002-1. | ||||
| GC73767 | PKM2-IN-6 | 771467-00-6 | >98.00% | |
PKM2-IN-6 (compuesto 7d) es un potente inhibidor de la PKM2 con un valor de IC50 de 23 nM. | ||||
| GC73773 | PLK1/BRD4-IN-5 | - | >99.00% | |
PLK1/BRD4-IN-5 (compuesto SC10) es un inhibiplk1 y BRD4 activos por vía oral con valores de IC50 de 0.3 nM y 60.8 nM, respectivamente. | ||||
| GC73774 | YCH2823 | - | >99.00% | |
YCH2823 es un inhibidor de USP7 (IC50 = 49.6 nM; Kd = 0,117 μM). | ||||
| GC73786 | ARV-393 | 2851885-95-3 | >98.00% | |
ARV-393 es un PROTAC activo por vía oral que utiliza el sistema ubiquitin-proteasome para dirigir la degradación del BCL6. | ||||
| GC73793 | PSMA binder-1 | 2170653-14-0 | >98.00% | |
PSMA binder-1 es un ligando para PSMA y puede ser usado para sintetizar Ac-PSMA-trillium. | ||||
