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.
- 5-Lipoxygenase(11)
- Papain(1)
- PGDS(1)
- PGE synthase(24)
- SIKs(12)
- IκB/IKK(67)
- AP-1(6)
- KEAP1-Nrf2(65)
- NOD1(1)
- TLR(140)
- NF-κB(241)
- Interleukin Related(171)
- 15-lipoxygenase(2)
- Others(63)
- Aryl Hydrocarbon Receptor(36)
- CD73(14)
- Complement System(58)
- Galectin(12)
- IFNAR(25)
- NO Synthase(77)
- NOD-like Receptor (NLR)(51)
- STING(110)
- Reactive Oxygen Species(465)
- Apoptosis(802)
- FKBP(20)
- eNOS(5)
- iNOS(29)
- nNOS(20)
- Glutathione(57)
- Adaptive Immunity(222)
- Allergy(130)
- Arthritis(34)
- Autoimmunity(190)
- Gastric Disease(101)
- Immunosuppressants(39)
- Immunotherapeutics(5)
- Innate Immunity(593)
- Pulmonary Diseases(119)
- Reactive Nitrogen Species(55)
- Reactive Sulfur Species(28)
- Specialized Pro-Resolving Mediators(50)
- Cyclic GMP-AMP Synthase(2)
- BCL6(3)
- CD20(3)
- CD22
- CD28(1)
- FAP(7)
- PSMA(7)
- Nuclear Factor of activated T Cells (NFAT)(1)
- Glycoprotein VI(1)
- Tim3(2)
- Hapten(1)
- Nectin-4(2)
Immunology/Inflammation 相关产品(4245)
- GC63845Eribulin-d3 mesylate
Eribulin-d3 mesylate 是 Eribulin mesylate 的氘代物。Eribulin mesylate 是靶向微管 (microtubule) 的抗癌剂,可用于研究癌症。
- GC63871Echitamine chlorideCAS: 6878-36-0纯度: >98.00%
Echitamine chloride 是存在于 Alstonia 中的主要单萜吲哚生物碱,具有有效的抗肿瘤活性。Echitamine chloride 会诱导 DNA 片段化和细胞凋亡 (apoptosis)。Echitamine chloride 抑制胰腺脂肪酶 (pancreatic lipase),IC50 为 10.92 µM。
- GC63902Hematoporphyrin monomethyl etherCAS: 148471-91-4纯度: >95.00%
Hematoporphyrin monomethyl ether 是第二代卟啉类光敏剂,具有形态单一、单线态氧产率高、选择性高、毒性低等特点,广泛应用于各种肿瘤的诊断和治疗,包括肺癌、膀胱癌,脑胶质瘤与焰色痣。
- GC63916PROTAC-O4I2纯度: >98.00%
PROTAC-O4I2是一种2-氨基噻唑衍生物,能够选择性降解SF3B1并以CRBN依赖的方式诱导细胞凋亡(IC 50 = 0.244μM)。
- GC63918L-Arginine-15N4 hydrochlorideCAS: 204633-95-4
L-Arginine-15N4 ((S)-(+)-Arginine-15N4) hydrochloride 是一种 15N 标记的 L-Arginine hydrochloride。L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) 为合成一氧化氮的氮供体,是血管扩张剂。
- GC63932AmsilaroteneCAS: 125973-56-0纯度: >99.00%
Amsilarotene (TAC-101; Am 555S) 是一种具有口服活性的合成类视黄醇,对视黄酸受体 α (RAR-α) 具有选择性亲和力,对 RAR-α 和 RAR-β 的 Ki 值为 2.4 nM 和 400 nM。Amsilarotene 诱导人胃癌、肝细胞癌和卵巢癌细胞的凋亡 (apoptotic)。Amsilarotene 可用于癌症研究。
- GC63933S-AllylmercaptocysteineCAS: 2281-22-3纯度: >95.00%
S-allylmercaptocysteine 是一种从大蒜中提取的有机硫化合物,对各种肺部疾病具有抗炎和抗氧化作用。S-allylmercaptocysteine 通过多种途径发挥抗癌作用,如通过 TGF-β 信号通路诱导癌细胞凋亡 (apoptosis),或通过降低 NF-κb 活性和上调 Nrf2 来达到抗炎和抗氧化的作用。
- GC63941α-SolanineCAS: 20562-02-1
α-solanine 是马铃薯中的一种生物活性成分,是主要的甾体类生物碱之一,可抑制癌细胞的生长并诱导其凋亡 (apoptosis)。
- GC63942OxysophoridineCAS: 54809-74-4纯度: >98.00%
