Immunology/Inflammation
Immunology/Inflammation(免疫及炎症)
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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Immunology/Inflammation 相关产品(4245)
- GC393262-Iminobiotin hydrobromideCAS: 76985-52-9纯度: >98.00%
2-Iminobiotin hydrobromide (Guanidinobiotin hydrobromide) 是一种生物素 (维生素 H 或 B7) 类似物。2-Iminobiotin hydrobromide 是一种可逆的 NO 合酶抑制剂,作用于小鼠 iNOS 和大鼠 n-cNOS,Ki 值分别为 21.8 和 37.5 μM。2-Iminobiotin hydrobromide 与低温环境可保护人类神经细胞免受缺氧诱导的细胞损伤。
- GC39346BenralizumabCAS: 1044511-01-4纯度: >99.00%
Benralizumab (MEDI-563) 是一种白介素 5 受体 α (IL-5Rα) 定向的溶细胞单克隆抗体,通过增强抗体依赖性细胞介导的细胞毒性诱导嗜酸性粒细胞直接,快速和几乎完全耗尽。Benralizumab 可用于严重的嗜酸性哮喘。
- GC39355BTSA1CAS: 314761-14-3纯度: >99.00%
BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells.
- GC39372Desethyl chloroquine diphosphateCAS: 247912-76-1纯度: >99.00%
Desethyl chloroquine diphosphate 是 Chloroquine 的主要去乙基代谢产物。Chloroquine 是一种自噬和 toll-like receptors (TLRs) 的抑制剂。Desethyl chloroquine diphosphate 具有抗疟原虫活性。
- GC39388GW274150 phosphateCAS: 438542-15-5纯度: >98.50%
GW274150 phosphate 是一种有效的,选择性的,口服活性的 NADPH 依赖型人一氧化氮合成酶 (iNOS) (Kd=40 nM) 和大鼠 iNOS 抑制剂,对人和大鼠 eNOS 和 nNOS 均显示较低效力。GW274150 phosphate 在急性肺损伤炎症模型中发挥保护作用。
- GC39428QuinoclamineCAS: 2797-51-5纯度: >99.00%
Quinoclamine 是一种萘醌衍生物,是一种 NF-κB 抑制剂。Quinoclamine 具有抗肿瘤活性。
- GC39450Tea polyphenolCAS: 84650-60-2纯度: >99.00%
Tea polyphenols are chemical compounds such as flavanoids and tannins found naturally in tea. Several biological properties have been associated to tea polyphenols (TP), including antioxidant, anti-carcinogenic and antimicrobial activities.
- GC39489GPNA hydrochlorideCAS: 67953-08-6纯度: >99.00%
GPNA hydrochloride作为γ-谷氨酰转移酶(GGT)的底物,可抑制谷氨酰胺(Gln)转运蛋白ASCT2的活性,IC 50 为250μM。
- GC39500PDK4-IN-1 hydrochlorideCAS: 2310262-11-2纯度: >98.00%
PDK4-IN-1 hydrochloride 是一种蒽醌衍生物,也是一种有效的,口服活性的丙酮酸脱氢酶激酶 4 (PDK4) 抑制剂,IC50 值为 84 nM。PDK4-IN-1 hydrochloride 有效抑制细胞转化和细胞增殖并诱导细胞凋亡 (apoptosis)。PDK4-IN-1 hydrochloride 具有抗糖尿病,抗癌和抗过敏作用。
- GC39503PROTAC FKBP Degrader-3CAS: 2079056-43-0纯度: >98.00%
PROTAC FKBP Degrader-3 是一种包含 FKBP 配体结合基团,linker 和 VHL 结合基团的 PROTAC。PROTAC FKBP Degrader-3 是一种有效的 FKBP 降解剂。
- GC39555CDDO-2P-ImCAS: 1883650-96-1纯度: >98.00%
CDDO-2P-Im 是 CDDO 咪唑胺类似物,具有化学预防作用。CDDO-2P-Im 可降低小鼠肺癌模型肺肿瘤的大小和严重程度。
