24
3
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T77353 |
MyD88-IN-1
|
IL Receptor; NF-κB; TLR; MyD88 | Immunology/Inflammation; NF-κB |
MyD88-IN-1 是一种有效的 MyD88 抑制剂。MyD88-IN-1 具有抗炎活性,可抑制 Toll 样受体 (TLR) 和白细胞介素-1 (IL-1) 受体家族成员下游炎症信号通路 ,包括NF-κB 通路。MyD88-IN-1 可用于研究癌症和治疗炎症。 | |||
T9765 |
TJ-M2010-5
|
MyD88 | Immunology/Inflammation |
TJ-M2010-5 是一种 MyD88 抑制剂,可与 TIR 结构域结合以干扰其同源二聚化并抑制 MyD88 信号传导。 TJ-M2010-5 可用于心肌缺血/再灌注损伤研究。 | |||
T13932 |
TLR1
N-[(1S)-2-甲基-1-(1-吡咯烷羰基)丙基]-苯丙酰胺 |
Others; MyD88 | Immunology/Inflammation; Others |
TLR1 是细胞穿透 Toll/IL-1 receptor/resistance (TIR) domain/BB-Loop 的小分子模拟物,能够阻碍 IL-1 受体介导的反应。 | |||
T9203 |
JH-X-119-01
|
IRAK | Immunology/Inflammation; NF-κB |
JH-X-119-01 是白介素 1 受体相关激酶 1 的选择性抑制剂。它能够改善 LPS 诱导的小鼠败血症。它可以抑制 IRAK1(IC50:9 nM),在浓度达到 10 μM 时,也不会对 IRAK4 产生抑制作用。 | |||
T9027 |
CA-4948
Emavusertib |
IRAK; FLT | Angiogenesis; Immunology/Inflammation; NF-κB; Tyrosine Kinase/Adaptors |
CA-4948 (Emavusertib) 是一种IRAK4抑制剂,也是一种FLT3抑制剂,具有抗肿瘤作用。 | |||
TQ0181 |
Resatorvid
CLI-095,TAK-242,瑞沙托维 |
TNF; TLR; Autophagy; Interleukin | Apoptosis; Autophagy; Immunology/Inflammation |
Resatorvid (TAK-242) 是一种 Toll 样受体 4 (TLR4) 的抑制剂,具有选择性。Resatorvid 直接与 Cys747 结合,阻止 TLR4 与 TIRAP 结合,从而阻止下游信号转导。Resatorvid 具有抗肿瘤活性、抗炎活性和神经保护作用。 | |||
T13063 |
T6167923
|
MyD88 | Immunology/Inflammation |
T6167923是一种有效的、选择性的MyD88依赖性信号通路抑制剂。T6167923 与 MyD88 的 Toll/IL1 受体 (TIR) 结构域结合良好,破坏 MyD88 的同二聚体形成。T6167923 抑制 NF-κB 驱动的葡萄球菌肠毒素AP (SEAP) 活性,并且改善抗炎活性,对 IFN-γ,IL-1β,IL-6 和 TNF-α 的 IC50分别为 2.7 μM,2.9 μM,2.66 μM 和 2.66 μM。 | |||
T27034 |
CL075
3M002,CL-075 |
NF-κB; TLR; MyD88 | Immunology/Inflammation; NF-κB |
CL075 (3M002) 是一种选择性TLR8 激动剂。CL075具有免疫调节活性,通过触发 MyD88 依赖性信号通路,激活 NF-κB 和 IRF7 引发炎症性细胞因子和 I 型干扰素 (IFN) 的产生。 | |||
T41142 |
EM 163
|
IL Receptor; p38 MAPK; MyD88 | Immunology/Inflammation; MAPK |
EM 163是一种 TIR-TIR 相互作用抑制剂,它是MyD88蛋白的TIR(Toll/白细胞介素-1受体)结构域拟态。EM 163针对IL-1受体中的TIR 结构域,阻断与MyD88的相互作用。EM 163抑制葡萄球菌肠毒素B(SEB)引起的体内炎症细胞因子的产生。EM 163能保护小鼠免受SEB 冲击引起的死亡。在体外的大鼠海马神经元中,EM 163阻断p38的激活和IL-1β对化学诱导的长期电位(LTP)引发的蛋白质合成的抑制作用。 | |||
T16937 |
ST 2825
|
Others | Others |
ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 inhibition of IL-1β-mediated activation of NF-κB transcriptional activity. | |||
T69722 |
TSI-13-48
|
||
TSI-13-48 is a MyD88 inhibitor. | |||
T69733 |
LM9
|
||
LM9 is a MyD88 inhibitor which prevents atherosclerosis by regulating inflammatory responses and oxidative stress in macrophages. | |||
T11674 |
IRAK4-IN-6
|
Others | Others |
IRAK4-IN-6 是一种选择性的、口服有效的IRAK 抑制剂,IC50为 4 nM,靶向 MyD88 L265P 突变型弥漫性大 B 细胞淋巴瘤。 | |||
T69719 |
TSI-13-57
|
||
TSI-13-57 is a MyD88 inhibitor. | |||
T68261 |
T5996207
|
||
T5996207 is a inhibitor of MyD88-dependent signaling pathways | |||
T75223 | RDR 02308 | ||
RDR 02308 是 TLR4-MyD88结合抑制剂,可抑制全长β-lactamase。 | |||
T61734 |
IRAK4-IN-9
|
||
