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)
- GC39095Isoliquiritin apiosideCAS: 120926-46-7纯度: >99.50%
Isoliquiritin apioside (ISLA, ILA), a component isolated from Glycyrrhizae radix rhizome (GR), significantly decreases PMA-induced increases in matrix metalloproteinase (MMP) activities and suppresses PMA-induced activation of mitogen-activated protein kinase (MAPK) and NF-κB. Isoliquiritin apioside possesses anti-metastatic and anti-angiogenic abilities in malignant cancer cells and ECs, with no cytotoxicity.
- GC39109IsodeoxyelephantopinCAS: 38927-54-7
Isodeoxyelephantopin 是一种倍半萜烯内酯,可从Elephantopus scaber 中分离得到。Isodeoxyelephantopin 可诱导活性氧的生成,抑制NF-κB 的激活。Isodeoxyelephantopin 还能调节LncRNA 的表达,有抗乳腺癌的作用。
- GC39134IsofraxidinCAS: 486-21-5纯度: >98.00%
Isofraxidin (6,8-Dimethoxyumbelliferone), a bioactive coumarin compound isolated from the functional foods Siberian ginseng and Apium graveolens, is an anti-bacterial, anti-oxidant, and anti-inflammatory agent.
- GC39148Pterosin BCAS: 34175-96-7纯度: >99.00%
Pterosin B 是一种从蕨菜 (Pteridium aquilinum) 中发现的茚满酮,是盐诱导性激酶 3 (Sik3) 信号转导的抑制剂。Pterosin B 通过抑制 Sik3 预防小鼠软骨细胞肥大和骨关节炎。
- GC39161ADU-S100 disodium saltCAS: 1638750-95-4纯度: >99.00% / >98.00%
ADU-S100 disodium salt(MIW815 disodium salt)是干扰素基因刺激蛋白(STING)的激活剂,Kd为4.61±0.42μM。
- GC39195YKL-06-062CAS: 2172617-16-0纯度: >98.00%
YKL-06-062 是第二代 salt-inducible kinase (SIK) 抑制剂,其 IC50 为 2.12 nM/1.40 nM/2.86 nM。YKL-06-062 是 YKL-06-061 的结构类似物。
- GC39209LCH-7749944CAS: 796888-12-5纯度: >99.00%
LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4.
- GC39239Rifamycin SCAS: 13553-79-2纯度: >98.00%
Rifamycin S, a quinone and an antibiotic against Gram-positive bacteria (including MRSA), is a clinical drug used to treat tuberculosis and leprosy. Rifamycin S generates reactive oxygen species (ROS) and inhibits microsomal lipid peroxidation.
- GC39254Anatabine dicitrate纯度: >99.00%
Anatabine dicitrate 是一种烟草生物碱,可以穿过血脑屏障。Anatabine dicitrate 是一种有效的 α4β2 nAChR 激动剂。Anatabine dicitrate 通过阻止淀粉样蛋白前体蛋白的 β 裂解,抑制 NF-κB 激活,并降低淀粉样 β (Aβ) 的产生。Anatabine dicitrate 具有抗炎作用,可用于神经退行性疾病的研究。
- GC39302PARP14 inhibitor H10CAS: 2084811-68-5纯度: >98.00%
PARP14 inhibitor H10 (化合物 H10) 是针对 PARP14 的选择性抑制剂 (IC50=490 nM),是其他 PARP 的抑制剂 (约为 PARP1 的 24 倍)。PARP14 抑制剂 H10 诱导 caspase-3/7 介导的细胞凋亡 (apoptosis)。
- GC39321(Rac)-MyrislignanCAS: 41535-95-9
(Rac)-Myrislignan 是Myrislignan 的外消旋体。 Myrislignan 是从Myristica fragrans Houtt 分离得到的一种木酚素,具有抗炎活性。Myrislignan 通过抑制NF-kB信号通路的激活,减轻LPS诱导的小鼠巨噬细胞炎症反应。
- GC393252,5-DihydroxyacetophenoneCAS: 490-78-8纯度: >99.50%
2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways.