- GC39556CDDO-3P-ImCAS: 1883650-95-0纯度: >98.00%
CDDO-3P-Im 是 CDDO 咪唑胺类似物,具有化学预防作用。CDDO-3P-Im 可降低小鼠肺癌模型肺肿瘤的大小和严重程度。
- GC39564VamoroloneCAS: 13209-41-1纯度: >99.00%
Vamorolone (VBP15) 是首创的,具有口服活性的解离性类固醇 (dissociative steroidal) 抗炎药和膜稳定剂。Vamorolone 改善肌营养不良,无副作用。Vamorolone 抑制 (NF-κB) 抑制作用,并降低了激素的影响。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC39326 | 2-Iminobiotin hydrobromide | 76985-52-9 | >98.00% | |
2-Iminobiotin hydrobromide (Guanidinobiotin hydrobromide) 是一种生物素 (维生素 H 或 B7) 类似物。2-Iminobiotin hydrobromide 是一种可逆的 NO 合酶抑制剂,作用于小鼠 iNOS 和大鼠 n-cNOS,Ki 值分别为 21.8 和 37.5 μM。2-Iminobiotin hydrobromide 与低温环境可保护人类神经细胞免受缺氧诱导的细胞损伤。 | ||||
| GC39346 | Benralizumab | 1044511-01-4 | >99.00% | |
Benralizumab (MEDI-563) 是一种白介素 5 受体 α (IL-5Rα) 定向的溶细胞单克隆抗体,通过增强抗体依赖性细胞介导的细胞毒性诱导嗜酸性粒细胞直接,快速和几乎完全耗尽。Benralizumab 可用于严重的嗜酸性哮喘。 | ||||
| GC39355 | BTSA1 | 314761-14-3 | >99.00% | |
BTSA1 is a pharmacologically optimized BAX activator that binds with high affinity and specificity to the N-terminal activation site and induces conformational changes to BAX leading to BAX-mediated apoptosis. It effectively promotes apoptosis in leukemia cell lines and patient samples while sparing healthy cells. | ||||
| GC39365 | CPTH2 | 357649-93-5 | >99.50% | |
A HAT inhibitor | ||||
| GC39372 | Desethyl chloroquine diphosphate | 247912-76-1 | >99.00% | |
Desethyl chloroquine diphosphate 是 Chloroquine 的主要去乙基代谢产物。Chloroquine 是一种自噬和 toll-like receptors (TLRs) 的抑制剂。Desethyl chloroquine diphosphate 具有抗疟原虫活性。 | ||||
| GC39377 | EB-3D | 1839150-63-8 | >98.50% | |
EB-3D is a potent and selective inhibitor of choline kinase α (ChoKα) with IC50 of 1 μM for ChoKα1. EB-3D induces deregulation of the AMPK-mTOR pathway and apoptosis in leukemia T-cells. | ||||
| GC39382 | FW1256 | 117089-08-4 | >98.00% | |
FW1256 是一种苯基类似物,也是一种缓释硫化氢 (H2S) 供体。FW1256 抑制 NF-κB 活性,并可诱导细胞凋亡 (apoptosis),并可用于癌症,炎症和心血管疾病的研究。 | ||||
| GC39388 | GW274150 phosphate | 438542-15-5 | >98.50% | |
GW274150 phosphate 是一种有效的,选择性的,口服活性的 NADPH 依赖型人一氧化氮合成酶 (iNOS) (Kd=40 nM) 和大鼠 iNOS 抑制剂,对人和大鼠 eNOS 和 nNOS 均显示较低效力。GW274150 phosphate 在急性肺损伤炎症模型中发挥保护作用。 | ||||
| GC39415 | OR-1896 | 220246-81-1 | >98.50% | |
OR-1896 是 Levosimendan 的活性长寿代谢产物。OR-1896 是一种高选择性磷酸二酯酶 (PDE III) 抑制剂,是一种功能强大的血管扩张剂。OR-1896 可以打开 ATP 敏感的 K+ 通道,并具有 Ca2+ 致敏作用。OR-1896 可减轻心肌细胞的凋亡,心脏重塑和心肌炎症。 | ||||
