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)
- GC61466DMU-212CAS: 134029-62-2纯度: >99.50%
DMU-212 is a methylated derivative of Resveratrol, with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities, which can induce mitotic arrest via induction of apoptosis and activation of extracellular-signal-regulated kinase1/2 (ERK1/2) protein.
- GC61469Compstatin TFA纯度: >99.00%
Compstatin binds to complement component C3 and inhibits complement activation with IC50 of 12 μM.
- GC61564(E/Z)-IT-603CAS: 292168-90-2纯度: >98.00%
(E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603. IT-603 is a NF-κB family member c-Rel inhibitor with an IC50 of 3 μM in electrophoretic mobility shift assay (EMSA).
- GC61608HLI373 dihydrochlorideCAS: 1782531-99-0
HLI373dihydrochloride是一种有效的Hdm2抑制剂。HLI373抑制Hdm2泛素连接酶活性。HLI373dihydrochloride可有效诱导肿瘤细胞(对DNA破坏剂敏感的)凋亡(apoptosis)。具有抗疟疾(antimalarial)活性。
- GC61623NAE-IN-M22CAS: 864420-54-2纯度: >99.50%
NEDD8 inhibitor M22 (NAE-IN-M22) is a novel selective NEDD8 activating enzyme (NAE) inhibitor with GI50 of 5.5 μM in A549 cells.
- GC61628NeriifolinCAS: 466-07-9纯度: >96.00%
Neriifolin是一种穿透中枢神经系统的强心苷,是一种Na+,K+-ATPase的抑制剂。Neriifolin可靶向beclin1,抑制LC3相关吞噬体的形成,改善实验性自身免疫性脑脊髓炎(EAE)的发展。Neriifolin诱导人肝癌HepG2细胞周期阻滞和凋亡。
- GC616385-HydroxyoxindoleCAS: 3416-18-0纯度: >95.00%
5-Hydroxyoxindole是尿酸的一种结构类似物。5-Hydroxyoxindole具有自由基DPPH清除活性和脂质过氧化抑制活性。5-Hydroxyoxindole可用于氧化应激介导的疾病的研究。
- GC61668(E)-3,4-Dimethoxycinnamic acidCAS: 14737-89-4
(E)-3,4-Dimethoxycinnamicacid是3,4-Dimethoxycinnamicacid的低活性异构体。3,4-Dimethoxycinnamicacid是从Securidacainappendiculata中提取和纯化的单体。3,4-Dimethoxycinnamicacid通过ROS介导的信号途径对L-02细胞发挥抗凋亡作用。
- GC61669Ethyl 3,4-dihydroxybenzoateCAS: 3943-89-3纯度: >99.00%
Ethyl3,4-dihydroxybenzoate(Ethylprotocatechuate)是一种抗氧化剂,是一种在花生种子的种皮中发现的脯氨酰羟化酶(prolyl-hydroxylase)抑制剂。Ethyl3,4-dihydroxybenzoate通过激活NO合酶(NOsynthase)并产生线粒体ROS来保护心肌。Ethyl3,4-dihydroxybenzoate可诱导ESCC细胞自噬(autophagy)和凋亡(apoptosis)。Ethyl3,4-dihydroxybenzoate是胶原蛋白合成抑制剂,具有骨骼保护作用。
- GC616733,5-Di-tert-butylphenolCAS: 1138-52-9纯度: >99.50%
3,5-Di-tert-butylphenol是一种具有抗生物膜和抗真菌活性的挥发性有机化合物。3,5-Di-tert-butylphenol会引起活性氧(ROS)的积累。
- GC61745AP1867-2-(carboxymethoxy)CAS: 2230613-03-1
AP1867-2-(carboxymethoxy)是一种基于AP1867(一种合成的FKBP12F36V配体)的配体,可通过linker与CRBN配体结合从而形成dTAG分子。
- GC61750(Rac)-IndoximodCAS: 26988-72-7纯度: >97.00%
(Rac)-Indoximod(1-Methyl-DL-tryptophan)是吲哚胺-2,3-双加氧酶(IDO)抑制剂。(Rac)-Indoximod和IFN-γ联用显著降低了表达α-SMA的人心肌成纤维细胞活性,并通过上调IRF-1,Fas和FasL基因诱导凋亡(apoptosis)。
- GC61776Ingenol 3,20-dibenzoateCAS: 59086-90-7纯度: >99.00%
Ingenol3,20-dibenzoate是一种有效的蛋白激酶C(PKC)亚型选择性激动剂。Ingenol3,20-dibenzoate诱导nPKC-delta、-epsilon和-theta和PKC-mu从胞质部分选择性转移到颗粒组分,并通过从头合成大分子诱导形态上典型的凋亡(apoptosis)。Ingenol3,20-dibenzoate可促进NK细胞产生IFN-γ和脱颗粒,尤其是当NSCLC细胞刺激NK细胞时。
