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.
Products for Immunology/Inflammation
- 5-Lipoxygenase(10)
- Papain(1)
- PGDS(1)
- PGE synthase(24)
- SIKs(11)
- IκB/IKK(64)
- AP-1(6)
- KEAP1-Nrf2(65)
- NOD1(1)
- TLR(139)
- NF-κB(235)
- Interleukin Related(167)
- 15-lipoxygenase(2)
- Others(63)
- Aryl Hydrocarbon Receptor(35)
- CD73(14)
- Complement System(57)
- Galectin(12)
- IFNAR(25)
- NO Synthase(74)
- NOD-like Receptor (NLR)(50)
- STING(104)
- Reactive Oxygen Species(454)
- Apoptosis(780)
- FKBP(20)
- eNOS(5)
- iNOS(29)
- nNOS(20)
- Glutathione(55)
- Adaptive Immunity(209)
- Allergy(124)
- Arthritis(34)
- Autoimmunity(179)
- Gastric Disease(95)
- Immunosuppressants(37)
- Immunotherapeutics(4)
- Innate Immunity(560)
- Pulmonary Diseases(108)
- Reactive Nitrogen Species(50)
- Reactive Sulfur Species(28)
- Specialized Pro-Resolving Mediators(50)
- Cyclic GMP-AMP Synthase(2)
- BCL6(3)
- CD20(3)
- CD28(1)
- FAP(7)
- PSMA(7)
- Nuclear Factor of activated T Cells (NFAT)(1)
- Glycoprotein VI(1)
- Tim3(2)
- Hapten(1)
- Nectin-4(2)
- Cat.No. 产品名称 Information
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GC49781
Benomyl
苯菌灵
A carbamate pesticide -
GC49780
Omeprazole N-oxide
奥美拉唑N-氧化物
A metabolite of omeprazole -
GC49776
Apricitabine
阿立他滨,SPD754; AVX754
A nucleoside reverse transcriptase inhibitor -
GC49774
Ipronidazole
异丙硝唑
A nitroimidazole antiprotozoal agent -
GC49773
Albendazole sulfone-d3
阿苯哒唑砜-D3
An internal standard for the quantification of albendazole sulfone -
GC49769
β-Glucogallin
1-没食子酸酰葡萄糖
A plant metabolite and an aldose reductase 2 inhibitor -
GC49768
1,1’-Ethylidene-bis-(L-tryptophan)
粉色E
A potential impurity found in commercial preparations of L-tryptophan
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GC49766
Abafungin
阿巴芬净,BAY-W-6341
An antifungal agent -
GC49765
PF-04753299
An inhibitor of LpxC
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GC49761
Capsaicin-d3
TRANS-辣椒素-D3,(E)-Capsaicin-d3
An internal standard for the quantification of capsaicin -
GC49759
13C17-Mycophenolic Acid
霉酚酸-(全碳-13)
An internal standard for the quantification of mycophenolic acid -
GC49758
CAY10788
A CysLT1 receptor antagonist
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GC49755
Meclizine N-oxide
美克洛嗪N-氧化物
A metabolite of meclizine -
GC49753
LCS3
An inhibitor of glutathione reductase and thioredoxin reductase
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GC49751
Lefamulin
来法莫林,BC-3781
A pleuromutilin antibiotic -
GC49749
6-Deoxypenciclovir
泛昔洛韦USPRCA
An inactive metabolite of famciclovir -
GC19933
Leukotriene B4
[5S,12R]-二羟基-[6Z,8E,10E,14Z]-二十碳四烯酸,LTB4; 5(S),12(R)-DiHETE
A leukotriene involved in inflammation -
