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)
- GC60354Tat-NR2BaaCAS: 847829-41-8
Tat-NR2BAA 是 Tat-NR2B9c 的对照肽 (control peptide),没有活性。Tat-NR2BAA 的序列与 Tat-NR2B9c 相似,但在 COOH 末端 tSXV 基序中有一个双点突变,这使得它无法结合 PSD-95。Tat-NR2B9c 是一种可通透细胞膜的多肽,破坏 PSD-95/NMDAR 的结合。
- GC60364ThienopyridoneCAS: 1018454-97-1纯度: >98.00%
Thienopyridone 是一种有效的选择性的肝再生磷酸酶 (PRL) 磷酸酶抑制剂,对于 PRL-1,PRL-2 和 PRL-3,IC50 值分别为 173 nM,277 nM 和 128 nM。Thienopyridone 对其他磷酸酶的影响很小。Thienopyridone 可诱导 p130Cas 裂解和细胞凋亡 (apoptosis),并具有抗癌作用。
- GC60377Urolithin CCAS: 165393-06-6纯度: >97.00%
UrolithinC,是鞣花酸的多酚类肠道微生物代谢产物,是胰岛素分泌(insulinsecretion)的葡萄糖依赖性激活剂。UrolithinC是一种L型Ca2+通道开放剂,可增强Ca2+的流入。UrolithinC通过线粒体介导的途径诱导细胞凋亡(apoptosis),并刺激活性氧(ROS)的形成。
- GC60398(6R)-FR054CAS: 10378-06-0纯度: >98.00%
(6R)-FR054是FR054的一个活性异构体。FR054是HBP酶PGM3的抑制剂,具有显著的抗乳腺癌活性。FR054可诱导内质网应激和ROS依赖的细胞凋亡。
- GC60407(R)-Verapamil D7 hydrochloride
(R)-VerapamilD7hydrochloride((R)-(+)-VerapamilD7hydrochloride)是(R)-Verapamilhydrochloride的一种氘代化合物。(R)-Verapamilhydrochloride((R)-(+)-Verapamilhydrochloride)是一种P-糖蛋白抑制剂。(R)-Verapamilhydrochloride抑制MRP1介导的转运,导致MRP1过表达细胞对抗癌药产生化学敏感性。
- GC60408(R)-Verapamil hydrochlorideCAS: 38176-02-2纯度: >98.50%
(R)-Verapamilhydrochloride((R)-(+)-Verapamilhydrochloride)是一种P-糖蛋白(P-Glycoprotein)抑制剂。(R)-Verapamilhydrochloride抑制MRP1介导的转运,导致MRP1过表达细胞对抗癌药产生化学敏感性。
- GC60425(S)-Verapamil D7 hydrochloride
(S)-VerapamilD7hydrochloride((S)-(-)-VerapamilD7hydrochloride)是(S)-Verapamilhydrochloride的一种氘代化合物。(S)-Verapamilhydrochloride(S(-)-Verapamilhydrochloride)通过MRP1抑制白三烯C4(LTC4)和钙黄绿素的转运。(S)-Verapamilhydrochloride导致潜在耐药性肿瘤细胞死亡。
- GC6046721-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dioneCAS: 37413-91-5纯度: >99.50%
21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione是delta9,11类固醇类合成的中间体(intermediate),如Vamorolone 。delta9,11steroids是糖皮质激素的修饰后的产物,具有抗炎(anti-inflammatory)特性。delta9,11类固醇类可以用作保护细胞损伤(脂质过氧化)和抑制新生血管的试剂。
- GC605073-O-Methylgallic acidCAS: 3934-84-7纯度: >97.00%
3-O-Methylgallicacid(3,4-Dihydroxy-5-methoxybenzoicacid)是一种花青素代谢产物,具有强大的抗氧化能力。3-O-Methylgallicacid能抑制Caco-2细胞增殖,IC50值为24.1μM。3-O-Methylgallicacid还诱导细胞凋亡(apoptosis)并具有抗癌作用。
- GC605254-Vinylphenol (10%w/w in propylene glycol)CAS: 2628-17-3纯度: 不显示
4-Vinylphenol存在于药用草白花蛇舌草,野生稻中,也是葡萄酒中乳酸菌对对香豆酸和阿魏酸的代谢产物。4-Vinylphenol诱导凋亡(apoptosis),在体内抑制血管形成并抑制浸润性乳腺肿瘤生长。
- GC60584Angiotensin II human acetateCAS: 68521-88-0纯度: {{1-5}>99.00% / {6-13}>98.00%}
A peptide hormone
- GC60603Asperosaponin VICAS: 39524-08-8纯度: >98.00%
A triterpenoid saponin with diverse biological activities
- GC60616AZT triphosphateCAS: 92586-35-1
