Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T36527 |
IL-4-inhibitor-1
|
IL Receptor | Immunology/Inflammation |
IL-4-inhibitor-1 是 IL-4 的抑制剂 (EC50 = 1.81 µM)。 | |||
T9631 |
IRAK-4 protein kinase inhibitor 2
|
IRAK | Immunology/Inflammation; NF-κB |
IRAK-4 protein kinase inhibitor 2 是有效的白介素 1 受体相关激酶 4 抑制剂,IC50为 4 μM。它在与炎症和免疫相关的疾病领域有研究价值。 | |||
T2457 |
IRAK-1-4 Inhibitor I
IRAK-1/4 Inhibitor I,IRAK-1/4 Inhibitor |
IRAK | Immunology/Inflammation; NF-κB |
IRAK-1-4 Inhibitor I 是一种IRAK1/4双重抑制剂,其IC50分别为 0.2 μM 和 0.3 μM。 | |||
T4140 |
IRAK4-IN-1
|
IRAK | Immunology/Inflammation; NF-κB |
IRAK4-IN-1 是白细胞介素-1 受体相关激酶 4 抑制剂(IC50:7 nM)。 | |||
T11673 |
IRAK4-IN-4
|
IRAK; cGAS | Immunology/Inflammation; NF-κB |
IRAK4-IN-4 (化合物 15) 是白介素-1 受体相关激酶抑制剂,IC50为 2.8 nM。它还抑制环 GMP-AM 合酶 ,IC50为 2.1 nM。 | |||
T4299 | AS-2444697 | IRAK | Immunology/Inflammation; NF-κB |
AS2444697 是一种口服有效的IRAK-4抑制剂,IC50为 21 nM。它对人和大鼠 IRAK-4 活性具有抑制作用。它通过抗炎作用表现出肾脏保护作用。 | |||
T14367 |
AZ1495
|
IRAK; CDK; Haspin Kinase | Cell Cycle/Checkpoint; Immunology/Inflammation; NF-κB |
AZ1495 是一种口服有活性的白介素-1受体相关激酶 4(IRAK4)抑制剂,能够作用于 IRAK4 (IC50:5 nM)和 IRAK1 (IC50:23 nM)。可用于研究突变型 MYD88L265P 弥漫性 B 细胞淋巴瘤 (DLBCL) 。 | |||
T5354 |
IRAK4-IN-7
CA-4948 |
IRAK | Immunology/Inflammation; NF-κB |
IRAK4-IN-7 (CA-4948) 是白介素 1 受体相关激酶 4 (IRAK4) 的选择性抑制剂,口服有活性。它可用于研究癌症以及炎症疾病。 | |||
T25150 |
BI-69A11
BI 69A11,(E)-3-(1H-Benzo[d]imidazol-2-yl)-1-(6-chloro-2-hydroxy-4-phenylquinolin-3-yl)prop-2-en-1-one |
NF-κB; Akt | Cytoskeletal Signaling; NF-κB; PI3K/Akt/mTOR signaling |
BI-69A11 ((E)-3-(1H-Benzo[d]imidazol-2-yl)-1-(6-chloro-2-hydroxy-4-phenylquinolin-3-yl)prop-2-en-1-one) 是一种双重 AKT 和 NFkB 通路抑制剂。它通过靶向 Akt 增强结肠癌细胞对 mda-7/IL-24 诱导的生长抑制的敏感性。 | |||
T7672 |
MD2-TLR4-IN-1
|
TLR | Immunology/Inflammation |
MD2-TLR4-IN-1 是一种骨髓分化蛋白 2/toll 样受体 4 (MD2-TLR4) 复合物抑制剂,能够抑制巨噬细胞 LPS 诱导的 TNF-α 和 IL-6 的表达,IC50值分别为 0.89 和 0.53 μM。 | |||
T9948 |
NecroX-7
LC-280126,LC28-0126,LC28 0126 |
NADPH-oxidase | Immunology/Inflammation |
NecroX-7 (LC-280126) 是一种有效的自由基清除剂和 HMGB1(高迁移率族蛋白 1) 抑制剂。NecroX-7 可以作为对乙酰氨基酚毒性的解毒剂。NecroX-7 通过抑制缺血/再灌注损伤中 HMGB1 的释放发挥保护作用。NecroX-7 抑制 HMGB1 诱导的 TNF 和 IL-6的释放,以及TLR-4和晚期糖基化终产物受体的表达,用于移植物抗宿主病 (GVHD) 研究。 | |||
T0097 |
MRT67307
MRT67307 HCl |
IκB/IKK; Autophagy | Autophagy; NF-κB |
MRT67307 是一种IKKε和TBK-1的双抑制剂,IC50分别为 160 和 19 nM。它抑制细胞自噬,也可抑制ULK1和ULK2,IC50分别为 45 和 38 nM。 | |||
T79256 |
DPP-4-IN-8
|
||
DPP-4-IN-8 (compound 27) 是一种高效的选择性DPP4抑制剂,具有 0.96 μM 的 Ki。该化合物能够抑制 Caco-2 和 HepG-2 细胞中的 DPP4 二肽酶活性,并剂量依赖性地降低 TNF-α、IL-6 和 IL-1β 的表达水平[1]。 | |||