GC64375
Difopein TFA
Difopein (TFA) 是 14-3-3 protein (一种高度保守的真核调节分子) 的特异性竞争性抑制剂,可阻止 14-3-3 与靶蛋白结合的能力,并抑制 14-3-3/配体的相互作用。Difopein (TFA) 诱导细胞凋亡 (apoptosis) 并增强顺铂杀死细胞的能力。
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GC64373
Tezacitabine
替扎西他滨
Tezacitabine 是一种具有细胞生长抑制和细胞毒性的抗代谢药,是一种核苷类似物。Tezacitabine 不可逆地抑制核糖核苷酸还原酶 (ribonucleotide reductase) 并干扰 DNA 复制和修复。Tezacitabine 有效诱导细胞凋亡 (apoptotic),可用于白血病和实体瘤的研究。 -
GC64370
Kongensin A
Kongensin A 是一种从 Croton kongensis 中分离的天然产物。 Kongensin A 是一种有效的,共价的 HSP90 抑制剂,可阻断 RIP3 依赖性坏死病。Kongensin A 是一种有效的坏死性抑制剂和凋亡诱导剂,并具有潜在的抗坏死性和消炎性应用。
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GC64354
Bendamustine
宾达氮芥,SDX-105 free base
Bendamustine (SDX105) is a nitrogen mustard drug used in the treatment of chronic lymphocytic leukemia (CLL), multiple myeloma, and non-Hodgkin's lymphoma. -
GC64352
L-Glutamic acid-15N
L-谷氨酸 15N
L-Glutamic acid-15N 是一种 15N 标记的 L-Glutamic acid。L-Glutamic acid 作为一种兴奋性氨基酸神经递质,为谷氨酸盐受体所有亚型(代谢型红藻氨酸、NMDA 和 AMPA)的激动剂。对 DA 从多巴胺能神经末梢释放的过程有激动作用。 -
GC64331
Ritonavir-13C,d3
ABT 538-13C,d3; RTV-13C,d3
Ritonavir-13C,d3 (ABT 538-13C,d3) 是一种 13C- 和氘代标记的 Ritonavir。Ritonavir (ABT 538) 是用于研究 HIV 感染和 AIDS 的 HIV 蛋白酶的抑制剂。Ritonavir 也是 SARS-CoV 3CLpro 的抑制剂,IC50 为 1.61 μM。 -
GC64325
Ligustilide
蒿本内酯
Ligustilide is the most abundant bioactive ingredient in Rhizoma Chuanxiong, a Chinese medicinal herb commonly used for the treatment of cardiovascular ailments. Solutions are best fresh-prepared. -
GC64303
S2116
S2116 是 N-烷基化的反式环丙胺 (TCP) 衍生物,是一种有效的赖氨酸特异性脱甲基酶 1 (LSD1) 抑制剂。S2116 在超级增强子区域增加 H3K9 甲基化和相应的 H3K27 脱乙酰化。S2116 抑制 NOTCH3 和 TAL1 基因的转录,从而诱导 TCP 抵抗性急性淋巴细胞白血病 T-ALL 细胞凋亡 (apoptosis)。S2116 显着延迟异种移植小鼠中 T-ALL 细胞的生长。
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GC64275
AHR antagonist 5
AHR antagonist 5 是有效的,具有口服活性的芳香烃受体 (AHR) 拮抗剂,IC50 为 < 0.5 μM。AHR antagonist 5 联合检测点抑制剂 anti-PD-1 对肿瘤生长有抑制作用,详细信息请参见专利 WO2018195397,example 39。
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GC64269
IL-17A modulator-2
IL-17A modulator-2 是一种 IL-17A 调节剂,来自专利 WO2021239743+A1,example 27。IL-17A modulator-2 抑制 IL-17A 的生物学效应,pIC50 为 8.3。IL-17A modulator-2 可用于研究与调节 IL-17A 活性相关的疾病或病症,包括具有免疫成分或自身免疫病理的疾病、癌症和神经退行性疾病。
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GC64262
Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH
Tri(TLR4-IN-C34-PEG2-amide-PEG1)-amide-C3-COOH 是一种含有 TLR4 抑制剂 TLR4-IN-C34 的连接子。TLR4-IN-C34 抑制肠细胞和巨噬细胞中的 TLR4,减少内毒素血症和坏死性小肠结肠炎小鼠模型的全身炎症。
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GC64257
Gelsevirine
钩吻绿碱
Gelsevirine 是 Gelsemium elegans 中的主要生物碱,具有有效的抗焦虑作用。Gelsevirine 的抗焦虑机制可能与大脑中甘氨酸受体的激动作用有关。Gelsevirine 具有抗增殖活性,对 SW480 细胞和 MGC80-3 细胞的 IC50 值分别为 1.41 mM 和 1.22 mM。 -