IRAK4-IN-9 (compound 73) is a highly potent inhibitor of IRAK4, displaying an impressive IC50 value of 1.5 nM. By blocking MyD88-dependent signaling, IRAK4-IN-9 exhibits promising potential for the investigation of inflammatory diseases, autoimmune diseases, and cancer [1]. | |||
T63262 |
IRAK4-IN-15
|
||
IRAK4-IN-15 是选择性的、有效的 IRAK4 抑制剂 (IC50: 0.002 μM),具有良好的人类 PK 预测且具有低内在清除率。IRAK4-IN-15 与 Acalabrutinib 联用对 MyD88/CD79 双突变体 ABC-DLBCL 的表现出强大的协同体外活性。 | |||
T70145 |
LYRM03
|
||
LYRM03 is an aminopeptidase inhibitor. LYRM03 is also an ubenimex derivative. LYRM03 attenuates LPS-induced acute lung injury in mice by suppressing the TLR4 signaling pathway. LYRM03 effectively attenuates LPS-induced ALI by inhibiting the expression of pro-inflammatory mediators and Myd88-dependent TLR4 signaling pathways in alveolar macrophages. LYRM03 may serve as a potential treatment for sepsis-mediated lung injuries. | |||
T61931 |
IRAK4-IN-10
|
||
IRAK4-IN-10 (compound 75) 是有效的 IRAK4抑制剂(IC50为 1.5 nM),对 MyD88 依赖的信号通路具有阻断作用。IRAK4-IN-10 在炎症性疾病、自身免疫性疾病和癌症中具有研究的潜力。 | |||
T70595 |
Artemisinin B
|
||
Artemisinin B is a drug which may improve spatial memory in dementia patients and alter the levels of inflammatory cytokines in the hippocampus and the cortex. Artemisinin B may inhibit neuroinflammation and exert neuroprotective effects on cognitive functions by modulating the TLR4-MyD88-NF-κB signaling pathway. Artemisinin B has shown potential in the treatment of neuroinflammatory diseases. | |||
T74664 |
KTX-582
|
||
KTX-582为一有效IRAK4降解剂,DC50对IRAK4及Ikaros分别为4 nM与5 nM。KTX-582能诱导MYD88MTDLBCL细胞凋亡(apoptosis),在淋巴瘤模型中有效促进体内肿瘤消退。 | |||
T79485 |
IRAK4-IN-27
|
IRAK | Immunology/Inflammation; NF-κB |
IRAK4-IN-27(Compound 22)为高效选择性IRAK4抑制剂,具IC50值8.7 nM。该化合物能够抑制含MYD88L265P突变的DLBCL细胞系生长并促进其细胞凋亡(apoptosis),适用于弥漫大B细胞淋巴瘤(DLBCL)的研究。 | |||
T63278 | IRAK4-IN-14 | ||
IRAK4-IN-14 是选择性的、有效的、口服具有活力的 IRAK4 抑制剂 (IC50: 0.003 μM),在大鼠和小鼠中具有出良好的 PK 参数。IRAK4-IN-14 与 Acalabrutinib 联合使用对 MyD88/CD79 双突变体 ABC-DLBCL 表现出协同体外作用。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T3898 |
Schaftoside
夏佛塔苷,APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE,Shaftoside |
Dynamin; Antioxidant; TLR; MyD88; Mitochondrial Metabolism; Autophagy | Autophagy; Cytoskeletal Signaling; Immunology/Inflammation; Metabolism; oxidation-reduction |
Schaftoside (APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE) 是在多种中草药中发现的一种黄酮类天然产物。它抑制 TLR4 和 Myd88 表达,还降低 Drp1 表达和磷酸化,并减少线粒体分裂,具有抗氧化和抗癌活性。 | |||
T5S0167 |
Atractylenolide I
白术内酯 I,白术内酯I;苍术内酯I |
IL Receptor; TNF; TLR; JAK; STAT | Angiogenesis; Apoptosis; Chromatin/Epigenetic; Immunology/Inflammation; JAK/STAT signaling; Stem Cells |
Atractylenolide I 是从白术根中得到的一种倍半萜烯,具有神经保护、抗过敏、抗炎和抗癌等多种生物活性。它是一种TLR4拮抗剂,在 A375 细胞中,能够降低JAK2和STAT3的磷酸化水平。 | |||
T27191 |
D-Mannuronic Acid
|
||
D-Mannuronic Acid is a blocker of the TLR2 and TLR4 downstream signaling pathway. D-Mannuronic Acid effectively inhibits mRNA expression of MyD88 and p65, major subunit of nuclear factor-kappaB. |