T23028 |
MRT67307 HCl (1190378-57-4 free base)
MRT67307 HCl |
Others | Others |
MRT67307 is an inhibitor for TBK1, IKKε , MARK1-4 and NUAK1 with IC50 value of 19, 160, 27-52 and 230nM , respectively [1]. It is an inhibitor for ULK1and ULK2 with IC50 value of 45 and 38nM, respectively [2]. Also, it is a salt inducible kinase (SIK) inhibitor with IC50 value of 250, 67 and 430nM for SIK1, SIK2 and SIK3, respectively.<br />SIKs prevent the formation of regulatory macrophages and their inhibition induces increasing in some markers of regulatory macrophages, such as IL-10 and oth... | |||
T37590 |
ML 3403
|
||
p38 MAPK inhibitor (IC50 = 0.38 μM). Inhibits the release of IL-1β and TNF-α in a peripheral blood mononuclear cell (PBMC) assay (IC50 values are 0.039 and 0.16 μM respectively). Laufer et al (2003) Novel substituted pyridinyl imidazoles as potent anticytokine agents with low activity against hepatic cytochrome P450 enzymes. J.Med.Chem. 46 3230 PMID:12852754 |Kammerer et al (2007) Pharmacokinetics of ML3403 ({4-[5-(4-fluorophenyl)-2-methylsulfanyl-3H-imidazol-4-yl]-pyridin-2-yl}-(1-phenylethyl)-... | |||
T73330 |
JAK-IN-24
|
||
JAK-IN-24 是一种 JAK 抑制剂,在 4 μM 或 1 mM ATP 存在时,IC50分别为 0.534 和 24 nM。JAK-IN-24 还抑制 PBMCIL-15诱导的 STAT5磷酸化,IC50为 86.171 nM。 | |||
T79362 |
COX-2/15-LOX-IN-4
|
Lipoxygenase | Metabolism |
COX-2/15-LOX-IN-4(compound 5i)是一种针对COX-2和15-LOX的双重抑制剂,其IC50值分别为0.075 μM和1.97 μM。该化合物能有效地阻止LPS诱发的细胞内促炎细胞因子(IL-6, ROS)的产生,表现出明确的抗炎活性。 | |||
T60921 |
PF-07038124
|
||
PF-07038124是 PDE4 的抑制剂。PF-07038124 对 PDE4B2 的 IC50值为0.5 nM。PF-07038124 对IFNγ、IL-4 和 IL-13具有抑制活性,IC50值分别为 1.06、4.1 和125 nM。 | |||
T36629 | Givinostat | ||
Givinostat (ITF-2357) is a HDAC inhibitor with an IC50 of 198 and 157 nM for HDAC1 and HDAC3, respectively. Givinostat (ITF2357) suppresses total LPS-induced IL-1β production robustly compared with the reduction by ITF3056. At 25, 50, and 100 nM, Givinostat reduced IL-1β secretion more than 70%. Givinostat (ITF-2357) suppresses the production of IL-6 in PBMCs stimulated with TLR agonists as well as the combination of IL-12 plus IL-18. IL-6 secretion decreases to 50% at 50 nM Givinostat, but at 1... | |||
T38106 |
JC-171
|
||
JC-171 is a selective NLRP3 inflammasome inhibitor, with an IC50 of 8.45 μM for inhibiting LPS/ATP-induced interleukin-1β (IL-1β) release from J774A.1 macrophages[1]. JC-171 (0-100 μM) blocks NLRP3 inflammasome activation and IL-1β production in primary macrophages dose dependently[1]. ... | |||