Oxysophoridine (Sophoridine N-oxide) 是从 Sophora alopecuroides Linn 中提取的具有生物活性生物碱。Oxysophoridine (Sophoridine N-oxide) 具有抗发炎,抗氧化应激和抗凋亡的作用。
- GC639586α-Hydroxy Paclitaxel-d5CAS: 1315376-90-9
6α-Hydroxy Paclitaxel-d5 是 6α-Hydroxy paclitaxel 的氘代物。6α-Hydroxy paclitaxel 是紫杉醇的初级代谢物。6α-Hydroxy paclitaxel 对有机阴离子转运多肽 1B1/SLCO1B1 (OATP1B1) 具有与紫杉醇相似的时间依赖性抑制效力,但它对 OATP1B3 不具有时间依赖性作用。6α-Hydroxy paclitaxel 可用于癌症研究。
- GC63969(+)-Schisandrin BCAS: 82467-52-5
(+)-Schisandrin B 是五味子甲素 B 的一种对映体。Schisandrin B 是从五味子果实中分离出来的有效成分,对啮鼠的肝脏和心脏有抗氧化作用。
- GC63975Acanthoside BCAS: 7374-79-0
Acanthoside B 是一种具有抗炎、抗遗忘活性的生物活性木脂素。Acanthoside B 可用于阿尔茨海默病和肺部炎症等疾病的研究。
- GC64028Chrysosplenol DCAS: 14965-20-9纯度: >99.50%
Chrysosplenol D 是一种甲氧基黄酮类化合物,可在三阴性人乳腺癌细胞中诱导 ERK1/2 介导的细胞凋亡。Chrysosplenol D 还具有抗炎和中等抗锥虫活性。
- GC64032Salicylic acid-d6CAS: 285979-87-5纯度: >99.50%
Salicylic acid-D6 (2-Hydroxybenzoic acid-D6) 是 Salicylic acid 的一种氘代化合物。Salicylic acid 抑制 COX-2 活性,抑制作用与转录因子 (NF-κB) 激活无关。
- GC64040VTP50469 fumarateCAS: 2169919-29-1纯度: >98.00%
VTP50469 fumarate 是一种有效的,高选择性和口服活性的 Menin-MLL 相互作用抑制剂,Ki 为 104 pM。VTP50469 fumarate 具有高效的抗白血病活性。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC63845 | Eribulin-d3 mesylate | - | - | |
Eribulin-d3 mesylate 是 Eribulin mesylate 的氘代物。Eribulin mesylate 是靶向微管 (microtubule) 的抗癌剂,可用于研究癌症。 | ||||
| GC63858 | Vemircopan | 2086178-00-7 | >98.00% | |
Vemircopan (ALXN2050) 是一种具有口服活性的补体因子 D (FD) 抑制剂。 | ||||
| GC63860 | Rapanone | 573-40-0 | >99.00% | |
Rapanone是一种天然存在的具有优势螯合结构的羟基苯醌,具有广泛的生物活性,特别是其抗炎、驱虫和细胞毒性活性。 | ||||
| GC63871 | Echitamine chloride | 6878-36-0 | >98.00% | |
Echitamine chloride 是存在于 Alstonia 中的主要单萜吲哚生物碱,具有有效的抗肿瘤活性。Echitamine chloride 会诱导 DNA 片段化和细胞凋亡 (apoptosis)。Echitamine chloride 抑制胰腺脂肪酶 (pancreatic lipase),IC50 为 10.92 µM。 | ||||
| GC63902 | Hematoporphyrin monomethyl ether | 148471-91-4 | >95.00% | |
Hematoporphyrin monomethyl ether 是第二代卟啉类光敏剂,具有形态单一、单线态氧产率高、选择性高、毒性低等特点,广泛应用于各种肿瘤的诊断和治疗,包括肺癌、膀胱癌,脑胶质瘤与焰色痣。 | ||||
| GC63905 | SN-008 | 2249106-01-0 | >98.00% | |
SN-008 是 SN-011 的低活性类似物,可用来作为阴性对照。 | ||||
| GC63916 | PROTAC-O4I2 | - | >98.00% | |
PROTAC-O4I2是一种2-氨基噻唑衍生物,能够选择性降解SF3B1并以CRBN依赖的方式诱导细胞凋亡(IC 50 = 0.244μM)。 | ||||
| GC63918 | L-Arginine-15N4 hydrochloride | 204633-95-4 | - | |
L-Arginine-15N4 ((S)-(+)-Arginine-15N4) hydrochloride 是一种 15N 标记的 L-Arginine hydrochloride。L-Arginine hydrochloride ((S)-(+)-Arginine hydrochloride) 为合成一氧化氮的氮供体,是血管扩张剂。 | ||||
| GC63932 | Amsilarotene | 125973-56-0 | >99.00% | |
Amsilarotene (TAC-101; Am 555S) 是一种具有口服活性的合成类视黄醇,对视黄酸受体 α (RAR-α) 具有选择性亲和力,对 RAR-α 和 RAR-β 的 Ki 值为 2.4 nM 和 400 nM。Amsilarotene 诱导人胃癌、肝细胞癌和卵巢癌细胞的凋亡 (apoptotic)。Amsilarotene 可用于癌症研究。 | ||||