- GC61777RWJ-56110 dihydrochlorideCAS: 2387505-58-8
RWJ-56110dihydrochloride是一种有效的、选择性的、拟肽抑制剂,抑制PAR-1激活和内化(结合IC50=0.44uM),对PAR-2,PAR-3和PAR-4无影响。RWJ-56110dihydrochloride抑制由SFLLRN-NH2 (IC50=0.16μM)和凝血酶(IC50=0.34μM)诱导的血小板聚集,相对于U46619具有相当的选择性。RWJ-56110dihydrochloride在体内阻断血管生成和新血管的形成。RWJ-56110dihydrochloride诱导细胞凋亡(apoptosis)。
- GC61796Armillarisin ACAS: 53696-74-5纯度: >99.50%
ArmillarisinA有用于溃疡性结肠炎(UC)研究的潜力。ArmillarisinA可上调IL-4、下调IL-1β的作用。
- GC61799PaeoniflorigenoneCAS: 80454-42-8纯度: >98.00%
Paeoniflorigenone是从牡丹皮中提取的一种有效成分,具有选择性诱导肿瘤细胞凋亡(apoptosis)和抗增殖作用。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC61461 | SLF TFA | 2378802-47-0 | >95.00% | |
SLFTFA是FK506结合蛋白(FKBP)的合成配体,对FKBP51的亲和力为3.1μM,对FKBP12的IC50为2.6μM,可用于合成PROTAC分子。 | ||||
| GC61466 | DMU-212 | 134029-62-2 | >99.50% | |
DMU-212 is a methylated derivative of Resveratrol, with antimitotic, anti-proliferative, antioxidant and apoptosis promoting activities, which can induce mitotic arrest via induction of apoptosis and activation of extracellular-signal-regulated kinase1/2 (ERK1/2) protein. | ||||
| GC61469 | Compstatin TFA | - | >99.00% | |
Compstatin binds to complement component C3 and inhibits complement activation with IC50 of 12 μM. | ||||
| GC61492 | SW106065 | 62289-81-0 | >99.50% | |
SW-106065 is an apoptosis inducer in malignant peripheral nerve sheath tumors (MPNST), which can inhibit ATP consumption of sporadic MPNST and other models of MPNST with an EC50 of 1 ?M. | ||||
| GC61524 | SC-43 | 1400989-25-4 | >98.00% | |
An SHP-1 activator | ||||
| GC61532 | CCI-007 | 939228-52-1 | >98.00% | |
CCI-007 is a novel small molecule with cytotoxic activity against infant leukemia with MLL rearrangements. | ||||
| GC61552 | PAO-Nap | 1613402-20-2 | - | |
PAO-Nap是NAP(naphthalimide)荧光基团修饰的PAO。PAO通过选择性靶向硫氧蛋白还原酶诱导HL-60细胞氧化应激介导的凋亡。 | ||||
| GC61564 | (E/Z)-IT-603 | 292168-90-2 | >98.00% | |
(E/Z)-IT-603 is a mixture of E-IT-603 and Z-IT-603. IT-603 is a NF-κB family member c-Rel inhibitor with an IC50 of 3 μM in electrophoretic mobility shift assay (EMSA). | ||||
| GC61567 | CMLD-2 | 958843-91-9 | >98.00% | |
CMLD-2是一种HuR-ARE相互作用的抑制剂。CMLD-2竞争性结合HuR蛋白,破坏其与富含腺嘌呤-尿苷元素(ARE)的mRNA靶标的相互作用(Ki=350nM)。CMLD-2可诱导凋亡并在结肠癌,胰腺癌,甲状腺癌和肺癌细胞系中表现出抗肿瘤活性。Hu抗原R(HuR)是一种RNA结合蛋白,可以调节靶标mRNA的稳定性和翻译。 | ||||
| GC61608 | HLI373 dihydrochloride | 1782531-99-0 | - | |
HLI373dihydrochloride是一种有效的Hdm2抑制剂。HLI373抑制Hdm2泛素连接酶活性。HLI373dihydrochloride可有效诱导肿瘤细胞(对DNA破坏剂敏感的)凋亡(apoptosis)。具有抗疟疾(antimalarial)活性。 | ||||
| GC61623 | NAE-IN-M22 | 864420-54-2 | >99.50% | |
