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)
- GC36578MD2-TLR4-IN-1CAS: 2249801-12-3纯度: >99.50%
MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively.
- GC36649mPGES1-IN-3CAS: 1469976-70-2
mPGES1-IN-3 (Compound 17d) 是一种有效的选择性微粒体前列腺素 E2 合成酶-1 (mPGES-1) 抑制剂,抑制 mPGES-1 酶,IC50 为 8 nM,抑制 A549 细胞,IC50 为 16.24 nM。
- GC36757NO-prednisoloneCAS: 327610-87-7纯度: >98.50%
NO-prednisolone 是释放一氧化氮 (NO) 的 Prednisolone 衍生物。NO-prednisolone 有效刺激体内 IL-10 产生。
- GC36914Piceatannol 3'-O-glucosideCAS: 94356-26-0纯度: >99.50%
Piceatannol 3'-O-glucoside 是 Rhubarb 的一种活性成分,通过抑制精氨酸酶 (Arginase) 活性激活内皮细胞一氧化氮合酶 (NO synthase),抑制 Arginase I 和 Arginase II,IC50 值分别为 11.22 μM 和 11.06 μM。
- GC37036PTD-p65-P1 Peptide
PTD-p65-P1 Peptide 是一种核转录因子 NF-kappaB 抑制剂,由一个 antennapedia 衍生的膜转运肽序列 (PTD) 连接 p65-P1 构成, 选择性地抑制由各种刺激诱导的 NF-kappaB 活性。
- GC37531Riboflavin TetrabutyrateCAS: 752-56-7纯度: >98.00%
Riboflavin tetrabutyrate is a lipophilic flavin derivative with antioxidative and lipid peroxide-removing activity.
- GC37661Sodium formononetin-3'-sulfonateCAS: 949021-68-5纯度: >99.50%
Sodium formononetin-3'-sulfonate (Sul-F)是formononetin的水溶性衍生物。
- GC37686StachydrineCAS: 471-87-4纯度: >98.00%
A pyrrolidine betaine with anticancer and cardiopro tective effects
- GC37700Succinyl phosphonate trisodium saltCAS: 864167-45-3纯度: >98.00% / >99.50%
Succinyl phosphonate trisodium salt (SP) 琥珀酰膦酸三钠盐是 α-酮戊二酸脱氢酶 (KGDHC ) 抑制剂,可有效抑制肌肉,细菌,脑和人成纤维细胞中的 KGDHC。Succinyl phosphonate trisodium salt (SP) 抑制 2-氧代戊二酸脱氢酶 (OGDH),以细胞特异性代谢依赖性方式损害癌细胞的活力。Succinyl phosphonate trisodium salt (SP) 抑制谷氨酸诱导的谷氨酸刺激的海马神经元中的 ROS 产生。
- GC37747TBK1/IKKε-IN-1CAS: 2058264-32-5
TBK1/IKKε-IN-1 是一种双重 TBK1 和 IKKε 抑制剂,IC50s 值 <100 nM。详细信息请参考专利文献 US20160376283 A1 中 Example 60 中的化合物 274。
- GC37748TBK1/IKKε-IN-5CAS: 1893397-65-3纯度: >99.50%
TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo.
- GC37850Tyrphostin A1CAS: 2826-26-8纯度: >99.50%
Tyrphostin A1(AG9)能抑制巨噬细胞培养中CD40L刺激的IL-12产生和抗原诱导的Th1细胞生成。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC36472 | LNP023 | 1644670-37-0 | >99.50% | |
LNP023 (LNP023) 是一流的、具有口服生物利用度的、高效和高选择性的因子 B 抑制剂,IC50 值为 10 nM。 | ||||
| GC36492 | Luciferase | 9014-00-0 | - | |
Luciferase是一种能够催化生物发光反应的酶。 | ||||
| GC36578 | MD2-TLR4-IN-1 | 2249801-12-3 | >99.50% | |
MD2-TLR4-IN-1 (Compound 22m) is a potent inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4). MD2-TLR4-IN-1 (compound 22m) inhibits lipopolysaccharide (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 of 0.89 μM and 0.53 μM, respectively. | ||||
| GC36587 | MethADP | 3768-14-7 | - | |
MethADP 是一个特异性的 CD73 抑制剂。 | ||||
| GC36588 | MethADP sodium salt | 89016-30-8 | - | |
MethADP (sodium salt) 是一个特异性的 CD73 抑制剂。 | ||||
| GC36649 | mPGES1-IN-3 | 1469976-70-2 | - | |
mPGES1-IN-3 (Compound 17d) 是一种有效的选择性微粒体前列腺素 E2 合成酶-1 (mPGES-1) 抑制剂,抑制 mPGES-1 酶,IC50 为 8 nM,抑制 A549 细胞,IC50 为 16.24 nM。 | ||||