AZTtriphosphate(3'-Azido-3'-deoxythymidine-5'-triphosphate)是一种Zidovudine(AZT)的活性三磷酸酯代谢产物。AZTtriphosphate具有抗逆转录病毒的活性,并抑制HIV复制。AZTtriphosphate还可抑制HBV的DNA聚合酶。AZTtriphosphate可激活线粒体介导的凋亡(apoptosis)途径。
- GC60617AZT triphosphate TEA
AZTtriphosphateTFA(3'-Azido-3'-deoxythymidine-5'-triphosphateTFA)是一种Zidovudine(AZT)的活性三磷酸酯代谢产物。AZTtriphosphateTFA具有抗逆转录病毒的活性,并抑制HIV复制。AZTtriphosphateTFA还可抑制HBV的DNA聚合酶。AZTtriphosphateTFA可激活线粒体介导的凋亡(apoptosis)途径。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC60344 | Sparstolonin B | 1259330-61-4 | - | |
An isocoumarin with diverse biological activities | ||||
| GC60348 | Supinoxin | 888478-45-3 | >99.50% | |
Supinoxin (RX-5902) 是磷酸化 p68 RNA 解旋酶 (P-p68) 的强效口服活性抑制剂,并且是一个一流的抗肿瘤试剂 (anti-cancer agent)。Supinoxin 与 Y593 磷酸化的 p68 相互作用并减弱 β-catenin 的核穿梭性。 Supinoxin 诱导细胞凋亡 (apoptosis) 并抑制 TNBC 癌细胞系的生长,IC50 的范围为 10 nM 至 20 nM。 | ||||
| GC60352 | Taraxerol | 127-22-0 | >98.00% | |
Taraxerol 具有抗炎和抗癌作用。 | ||||
| GC60354 | Tat-NR2Baa | 847829-41-8 | - | |
Tat-NR2BAA 是 Tat-NR2B9c 的对照肽 (control peptide),没有活性。Tat-NR2BAA 的序列与 Tat-NR2B9c 相似,但在 COOH 末端 tSXV 基序中有一个双点突变,这使得它无法结合 PSD-95。Tat-NR2B9c 是一种可通透细胞膜的多肽,破坏 PSD-95/NMDAR 的结合。 | ||||
| GC60364 | Thienopyridone | 1018454-97-1 | >98.00% | |
Thienopyridone 是一种有效的选择性的肝再生磷酸酶 (PRL) 磷酸酶抑制剂,对于 PRL-1,PRL-2 和 PRL-3,IC50 值分别为 173 nM,277 nM 和 128 nM。Thienopyridone 对其他磷酸酶的影响很小。Thienopyridone 可诱导 p130Cas 裂解和细胞凋亡 (apoptosis),并具有抗癌作用。 | ||||
| GC60376 | UC2288 | 1394011-91-6 | >99.50% | |
UC2288 is a novel, cell-permeable, and orally active p21 attenuator, decreases p21 mRNA expression independently of p53, and attenuates p21 protein levels with minimal effect on p21 protein stability. | ||||
| GC60377 | Urolithin C | 165393-06-6 | >97.00% | |
UrolithinC,是鞣花酸的多酚类肠道微生物代谢产物,是胰岛素分泌(insulinsecretion)的葡萄糖依赖性激活剂。UrolithinC是一种L型Ca2+通道开放剂,可增强Ca2+的流入。UrolithinC通过线粒体介导的途径诱导细胞凋亡(apoptosis),并刺激活性氧(ROS)的形成。 | ||||
| GC60397 | (5Z,2E)-CU-3 | 1815598-71-0 | >98.00% | |
A DGK-α inhibitor | ||||
| GC60398 | (6R)-FR054 | 10378-06-0 | >98.00% | |
(6R)-FR054是FR054的一个活性异构体。FR054是HBP酶PGM3的抑制剂,具有显著的抗乳腺癌活性。FR054可诱导内质网应激和ROS依赖的细胞凋亡。 | ||||
| GC60407 | (R)-Verapamil D7 hydrochloride | - | - | |
(R)-VerapamilD7hydrochloride((R)-(+)-VerapamilD7hydrochloride)是(R)-Verapamilhydrochloride的一种氘代化合物。(R)-Verapamilhydrochloride((R)-(+)-Verapamilhydrochloride)是一种P-糖蛋白抑制剂。(R)-Verapamilhydrochloride抑制MRP1介导的转运,导致MRP1过表达细胞对抗癌药产生化学敏感性。 | ||||
| GC60408 | (R)-Verapamil hydrochloride | 38176-02-2 | >98.50% | |
(R)-Verapamilhydrochloride((R)-(+)-Verapamilhydrochloride)是一种P-糖蛋白(P-Glycoprotein)抑制剂。(R)-Verapamilhydrochloride抑制MRP1介导的转运,导致MRP1过表达细胞对抗癌药产生化学敏感性。 | ||||
