Immunology/Inflammation
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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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Products Related to Immunology/Inflammation(4844)
- GC73272PARP-1-IN-3CAS: 2976342-33-1Purity: >99.00%
PARP-1-IN-3 페닐메틸아미드 유도체는 PARP-1 억제제로서 PARP-1과 PARP-2의 IC50 값은 각각 0.25nM과 2.34nM이다.
- GC73274EGFR T790M/L858R-IN-2CAS: 2955607-40-4Purity: >99.00%
EGFR T790M/L858R-IN-2는 EGFRT790M/L858R, EGFR WT에 대해 각각 3.5, 1290 nM의 IC50 값을 갖는 강력하고 선택적인 EGFRT790M/L858R 억제제입니다.
- GC73288CDK8-IN-13CAS: 918523-75-8Purity: >98.00%
CDK8-IN-13는 강력하고 선택적이고 경구 투여 가능한 CDK8 억제제로 IC50 값이 51.9nM이다.
- GC733015-Aminosalicylic acid-d3CAS: 1309283-32-6Purity: >99.00%
5-Aminosalicylic acid-d3 는 듀테륨 표시 5 - 아미노살리실산입니다.
- GC73309Anti-melanoma agent 1CAS: 2418579-17-4Purity: >99.00%
Anti-melanoma agent 1 (화합물 5m)은 항 흑색종 제제이며 세포 사멸을 유도합니다.
- GC73313PI3Kα-IN-9CAS: 2715287-67-3Purity: >99.00%
PI3Kα-IN-9 (화합물 27) 는 선택적이고 장기적이며 경구 활성인 PI3K 알파 억제제로서 PI3K 알파, PI3K 감마, PI3K 델타, PI3K 베타에 대한 IC50 값은 각각 4.4, 128, 146, 153 nM이다.
- GC73319FITC-labeled ODN 2216 sodiumPurity: >97.00%
FITC-labeled ODN 2216 sodium 는 인간 특이성 TLR9 toll 샘플 수용체 9 배합체 또는 흥분제입니다.
- GC73326ODN D-SL03 sodiumPurity: >99.00%
ODN D-SL03 sodium는 CpG C 클래스 oligonucleotides, PBMCs 자극을 유도 할 수 있고 높은 수준의 IFN-α를 생산 하도 록 합니다.
- GC73355STAT3-SH2 domain inhibitor 1CAS: 2816059-41-1Purity: >98.50%
STAT3-SH2 domain inhibitor 1는 STAT3(STAT3-SH2 구조역)의 강력한 Src 동원2(SH2) 구조역 억제제로, Kd값은 1.57μM이다.
- GC73371Enpp/Carbonic anhydrase-IN-2CAS: 2883495-39-2Purity: >99.00%
Enpp/Carbonic anhydrase-IN-2 는 강력한 Enpp 및 탄산수소 효소 억제제로서 NPP1, NPP2, NPP3, CA-IX, CA-XII의 IC50은 각각 1.13, 1.07, 0.74, 0.33, 0.68이다.
- GC73396PRMT6-IN-3CAS: 2890765-10-1Purity: >99.00%
PRMT6-IN-3 (화합물 25)는 192 nM의 IC50 값을 갖는 선택적 PRMT6억제제이다.
- GC73407STING agonist-26CAS: 2868261-48-5Purity: >99.00%
STING agonist-26 (CF508)은 non-nucleotide small molecule STING agonist이다.
- GC73413ARC186 sodiumPurity: >94.00%
ARC186 sodium는 0 Avacincaptad pegol ARC1905 sodium과 동일한 염기서열을 갖는 미결합 40KDa PEG 압타머이다.
- GC73417CASP8-IN-1CAS: 1956368-39-0Purity: >98.00%
CASP8-IN-1 (화합물 63 - R) 는 방광 단백질 효소 8 (CASP8) 의 선택적 억제제로서 IC50은 0.7 μM입니다.
- GC73424PRT062607 acetateCAS: 1370261-98-5Purity: >99.00%
PRT062607 acetate은 염증 및 유도 세포 사멸을 억제하는 경구 사용 가능한 Syk 억제제 (IC50:1 nM)이다.