T35864 |
T-5342126
|
||
T-5342126 is a toll-like receptor 4 (TLR4) antagonist.1It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50= 27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s = 110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-depen... | |||
T37604 | ITK inhibitor | ||
Interleukin-2-inducible T cell kinase (ITK) is a non-receptor tyrosine kinase expressed in T cells, NKT cells and mast cells which plays a crucial role in regulating the T cell receptor (TCR), CD28, CD2, chemokine receptor CXCR4, and FcepsilonR-mediated signaling pathways. ITK inhibitors can be used for the treatment of inflammation and immune-mediated disorders. ITK inhibitor (N-[5-[[3-[(4-Acetylpiperazin-1-yl)carbonyl]-4-methyl-6-methoxy-phenyl]thio]thiazol-2-yl]-4-(N-1,2-dimethylpropylaminome... | |||
T35829 | CC-90005 | ||
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS... | |||
T60935 |
H-Tyr-Phe-OH
|
||
H-Tyr-Phe-OH (L-Tyrosyl-L-phenylalanine) 可用作区分良性甲状腺结节和甲状腺癌的生物标志物。H-Tyr-Phe-OH 是一种口服活性的血管紧张素转换酶抑制剂,在50 μM 时抑制率为 48%。H-Tyr-Phe-OH 具有黄嘌呤氧化酶抑制活性 (降低尿酸) ,可调节中性粒细胞样细胞中 IL-8 的产生。 | |||
T60511 |
Theophylline sodium glycinate
|
||
Theophylline (1,3-Dimethylxanthine) sodium glycinate 是一种有效的磷酸二酯酶 (PDE) 抑制剂,可抑制 PDE3 活性以松弛气道平滑肌。Theophylline sodium glycinate 可用于研究哮喘和慢性阻塞性肺疾病 (COPD) 。Theophylline sodium glycinate 也是一种腺苷受体拮抗剂和组蛋白脱乙酰酶 (HDAC) 激活剂。 Theophylline sodium glycinate 通过增加 IL-10 和抑制 NF-κB 的核输入而具有抗炎活性。Theophyllin sodium glycinate 可诱导细胞凋亡。 | |||
T37614 |
LDN-0088050
|
||
LDN 0088050 is selectivity adipocyte fatty acid binding protein (AFABP, FABP4) inhibitor with Ki values of 0.29 and 1.3 μM for FABP4 and FABP3, respectively. LDN 0088050 binds to FABP4 with a Kd of 2.05 μM[1]. Ki: 0.29 μM (FABP4), 1.3 μM (FABP3)[1]Kd: 2.05 μM (FABP4)[1] LDN 0088050 significantly inhibits LPS-induced expression of both TNFα and IL-6 in RAW264.7 cells[1]. [1]. Zhou Y, et al. The discovery of novel and selective fatty acid binding protein 4 inhibitors by virtual screening and biolo... | |||
T36648 | Tucatinib hemiethanolate | ||
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM. Tucatinib hemiethanolate has nanomolar activity against purified HER2 enzyme and is approximately 500-fold selective for HER2 versus EGFR in cell-based assays. Tucatinib selectively inhibits the receptor tyrosine kinase HER2 relative to EGFR[1].Tucatinib blocks proliferation and the phosphorylation of HER2 and its downstream effector, Akt in HER2 overexpressing cell lines. In the ... |