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC39095 | Isoliquiritin apioside | 120926-46-7 | >99.50% | |
Isoliquiritin apioside (ISLA, ILA), a component isolated from Glycyrrhizae radix rhizome (GR), significantly decreases PMA-induced increases in matrix metalloproteinase (MMP) activities and suppresses PMA-induced activation of mitogen-activated protein kinase (MAPK) and NF-κB. Isoliquiritin apioside possesses anti-metastatic and anti-angiogenic abilities in malignant cancer cells and ECs, with no cytotoxicity. | ||||
| GC39100 | Rutaevin | 33237-37-5 | - | |
Rutaevin 从 Euodia rutaecarpa 中分离。 Rutaevin 能够抑制 Raw 264.7 巨噬细胞中 LPS 诱导的 NO 的产生。 | ||||
| GC39109 | Isodeoxyelephantopin | 38927-54-7 | - | |
Isodeoxyelephantopin 是一种倍半萜烯内酯,可从Elephantopus scaber 中分离得到。Isodeoxyelephantopin 可诱导活性氧的生成,抑制NF-κB 的激活。Isodeoxyelephantopin 还能调节LncRNA 的表达,有抗乳腺癌的作用。 | ||||
| GC39134 | Isofraxidin | 486-21-5 | >98.00% | |
Isofraxidin (6,8-Dimethoxyumbelliferone), a bioactive coumarin compound isolated from the functional foods Siberian ginseng and Apium graveolens, is an anti-bacterial, anti-oxidant, and anti-inflammatory agent. | ||||
| GC39135 | Ranaconitine | 1360-76-5 | - | |
An alkaloid with analgesic and anesthetic activities | ||||
| GC39148 | Pterosin B | 34175-96-7 | >99.00% | |
Pterosin B 是一种从蕨菜 (Pteridium aquilinum) 中发现的茚满酮,是盐诱导性激酶 3 (Sik3) 信号转导的抑制剂。Pterosin B 通过抑制 Sik3 预防小鼠软骨细胞肥大和骨关节炎。 | ||||
| GC39161 | ADU-S100 disodium salt | 1638750-95-4 | >99.00% / >98.00% | |
ADU-S100 disodium salt(MIW815 disodium salt)是干扰素基因刺激蛋白(STING)的激活剂,Kd为4.61±0.42μM。 | ||||
| GC39195 | YKL-06-062 | 2172617-16-0 | >98.00% | |
YKL-06-062 是第二代 salt-inducible kinase (SIK) 抑制剂,其 IC50 为 2.12 nM/1.40 nM/2.86 nM。YKL-06-062 是 YKL-06-061 的结构类似物。 | ||||
| GC39209 | LCH-7749944 | 796888-12-5 | >99.00% | |
LCH-7749944 (GNF-PF-2356) is a novel and potent p21-activated kinase 4 (PAK4) inhibitor with an IC50 of 14.93 μM and has less potently inhibitory effect against PAK1, PAK5 and PAK6. LCH-7749944 causes successful inhibition of EGFR activity due to its inhibitory effect on PAK4. | ||||
| GC39232 | Valepotriate | 18296-44-1 | - | |
A valepotriate with diverse biological activities | ||||
| GC39239 | Rifamycin S | 13553-79-2 | >98.00% | |
Rifamycin S, a quinone and an antibiotic against Gram-positive bacteria (including MRSA), is a clinical drug used to treat tuberculosis and leprosy. Rifamycin S generates reactive oxygen species (ROS) and inhibits microsomal lipid peroxidation. | ||||