| GC39428 | Quinoclamine | 2797-51-5 | >99.00% | |
Quinoclamine 是一种萘醌衍生物,是一种 NF-κB 抑制剂。Quinoclamine 具有抗肿瘤活性。 | ||||
| GC39430 | Reslizumab | 241473-69-8 | >99.00% | |
Reslizumab是一种靶向IL-5分子的人源化IgG4/κ单克隆抗体,K d 值为81pM。 | ||||
| GC39450 | Tea polyphenol | 84650-60-2 | >99.00% | |
Tea polyphenols are chemical compounds such as flavanoids and tannins found naturally in tea. Several biological properties have been associated to tea polyphenols (TP), including antioxidant, anti-carcinogenic and antimicrobial activities. | ||||
| GC39483 | BO-264 | 2408648-20-2 | >99.50% | |
A TACC3 inhibitor | ||||
| GC39485 | CK2/ERK8-IN-1 | 1085822-09-8 | >99.00% | |
A dual inhibitor of CK2 and ERK8 | ||||
| GC39489 | GPNA hydrochloride | 67953-08-6 | >99.00% | |
GPNA hydrochloride作为γ-谷氨酰转移酶(GGT)的底物,可抑制谷氨酰胺(Gln)转运蛋白ASCT2的活性,IC 50 为250μM。 | ||||
| GC39500 | PDK4-IN-1 hydrochloride | 2310262-11-2 | >98.00% | |
PDK4-IN-1 hydrochloride 是一种蒽醌衍生物,也是一种有效的,口服活性的丙酮酸脱氢酶激酶 4 (PDK4) 抑制剂,IC50 值为 84 nM。PDK4-IN-1 hydrochloride 有效抑制细胞转化和细胞增殖并诱导细胞凋亡 (apoptosis)。PDK4-IN-1 hydrochloride 具有抗糖尿病,抗癌和抗过敏作用。 | ||||
| GC39503 | PROTAC FKBP Degrader-3 | 2079056-43-0 | >98.00% | |
PROTAC FKBP Degrader-3 是一种包含 FKBP 配体结合基团,linker 和 VHL 结合基团的 PROTAC。PROTAC FKBP Degrader-3 是一种有效的 FKBP 降解剂。 | ||||
| GC39512 | Tempo | 2564-83-2 | - | |
Tempo 是一种经典的一氧化氮自由基,也 是一种线粒体 ROS 的选择性清除剂,可在催化循环中使超氧化物歧化。Tempo 可诱导 DNA 链断裂,并可用作将伯醇氧化为醛的有机催化剂。Tempo 具有诱变和抗氧化作用。 | ||||
| GC39515 | TP508 TFA | - | >99.00% | |
TP508 TFA 是一种 23 个氨基酸的非蛋白水解凝血酶肽,代表凝血酶分子受体结合结构域的一部分。TP508 TFA 可激活内皮 NO synthase (eNOS) 并刺激人内皮细胞中 NO 的产生。TP508 TFA 通过激活内皮细胞和干细胞以使血管再生和组织再生。 | ||||
| GC39551 | BRD3308 | 1550053-02-5 | >98.00% | |
An HDAC3 inhibitor | ||||
| GC39554 | AT2 receptor agonist C21 | 477775-14-7 | >99.00% | |
An AT 2 receptor agonist | ||||
| GC39555 | CDDO-2P-Im | 1883650-96-1 | >98.00% | |
CDDO-2P-Im 是 CDDO 咪唑胺类似物,具有化学预防作用。CDDO-2P-Im 可降低小鼠肺癌模型肺肿瘤的大小和严重程度。 | ||||
| GC39556 | CDDO-3P-Im | 1883650-95-0 | >98.00% | |
CDDO-3P-Im 是 CDDO 咪唑胺类似物,具有化学预防作用。CDDO-3P-Im 可降低小鼠肺癌模型肺肿瘤的大小和严重程度。 | ||||
| GC39564 | Vamorolone | 13209-41-1 | >99.00% | |
Vamorolone (VBP15) 是首创的,具有口服活性的解离性类固醇 (dissociative steroidal) 抗炎药和膜稳定剂。Vamorolone 改善肌营养不良,无副作用。Vamorolone 抑制 (NF-κB) 抑制作用,并降低了激素的影响。 | ||||