NEDD8 inhibitor M22 (NAE-IN-M22) is a novel selective NEDD8 activating enzyme (NAE) inhibitor with GI50 of 5.5 μM in A549 cells. | ||||
| GC61628 | Neriifolin | 466-07-9 | >96.00% | |
Neriifolin是一种穿透中枢神经系统的强心苷,是一种Na+,K+-ATPase的抑制剂。Neriifolin可靶向beclin1,抑制LC3相关吞噬体的形成,改善实验性自身免疫性脑脊髓炎(EAE)的发展。Neriifolin诱导人肝癌HepG2细胞周期阻滞和凋亡。 | ||||
| GC61636 | CBR-470-2 | 2416095-00-4 | >99.00% | |
CBR-470-2是甘氨酸取代的类似物,可以激活NRF2信号传导。CBR-470-2可用于调节糖酵解。 | ||||
| GC61638 | 5-Hydroxyoxindole | 3416-18-0 | >95.00% | |
5-Hydroxyoxindole是尿酸的一种结构类似物。5-Hydroxyoxindole具有自由基DPPH清除活性和脂质过氧化抑制活性。5-Hydroxyoxindole可用于氧化应激介导的疾病的研究。 | ||||
| GC61665 | Tetrahydroxyquinone monohydrate | 1215458-51-7 | >97.00% | |
A redox-active hydroxyquinone | ||||
| GC61668 | (E)-3,4-Dimethoxycinnamic acid | 14737-89-4 | - | |
(E)-3,4-Dimethoxycinnamicacid是3,4-Dimethoxycinnamicacid的低活性异构体。3,4-Dimethoxycinnamicacid是从Securidacainappendiculata中提取和纯化的单体。3,4-Dimethoxycinnamicacid通过ROS介导的信号途径对L-02细胞发挥抗凋亡作用。 | ||||
| GC61669 | Ethyl 3,4-dihydroxybenzoate | 3943-89-3 | >99.00% | |
Ethyl3,4-dihydroxybenzoate(Ethylprotocatechuate)是一种抗氧化剂,是一种在花生种子的种皮中发现的脯氨酰羟化酶(prolyl-hydroxylase)抑制剂。Ethyl3,4-dihydroxybenzoate通过激活NO合酶(NOsynthase)并产生线粒体ROS来保护心肌。Ethyl3,4-dihydroxybenzoate可诱导ESCC细胞自噬(autophagy)和凋亡(apoptosis)。Ethyl3,4-dihydroxybenzoate是胶原蛋白合成抑制剂,具有骨骼保护作用。 | ||||
| GC61673 | 3,5-Di-tert-butylphenol | 1138-52-9 | >99.50% | |
3,5-Di-tert-butylphenol是一种具有抗生物膜和抗真菌活性的挥发性有机化合物。3,5-Di-tert-butylphenol会引起活性氧(ROS)的积累。 | ||||
| GC61745 | AP1867-2-(carboxymethoxy) | 2230613-03-1 | - | |
AP1867-2-(carboxymethoxy)是一种基于AP1867(一种合成的FKBP12F36V配体)的配体,可通过linker与CRBN配体结合从而形成dTAG分子。 | ||||
| GC61750 | (Rac)-Indoximod | 26988-72-7 | >97.00% | |
(Rac)-Indoximod(1-Methyl-DL-tryptophan)是吲哚胺-2,3-双加氧酶(IDO)抑制剂。(Rac)-Indoximod和IFN-γ联用显著降低了表达α-SMA的人心肌成纤维细胞活性,并通过上调IRF-1,Fas和FasL基因诱导凋亡(apoptosis)。 | ||||
| GC61776 | Ingenol 3,20-dibenzoate | 59086-90-7 | >99.00% | |
Ingenol3,20-dibenzoate是一种有效的蛋白激酶C(PKC)亚型选择性激动剂。Ingenol3,20-dibenzoate诱导nPKC-delta、-epsilon和-theta和PKC-mu从胞质部分选择性转移到颗粒组分,并通过从头合成大分子诱导形态上典型的凋亡(apoptosis)。Ingenol3,20-dibenzoate可促进NK细胞产生IFN-γ和脱颗粒,尤其是当NSCLC细胞刺激NK细胞时。 | ||||
| GC61777 | RWJ-56110 dihydrochloride | 2387505-58-8 | - | |
RWJ-56110dihydrochloride是一种有效的、选择性的、拟肽抑制剂,抑制PAR-1激活和内化(结合IC50=0.44uM),对PAR-2,PAR-3和PAR-4无影响。RWJ-56110dihydrochloride抑制由SFLLRN-NH2 (IC50=0.16μM)和凝血酶(IC50=0.34μM)诱导的血小板聚集,相对于U46619具有相当的选择性。RWJ-56110dihydrochloride在体内阻断血管生成和新血管的形成。RWJ-56110dihydrochloride诱导细胞凋亡(apoptosis)。 | ||||
| GC61796 | Armillarisin A | 53696-74-5 | >99.50% | |
ArmillarisinA有用于溃疡性结肠炎(UC)研究的潜力。ArmillarisinA可上调IL-4、下调IL-1β的作用。 | ||||
| GC61799 | Paeoniflorigenone | 80454-42-8 | >98.00% | |
Paeoniflorigenone是从牡丹皮中提取的一种有效成分,具有选择性诱导肿瘤细胞凋亡(apoptosis)和抗增殖作用。 | ||||