| GC39254 | Anatabine dicitrate | - | >99.00% | |
Anatabine dicitrate 是一种烟草生物碱,可以穿过血脑屏障。Anatabine dicitrate 是一种有效的 α4β2 nAChR 激动剂。Anatabine dicitrate 通过阻止淀粉样蛋白前体蛋白的 β 裂解,抑制 NF-κB 激活,并降低淀粉样 β (Aβ) 的产生。Anatabine dicitrate 具有抗炎作用,可用于神经退行性疾病的研究。 | ||||
| GC39266 | Hematein | 475-25-2 | >65.00% | |
Hematein inhibits casein kinase II activity in a selective, dose-dependent and ATP non-competitive manner in vitro, with IC50 of 0.55 μM in the presence of 10 μM ATP. | ||||
| GC39271 | (±)-Naringenin | 67604-48-2 | >98.50% | |
A citrus- derived flavonoid | ||||
| GC39280 | B022 | 1202764-53-1 | >98.00% | |
B022是一种强效且选择性的NF-κB-inducing kinase (NIK)抑制剂,IC 50 值为15.1nM。 | ||||
| GC39281 | (R)-CR8 trihydrochloride | 1786438-30-9 | >99.00% | |
An inhibitor of cyclin-dependent kinases | ||||
| GC39284 | ANI-7 | 931417-26-4 | >99.00% | |
ANI-7 是一种 AhR 途径的激活剂。ANI-7 抑制多种癌细胞的生长,并有选择地抑制 MCF-7 乳腺癌细胞的生长,GI50 为 0.56 μM。ANI-7 通过激活 AhR 途径诱导 CYP1 代谢单加氧酶,并在敏感的乳腺癌细胞系中诱导 DNA 损伤,检查点激酶 (Chk2) 激活,S 期细胞周期停滞和细胞死亡。 | ||||
| GC39285 | CU-T12-9 | 1821387-73-8 | >98.00% / >99.00% | |
CU-T12-9是一种特异性Toll样受体TLR1/TLR2异二聚体的小分子激动剂,其EC 50 为52.9nM,CU-T12-9通过促进TLR1和TLR2二聚化,进而激活NF-κB信号通路 | ||||
| GC39295 | DJ001 | 2161305-12-8 | >99.50% | |
DJ001 是一种高度特异性,选择性和非竞争性的蛋白酪氨酸磷酸酶-σ (PTPσ) 抑制剂,IC50 为 1.43 μM。DJ001 对其他磷酸酶无抑制活性,对蛋白质磷酸酶 5 仅有中等抑制活性。DJ001 促进造血干细胞再生。 | ||||
| GC39296 | 1G244 | 847928-32-9 | >98.50% | |
1G244 是一种有效的 DPP8/9 抑制剂,IC50 分别为 12 nM 和 84 nM,但不抑制 DPPIV 和 DPPII。1G244 可诱导多发性骨髓瘤细胞凋亡,并具有抗骨髓瘤作用。 | ||||
| GC39302 | PARP14 inhibitor H10 | 2084811-68-5 | >98.00% | |
PARP14 inhibitor H10 (化合物 H10) 是针对 PARP14 的选择性抑制剂 (IC50=490 nM),是其他 PARP 的抑制剂 (约为 PARP1 的 24 倍)。PARP14 抑制剂 H10 诱导 caspase-3/7 介导的细胞凋亡 (apoptosis)。 | ||||
| GC39311 | YQ128 | 2454246-18-3 | >99.50% | |
An NLRP3 inflammasome inhibitor | ||||
| GC39321 | (Rac)-Myrislignan | 41535-95-9 | - | |
(Rac)-Myrislignan 是Myrislignan 的外消旋体。 Myrislignan 是从Myristica fragrans Houtt 分离得到的一种木酚素,具有抗炎活性。Myrislignan 通过抑制NF-kB信号通路的激活,减轻LPS诱导的小鼠巨噬细胞炎症反应。 | ||||
| GC39325 | 2,5-Dihydroxyacetophenone | 490-78-8 | >99.50% | |
2',5'-Dihydroxyacetophenone (DHAP, 2-Acetylhydroquinone, Quinacetophenone) is a mixture of dihydroxyacetophenone isomers is used in food flavouring. 2',5'-Dihydroxyacetophenone significantly inhibits NO production via the suppression of iNOS expression. 2',5'-Dihydroxyacetophenone significantly decreases levels of the pro-inflammatory cytokines TNF-α and IL-6 by blocking the ERK1/2 and NF-κB signaling pathways. | ||||