GC64236
IL-17A modulator-1
IL-17A modulator-1 是一种 IL-17A 调节剂,来自专利 WO2021239743+A1,example 9。IL-17A modulator-1 抑制 IL-17A 的生物学效应,pIC50 为 8.2。IL-17A modulator-1 可用于研究与调节 IL-17A 活性相关的疾病或病症,包括具有免疫成分或自身免疫病理的疾病、癌症和神经退行性疾病。
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GC64234
Spiraeoside
绣线菊甙,Quercetin 4′-O-glucoside
Spiraeoside 是具有口服活性的天然产物,具有抗氧化活性,抑制活性氧和丙二醛的生成。Spiraeoside 具有抗过敏、抗炎、抗肿瘤活性。 -
GC64223
Sophocarpine monohydrate
槐果碱水合物
An alkaloid with diverse biological activities -
GC64208
AHR antagonist 5 free base
AHR antagonist 5 free base 是一种选择性的、具有口服活性的芳烃受体 (AHR) 抑制剂。AHR antagonist 5 free base 有效阻止 AHR 从细胞质转移到细胞核。AHR antagonist 5 free base 对 AHR 的选择性高于其他受体、转运蛋白和激酶,并具有抗癌作用。
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GC64139
Dibromoacetic acid
二溴乙酸
Dibromoacetic acid 是一种卤乙酸,常作为消毒副产品存在于饮用水中的,可引起许多不良反应,包括免疫毒性和诱导凋亡 (apoptosis) 等。 -
GC64127
Xylopine
木番荔枝碱
Xylopine 是一种阿朴啡生物碱,对癌细胞具有细胞毒活性。Xylopine 诱导氧化应激,导致癌细胞的 G2/M 细胞周期停滞和细胞凋亡 (apoptosis)。 -
GC64126
Neoechinulin A
Neoechinulin A 是一种异戊烯基吲哚生物碱,具有清除、神经营养因子样和抗凋亡活性。Neoechinulin A 诱导小鼠记忆改善和抗抑郁样作用。
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GC64119
Saponarin
皂草甙
A flavonoid glycoside with diverse biological activities -
GC64115
Gypenoside LI
Gypenoside LI 是一种绞股蓝赶单体,具有抗肿瘤活性。Gypenoside LI 诱导癌细胞凋亡、细胞周期阻滞和迁移。
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GC64110
Carubicin hydrochloride
盐酸洋红霉素,Carminomycin hydrochloride; Carminomicin I hydrochloride
An anthracycline with anticancer activity -
GC64089
Selnoflast
Selnoflast (example 6) 是 NLRP3 的抑制剂 (信息来自专利WO2019008025)。
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GC64040
VTP50469 fumarate
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。
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GC64032
Salicylic acid-d6
水杨酸-D6; 2-Hydroxybenzoic acid-d6
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。 -
GC64028
Chrysosplenol D
猫眼草酚D
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。 -
GC64013
ZX-29
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.
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GC63986
VAS 3947
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)。
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GC63979
Ro24-7429
7-氯-N-甲基-5-(1H-吡咯-2-基)-3H-1,4-苯并二氮杂卓-2-胺
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。 -
GC63975
Acanthoside B
刺五加提取物
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。 -
GC63969
(+)-Schisandrin B
(+)-五味子乙素
(+)-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。 -
GC63967
Cycleanine
轮环藤碱
An alkaloid with anticancer and antimalarial activities -
GC63958
6α-Hydroxy Paclitaxel-d5
紫杉醇杂质
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。