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)
- GC62442Casein Kinase inhibitor A51CAS: 2079068-74-7纯度: >98.00%
Casein Kinase inhibitor A51 是一种有效且具有口服活性的酪蛋白激酶 1α (CK1α) 抑制剂。Casein Kinase inhibitor A51 可诱导白血病细胞凋亡 (apoptosis),并具有有效的抗白血病活性。
- GC62444SDZ 224-015CAS: 161511-45-1
SDZ 224-015 是具有口服活性的、IL-1β 转化酶和 caspase-1 的抑制剂。SDZ 224-015 具有抗COVID-19的活性,靶向 Mpro (IC50 of 30 nM)。
- GC62453GZD856 formicCAS: 2804039-78-7纯度: >98.00%
GZD856 formic 是一种有效的和具有口服活性的 PDGFRα/β 抑制剂,IC50 值分别为 68.6 和 136.6 nM。GZD856 formic 也是 Bcr-AblT315I 的抑制剂,对天然 Bcr-Abl 和 T315I 突变型的 IC50 值分别为 19.9 和 15.4 nM。GZD856 formic 具有抗肿瘤活性。
- GC62454MCC7840 sodiumCAS: 2380032-29-9纯度: >98.00%
MCC7840 (Emlenoflast), a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM.
- GC62471Enpatoran hydrochlorideCAS: 2101945-93-9纯度: >98.50%
Enpatoran (M5049) hydrochloride 是一种有效的、具有口服活性的 TLR7/8 抑制剂,在HEK293 细胞中,其IC50s 分别为 11.1 nM 和 24.1 nM。Enpatoran hydrochloride 对 TLR3, TLR4 和 TLR9 无活性。Enpatoran hydrochloride 可以阻断分子合成配体和天然内源性 RNA 配体。Enpatoran hydrochloride 在体内的表现出良好的药代动力学特性。Enpatoran hydrochloride 可用于先天性和适应性自身免疫阻断的相关研究。
- GC62479Iptacopan hydrochlorideCAS: 1646321-63-2纯度: >98.00%
LNP023 hydrochloride 是一种有效的,具有口服活性的高选择性的 factor B 抑制剂。LNP023 直接可逆且高亲和力结合 factor B,KD为 7.9 nM。LNP023 抑制 factor B 的 IC50 值为 10 nM。
- GC62483Pomolic acidCAS: 13849-91-7纯度: >98.00%
Pomolic acid is a pentacyclic triterpene isolated from Euscaphis japonica, and is highly effective in inhibiting cell growth and induces apoptosis.
- GC62507BMS-986299CAS: 2242952-69-6纯度: >99.50% / >98.00%
BMS-986299 is a novel NLRP3 agonist that induces IL8 release to activate natural killer (NK) cells.
- GC62527Kansuinine ACAS: 57701-86-7纯度: >99.00%
Kansuinine A 抑制 IL-6 诱导的 Stat3 的激活。Kansuinine A 有抗病毒和抗肿瘤活性。
- GC62528(Rac)-HesperetinCAS: 69097-99-0纯度: >97.00%
(Rac)-Hesperetin 是Hesperetin 的外消旋体。 Hesperetin 是一种天然黄烷酮类物质,为有效的,广谱的人 UGT 抑制剂。Hesperetin 可通过激活 p38 MAPK 来诱导凋亡。
- GC62562EGFR-IN-11CAS: 2463200-44-2纯度: >99.50%
EGFR-IN-11 是第四代 EGFR-酪氨酸激酶抑制剂 (EGFR-TKI),对三重突变的 EGFRL858R/T790M/C797S 的 IC50 为 18 nM。EGFR-IN-11 显著抑制 EGFR 磷酸化,诱导细胞凋亡,将细胞周期阻滞在 G0/G1处。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC62426 | ASK1-IN-2 | 2541792-70-3 | >98.00% | |
ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC50 of 32.8 nM. | ||||
| GC62442 | Casein Kinase inhibitor A51 | 2079068-74-7 | >98.00% | |
Casein Kinase inhibitor A51 是一种有效且具有口服活性的酪蛋白激酶 1α (CK1α) 抑制剂。Casein Kinase inhibitor A51 可诱导白血病细胞凋亡 (apoptosis),并具有有效的抗白血病活性。 | ||||
| GC62444 | SDZ 224-015 | 161511-45-1 | - | |
SDZ 224-015 是具有口服活性的、IL-1β 转化酶和 caspase-1 的抑制剂。SDZ 224-015 具有抗COVID-19的活性,靶向 Mpro (IC50 of 30 nM)。 | ||||
| GC62452 | CD73-IN-4 | 2216764-29-1 | >99.50% | |
CD73-IN-4 是一种高效、选择性的亚甲基膦酸 CD73 抑制剂,对人 CD73 作用的 IC50 值为 2.6 nM。CD73-IN-4 在癌症免疫学研究中具有潜在的应用价值。 | ||||
| GC62453 | GZD856 formic | 2804039-78-7 | >98.00% | |
GZD856 formic 是一种有效的和具有口服活性的 PDGFRα/β 抑制剂,IC50 值分别为 68.6 和 136.6 nM。GZD856 formic 也是 Bcr-AblT315I 的抑制剂,对天然 Bcr-Abl 和 T315I 突变型的 IC50 值分别为 19.9 和 15.4 nM。GZD856 formic 具有抗肿瘤活性。 | ||||
| GC62454 | MCC7840 sodium | 2380032-29-9 | >98.00% | |
MCC7840 (Emlenoflast), a sulfonylurea, is a potent and selective inhibitor of NLRP3 inflammasome, with an IC50 of <100 nM. | ||||
| GC62457 | UZH1 | - | >99.50% | |
UZH1 是 UZH1a 和 UZH1b 的外消旋体。UZH1a 是一种有效和选择性的 METTL3 抑制剂,IC50 值为 280 nM。UZH1b (IC50=28 µM) 基本无活性。UZH1 可用于细胞进程的转录组调控。UZH1 具有抗肿瘤活性。UZH1 也可用作研究 METTL3 的化学探针。 | ||||
| GC62471 | Enpatoran hydrochloride | 2101945-93-9 | >98.50% | |
Enpatoran (M5049) hydrochloride 是一种有效的、具有口服活性的 TLR7/8 抑制剂,在HEK293 细胞中,其IC50s 分别为 11.1 nM 和 24.1 nM。Enpatoran hydrochloride 对 TLR3, TLR4 和 TLR9 无活性。Enpatoran hydrochloride 可以阻断分子合成配体和天然内源性 RNA 配体。Enpatoran hydrochloride 在体内的表现出良好的药代动力学特性。Enpatoran hydrochloride 可用于先天性和适应性自身免疫阻断的相关研究。 | ||||
| GC62478 | ζ-Stat | 3316-02-7 | >99.50% | |
ζ-Stat (NSC37044) is a specific and atypical protein kinase Cζ (PKCζ) inhibitor, with an IC50 of 5 μM. | ||||
| GC62479 | Iptacopan hydrochloride | 1646321-63-2 | >98.00% | |
LNP023 hydrochloride 是一种有效的,具有口服活性的高选择性的 factor B 抑制剂。LNP023 直接可逆且高亲和力结合 factor B,KD为 7.9 nM。LNP023 抑制 factor B 的 IC50 值为 10 nM。 | ||||
| GC62483 | Pomolic acid | 13849-91-7 | >98.00% | |
Pomolic acid is a pentacyclic triterpene isolated from Euscaphis japonica, and is highly effective in inhibiting cell growth and induces apoptosis. | ||||
| GC62487 | POMHEX | 2004714-34-3 | >98.00% | |
