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)
- GC61803Sulfo-ara-F-NMNCAS: 1374663-29-2纯度: >98.00%
Sulfo-ara-F-NMN(CZ-48)是一种烟酰胺单核苷酸(NMN)的类似物。Sulfo-ara-F-NMN选择性激活SARM1,但抑制CD38(IC50约为10μM)。Sulfo-ara-F-NMN诱导细胞内环状ADP-核糖(cADPR)的产生。
- GC61809Olanzapine D3CAS: 786686-79-1纯度: >99.00%
OlanzapineD3(LY170053D3)是Olanzapine的氘代物。Olanzapine是一种选择性单胺能拮抗剂,高亲和力结合5-羟色胺H1,5HT2A/2C,5HT3,5HT6(Ki分别为7、4、11、57和5nM),多巴胺D1-4(Ki=11-31nM),毒蕈碱M1-5(Ki=1.9-25nM)和肾上腺素α1受体(Ki=19nM)。Olanzapine是一种非典型的抗精神病剂。
- GC61896trans-ChalconeCAS: 614-47-1
Trans-Chalcone, the backbone of flavonoids, also is a potent fatty acid synthase (FAS) with IC50 of 17.1 μg/mL, and α-amylase inhibitor, causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7, exerting antifungal and anticancer activities.
- GC61948InecalcitolCAS: 163217-09-2纯度: >98.00%
Inecalcitol (TX 522) 是一种独特的维生素 D3 类似物,是一种具有口服活性维生素 D 受体 (VDR) 激动剂。Inecalcitol 可诱导细胞凋亡 (apoptosis),并具有有效的抗癌活性。
- GC61993Kaempferol 3-O-β-D-glucuronideCAS: 22688-78-4纯度: >98.00%
A flavonol glycoside and an active metabolite of kaempferol with diverse biological activities
- GC62040Cinnamyl-3,4-dihydroxy-α-cyanocinnamateCAS: 132465-11-3纯度: >99.50%
Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) 是一种有效的 12/15 脂氧合酶 (12/15-LO) 抑制剂。Cinnamyl-3,4-dihydroxy-α-cyanocinnamate 可用于研究1型糖尿病。
- GC62125PD-1/PD-L1-IN-10CAS: 2487550-41-2纯度: >99.00%
PD-1/PD-L1-IN-10 (compound B2) 是具有口服活性的 PD-1/PD-L1 抑制剂 (IC50 of 2.7 nM),具有抗肿瘤活性。
- GC62167FluorizolineCAS: 1362243-70-6纯度: >99.50%
Fluorizoline 选择性地直接结合到 prohibitin 1 (PHB1) 和 2 (PHB2),并诱导凋亡。Fluorizoline 通过上调 NOXA 和 BIM 降低慢性淋巴细胞性白血病 (CLL) 细胞的活力。Fluorizoline 以 p53 非依赖性方式发挥抗肿瘤作用。
- GC62193(1S,2S)-BortezomibCAS: 1132709-14-8纯度: >96.00%
(1S,2S)-Bortezomib 是 Bortezomib 的对映异构体。Bortezomib 是一种细胞渗透性、可逆性和选择性的蛋白酶体抑制剂,通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki 为 0.6 nM)。Bortezomib 破坏细胞周期、诱导细胞凋亡以及抑制核因子 NF-κB。Bortezomib 是一种抗癌药物,也是第一种用于人类的蛋白酶体抑制剂。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC61803 | Sulfo-ara-F-NMN | 1374663-29-2 | >98.00% | |
Sulfo-ara-F-NMN(CZ-48)是一种烟酰胺单核苷酸(NMN)的类似物。Sulfo-ara-F-NMN选择性激活SARM1,但抑制CD38(IC50约为10μM)。Sulfo-ara-F-NMN诱导细胞内环状ADP-核糖(cADPR)的产生。 | ||||
| GC61809 | Olanzapine D3 | 786686-79-1 | >99.00% | |
OlanzapineD3(LY170053D3)是Olanzapine的氘代物。Olanzapine是一种选择性单胺能拮抗剂,高亲和力结合5-羟色胺H1,5HT2A/2C,5HT3,5HT6(Ki分别为7、4、11、57和5nM),多巴胺D1-4(Ki=11-31nM),毒蕈碱M1-5(Ki=1.9-25nM)和肾上腺素α1受体(Ki=19nM)。Olanzapine是一种非典型的抗精神病剂。 | ||||
| GC61843 | Mofezolac | 78967-07-4 | >98.50% | |
A COX-1 inhibitor | ||||
| GC61865 | Cearoin | 52811-37-7 | >98.00% | |
Cearoin 通过促进 ROS 产生和激活 ERK 来增强自噬 (autophagy) 和诱导细胞凋亡(apoptosis)。 | ||||
| GC61896 | trans-Chalcone | 614-47-1 | - | |
Trans-Chalcone, the backbone of flavonoids, also is a potent fatty acid synthase (FAS) with IC50 of 17.1 μg/mL, and α-amylase inhibitor, causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7, exerting antifungal and anticancer activities. | ||||
| GC61945 | PR-924 | 1416709-79-9 | - | |
PR-924 是一种选择性三肽环氧酮免疫蛋白酶亚单位 LMP-7 的抑制剂,IC50 为 22 nM。PR-924 共价修饰蛋白酶体的 N 端苏氨酸活性位点。PR-924 在多发性骨髓瘤细胞中抑制细胞生长并触发凋亡 (apoptosis),并具有抗肿瘤活性。 | ||||