| GC36696 | Naringin Dihydrochalcone | 18916-17-1 | >99.50% | |
A flavonoid with antioxidant activity | ||||
| GC36757 | NO-prednisolone | 327610-87-7 | >98.50% | |
NO-prednisolone 是释放一氧化氮 (NO) 的 Prednisolone 衍生物。NO-prednisolone 有效刺激体内 IL-10 产生。 | ||||
| GC36773 | Nrf2-IN-1 | 1610022-76-8 | >98.50% / >98.00% | |
Nrf2-IN-1是nuclear factor-erythroid 2-related factor 2 (Nrf2)的抑制剂,用于急性髓系白血病(AML)的研究。 | ||||
| GC36794 | Okanin | 484-76-4 | >98.00% | |
Okanin 是 Coreopsis tinctoria 的有效成分。Okanin 通过抑制 TLR4/NF-κB 信号通路减弱 LPS 诱导的小胶质细胞活化。 | ||||
| GC36914 | Piceatannol 3'-O-glucoside | 94356-26-0 | >99.50% | |
Piceatannol 3'-O-glucoside 是 Rhubarb 的一种活性成分,通过抑制精氨酸酶 (Arginase) 活性激活内皮细胞一氧化氮合酶 (NO synthase),抑制 Arginase I 和 Arginase II,IC50 值分别为 11.22 μM 和 11.06 μM。 | ||||
| GC37036 | PTD-p65-P1 Peptide | - | - | |
PTD-p65-P1 Peptide 是一种核转录因子 NF-kappaB 抑制剂,由一个 antennapedia 衍生的膜转运肽序列 (PTD) 连接 p65-P1 构成, 选择性地抑制由各种刺激诱导的 NF-kappaB 活性。 | ||||
| GC37531 | Riboflavin Tetrabutyrate | 752-56-7 | >98.00% | |
Riboflavin tetrabutyrate is a lipophilic flavin derivative with antioxidative and lipid peroxide-removing activity. | ||||
| GC37603 | SC144 hydrochloride | 917497-70-2 | >99.00% | |
A gp130 inhibitor | ||||
| GC37661 | Sodium formononetin-3'-sulfonate | 949021-68-5 | >99.50% | |
Sodium formononetin-3'-sulfonate (Sul-F)是formononetin的水溶性衍生物。 | ||||
| GC37686 | Stachydrine | 471-87-4 | >98.00% | |
A pyrrolidine betaine with anticancer and cardiopro tective effects | ||||
| GC37692 | STING agonist-3 | 2138299-29-1 | >99.50% | |
A STING agonist | ||||
| GC37693 | STING agonist-4 | 2138300-40-8 | >98.00% | |
A STING agonist | ||||
| GC37700 | Succinyl phosphonate trisodium salt | 864167-45-3 | >98.00% / >99.50% | |
Succinyl phosphonate trisodium salt (SP) 琥珀酰膦酸三钠盐是 α-酮戊二酸脱氢酶 (KGDHC ) 抑制剂,可有效抑制肌肉,细菌,脑和人成纤维细胞中的 KGDHC。Succinyl phosphonate trisodium salt (SP) 抑制 2-氧代戊二酸脱氢酶 (OGDH),以细胞特异性代谢依赖性方式损害癌细胞的活力。Succinyl phosphonate trisodium salt (SP) 抑制谷氨酸诱导的谷氨酸刺激的海马神经元中的 ROS 产生。 | ||||
| GC37705 | Suramin | 145-63-1 | >98.00% | |
A polysulfonated naphthylurea with antiviral, antiparasitic, and anticancer activities | ||||
| GC37747 | TBK1/IKKε-IN-1 | 2058264-32-5 | - | |
TBK1/IKKε-IN-1 是一种双重 TBK1 和 IKKε 抑制剂,IC50s 值 <100 nM。详细信息请参考专利文献 US20160376283 A1 中 Example 60 中的化合物 274。 | ||||
| GC37748 | TBK1/IKKε-IN-5 | 1893397-65-3 | >99.50% | |
TBK1/IKKε-IN-1 (compound 1) is a dual inhibitor of TANK-binding kinase 1 (TBK1) and IκB kinase-ε (IKKε/IKK-i) with IC50 of 1.0 nM and 5.6 nM for TBK1 and IKKε, respectively. TBK1/IKKε inhibition enhances response to PD-1 blockade, which effectively predicts tumor response in vivo. | ||||
| GC37809 | Tocilizumab | 375823-41-9 | >99.50% | |
Tocilizumab 作为一种人源化单克隆抗体,可以靶向 IL-6 受体的膜结合和可溶形式。 | ||||
| GC37850 | Tyrphostin A1 | 2826-26-8 | >99.50% | |
Tyrphostin A1(AG9)能抑制巨噬细胞培养中CD40L刺激的IL-12产生和抗原诱导的Th1细胞生成。 | ||||
