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(4794)
- GC73915PSMA-Val-Cit-PAB-AzideCAS: 2374814-84-1Purity: >99.00%
PSMA-Val-Cit-PAB-Azide 는 ADC의 약물 접선 우연물입니다.
- GC73943Polθ/PARP-IN-1Purity: >99.00%
Polθ/PARP-IN-1 (복합 25d)는 강력 한 이중 DNA 진 세 타 (Pol θ)과지 억제 IC50 값의 45., 각각 5. 4 nM 위를 차지 했다.
- GC73996PROTAC AR/AR-V7 degrader-1CAS: 2841308-96-9Purity: >98.00%
PROTAC AR/AR-V7 degrader-1(27c)는 PROTAC 기반 듀얼 AR AR-V7 분해기로, AR과 AR-V7의 DC50 값은 각각 2.67과 2.64μM이다.
- GC74013FOSL1 degrader 1
FOSL1 degrader 1 (4)는 T-5224-PROTAC 이며, FOSL1 (AP-1)을 강력하게 분해하여 HNSCC에서 암 stemness 유전자 발현을 억제한다.
| Catalog No. | Product Name | CAS No. | Purity | Structure |
|---|---|---|---|---|
| GC73868 | WD6305 TFA | - | >98.00% | |
WD6305 TFA은 강력한 METTL3-targeted PROTAC degrader입니다. | ||||
| GC73881 | PRO-6E | 2353493-69-1 | >99.00% | |
PRO-6E은 구술을 바탕으로 활성 PROTAC Cereblon 간 드, 및과만 났의 문란을 유도하 최대 저하의 1 μ M에서 81.9% MKN-45 세포다. | ||||
| GC73893 | BLU-222 | 2888704-84-3 | >98.00% | |
BLU-222는 구강 활성 및 매우 선택적인 CDK2억제제입니다. | ||||
| GC73900 | HA-9104 | 2412367-83-8 | >98.00% | |
HA-9104 UBE2F의 V30 포켓을 거의 표적으로 하여 cullin-5 nedylation을 억제하는 효과적인 선택적 억제제입니다. | ||||
| GC73915 | PSMA-Val-Cit-PAB-Azide | 2374814-84-1 | >99.00% | |
PSMA-Val-Cit-PAB-Azide 는 ADC의 약물 접선 우연물입니다. | ||||
| GC73925 | YSR734 | 3032969-58-4 | >98.00% | |
YSR734 (화합물 21)은 HDAC1, HDAC2 및 HDAC3에 대해 각각 110 nM, 154 nM 및 143 nM의 IC50 값을 갖는 공유결합 HDAC 억제제이다. | ||||
| GC73928 | BDM19 | 500273-31-4 | >98.00% | |
BDM19 는 BCL-2/BCL-XL 억제제 Navitoclax와 단독으로 또는 단독으로 연합하여 세포의 사멸을 유도한다. | ||||
| GC73932 | WK369 | - | >99.00% | |
WK369은 우수한 항 난소암 생체 활성을 나타내며 세포 주기 정지를 유도하고 세포 사멸을 유발하는 새로운 BCL6 소분자 억제제입니다. | ||||
| GC73939 | ATPase-IN-3 | 1134203-12-5 | >99.00% | |
ATPase-IN-3 (화합물 6) 는 ATP 효소 억제제입니다. | ||||
| GC73940 | BFC1108 | 692774-37-1 | >98.00% | |
BFC1108는 작은 분자 Bcl-2기능성 컨버터입니다. | ||||
| GC73942 | NT-0249 free base | - | - | |
NT-0249 free base는 구강 활성 NLRP3억제제이다. | ||||
| GC73943 | Polθ/PARP-IN-1 | - | >99.00% | |
Polθ/PARP-IN-1 (복합 25d)는 강력 한 이중 DNA 진 세 타 (Pol θ)과지 억제 IC50 값의 45., 각각 5. 4 nM 위를 차지 했다. | ||||
| GC73950 | SC912 | - | >99.00% | |
SC912은 AR-V7 억제제(IC50=0.36μM)의 일종이다. | ||||
| GC73973 | MY-1442 | 3050871-87-6 | >99.00% | |
MY-1442 (I-3) 는 마이크로튜브 단백질 중합 억제제입니다. | ||||
| GC73980 | GGTI-2417 | 501010-05-5 | >98.00% | |
GGTI-2417 는 GGTase I의 강력한 선택성 억제제입니다. | ||||
| GC73982 | NSD-IN-3 | 744260-15-9 | >98.00% | |
NSD-IN-3 (화합물 3)는 강력한 핵 수용체 결합 SET 구조 도메인 (NSD) 억제제입니다. | ||||
| GC73990 | SDU-071 | - | >98.00% | |
SDU-071 는 BRD4-p53 억제제의 강력한 경구 활성 억제제입니다. | ||||
| GC73994 | UM4118 | 324530-92-9 | >99.00% | |
UM4118 은 미토콘드리아에 기반한 비정규 형태의 세포 사멸을 유발할 수 있는 구리 이온 운반체로 구리 중독이라고 한다. | ||||
| GC73995 | XL44 | 2637949-91-6 | >98.00% | |
hRpn13 바인더인 XL44는 hRpn13의존적 세포사멸을 유도하고 또한 PCLAF-dependent mechanism에 의해 세포의 생존성을 제한한다. | ||||
| GC73996 | PROTAC AR/AR-V7 degrader-1 | 2841308-96-9 | >98.00% | |
PROTAC AR/AR-V7 degrader-1(27c)는 PROTAC 기반 듀얼 AR AR-V7 분해기로, AR과 AR-V7의 DC50 값은 각각 2.67과 2.64μM이다. | ||||
| GC74001 | TS-24 | 1563260-97-8 | >98.00% | |
TS-24 는 조직단백질효소S의 억제제로서 IC50은 4.3μM이다. | ||||
| GC74005 | AK59 | - | >98.00% | |
AK59은 HECT 도메인 E3 리가제 HERC4를 활용하는 STING 분해제이다. | ||||
| GC74007 | SelSA | 1225038-92-5 | >99.00% | |
SelSA은 56.9 nM의 IC50을 갖는 히스톤 탈아세틸라제6 (HDAC6)에 대한 선택적, 경구 활성 억제제이다. | ||||
| GC74013 | FOSL1 degrader 1 | - | - | |
FOSL1 degrader 1 (4)는 T-5224-PROTAC 이며, FOSL1 (AP-1)을 강력하게 분해하여 HNSCC에서 암 stemness 유전자 발현을 억제한다. | ||||
