Immunology/Inflammation
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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.
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Products Related to Immunology/Inflammation(4696)
- GC79058PARP1/NAMPT-IN-1CAS: 3084810-86-3Purity: >98.00%
PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC 50 values of 1.2 nM and 6.7 nM, respectively.
- GC79059SAP15 acetatePurity: >98.00%
SAP15 (Synthetic anti-inflammatory peptide 15) acetate is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3.
- GC79067ADAR1i-124Purity: >98.50%
ADAR1i-124 is an A-to-I RNA editing inhibitor by inhibiting the catalytic activities of both ADAR1p150 and ADAR1p110.
- GC79068Telomeric G4s ligand 2CAS: 3094716-52-3Purity: >98.00%
Telomeric G4s ligand 2 is an orally active, selective ligand of telomeric G-quadruplex (G4), with an IC 50 of 0.4 μM.
- GC79070WWQ-03-012CAS: 3076807-15-0Purity: >98.00%
WWQ-03-012 is a selective DESI2 inhibitor with an IC 50 of 47.3 nM.
- GC79103Berzosertib hydrochlorideCAS: 1428935-04-9Purity: >98.50%
Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor.
- GC79109CZS-241 hydrochloridePurity: >98.50%
CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 ( PLK4 ) ( IC 50 =2.6 nM).
- GC79141T7 Peptide TFAPurity: >98.00%
T7 Peptide TFA is a protein synthesis inhibitor and anti-angiogenic agent, with a K d of 10 nM for human transferrin receptor.
- GC79143BRD4-IN-12CAS: 3112325-99-9Purity: >98.00%
BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC 50 of 7.9 nM.
- GC79195Semaglutide-FITCPurity: >96.50%
Semaglutide -FITC (Semaglutide-Lys(FITC)) is a fluorescent tracer probe (Ex/Em = 495/520 nm) obtained by covalently coupling the green fluorescent dye fluorescein isothiocyanate (FITC) to the long-acting analogue of GLP-1, Semaglutide.
- GC79196Semaglutide, Cy5 labeledPurity: >98.00%
Semaglutide, Cy5-labeled (Semaglutide-Cys(Cy5)) is a CY5 -labeled version of Semaglutide (Ex/Em = 633/670 nm).
- GC79227SphingomabPurity: >97.50%
Sphingomab (LT1002) is a mouse-derived IgG1 κ monoclonal antibody and also an inhibitor targeting S1P, with high affinity for S1P and a K d value of 0.03 ± 0.002 nM.
- GC79231RMC-4998 TFAPurity: >99.00%
RMC-4998 TFA is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC79058 | PARP1/NAMPT-IN-1 | 3084810-86-3 | >98.00% | |
PARP1/NAMPT-IN-1 is a potent and dual PARP1 and NAMPT inhibitor with IC 50 values of 1.2 nM and 6.7 nM, respectively. | ||||
| GC79059 | SAP15 acetate | - | >98.00% | |
SAP15 (Synthetic anti-inflammatory peptide 15) acetate is a synthetic anti-inflammatory peptide consisting of 15 amino acids designed from human beta-defensin 3. | ||||
| GC79067 | ADAR1i-124 | - | >98.50% | |
ADAR1i-124 is an A-to-I RNA editing inhibitor by inhibiting the catalytic activities of both ADAR1p150 and ADAR1p110. | ||||
| GC79068 | Telomeric G4s ligand 2 | 3094716-52-3 | >98.00% | |
Telomeric G4s ligand 2 is an orally active, selective ligand of telomeric G-quadruplex (G4), with an IC 50 of 0.4 μM. | ||||
| GC79070 | WWQ-03-012 | 3076807-15-0 | >98.00% | |
WWQ-03-012 is a selective DESI2 inhibitor with an IC 50 of 47.3 nM. | ||||
| GC79072 | MS6076 | - | >98.00% | |
MS6076 is a mitochondrial protease ClpP agonist. | ||||
| GC79077 | DDO-6600 | 2640292-37-9 | >98.00% | |
DDO-6600 is a covalent Hsp90 inhibitor. | ||||
| GC79103 | Berzosertib hydrochloride | 1428935-04-9 | >98.50% | |
Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. | ||||
| GC79109 | CZS-241 hydrochloride | - | >98.50% | |
CZS-241 hydrochloride is an orally active and selective inhibitor of Polo-like Kinase 4 ( PLK4 ) ( IC 50 =2.6 nM). | ||||
| GC79111 | CK2-TN03 | 313226-24-3 | >98.00% | |
CK2-TN03 is an ATP-competitive casein kinase 2 ( CK2 ) inhibitor, with an IC 50 of 165 nM and a K i of 20 nM. | ||||
| GC79122 | Opitor-0 | - | >98.00% | |
Opitor-0 is a OPA1 GTPase inhibitor with an IC 50 of 3.0 μM. | ||||
| GC79141 | T7 Peptide TFA | - | >98.00% | |
T7 Peptide TFA is a protein synthesis inhibitor and anti-angiogenic agent, with a K d of 10 nM for human transferrin receptor. | ||||
| GC79143 | BRD4-IN-12 | 3112325-99-9 | >98.00% | |
BRD4-IN-12 is a potent and orally active BRD4 inhibitor with an IC 50 of 7.9 nM. | ||||
| GC79144 | MC3817 free base | - | >98.00% | |
MC3817 free base is a selective DNMT1 inhibitor. | ||||
| GC79145 | MC3817 | - | >99.50% | |
MC3817 is a selective DNMT1 inhibitor. | ||||
| GC79146 | Ischemin | 1357059-00-7 | >99.50% | |
Ischemin is a CBP bromodomain inhibitor that inhibits p53 interaction with CBP and transcriptional activity in cells. | ||||
| GC79147 | HLC40 | - | >99.50% | |
HLC40 is a MLL1 histone methyltransferase inhibitor with an IC 50 of 0.82 μM by binding to WDR5. | ||||
| GC79148 | ZINC13000658 | 1324070-76-9 | >99.50% | |
ZINC13000658 is a METTL inhibitor. | ||||
| GC79194 | Exendin-4-Cys | - | >99.50% | |
Exendin-4 -Cys is a cysteine-modified Exendin-4. | ||||
| GC79195 | Semaglutide-FITC | - | >96.50% | |
Semaglutide -FITC (Semaglutide-Lys(FITC)) is a fluorescent tracer probe (Ex/Em = 495/520 nm) obtained by covalently coupling the green fluorescent dye fluorescein isothiocyanate (FITC) to the long-acting analogue of GLP-1, Semaglutide. | ||||
| GC79196 | Semaglutide, Cy5 labeled | - | >98.00% | |
Semaglutide, Cy5-labeled (Semaglutide-Cys(Cy5)) is a CY5 -labeled version of Semaglutide (Ex/Em = 633/670 nm). | ||||
| GC79227 | Sphingomab | - | >97.50% | |
Sphingomab (LT1002) is a mouse-derived IgG1 κ monoclonal antibody and also an inhibitor targeting S1P, with high affinity for S1P and a K d value of 0.03 ± 0.002 nM. | ||||
| GC79230 | BBO-11818 | 3029443-36-2 | >99.50% | |
BBO-11818 is an orally active, highly selective (relative to NRAS and HRAS ), non-covalent pan- KRAS inhibitor ( IC 50 =28-120 nM). | ||||
| GC79231 | RMC-4998 TFA | - | >99.00% | |
RMC-4998 TFA is an orally active inhibitor targeting the active or GTP-bound state of the KRAS G12C mutant. | ||||
