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)
- GC81638PROTAC GPX4 degrader-5CAS: 3119292-91-7Purity: >95.00%
PROTAC GPX4 degrader-5 (compound N15) is an efficient and highly selective PROTAC GPX4 degrader ( DC 50 = 28 nM).
- GC81669ATP- 13 C 10 , 15 N 5 ,d 14 (dilithium)Purity: >98.00%
ATP- 13 C 10, 15 N 5,d 14 ( Adenosine 5'-triphosphate- 13 C 10, 15 N 5,d 14 ) dilithium is the 13 C-, 15 N- and deuterium labeled ATP dilithium.
- GC81695DIM-3,5-Cl2CAS: 2595179-74-9Purity: >99.00%
DIM-3,5-Cl2 is an inverse NR4A1/NR4A2 agonist with K D values of 7.7 μM and 12.0 μM for NR4A1 and NR4A2, respectively.
- GC81725TRPV1 antagonist 10CAS: 896584-55-7Purity: >98.50%
TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist ( IC 50 = 33.06 nM), moderate to weak URAT1 ( IC 50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor.
- GC81730Misitatug blivedotinPurity: >98.00%
Misitatug blivedotin (RC88) is an antibody-drug conjugate ( ADC ) targeting mesothelin ( MSLN ).
- GC81731Hericene ACAS: 157207-54-0Purity: >98.50%
Hericene A is an orally active aromatic hericene derivative.
- GC817528-DeoxylactucinCAS: 65725-10-2Purity: >95.00%
8-Deoxylactucin is an orally active sesquiterpene lactone.
- GC81754(E)-FOBISIN101CAS: 1370281-06-3Purity: >95.50%
(E)-FOBISIN101 is a 14-3-3 protein-protein interaction ( 14-3-3 protein-protein interaction ) inhibitor, with IC 50 values of 9.3 and 16.4 μM for disrupting the binding of 14-3-3ζ or 14-3-3γ to PRAS40, respectively.
- GC817573-Ethoxy-5,6-dibromosalicylaldehydeCAS: 20041-64-9Purity: >99.50%
3-Ethoxy-5,6-dibromosalicylaldehyde is an IRE1/ERN1 inhibitor, with an IC 50 of 0.12 μM, a K i of 71-88 nM, and a K d of 100 nM against the ribonuclease activity of hIRE1α, as well as an IC 50 of 4.8 μM against yeast Ire1.
- GC81758HDAC11-IN-5Purity: >98.00%
HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC 50 of 0.021 μM.
- GC81760ShepherdineCAS: 3000-36-0Purity: >98.00%
Shepherdine, a harmala-type indole and tetrahydro-β-carboline alkaloid, is an antioxidant.
- GC817614-Methoxycinnamic acid ethyl esterCAS: 1929-30-2Purity: >98.50%
4-Methoxycinnamic acid ethyl ester (Ethyl p-methoxycinnamate) is an orally active natural compound found.
- GC81763Coelenterazine TFAPurity: >99.00%
Coelenterazine TFA is a luminescent enzyme substrate for apoaequorin and Renilla luciferase.
- GC81767BAY-1128688CAS: 1428988-21-9Purity: >98.00%
BAY-1128688 is a potent, orally active and selective AKR1C3 inhibitor with IC 50 < 2 nM.
- GC81771RANKL-IN-1 formatePurity: >99.50%
RANKL-IN-1 formate is a selective receptor activator of nuclear factor-κB ligand inhibitor ligand ( RANKL ) inhibitor with a K D value of 7.6 μM.