| GC61948 | Inecalcitol | 163217-09-2 | >98.00% | |
Inecalcitol (TX 522) 是一种独特的维生素 D3 类似物,是一种具有口服活性维生素 D 受体 (VDR) 激动剂。Inecalcitol 可诱导细胞凋亡 (apoptosis),并具有有效的抗癌活性。 | ||||
| GC61993 | Kaempferol 3-O-β-D-glucuronide | 22688-78-4 | >98.00% | |
A flavonol glycoside and an active metabolite of kaempferol with diverse biological activities | ||||
| GC61995 | PKCβ inhibitor 1 | 257879-35-9 | >98.00% | |
A PKCβ Inhibitor | ||||
| GC62033 | 3α-Hydroxy pravastatin sodium | 81093-43-8 | - | |
A metabolite of pravastatin | ||||
| GC62040 | Cinnamyl-3,4-dihydroxy-α-cyanocinnamate | 132465-11-3 | >99.50% | |
Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) 是一种有效的 12/15 脂氧合酶 (12/15-LO) 抑制剂。Cinnamyl-3,4-dihydroxy-α-cyanocinnamate 可用于研究1型糖尿病。 | ||||
| GC62104 | WM-3835 | 2229025-70-9 | >98.00% | |
WM-3835 is a novel and high-specific small molecule Lysine Acetyltransferase 7 (KAT7, MYST2, HBO1) inhibitor, able to potently suppressed OS cell proliferation and migration, and leads to apoptosis activation. | ||||
| GC62111 | PND-1186 hydrochloride | 1356154-94-3 | >98.50% | |
A potent FAK inhibitor | ||||
| GC62125 | PD-1/PD-L1-IN-10 | 2487550-41-2 | >99.00% | |
PD-1/PD-L1-IN-10 (compound B2) 是具有口服活性的 PD-1/PD-L1 抑制剂 (IC50 of 2.7 nM),具有抗肿瘤活性。 | ||||
| GC62127 | OATD-01 | 2088453-21-6 | >99.00% | |
An inhibitor of CHIT1 and CHIA | ||||
| GC62142 | WH-4-025 | 1876463-35-2 | >98.50% | |
WH-4-025 是盐诱导激酶 (SIK) 的抑制剂 (WO2016023014 A2)。 | ||||
| GC62161 | HOIPIN-1 | - | >97.00% | |
HOIPIN-1 (JTP-0819958, HOIP inhibitor-1) is a linear ubiquitin chain assembly complex (LUBAC) inhibitor with an IC50 of 2.8 μM for inhibiting the in vitro linear ubiquitination activity of the petit-LUBAC. | ||||
| GC62164 | BAY1082439 | 1375469-38-7 | >99.00% | |
An inhibitor of PI3Kα, PI3Kβ, and PI3Kδ | ||||
| GC62167 | Fluorizoline | 1362243-70-6 | >99.50% | |
Fluorizoline 选择性地直接结合到 prohibitin 1 (PHB1) 和 2 (PHB2),并诱导凋亡。Fluorizoline 通过上调 NOXA 和 BIM 降低慢性淋巴细胞性白血病 (CLL) 细胞的活力。Fluorizoline 以 p53 非依赖性方式发挥抗肿瘤作用。 | ||||
| GC62174 | ON1231320 | 1312471-39-8 | >98.00% | |
ON1231320 (7ao), an arylsulfonyl pyrido-pyrimidinone, is a highly specific inhibitor of polo like kinase 2 (PLK2). It also blocks tumor cell cycle progression in the G2/M phase in mitosis and causes apoptosis. | ||||
| GC62186 | KB02-SLF | 2384184-40-9 | >99.00% | |
KB02-SLF 是一种基于 PROTAC 的核 FKBP12 降解剂 (molecular glue)。KB02-SLF 通过共价修饰 DCAF16 (E3 ligase) 促进 FKBP12 降解,并可以提高生物系统中蛋白质降解的持久性。KB02-SLF 由 SLF 与泛素 E3 连接酶配体 (KB02) 通过 linker 连接而成。 | ||||
| GC62191 | TD52 | 1798328-24-1 | >99.00% | |
A derivative of erlotinib | ||||
| GC62192 | COG1410 | 878009-24-6 | >98.00% | |
COG1410 是一种载脂蛋白 E 的衍生肽。COG1410 在小鼠颅脑损伤 (TBI) 模型中发挥神经保护和抗炎作用。COG1410 可用于神经系统疾病的研究。 | ||||
| GC62193 | (1S,2S)-Bortezomib | 1132709-14-8 | >96.00% | |
(1S,2S)-Bortezomib 是 Bortezomib 的对映异构体。Bortezomib 是一种细胞渗透性、可逆性和选择性的蛋白酶体抑制剂,通过靶向苏氨酸残基有效抑制 20S 蛋白酶体 (Ki 为 0.6 nM)。Bortezomib 破坏细胞周期、诱导细胞凋亡以及抑制核因子 NF-κB。Bortezomib 是一种抗癌药物,也是第一种用于人类的蛋白酶体抑制剂。 | ||||
