Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T16812 |
RWJ-67657
JNJ 3026582 |
p38 MAPK | MAPK |
RWJ-67657 (JNJ 3026582) 是一种可口服的选择性p38α和p38β抑制剂,IC50分别为 1 和 11 μM。它是心脏保护剂,具有抗炎和抗肿瘤活性。 | |||
T6927 |
Pamapimod
R1503,帕吡莫德,Ro4402257 |
p38 MAPK; Autophagy | Autophagy; MAPK |
Pamapimod (R1503) 是一种新型的选择性 p38 丝裂原活化蛋白激酶抑制剂,对于p38α和p38β的IC50分别为 14 nM 和 480 nM,Ki 分别为 1.3 nM 和 120 nM,对 p38δ 或 p38γ 亚型没有活性,可研究类风湿关节炎和其他自身免疫性疾病。 | |||
T36012 |
p38α inhibitor 2
|
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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。 | |||
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。 | |||
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]. | |||
T1974 |
PH-797804
PH797804 |
p38 MAPK; Autophagy | Autophagy; MAPK |
PH-797804 是一种 ATP 竞争性的,选择性的p38α/p38β抑制剂,对 p38α 的IC50为 26 nM,Ki 值为 5.8 nM,对 p38β 的Ki 值为 40 nM。 | |||
T10277 |
AL 8697
|
p38 MAPK | MAPK |
AL 8697 是一种特异性 p38α MAPK 抑制剂 (IC50 = 6 nM),其特异性是 p38β (IC50 = 82 nM) 的 14 倍,是其他 91 种激酶的 300 倍。 AL 8697 具有抗炎活性。 | |||
T12871 |
Talmapimod
他匹莫德,SCIO-469 |
p38 MAPK | MAPK |
Talmapimod (SCIO-469) 是 选择性的,具有口服活性的,ATP 竞争性的 p38α抑制剂,对 p38α和 p38β的 IC50 值分别是 9 nM 和90 nM。Talmapimod 在 20 个其他激酶 (包括其他 MAPKs) 上显示出至少 2000 倍的选择性。 | |||
T6089 |
Neflamapimod
VX-745 |
p38 MAPK; Autophagy | Autophagy; MAPK |
Neflamapimod (VX-745) 是一种可穿过血脑屏障的,高选择性的p38α抑制剂,对 p38α 的IC50值为 10 nM,p38β 的IC50值为 220 nM。它对 p38β 的特异性高 22 倍,具有抗炎活性。 | |||
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。 | |||
T7661 |
SD-169
SD 169,1H-吲哚-5-甲酰胺 |
p38 MAPK | MAPK |
SD-169 (SD 169) 是一种可口服的 ATP 竞争性MAPK p38α抑制剂,IC50值为 3.2 nM。它对p38β MAPK 的IC50值为 122 nM。它通过抑制 T 细胞的浸润和活化阻止糖尿病的发展。 | |||
T2513 |
VX-702
|
p38 MAPK; Autophagy | Autophagy; MAPK |
VX702 是一种高度特异性的 p38α MAPK 抑制剂,对 p38α 的选择性比 p38β 高 14 倍。它是一种小分子研究口服抗细胞因子疗法,用于治疗炎症性疾病,如类风湿性关节炎。 | |||
T4597 |
UM-164
UM164,DAS-DFGO-II |
p38 MAPK; Src; Autophagy | Angiogenesis; Autophagy; MAPK; Tyrosine Kinase/Adaptors |
UM-164 (DAS-DFGO-II) 是一种高效的c-Src 抑制剂,Kd 为 2.7 nM。它还抑制p38α和p38β活性。 | |||
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。 | |||
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。 | |||
T12871L |
Talmapimod hydrochloride
SCIO-469 hydrochloride |
p38 MAPK | MAPK |
Talmapimod hydrochloride is a selective and ATP-competitive p38α inhibitor (IC50: 9 nM). It also shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs. | |||
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。 | |||
T16477 | PF-03715455 | p38 MAPK | MAPK |
PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 is an effective inhibitor of inhaled p38 MAPK. PF-03715455 displays some selectivity for p38α over p38β (respective IC50: 0.88 and 23 nM). PF-0371545 | |||
T18682 |
SJFδ
|
Others | Others |
SJFδ is a 10-atom linker PROTAC. SJFδ degrades p38δ with a DC50 of 46.17 nM, but does not degrade p38α, p38β, or p38γ[1]. | |||
T10298L |
AMG-548
|
