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Cat. No. | Product Name | Target | Signaling Pathways |
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T11241 | p38 MAPK-IN-2 | Others | Others |
p38 MAPK-IN-2 is an inhibitor of p38 kinase. | |||
T63119 |
NF-κB/MAPK-IN-1
|
NF-κB; MAPK | MAPK; NF-κB |
NF-κB/MAPK-IN-1 是一种有效的 NF-κB 和 MAPK 通路双重抑制剂,具有潜在的抗炎活性,抑制 NO 生成,对 LPS 诱导的iNOS,COX-2,ERΚ和P38激活有抑制作用。 NF-κB/MAPK-IN-1 可用于预防和治疗类风湿关节炎 (RA) 。 | |||
T6934 |
Pexmetinib
ARRY-614 |
Tie-2; p38 MAPK; Autophagy | Autophagy; MAPK; Tyrosine Kinase/Adaptors |
Pexmetinib (ARRY-614) 是一种口服生物可利用的双重 p38 MAPK/Tie-2 抑制剂,可研究急性骨髓性白血病。在 HEK-293 细胞系中的 IC50 为 4 nM/18 nM。 | |||
T4431 |
Olodanrigan
PD-126055,EMA401 |
RAAS | Endocrinology/Hormones |
Olodanrigan (EMA401) 是具有口服活性、高选择性及外周受限的血管紧张素 Ⅱ 类型 2 受体(AT2R)拮抗剂。它的缓解疼痛的机制可能是:抑制增强的 AngII/AT2R 诱导的 p38 和 p42/p44 MAPK 激活,进而阻碍 DRG 神经元的过度兴奋性及 DRG 神经元的萌发。它可用于研究神经性疼痛。 | |||
T1496 |
Amiodarone hydrochloride
盐酸胺碘酮,Amiodar,Amiodarone HCl,Nexterone |
Potassium Channel; Adrenergic Receptor; Autophagy | Autophagy; GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience |
Amiodarone hydrochloride (Amiodarone HCl) 是一种抗心绞痛和 III 类抗心律失常药物,通过抑制钾通道和电压门控钠通道来增加心室和心房肌肉作用的持续时间,可导致心率和血管阻力降低。它通过成纤维细胞中的 ERK1/2和 p38 MAPK 信号传导诱导细胞增殖和肌成纤维细胞分化,可研究室上性和室性心律失常。 | |||
T37590 |
ML 3403
|
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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)-... | |||
T61755 |
E6201
|
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E6201 (ER-806201) is a potent dual kinase inhibitor targeting MEK1 and FLT3, inhibiting their activities in an ATP-competitive manner. It effectively suppresses MEK1-induced ERK2 phosphorylation (IC50 = 5.2 nM), MKK4-induced JNK phosphorylation (IC50 = 91 nM), and MKK6-induced p38 MAPK phosphorylation (IC50 = 19 nM). E6201 exhibits anti-tumor and anti-psoriasis effects [1] [2]. | |||
T41240 |
Verrucarin A
|
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Verrucarin A (Muconomycin A) 是一种 D 型大环真菌毒素。Verrucarin A 是一种蛋白质合成 (protein synthesis) 的抑制剂,来源于Myrothecium verrucaria,可抑制白血病细胞系生长,并激活巨噬细胞 caspases、凋亡和炎症信号。Verrucarin A 能有效提高 p38 MAPK 的磷酸化,降低 ERK/Akt 的磷酸化。Verrucarin A 通过 p21 和 p53 的诱导引起细胞周期调控的解除。 | |||
T79304 |
Semapimod
CPSI-2364,CNI-1493 free base |
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Semapimod是一种抑制促炎细胞因子产生的化合物,具有抑制TNF-α、IL-1β和IL-6功能。它通过抑制巨噬细胞的p38 MAPK以及一氧化氮的生成发挥作用,并且能够抑制TLR4信号传导(IC50约为0.3 μM)。Semapimod对于治疗各类炎症和自身免疫性疾病显示出潜在效用。 | |||
T35536 |
Tpl2 Kinase Inhibitor (hydrochloride)
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Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5... | |||
T68321 |
AS1940477
|
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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... | |||
T35463 |
(±)14(15)-EET
(±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET |
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(±)14(15)-EET is a metabolite of arachidonic acid that is formed via epoxidation of arachidonic acid by cytochrome P450.[1],[2] It prevents increases in leukotriene B4, ICAM-1, and chemokine (C-C motif) ligand 1 (CCL2) induced by oxidized LDL in primary rat pulmonary artery endothelial cells (RPAECs) when used at a concentration of 1 μM.[3] (±)14(15)-EET induces dilation of preconstricted isolated canine coronary arterioles (EC50 = 0.2 pM).[4] It reduces myocardial infarct size as a percentage o... |
