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)
- GC39600Iron sucroseCAS: 8047-67-4纯度: >98.00%
Iron sucrose (Iron saccharate, Sucroferric oxyhydroxide) is an intravenously administered iron product indicated in the treatment of iron deficiency anemia.
- GC39603Methylene blue trihydrateCAS: 7220-79-3纯度: >99.00%
Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) 是一种鸟苷酸环化酶 (sGC),单胺氧化酶 A (MAO-A) 和 NO 合酶 (NOS) 抑制剂。Methylene blue trihydrate 是一种血管加压药,在医疗中通常用作染料。Methylene blue trihydrate 具有抗伤害感受,抗疟疾,抗抑郁和抗焦虑作用,可用于高铁血红蛋白血症,神经退行性疾病和异环磷酰胺引起的脑病的研究。
- GC39640GPLGIAGQ TFA纯度: >99.50% / >98.00%
GPLGIAGQ TFA 是一种 MMP2 可切割的多肽,在脂质体和胶束纳米载体中都被用作刺激敏感的连接物,用于 MMP2 触发的肿瘤靶向治疗。GPLGIAGQ TFA可用于合成光动力治疗 (PDT) 中独特的 MMP2 靶向光敏剂。
- GC39669AHR antagonist 2CAS: 2338747-54-7纯度: >99.00%
AHR antagonist 2 是一种有效的芳香烃受体 (AHR) 拮抗剂,对人和小鼠的 IC50 值分别为 0.885,2.03 nM,详情请参见专利 WO2019101641A1,example 1。
- GC39699Aurintricarboxylic acidCAS: 4431-00-9
A protein synthesis inhibitor with diverse biological activities
- GC39701ConvallatoxinCAS: 508-75-8纯度: >98.00%
Convallatoxin 是从 Adonis amurensis Regel et Radde 分离得到的强心苷。Convallatoxin 通过激活 PPARγ 和抑制 NF-κB 改善结肠炎。Convallatoxin 是一种 P-糖蛋白 (P-gp) 底物,并识别 Val982 是参与其转运的重要氨基酸。Convallatoxin 是配体诱导的 MOR 胞吞作用的增强剂,具有很高的效力和功效。具有抗炎和抗增殖特性。
- GC39747(E/Z)-GSK5182CAS: 2699724-40-6纯度: >98.50%
(E/Z)-GSK5182 是 (E)-GSK5182 和 (Z)-GSK5182 的消旋体。GSK5182 是一种高效选择性,具有口服活性的 ERRγ 反向激动剂,其 IC50 值为 79 nM。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。
- GC39798ScoulerineCAS: 6451-73-6纯度: >99.00%
A benzylisoquinoline alkaloid with diverse biological activities
- GC39808DidesmethylrocaglamideCAS: 177262-30-5纯度: >98.00%
Didesmethylrocaglamide 是一种 Rocaglamide 的衍生物,也是一种有效的真核起始因子 4A (eIF4A) 抑制剂。Didesmethylrocaglamide 具有有效的生长抑制活性,IC50 为 5 nM。Didesmethylrocaglamide 抑制多种促进生长的信号通路,并诱导肿瘤细胞凋亡 (apoptosis)。抗肿瘤活性。
- GC39814MitoguazoneCAS: 459-86-9纯度: >98.00%
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) 是一种具有有效抗肿瘤活性的合成多羰基衍生物。Mitoguazone 是一种可透过血脑屏障的竞争性的 S-腺苷-蛋氨酸脱羧酶 (S-adenosyl-methionine decarboxylase) 抑制剂,可破坏多胺的生物合成。Mitoguazone 诱导细胞凋亡 (apoptosis),可抑制 HIV DNA 整合到单核细胞和巨噬细胞中的细胞 DNA 中。Mitoguazone 具可用于急性白血病,霍奇金淋巴瘤和非霍奇金淋巴瘤的研究。
- GC39815Semapimod tetrahydrochlorideCAS: 164301-51-3纯度: >98.00%
