Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T12997 |
SR-318
|
p38 MAPK; TNF | Apoptosis; MAPK |
SR-318 是p38 MAPK 的选择性抑制剂,对 p38α,p38β 和 p38α/β 的IC50分别为 5 nM,32 nM 和 6.11 μM。它有效抑制全血中TNF-α的释放,IC50为 283 nM。它显示出抗癌和抗炎活性。 | |||
T67944 |
p38 MAP Kinase Inhibitor Ⅵ
|
p38 MAPK | MAPK |
p38 MAP Kinase Inhibitor Ⅵ是一种有效的p38 MAP Kinase 抑制剂,具有抗炎活性。 | |||
T67830 |
p38α inhibitor 3
|
p38 MAPK | MAPK |
p38α inhibitor 3是一种丝裂原活化蛋白激酶P38α的抑制剂,可以有效阻断成肌细胞分化。 | |||
T78652 |
p38α inhibitor 4
|
p38 MAPK | MAPK |
p38α inhibitor 4 是一种选择性 MAPK p38α抑制剂,看而用于研究糖尿病、疼痛和慢性炎症。 | |||
T6496 |
Vactosertib
TEW-7197,EW-7197 |
ALK; TGF-beta/Smad | Angiogenesis; Stem Cells; Tyrosine Kinase/Adaptors |
Vactosertib (EW-7197) 是有效的、具有 ATP 竞争性的、具有口服活性的激活素受体样激酶 5 (ALK5) 抑制剂(IC50:12.9 nM)。它还以纳摩尔浓度抑制 ALK2 和 ALK4 (IC50为 17.3 nM),表现出强大的抗转移活性和抗癌作用。 | |||
T36010 |
p38 MAPK Inhibitor
|
p38 MAPK | MAPK |
p38 MAPK Inhibitor 是p38 MAPK 激酶的有效抑制剂(IC50= 35 nM)。p38 MAPK Inhibitor 抑制癌基因RAS 诱导的衰老。 | |||
T36012 |
p38α inhibitor 2
|
||
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets[1]. [1]. Raubo P, et al. The discovery and evaluation of 3-amino-2(1H)-pyrazinones as a novel series of selective p38α MAP kinase inhibitors [published online ahead of pr... | |||
T36011 |
p38 MAP Kinase Inhibitor IV
p38 MAPK Inhibitor IV |
||
p38 MAPK inhibitor IV is an ATP-competitive inhibitor of p38 MAP kinases with IC50 values of 0.13, 0.55, 5.47, and 8.63 μM for p38α, p38β, p38x, and p38δ, respectively, in vitro.[1] It also inhibits LPS-induced TNF-α and IL-1β cytokine production (IC50s = 22 and 44 nM, respectively) in human peripheral blood mononuclear cells. | |||
T35420 |
(S)-p38 MAPK Inhibitor III
(S)-p38 MAPK Inhibitor III |
||
(S)-p38 MAPK inhibitor III is a methylsulfanylimidazole that inhibits p38 MAP kinase (IC50 = 0.90 μM in vitro). It is cell-permeable, potently blocking the release of TNF-α and IL-1β from human peripheral blood mononuclear cells (IC50s = 0.37 and 0.044 μM, respectively). | |||
T79028 |
p38 Kinase inhibitor 4
|
p38 MAPK | MAPK |
p38 Kinase inhibitor 4 (compound 135) 是高效的 p38 MAP Kinase 抑制剂,具有显著的生物活性。 | |||
T61803 | p38 MAPK-IN-3 | ||
p38 MAPK-IN-3 (Compound 2c) is a potent inhibitor of p38α MAPK, displaying antitumor properties by promoting apoptosis and increasing reactive oxygen species (ROS) production [1]. | |||
T81441 | PLK1/p38γ-IN-1 | p38 MAPK | MAPK |
PLK1/p38γ-IN-1(化合物14)为PLK1与p38γ多靶点抑制剂,体外有效抑制人肝细胞癌与肝母细胞瘤细胞增殖。 | |||
T2277 |
Losmapimod
GSK-AHAB,GW856553X,6-[5-(环丙基氨基甲酰基)-3-氟-2-甲基苯基]-N-(2,2-二甲基丙基)吡啶-3-甲酰胺,GW856553,洛批莫德,SB856553 |
p38 MAPK; Autophagy | Autophagy; MAPK |
Losmapimod (GSK-AHAB) 是一种可口服的特异性 p38 MAPK 抑制剂,抑制 p38α 和 p38β 的 pKi 值分别为 8.1 和 7.6。 | |||
T6150 |
TAK-715
|
p38 MAPK; Casein Kinase; JNK | MAPK; Metabolism; Stem Cells |
TAK-715 是一种具有口服活性的p38 MAPK 抑制剂,对 p38α 和 p38β 的IC50分别为 7.1 nM 和200 nM。它抑制酪蛋白激酶 I (CK1δ/ε),调节 Wnt/β-catenin 信号传导的激活,有抗炎活性。 | |||
T6976 |
SB 239063
SB239063 |
p38 MAPK; Autophagy | Autophagy; MAPK |
SB 239063 (SB239063) 是一种选择性、可口服的 p38 MAPK 抑制剂,对重组纯化的人 p38α 的 IC50值为 44 nM,具有抗哮喘作用,还被用于增强因衰老或疾病受损的记忆,如阿尔茨海默病。 | |||
T16721 |
Ralimetinib
LY2228820 |
Others | Others |
Ralimetinib selectively inhibits phosphorylation of MK2 (Thr334) and has no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc. Ralimetinib is an effective and selective, ATP-competitive inhibitor of p38 MAPK α/β (IC50s: 5.3 and 3. | |||
T18681 |
SJFα
|
Others | Others |
SJFα is a 13-atom linker PROTAC. SJFα degrades p38α with a DC50 of 7.16 nM, but is far less effective at degrading p38δ (DC50=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 μM[1]. | |||
T70638 |
p38-α MAPK-IN-5
|
||
p38-α MAPK-IN-5 是一种有效的 p38α抑制剂,对 p38α、p38 β、p38γ、p38δ 的 IC50分别为 0.1 nM、0.2 nM、944 nM、4100 nM。p38-α MAPK-IN-5 具有抗炎作用,并且具有用于哮喘和慢性阻塞性肺病 (COPD) 研究的潜力。 | |||
T69898 | NG25 trihydrochloride | ||
NG25 trihydrochloride is a type II kinase inhibitor that inhibits MAP4K2 and TAK1. It also inhibits the Src family kinases Src and LYN and Abl family kinases as well as CSK, FER, and p38α. NG 25 prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectively. NG 25 decreases cell viability of HCT116KRASWT, and to a greater degree of HCT116KRASG13D, colorectal cancer cells in a concentration... | |||
T68321 |
AS1940477
|
||
AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC(50)=0.45n M; PHA/TNFα, IC(50)=0.40 nM). In addition, equivalent c... | |||
T36779 |
NG 25 (hydrochloride hydrate)
|
||
NG 25 is a type II kinase inhibitor that inhibits MAP4K2 and TAK1 (IC50s = 21.7 and 149 nM, respectively).1It also inhibits the Src family kinases Src and LYN (IC50s = 113 and 12.9 nM, respectively) and Abl family kinases (IC50s = 75.2 nM), as well as CSK, FER, and p38α (IC50s = 56.4, 82.3, and 102 nM, respectively). NG 25 (100 nM) prevents TNF-α-induced IKKα/β phosphorylation and IκB-α degradation in L929 cells. It inhibits secretion of IFN-α and IFN-β induced by CpG type B and CL097, respectiv... |