POMHEX 是一个消旋混合物,是具有细胞渗透性的 HEX 的 POM 前体药物,是ENO2 的特异性抑制剂。POMHEX 对ENO1 缺失的细胞表现出低纳摩尔级别活性,并对 ENO1 缺失的肿瘤模型表现出良好的抗癌效果。POMHEX 是有效的糖酵解抑制剂。 | ||||
| GC62488 | AZD8848 | 866269-28-5 | >98.00% | |
AZD8848 是一种选择性的 TLR7 前体药激动剂,用于哮喘和过敏性鼻炎的研究。 | ||||
| GC62489 | Enpatoran | 2101938-42-3 | >99.50% | |
Enpatoran (M5049) 是一种有效的、具有口服活性的 TLR7/8 抑制剂,在HEK293 细胞中,其IC50s 分别为 11.1 nM 和 24.1 nM。Enpatoran 对 TLR3, TLR4 和 TLR9 无活性。Enpatoran 可以阻断分子合成配体和天然内源性 RNA 配体。Enpatoran 在体内的表现出良好的药代动力学特性。Enpatoran 可用于先天性和适应性自身免疫阻断的相关研究。 | ||||
| GC62499 | ATH686 | 853299-52-2 | >99.50% | |
ATH686 是一种有效的,选择性的,ATP 竞争性的 FLT3 抑制剂。ATH686 靶向突变 FLT3 蛋白激酶活性,并通过诱导凋亡 (apoptosis) 和抑制细胞周期来抑制具有 FLT3 突变的细胞的增殖。ATH686 具有抗白血病作用。 | ||||
| GC62505 | Pelcitoclax | 1619923-36-2 | - | |
Pelcitoclax (APG-1252) 是一种有效的 Bcl-2/Bcl-xl 抑制剂,具有抗肿瘤和促凋亡作用。 | ||||
| GC62507 | BMS-986299 | 2242952-69-6 | >99.50% / >98.00% | |
BMS-986299 is a novel NLRP3 agonist that induces IL8 release to activate natural killer (NK) cells. | ||||
| GC62527 | Kansuinine A | 57701-86-7 | >99.00% | |
Kansuinine A 抑制 IL-6 诱导的 Stat3 的激活。Kansuinine A 有抗病毒和抗肿瘤活性。 | ||||
| GC62528 | (Rac)-Hesperetin | 69097-99-0 | >97.00% | |
(Rac)-Hesperetin 是Hesperetin 的外消旋体。 Hesperetin 是一种天然黄烷酮类物质,为有效的,广谱的人 UGT 抑制剂。Hesperetin 可通过激活 p38 MAPK 来诱导凋亡。 | ||||
| GC62536 | Bromelain | 9001-00-7 | - | |
A mixture of proteolytic enzymes | ||||
| GC62554 | S65487 | 1644600-79-2 | >99.00% | |
S65487 (VOB560) 是一种有效的选择性 Bcl-2 抑制剂。 S65487 对 BCL-2 突变也有活性,例如 G101V 和 D103Y。S65487 对 MCL-1,BFL-1 和 BCL-XL 的亲和力较差。S65487 诱导细胞凋亡 (apoptosis) 并具有抗癌活性。 | ||||
| GC62558 | WDR5-IN-1 | 2408842-51-1 | >98.50% | |
WDR5-IN-1 是一种有效的选择性 WD 重复结构域 5 (WDR5) 抑制剂,Kd 为 <0.02 nM。WDR5-IN-1 抑制 MLL1 组蛋白甲基转移酶活性 (HMT),IC50为 2.2 nM。WDR5-IN-1 减少 WDR5 移位基因的 MYC 募集,并在 CHP-134 (神经母细胞瘤) 和 Ramos (Burkitt淋巴瘤) 细胞系中显示出有效的抗增殖作用。 | ||||
| GC62562 | EGFR-IN-11 | 2463200-44-2 | >99.50% | |
EGFR-IN-11 是第四代 EGFR-酪氨酸激酶抑制剂 (EGFR-TKI),对三重突变的 EGFRL858R/T790M/C797S 的 IC50 为 18 nM。EGFR-IN-11 显著抑制 EGFR 磷酸化,诱导细胞凋亡,将细胞周期阻滞在 G0/G1处。 | ||||
| GC62564 | Mito-LND | 2361564-49-8 | >97.00% | |
Mito-LND (Mito-Lonidamine) 是一种具有口服活性的且靶向线粒体的氧化磷酸化 (oxidative phosphorylation (OXPHOS)) 抑制剂。Mito-LND 抑制线粒体生物能,刺激活性氧 (reactive oxygen species) 的形成,并诱导肺癌细胞自噬细胞死亡。 | ||||
