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Cat. No. | Product Name | Target | Signaling Pathways |
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T16424 | p38 MAPK-IN-1 | p38 MAPK | MAPK |
p38 MAPK-IN-1 displays sustained levels, low clearance, and good bioavailability. p38 MAPK-IN-1 is a novel effective and selective inhibitor of p38 MAPK (IC50: 68 nM). | |||
T12347 |
p38-α MAPK-IN-1
|
p38 MAPK; Autophagy | Autophagy; MAPK |
p38-α MAPK-IN-1 是一种 MAPK14 (p38-α) 抑制剂,在 EFC 置换试验和 HTRF 试验中 IC50 分别为 2300 nM 和 5500 nM。 | |||
T9697 |
ASK1-IN-1
|
ASK | Apoptosis |
ASK1-IN-1 是一种凋亡信号调节激酶 1(SK1) 抑制剂,具有良好的效价 (细胞IC50=138 nM; BiochemicalIC50=21 nM)。ASK1-IN-1具有中枢神经系统渗透性。 | |||
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。 | |||
T2367 |
SKF-86002
SKF86002 |
p38 MAPK; TNF | Apoptosis; MAPK |
SKF-86002 是一种可口服的 p38 MAPK 抑制剂,具有抗炎和抗关节炎活性,可用于缓解疼痛的研究。它能抑制脂氧合酶和环氧合酶介导的花生四烯酸代谢,还抑制脂多糖 (LPS) 刺激人单核细胞产生 IL-1 和 TNF-α,IC50为 1 μM。 | |||
T26280 |
TL4-12
TL4 12 |
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TL4-12 is a MAP4K2 (GCK) inhibitor that inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation in vitro. | |||
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]. | |||
T61091 | p38-α MAPK-IN-4 | ||
p38-α MAPK-IN-4 (Compound 69) 是一种选择性的p38α MAPK 抑制剂,IC50为 1.5 μM。p38-α MAPK-IN-4 在体内可快速、强烈地抑制机械性触诱发痛 (mechanical allodynia) 的发生。 | |||
T36011 |
p38 MAP Kinase Inhibitor IV
p38 MAPK Inhibitor IV |
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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. | |||
T69748 |
AG-12286
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AG-12286 is a pan-CDK inhibitor. AG-012986 may be useful in the treatment of tumors by inhibiting p38 MAPK phosphorylation. Note: many vendors confused the structure of AG-12286 (CAT#573461, CAS# 223784-75-6) with AG-012986 (CAT#406184, CAS# is 486414-35-1). | |||
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]. | |||
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。 | |||
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。 | |||
T38048 |
Globotetraosylceramides (porcine RBC)
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Globotetraosylceramides are bioactive neutral glycosphingolipids. They are the major glycolipids in human erythrocytes. They act as receptors for the Shiga toxins Stx1, Stx2, and Stx2e, the cytotoxic protein pierisin-1, and parvovirus B19. Globotetraosylceramides increase the expression of proteins responsible for enamel deposition, including ameloblastin, amelogenin, and enamelin, in dental epithelial cells and activate the ERK and p38 MAPK signaling pathways. Levels of globotetraosylceramides ... | |||
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。 | |||
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。 | |||
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。 | |||
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。 | |||
T2768 |
Saikosaponin A
柴胡皂苷A,柴胡皂苷 A |
NF-κB; Antibacterial; Liver X Receptor | Metabolism; Microbiology/Virology; NF-κB |
Saikosaponin A 是银柴胡中的主要活性成分,有抗炎活性,可上调 LXRα的表达。 | |||
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。 | |||
T3S0737 |
Flavokawain A
2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A |
Apoptosis; p38 MAPK | Apoptosis; MAPK |
Flavokawain A (Flavokavain A) 是 kava 提取物中的查耳酮,是一种抗癌试剂,具有抗肿瘤活性。它通过 Bax 蛋白依赖和线粒体依赖的凋亡途径诱导细胞凋亡,有潜力用于膀胱癌的相关研究。 | |||
T6429 |
Caffeic Acid Phenethyl Ester
Phenylethyl Caffeate,咖啡酸苯乙酯,CAPE |
Apoptosis; NF-κB | Apoptosis; NF-κB |
Caffeic Acid Phenethyl Ester (Phenylethyl Caffeate) 是咖啡酸的苯乙醇酯,是蜂巢蜂胶的生物活性成分。它抑制核转录因子 NF-kappa B 的激活,具有抗肿瘤、细胞保护和免疫调节活性。它抑制 PDGF 诱导的血管平滑肌细胞增殖。 | |||
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。 | |||
TN5174 | Trichosanatine | MMP; LDL; p38 MAPK; Lipoxygenase; ROS | Immunology/Inflammation; MAPK; Metabolism; Proteases/Proteasome |
Trichosanatine and squamosamide, as potential candidates as lead compounds for further study in drug development process with the PP2A- α protein. Trichosanatine can alleviate oxidized low-density lipoprotein induced endothelial cells injury via inhibiting the LOX-1/p38 MAPK pathway. | |||
TN4635 | Neoechinulin A | NADPH-oxidase; Beta Amyloid; ASK; IκB/IKK; p38 MAPK; TNF; NOS; NF-κB; COX; Prostaglandin Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation; MAPK; Neuroscience; NF-κB |
Neoechinulin A has anti-inflammatory effect against LPS-stimulated RAW264.7 macrophages through inhibition of the NF-κB and p38 MAPK pathways, it may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regu |