| GC63933 | S-Allylmercaptocysteine | 2281-22-3 | >95.00% | |
S-allylmercaptocysteine 是一种从大蒜中提取的有机硫化合物,对各种肺部疾病具有抗炎和抗氧化作用。S-allylmercaptocysteine 通过多种途径发挥抗癌作用,如通过 TGF-β 信号通路诱导癌细胞凋亡 (apoptosis),或通过降低 NF-κb 活性和上调 Nrf2 来达到抗炎和抗氧化的作用。 | ||||
| GC63934 | Karanjin | 521-88-0 | - | |
Karanjin 是 Fordia cauliflora 中主要的活性呋喃黄酮醇成分。Karanjin 通过提高 AMPK 的方式诱导骨骼肌细胞 GLUT4 易位。Karanjin 可通过细胞周期阻滞诱导癌细胞死亡,促进细胞凋亡。 | ||||
| GC63941 | α-Solanine | 20562-02-1 | - | |
α-solanine 是马铃薯中的一种生物活性成分,是主要的甾体类生物碱之一,可抑制癌细胞的生长并诱导其凋亡 (apoptosis)。 | ||||
| GC63942 | Oxysophoridine | 54809-74-4 | >98.00% | |
Oxysophoridine (Sophoridine N-oxide) 是从 Sophora alopecuroides Linn 中提取的具有生物活性生物碱。Oxysophoridine (Sophoridine N-oxide) 具有抗发炎,抗氧化应激和抗凋亡的作用。 | ||||
| GC63958 | 6α-Hydroxy Paclitaxel-d5 | 1315376-90-9 | - | |
6α-Hydroxy Paclitaxel-d5 是 6α-Hydroxy paclitaxel 的氘代物。6α-Hydroxy paclitaxel 是紫杉醇的初级代谢物。6α-Hydroxy paclitaxel 对有机阴离子转运多肽 1B1/SLCO1B1 (OATP1B1) 具有与紫杉醇相似的时间依赖性抑制效力,但它对 OATP1B3 不具有时间依赖性作用。6α-Hydroxy paclitaxel 可用于癌症研究。 | ||||
| GC63967 | Cycleanine | 518-94-5 | >99.00% | |
An alkaloid with anticancer and antimalarial activities | ||||
| GC63969 | (+)-Schisandrin B | 82467-52-5 | - | |
(+)-Schisandrin B 是五味子甲素 B 的一种对映体。Schisandrin B 是从五味子果实中分离出来的有效成分,对啮鼠的肝脏和心脏有抗氧化作用。 | ||||
| GC63975 | Acanthoside B | 7374-79-0 | - | |
Acanthoside B 是一种具有抗炎、抗遗忘活性的生物活性木脂素。Acanthoside B 可用于阿尔茨海默病和肺部炎症等疾病的研究。 | ||||
| GC63979 | Ro24-7429 | 139339-45-0 | - | |
Ro24-7429 是一种有效且具有口服活性的 HIV-1 反式激活蛋白 Tat 拮抗剂。Ro24-7429 也是 RUNX1 抑制剂。Ro24-7429 具有抗 HIV、抗纤维化和抗炎作用。 | ||||
| GC63986 | VAS 3947 | 869853-70-3 | >99.00% | |
VAS 3947 是一种特异的 NADPH 氧化酶 (NOX) 抑制剂,具有强大的抗血小板作用。VAS 3947 通过 UPR 激活,主要由于蛋白质聚集和错误折叠,独立于抗 NOX 活性诱导细胞凋亡 (apoptosis)。 | ||||
| GC64013 | ZX-29 | 2254805-62-2 | >99.00% | |
ZX-29 is a potent and selective ALK inhibitor with an IC50s of 2.1, 1.3 and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. | ||||
| GC64028 | Chrysosplenol D | 14965-20-9 | >99.50% | |
Chrysosplenol D 是一种甲氧基黄酮类化合物,可在三阴性人乳腺癌细胞中诱导 ERK1/2 介导的细胞凋亡。Chrysosplenol D 还具有抗炎和中等抗锥虫活性。 | ||||
| GC64032 | Salicylic acid-d6 | 285979-87-5 | >99.50% | |
Salicylic acid-D6 (2-Hydroxybenzoic acid-D6) 是 Salicylic acid 的一种氘代化合物。Salicylic acid 抑制 COX-2 活性,抑制作用与转录因子 (NF-κB) 激活无关。 | ||||
| GC64040 | VTP50469 fumarate | 2169919-29-1 | >98.00% | |
VTP50469 fumarate 是一种有效的,高选择性和口服活性的 Menin-MLL 相互作用抑制剂,Ki 为 104 pM。VTP50469 fumarate 具有高效的抗白血病活性。 | ||||
| GC64089 | Selnoflast | 2260969-36-4 | - | |
Selnoflast (example 6) 是 NLRP3 的抑制剂 (信息来自专利WO2019008025)。 | ||||