- GC73428CWI1-2 hydrochlorideCAS: 2408590-37-2Purity: >98.00%
CWI1-2 hydrochloride 는 IGF2BP2와 결합하여 m6A로 수식된 표적전사물과의 상호작용을 억제하고 쇠망과 분화를 유도하는 IGF2BP2 억제제이다.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC73243 | Nrf2-IN-3 | 6325-13-9 | >99.00% | |
Nrf2-IN-3 (화합물 R16) 는 Nrf2 억제제입니다. | ||||
| GC73268 | PH14 | - | >99.00% | |
PH14은 이중 PI3K/HDAC 억제 IC50 값의 20. 3 nM과 24. 5에 대한 nM PI3K α와 HDAC3, 각각이다. | ||||
| GC73269 | ABBV-467 | 2287186-66-5 | >99.00% | |
ABBV-467는 선택적 MCL-1억제제이다 (Ki:<0.01 nM). | ||||
| GC73272 | PARP-1-IN-3 | 2976342-33-1 | >99.00% | |
PARP-1-IN-3 페닐메틸아미드 유도체는 PARP-1 억제제로서 PARP-1과 PARP-2의 IC50 값은 각각 0.25nM과 2.34nM이다. | ||||
| GC73274 | EGFR T790M/L858R-IN-2 | 2955607-40-4 | >99.00% | |
EGFR T790M/L858R-IN-2는 EGFRT790M/L858R, EGFR WT에 대해 각각 3.5, 1290 nM의 IC50 값을 갖는 강력하고 선택적인 EGFRT790M/L858R 억제제입니다. | ||||
| GC73288 | CDK8-IN-13 | 918523-75-8 | >98.00% | |
CDK8-IN-13는 강력하고 선택적이고 경구 투여 가능한 CDK8 억제제로 IC50 값이 51.9nM이다. | ||||
| GC73294 | F5446 | 2304465-89-0 | >99.00% | |
F5446 (화합물 1)는 SUV39H1 금속 전이 효소의 선택적 소분자 억제제입니다. | ||||
| GC73301 | 5-Aminosalicylic acid-d3 | 1309283-32-6 | >99.00% | |
5-Aminosalicylic acid-d3 는 듀테륨 표시 5 - 아미노살리실산입니다. | ||||
| GC73309 | Anti-melanoma agent 1 | 2418579-17-4 | >99.00% | |
Anti-melanoma agent 1 (화합물 5m)은 항 흑색종 제제이며 세포 사멸을 유도합니다. | ||||
| GC73311 | STAT3-IN-13 | 2248552-86-3 | >99.00% | |
STAT3-IN-13 (화합물 6f)는 강력한 STAT3억제제이다. | ||||
| GC73313 | PI3Kα-IN-9 | 2715287-67-3 | >99.00% | |
PI3Kα-IN-9 (화합물 27) 는 선택적이고 장기적이며 경구 활성인 PI3K 알파 억제제로서 PI3K 알파, PI3K 감마, PI3K 델타, PI3K 베타에 대한 IC50 값은 각각 4.4, 128, 146, 153 nM이다. | ||||
| GC73317 | ODN 1585 sodium | - | >93.00% | |
ODN 1585 sodium은 IFN과 TNFα에서 나오는 강력한 유도제다. | ||||
| GC73319 | FITC-labeled ODN 2216 sodium | - | >97.00% | |
FITC-labeled ODN 2216 sodium 는 인간 특이성 TLR9 toll 샘플 수용체 9 배합체 또는 흥분제입니다. | ||||
| GC73326 | ODN D-SL03 sodium | - | >99.00% | |
ODN D-SL03 sodium는 CpG C 클래스 oligonucleotides, PBMCs 자극을 유도 할 수 있고 높은 수준의 IFN-α를 생산 하도 록 합니다. | ||||
| GC73355 | STAT3-SH2 domain inhibitor 1 | 2816059-41-1 | >98.50% | |
STAT3-SH2 domain inhibitor 1는 STAT3(STAT3-SH2 구조역)의 강력한 Src 동원2(SH2) 구조역 억제제로, Kd값은 1.57μM이다. | ||||
| GC73371 | Enpp/Carbonic anhydrase-IN-2 | 2883495-39-2 | >99.00% | |
Enpp/Carbonic anhydrase-IN-2 는 강력한 Enpp 및 탄산수소 효소 억제제로서 NPP1, NPP2, NPP3, CA-IX, CA-XII의 IC50은 각각 1.13, 1.07, 0.74, 0.33, 0.68이다. | ||||
| GC73396 | PRMT6-IN-3 | 2890765-10-1 | >99.00% | |
PRMT6-IN-3 (화합물 25)는 192 nM의 IC50 값을 갖는 선택적 PRMT6억제제이다. | ||||
| GC73407 | STING agonist-26 | 2868261-48-5 | >99.00% | |
STING agonist-26 (CF508)은 non-nucleotide small molecule STING agonist이다. | ||||
| GC73413 | ARC186 sodium | - | >94.00% | |
ARC186 sodium는 0 Avacincaptad pegol ARC1905 sodium과 동일한 염기서열을 갖는 미결합 40KDa PEG 압타머이다. | ||||
| GC73417 | CASP8-IN-1 | 1956368-39-0 | >98.00% | |
CASP8-IN-1 (화합물 63 - R) 는 방광 단백질 효소 8 (CASP8) 의 선택적 억제제로서 IC50은 0.7 μM입니다. | ||||
| GC73424 | PRT062607 acetate | 1370261-98-5 | >99.00% | |
PRT062607 acetate은 염증 및 유도 세포 사멸을 억제하는 경구 사용 가능한 Syk 억제제 (IC50:1 nM)이다. | ||||
| GC73428 | CWI1-2 hydrochloride | 2408590-37-2 | >98.00% | |
CWI1-2 hydrochloride 는 IGF2BP2와 결합하여 m6A로 수식된 표적전사물과의 상호작용을 억제하고 쇠망과 분화를 유도하는 IGF2BP2 억제제이다. | ||||
| GC73441 | EAPB 02303 | 1958290-51-1 | >99.00% | |
EAPB 02303 는 미관 파괴제와 억제제의 일종이다. | ||||
| GC73452 | CCT374705 | 2640647-90-9 | >99.00% | |
CCT374705 는 경구용 활성 BCL6 억제제로서 체외에서 강력한 항증식 작용을 한다. | ||||