Cat. No. | Product Name | Target | Signaling Pathways |
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T5S2283 |
Sesamolin
|
p38 MAPK; Caspase; JNK | Apoptosis; MAPK; Proteases/Proteasome |
Sesaminol 是从Justicia orbiculata 中分离得到的一种天然产物,抑制脂质过氧化,具有神经保护作用和抗氧化活性。它通过抑制JNK、p38 MAPKs 和caspase-3磷酸化,抑制MAPK 的级联反应。 | |||
T5S2358 |
Dehydrocorydaline
Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine |
BCL; PARP; p38 MAPK; Caspase; Parasite; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Proteases/Proteasome |
Dehydrocorydaline (13-Methylpalmatine) 是一种生物碱。它调节Bax,Bcl-2蛋白表达,激活caspase-7,caspase-8,并使PARP 失活。它能增强p38 MAPK 活化,具有抗炎、抗癌等功效。它具有强大的抗疟疾作用,并具低细胞毒性。 | |||
T5S1058 |
Triptonide
雷公藤内酯酮,PG 492,NSC 165677 |
Apoptosis; Wnt/beta-catenin; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling; Stem Cells |
Triptonide (PG 492) 是从雷公藤中鉴定出的一种天然产物,是一种 Wnt 信号抑制剂,其 IC50约为 0.3 nM。它具有免疫抑制、抗炎、避育、神经保护和抗淋巴瘤作用。 | |||
T3008 |
Lawsone methyl ether
2-Methoxy-1,4-naphthoquinone,2-Methoxy-p-naphthoquinone,2-Methoxynaphthoquinone,2-甲氧基-1,4-萘并醌 |
Apoptosis; Antibacterial; Antifungal | Apoptosis; Microbiology/Virology |
Lawsone methyl ether (2-Methoxy-1,4-naphthoquinone) 是从凤仙花和Swertia calycina 中分离出的,有抗真菌和抗菌活性。 | |||
T3763 |
Fumaric acid
Lichenic acid,Fumarate,2-Butenedioic acid,Trans-Butenedioic acid,反丁烯二酸,Donitic acid,Allomaleic acid,富马酸 |
Endogenous Metabolite | Metabolism |
Fumaric acid (2-Butenedioic acid) 与烟酸酶缺乏症相关,是癌症相关的内源性代谢物。 | |||
TN5888 |
Toddaculin
|
Others | Others |
Toddaculin 是一种天然香豆素,抑制过度的破骨细胞活性并增强成骨细胞分化和矿化。它可诱导白血病细胞分化和凋亡,具有抗炎活性。 | |||
T3923 |
Calycosin
Cyclosin,3'-Hydroxyformononetin,异黄酮,毛异黄酮 |
Apoptosis; Tyrosinase | Apoptosis; Proteases/Proteasome |
Calycosin (Cyclosin) 是一抗氧化和抗炎症活性天然产物。 | |||
T6S1538 |
Neochlorogenic acid
新绿原酸,trans-5-O-Caffeoylquinic acid,Neochlorogenate,金银花,5-O-Caffeoylquinic acid |
TNF; NF-κB; COX; Antibacterial; Interleukin | Apoptosis; Immunology/Inflammation; Microbiology/Virology; Neuroscience; NF-κB |
Neochlorogenic acid (trans-5-O-Caffeoylquinic acid) 是在干果和其他植物中发现的一种多酚类天然产物,可抑制iNOS 和COX-2蛋白表达,抑制TNF-α和IL-1β产生,还抑制磷酸化的NF-κB p65和p38 MAPK 活化。 | |||
T6S1572 |
Sauchinone
|
ERK; p38 MAPK; NF-κB | MAPK; NF-κB |
Sauchinone 是一种从Saururus chinensis 中获得的非对映异构的木脂素。它通过抑制I-κBα磷酸化和p65核易位来抑制 LPS 诱导的 iNOS,TNF-α 和 COX-2 表达。它具有抗炎和抗氧化活性。 | |||
T2S2362 |
Dehydrocorydaline nitrate
去氢延胡索甲素硝酸盐,硝酸脱氢紫堇碱 |
BCL; Others; PARP; p38 MAPK; Caspase; Parasite; Autophagy | Apoptosis; Autophagy; Chromatin/Epigenetic; DNA Damage/DNA Repair; MAPK; Microbiology/Virology; Others; Proteases/Proteasome |
Dehydrocorydaline nitrate 是生物碱。Dehydrocorydaline 调节 Bax,Bcl-2蛋白表达,激活 caspase-7,caspase-8,并使 PARP 失活。它能增强 p38 MAPK 活化,具有抗炎、抗癌、抗疟疾等功效。 | |||
T4S2326 |
Cornuside
7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside |
ERK; p38 MAPK; NF-κB; JNK | MAPK; NF-κB |
Cornuside (Comuside) 是从山茱萸的果实中分离出的环烯醚萜苷,可用于炎症疾病的研究和促进血液循环。 它通过下调 MAPK 和 NF-κB 信号通路抑制肥大细胞介导的过敏反应,用于炎性过敏性疾病中的潜能。 | |||
TN5050 |
Sprengerinin C
|
NADPH-oxidase; VEGFR; p38 MAPK; ROS; Akt; PI3K; mTOR; p53 | Angiogenesis; Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; MAPK; PI3K/Akt/mTOR signaling; Tyrosine Kinase/Adaptors |
Sprengerinin C exerts anti-tumorigenic effects in hepatocellular carcinoma via inhibition of proliferation and angiogenesis and induction of apoptosis, it can strongly suppress tumor angiogenesis in human umbilical vein endothelial cells, it blocks vascul |