- GC81772Epibestatin hydrochlorideCAS: 100992-60-7Purity: >98.00%
Epibestatin hydrochloride is an epimer of Bestatin, a DPP4 inhibitor and protease inhibitor, with an IC 50 of 17 μM against DPP4.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC81638 | PROTAC GPX4 degrader-5 | 3119292-91-7 | >95.00% | |
PROTAC GPX4 degrader-5 (compound N15) is an efficient and highly selective PROTAC GPX4 degrader ( DC 50 = 28 nM). | ||||
| GC81639 | SH-26 | - | >98.00% | |
SH-26 is a PHD1 PROTAC degrader with DC 50 s of 1.06 μM, 4.16 μM and 4.91 μM in MDA-MB-231, HepG2 and HEK-293T cells, respectively. | ||||
| GC81669 | ATP- 13 C 10 , 15 N 5 ,d 14 (dilithium) | - | >98.00% | |
ATP- 13 C 10, 15 N 5,d 14 ( Adenosine 5'-triphosphate- 13 C 10, 15 N 5,d 14 ) dilithium is the 13 C-, 15 N- and deuterium labeled ATP dilithium. | ||||
| GC81674 | MKI-3 | 3084702-28-0 | >98.00% | |
MKI-3 is a selective microtubule-associated serine/threonine kinase-like ( MASTL ) inhibitor with an IC 50 of 5.72 nM and a K d of 1.89 nM. | ||||
| GC81678 | ML278 | 1604821-43-3 | >97.50% | |
ML278 is a scavenger receptor-BI ( SR-BI ) inhibitor with an IC 50 of 0.93 nM in mice. | ||||
| GC81679 | PLT012 | - | >98.50% | |
PLT012 is a humanized IgG4 antibody targeting CD36. | ||||
| GC81683 | AM9053 | 157469-21-1 | >98.00% | |
AM9053 is a selective, effective and slowly reversible inhibitor of N-acyl ethanolamine acid amidease ( NAAA ) ( IC 50 = 30 nM). | ||||
| GC81687 | cis-V-11-0711 | 1428338-79-7 | >98.00% | |
cis-V-11-0711 is the cis form of V-11-0711. | ||||
| GC81690 | BI1071 | - | >98.50% | |
BI1071 is an orally active Nur77-Bcl-2 apoptotic pathway modulator. | ||||
| GC81695 | DIM-3,5-Cl2 | 2595179-74-9 | >99.00% | |
DIM-3,5-Cl2 is an inverse NR4A1/NR4A2 agonist with K D values of 7.7 μM and 12.0 μM for NR4A1 and NR4A2, respectively. | ||||
| GC81725 | TRPV1 antagonist 10 | 896584-55-7 | >98.50% | |
TRPV1 antagonist 10 is an orally active and potent TRPV1 antagonist ( IC 50 = 33.06 nM), moderate to weak URAT1 ( IC 50 = 22.51 μM) and GLUT9 (60.25% at 50 μM) inhibitor. | ||||
| GC81730 | Misitatug blivedotin | - | >98.00% | |
Misitatug blivedotin (RC88) is an antibody-drug conjugate ( ADC ) targeting mesothelin ( MSLN ). | ||||
| GC81731 | Hericene A | 157207-54-0 | >98.50% | |
Hericene A is an orally active aromatic hericene derivative. | ||||
| GC81752 | 8-Deoxylactucin | 65725-10-2 | >95.00% | |
8-Deoxylactucin is an orally active sesquiterpene lactone. | ||||
| GC81754 | (E)-FOBISIN101 | 1370281-06-3 | >95.50% | |
(E)-FOBISIN101 is a 14-3-3 protein-protein interaction ( 14-3-3 protein-protein interaction ) inhibitor, with IC 50 values of 9.3 and 16.4 μM for disrupting the binding of 14-3-3ζ or 14-3-3γ to PRAS40, respectively. | ||||
| GC81757 | 3-Ethoxy-5,6-dibromosalicylaldehyde | 20041-64-9 | >99.50% | |
3-Ethoxy-5,6-dibromosalicylaldehyde is an IRE1/ERN1 inhibitor, with an IC 50 of 0.12 μM, a K i of 71-88 nM, and a K d of 100 nM against the ribonuclease activity of hIRE1α, as well as an IC 50 of 4.8 μM against yeast Ire1. | ||||
| GC81758 | HDAC11-IN-5 | - | >98.00% | |
HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC 50 of 0.021 μM. | ||||
| GC81760 | Shepherdine | 3000-36-0 | >98.00% | |
Shepherdine, a harmala-type indole and tetrahydro-β-carboline alkaloid, is an antioxidant. | ||||
| GC81761 | 4-Methoxycinnamic acid ethyl ester | 1929-30-2 | >98.50% | |
4-Methoxycinnamic acid ethyl ester (Ethyl p-methoxycinnamate) is an orally active natural compound found. | ||||
| GC81762 | Mitoflaxone | 87626-55-9 | >99.50% | |
| GC81763 | Coelenterazine TFA | - | >99.00% | |
Coelenterazine TFA is a luminescent enzyme substrate for apoaequorin and Renilla luciferase. | ||||
| GC81767 | BAY-1128688 | 1428988-21-9 | >98.00% | |
BAY-1128688 is a potent, orally active and selective AKR1C3 inhibitor with IC 50 < 2 nM. | ||||
| GC81771 | RANKL-IN-1 formate | - | >99.50% | |
RANKL-IN-1 formate is a selective receptor activator of nuclear factor-κB ligand inhibitor ligand ( RANKL ) inhibitor with a K D value of 7.6 μM. | ||||
| GC81772 | Epibestatin hydrochloride | 100992-60-7 | >98.00% | |
Epibestatin hydrochloride is an epimer of Bestatin, a DPP4 inhibitor and protease inhibitor, with an IC 50 of 17 μM against DPP4. | ||||
