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24

抑制剂 & 化合物

3

天然产物

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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。

化合物

MyD88-IN-1
Cat.No: T77353
Synonym:
Target: IL Receptor, NF-κB, TLR, MyD88
TJ-M2010-5
Cat.No: T9765
Synonym:
Target: MyD88
TLR1
Cat.No: T13932
Synonym: N-[(1S)-2-甲基-1-(1-吡咯烷羰基)丙基]-苯丙酰胺
Target: Others, MyD88
JH-X-119-01
Cat.No: T9203
Synonym:
Target: IRAK
CA-4948
Cat.No: T9027
Synonym: Emavusertib
Target: IRAK, FLT
Resatorvid
Cat.No: TQ0181
Synonym: CLI-095,TAK-242,瑞沙托维
Target: TNF, TLR, Autophagy, Interleukin
T6167923
Cat.No: T13063
Synonym:
Target: MyD88
CL075
Cat.No: T27034
Synonym: 3M002,CL-075
Target: NF-κB, TLR, MyD88
EM 163
Cat.No: T41142
Synonym:
Target: IL Receptor, p38 MAPK, MyD88
ST 2825
Cat.No: T16937
Synonym:
Target: Others
TSI-13-48
Cat.No: T69722
Synonym:
Target:
LM9
Cat.No: T69733
Synonym:
Target:
IRAK4-IN-6
Cat.No: T11674
Synonym:
Target: Others
TSI-13-57
Cat.No: T69719
Synonym:
Target:
T5996207
Cat.No: T68261
Synonym:
Target:
RDR 02308
Cat.No: T75223
Synonym:
Target:
IRAK4-IN-9
Cat.No: T61734
Synonym:
Target:
IRAK4-IN-15
Cat.No: T63262
Synonym:
Target:
LYRM03
Cat.No: T70145
Synonym:
Target:
IRAK4-IN-10
Cat.No: T61931
Synonym:
Target:
Artemisinin B
Cat.No: T70595
Synonym:
Target:
KTX-582
Cat.No: T74664
Synonym:
Target:
IRAK4-IN-27
Cat.No: T79485
Synonym:
Target: IRAK
IRAK4-IN-14
Cat.No: T63278
Synonym:
Target:
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.

天然产物

Schaftoside
Cat.No: T3898
Synonym: 夏佛塔苷,APIGENIN-6-GLUCOSIDE-8-ARABINOSIDE,Shaftoside
Target: Dynamin, Antioxidant, TLR, MyD88, Mitochondrial Metabolism, Autophagy
Atractylenolide I
Cat.No: T5S0167
Synonym: 白术内酯 I,白术内酯I;苍术内酯I
Target: IL Receptor, TNF, TLR, JAK, STAT
D-Mannuronic Acid
Cat.No: T27191
Synonym:
Target:
TargetMol Loading
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