p38 MAPK | MAPK |
AMG-548 is an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ and is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM | |||
T10298 |
AMG-548 hydrochloride (864249-60-5 free base)
AMG-548 hydrochloride |
p38 MAPK | MAPK |
AMG-548 hydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ/p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50: 3 nM). | |||
T7162 |
R1487 Hydrochloride
R1487 (Hydrochloride) |
p38 MAPK; Autophagy | Autophagy; MAPK |
R1487 Hydrochloride (R1487(Hydrochloride)) 是一种可口服的高选择性 p38α 抑制剂,对 p38α 和 p38β 的Kd 值分别为 0.2 nM 和 29 nM。 | |||
T63371 | AMG-548 hydrochloride | ||
AMG-548 hydrochloride 是选择性的、口服具有活力的 p38α 抑制剂,Ki 值为 0.5 nM,对p38β略有选择性 (Ki=36 nM) 并且对 p38γ 和 p38δ 具有高于1000 倍的选择性。AMG 548 hydrochloride 同时能够有效抑制全血 LPS 刺激的TNFα,IC50值为 3 nM。AMG-548 hydrochloride 能够直接抑制酪蛋白激酶 1 (Casein kinase 1) 同种型 δ 和 ε ,进而对 Wnt 信号传导具有抑制作用。 | |||
T63762 | AMG-548 dihydrochloride | ||
AMG-548 dihydrochloride 是选择性的、口服具有活力的 p38α 抑制剂,Ki 值为 0.5 nM,对 p38β略有选择性 (Ki=36 nM) 并且对 p38γ 和 p38δ 具有 >1000 倍的选择性。AMG-548 dihydrochloride 对全血 LPS 刺激的 TNFα 表现出抑制作用,IC50 值为 3 nM。AMG-548 dihydrochloride 能够直接抑制酪蛋白激酶 1 (Casein kinase 1) 同种型 δ 和 ε ,并抑制 Wnt 信号传导。 | |||
T10298L2 |
AMG-548 dihydrochloride (864249-60-5 free base)
AMG-548 dihydrochloride |
p38 MAPK | MAPK |
AMG-548 dihydrochloride is an orally active and selective p38α inhibitor (Ki: 0.5 nM) and shows slightly selective over p38β (Ki: 36 nM) and >1000 fold selective against p38γ/p38δ. It is also extremely potent in the inhibition of whole blood LPS stimulate | |||
T36260 | NR 7h | ||
Potent and selective p38α and p38β degrader (DC50 < 50 nM). Displays no significant degradation of p38γ, p38δ, JNK1/2 or ERK1/2. Inhibits phosphorylation of MK2 in UV-treated cancer cells and LPS-stimulated bone marrow-derived macrophages (BMDM). Exhibits similar effect to p38α gene knockout in BBL358 cells. Active in vivo. | |||
T2301 |
SB 202190
FHPI,SB202190 |
Apoptosis; p38 MAPK; Autophagy | Apoptosis; Autophagy; MAPK |
SB 202190 (FHPI) 是一种 p38 MAPK 抑制剂,可以抑制 p38α 和 p38β2 (IC50=50/100 nM),具有选择性和细胞渗透性。SB 202190 具有抗肿瘤活性,还可以诱导人胚胎干细胞向心肌细胞分化。 | |||
T37581 | SCIO 469 hydrochloride | ||
Selective, ATP-competitive p38 inhibitor (IC50 = 9 nM for p38α in vitro). Displays approximately 10-fold selectivity for p38α over p38β and 2000-fold selectivity for p38α over 20 other kinases. Reduces p38α phosphorylation in multiple myeloma cells in vitro and in vivo; activity results in decreased tumor burden and angiogenesis in murine models of multiple myeloma. Also enhances bortezomib-induced cytotoxicity against multiple myeloma cells. Hideshima et al (2004) p38 MAPK inhibition enhances P... | |||
T70638 |
p38-α MAPK-IN-5
|
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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。 | |||
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. |