| GC60425 | (S)-Verapamil D7 hydrochloride | - | - | |
(S)-VerapamilD7hydrochloride((S)-(-)-VerapamilD7hydrochloride)是(S)-Verapamilhydrochloride的一种氘代化合物。(S)-Verapamilhydrochloride(S(-)-Verapamilhydrochloride)通过MRP1抑制白三烯C4(LTC4)和钙黄绿素的转运。(S)-Verapamilhydrochloride导致潜在耐药性肿瘤细胞死亡。 | ||||
| GC60467 | 21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione | 37413-91-5 | >99.50% | |
21-Acetoxypregna-1,4,9(11),16-tetraene-3,20-dione是delta9,11类固醇类合成的中间体(intermediate),如Vamorolone 。delta9,11steroids是糖皮质激素的修饰后的产物,具有抗炎(anti-inflammatory)特性。delta9,11类固醇类可以用作保护细胞损伤(脂质过氧化)和抑制新生血管的试剂。 | ||||
| GC60507 | 3-O-Methylgallic acid | 3934-84-7 | >97.00% | |
3-O-Methylgallicacid(3,4-Dihydroxy-5-methoxybenzoicacid)是一种花青素代谢产物,具有强大的抗氧化能力。3-O-Methylgallicacid能抑制Caco-2细胞增殖,IC50值为24.1μM。3-O-Methylgallicacid还诱导细胞凋亡(apoptosis)并具有抗癌作用。 | ||||
| GC60525 | 4-Vinylphenol (10%w/w in propylene glycol) | 2628-17-3 | 不显示 | |
4-Vinylphenol存在于药用草白花蛇舌草,野生稻中,也是葡萄酒中乳酸菌对对香豆酸和阿魏酸的代谢产物。4-Vinylphenol诱导凋亡(apoptosis),在体内抑制血管形成并抑制浸润性乳腺肿瘤生长。 | ||||
| GC60544 | A-192621 | 195529-54-5 | >99.50% | |
A-192621是一种有效的非肽,口服活性,选择性内皮素B(ETB)受体拮抗剂,IC50为4.5nM,Ki为8.8nM。A-192621的选择性比ETA高636倍(IC50为4280nM,Ki为5600nM)。A-192621促进PASMC细胞凋亡,并引起动脉血压升高和血浆ET-1水平升高。 | ||||
| GC60548 | ABT-100 | 450839-40-4 | >98.00% | |
ABT-100是一种有效的,高选择性和口服活性的farnesyltransferase抑制剂。ABT-100抑制细胞增殖(对于EJ-1,DLD-1,MDA-MB-231,HCT-116,MiaPaCa-2,PC-3和DU-145细胞的IC50分别为2.2nM,3.8nM,5.9nM,6.9nM,9.2nM,70nM和818nM),可增加细胞凋亡并减少血管生成。ABT-100具有广谱抗肿瘤活性。 | ||||
| GC60584 | Angiotensin II human acetate | 68521-88-0 | {{1-5}>99.00% / {6-13}>98.00%} | |
A peptide hormone | ||||
| GC60601 | ARRY-382 | 1313407-95-2 | >99.00% | |
ARRY-382 is a highly selective, oral inhibitor of the CSF1R with an IC50 of 9 nM. | ||||
| GC60603 | Asperosaponin VI | 39524-08-8 | >98.00% | |
A triterpenoid saponin with diverse biological activities | ||||
| GC60616 | AZT triphosphate | 92586-35-1 | - | |
AZTtriphosphate(3'-Azido-3'-deoxythymidine-5'-triphosphate)是一种Zidovudine(AZT)的活性三磷酸酯代谢产物。AZTtriphosphate具有抗逆转录病毒的活性,并抑制HIV复制。AZTtriphosphate还可抑制HBV的DNA聚合酶。AZTtriphosphate可激活线粒体介导的凋亡(apoptosis)途径。 | ||||
| GC60617 | AZT triphosphate TEA | - | - | |
AZTtriphosphateTFA(3'-Azido-3'-deoxythymidine-5'-triphosphateTFA)是一种Zidovudine(AZT)的活性三磷酸酯代谢产物。AZTtriphosphateTFA具有抗逆转录病毒的活性,并抑制HIV复制。AZTtriphosphateTFA还可抑制HBV的DNA聚合酶。AZTtriphosphateTFA可激活线粒体介导的凋亡(apoptosis)途径。 | ||||
| GC60620 | Batabulin | 195533-53-0 | >99.50% | |
An inhibitor of tubulin polymerization | ||||
| GC60621 | Batabulin sodium | 195533-98-3 | >99.50% | |
An inhibitor of tubulin polymerization | ||||