Semapimod tetrahydrochloride (CNI-1493) 是促炎细胞因子产生 (proinflammatory cytokine) 的抑制剂,可抑制TNF-α、IL-1β 和 IL-6。Semapimod tetrahydrochloride 抑制巨噬细胞 p38 MAPK 和一氧化氮生成。Semapimod tetrahydrochloride 抑制 TLR4 信号 (IC50≈0.3 μM)。Semapimod tetrahydrochloride 在多种炎症和自身免疫性疾病中具有潜在的作用。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC39584 | AGN194204 | 220619-73-8 | >99.00% | |
AGN194204 (IRX4204) 是一种具有口服活性的,选择性 RXR 激动剂,对 RXRα,RXRβ 和 RXRγ 的 Kd 值分别为 0.4 nM,3.6 nM 和 3.8 nM,EC50 分别为 0.2 nM,0.8 nM 和 0.08 nM。AGN194204 对 RAR 无活性,并具有抗炎和抗癌作用。 | ||||
| GC39600 | Iron sucrose | 8047-67-4 | >98.00% | |
Iron sucrose (Iron saccharate, Sucroferric oxyhydroxide) is an intravenously administered iron product indicated in the treatment of iron deficiency anemia. | ||||
| GC39603 | Methylene blue trihydrate | 7220-79-3 | >99.00% | |
Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) 是一种鸟苷酸环化酶 (sGC),单胺氧化酶 A (MAO-A) 和 NO 合酶 (NOS) 抑制剂。Methylene blue trihydrate 是一种血管加压药,在医疗中通常用作染料。Methylene blue trihydrate 具有抗伤害感受,抗疟疾,抗抑郁和抗焦虑作用,可用于高铁血红蛋白血症,神经退行性疾病和异环磷酰胺引起的脑病的研究。 | ||||
| GC39623 | DCC-3014 | 1628606-05-2 | >99.00% | |
Vimseltinib (DCC-3014) is a c-FMS (CSF-IR) and c-Kit dual inhibitor extracted from patent WO2014145025A2, Compound Example 10, has IC50s of <0.01 μM and 0.1-1 μM, respectively. | ||||
| GC39640 | GPLGIAGQ TFA | - | >99.50% / >98.00% | |
GPLGIAGQ TFA 是一种 MMP2 可切割的多肽,在脂质体和胶束纳米载体中都被用作刺激敏感的连接物,用于 MMP2 触发的肿瘤靶向治疗。GPLGIAGQ TFA可用于合成光动力治疗 (PDT) 中独特的 MMP2 靶向光敏剂。 | ||||
| GC39664 | PF-3450074 | 1352879-65-2 | >99.00% | |
An inhibitor of HIV-1 capsid protein | ||||
| GC39669 | AHR antagonist 2 | 2338747-54-7 | >99.00% | |
AHR antagonist 2 是一种有效的芳香烃受体 (AHR) 拮抗剂,对人和小鼠的 IC50 值分别为 0.885,2.03 nM,详情请参见专利 WO2019101641A1,example 1。 | ||||
| GC39699 | Aurintricarboxylic acid | 4431-00-9 | - | |
A protein synthesis inhibitor with diverse biological activities | ||||
| GC39701 | Convallatoxin | 508-75-8 | >98.00% | |
Convallatoxin 是从 Adonis amurensis Regel et Radde 分离得到的强心苷。Convallatoxin 通过激活 PPARγ 和抑制 NF-κB 改善结肠炎。Convallatoxin 是一种 P-糖蛋白 (P-gp) 底物,并识别 Val982 是参与其转运的重要氨基酸。Convallatoxin 是配体诱导的 MOR 胞吞作用的增强剂,具有很高的效力和功效。具有抗炎和抗增殖特性。 | ||||
| GC39707 | Droloxifene | 82413-20-5 | >99.50% | |
A selective estrogen receptor modulator | ||||
| GC39708 | DT2216 | 2365172-42-3 | - | |
DT2216 是一种蛋白水解靶向嵌合体 (PROTAC),靶向 Bcl-xL 降解依赖于 Bcl-2 家族过表达蛋白(例如 Bcl-2、Bcl-xL 和 Mcl)的 T 细胞淋巴瘤-1.DT2216 抑制 G-68 细胞,IC50 值为 4.02 μM(72 小时)。 | ||||
| GC39719 | Nigericin | 28380-24-7 | >98.00% / >97.00% | |
A potassium ionophore | ||||
| GC39747 | (E/Z)-GSK5182 | 2699724-40-6 | >98.50% | |
(E/Z)-GSK5182 是 (E)-GSK5182 和 (Z)-GSK5182 的消旋体。GSK5182 是一种高效选择性,具有口服活性的 ERRγ 反向激动剂,其 IC50 值为 79 nM。GSK5182 还能增加肝癌细胞中 reactive oxyen species (ROS) 的产生。 | ||||
| GC39756 | N-Acetyl-D-cysteine | 26117-28-2 | - | |
N-Acetyl-D-cysteine 具有抗氧化活性,通过与巯基反应清除 ROS,但不能进入谷胱甘肽代谢途径。 | ||||
| GC39760 | 5-Galloylquinic acid | 53584-43-3 | - | |
5-Galloylquinic acid 是绿茶中活性氧 (ROS) 的主要清除剂。 | ||||
| GC39798 | Scoulerine | 6451-73-6 | >99.00% | |
A benzylisoquinoline alkaloid with diverse biological activities | ||||
| GC39808 | Didesmethylrocaglamide | 177262-30-5 | >98.00% | |
Didesmethylrocaglamide 是一种 Rocaglamide 的衍生物,也是一种有效的真核起始因子 4A (eIF4A) 抑制剂。Didesmethylrocaglamide 具有有效的生长抑制活性,IC50 为 5 nM。Didesmethylrocaglamide 抑制多种促进生长的信号通路,并诱导肿瘤细胞凋亡 (apoptosis)。抗肿瘤活性。 | ||||
| GC39811 | FIT-039 | 1113044-49-7 | >98.00% | |
A Cdk9 inhibitor | ||||
| GC39814 | Mitoguazone | 459-86-9 | >98.00% | |
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) 是一种具有有效抗肿瘤活性的合成多羰基衍生物。Mitoguazone 是一种可透过血脑屏障的竞争性的 S-腺苷-蛋氨酸脱羧酶 (S-adenosyl-methionine decarboxylase) 抑制剂,可破坏多胺的生物合成。Mitoguazone 诱导细胞凋亡 (apoptosis),可抑制 HIV DNA 整合到单核细胞和巨噬细胞中的细胞 DNA 中。Mitoguazone 具可用于急性白血病,霍奇金淋巴瘤和非霍奇金淋巴瘤的研究。 | ||||
| GC39815 | Semapimod tetrahydrochloride | 164301-51-3 | >98.00% | |
Semapimod tetrahydrochloride (CNI-1493) 是促炎细胞因子产生 (proinflammatory cytokine) 的抑制剂,可抑制TNF-α、IL-1β 和 IL-6。Semapimod tetrahydrochloride 抑制巨噬细胞 p38 MAPK 和一氧化氮生成。Semapimod tetrahydrochloride 抑制 TLR4 信号 (IC50≈0.3 μM)。Semapimod tetrahydrochloride 在多种炎症和自身免疫性疾病中具有潜在的作用。 | ||||
| GC39820 | Lometrexol hydrate | 1435784-14-7 | >99.00% | |
A GART inhibitor | ||||
| GC39827 | HM03 | 500565-15-1 | >99.50% | |
HM03 是一种有效的选择性的热休克 70 kDa 蛋白 5, HSPA5 (也称为 Bip,Grp78) 抑制剂,具有抗肿瘤活性。 | ||||
| GC40004 | Quinolactacin A | 319917-25-4 | >95.00% | |
A fungal metabolite | ||||
| GC40005 | Aurodox | 12704-90-4 | 85%(mixture of tautomers) | |
A polyketide antibiotic | ||||
