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26
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T60754 |
MAPK-IN-1
|
||
MAPK-IN-1 (Compound 2) 是MAPK 信号通路的抑制剂,具有抗神经炎症和神经保护活性,可用于研究阿尔兹海默症。MAPK-IN-1 以23.84 μM 的IC50值抑制AChE。 | |||
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。 | |||
T11943 |
MAPK13-IN-1
|
p38 MAPK | MAPK |
MAPK13-IN-1 是一种有效的 MAPK13 (p38δ) 抑制剂(IC50:620 nM)。 | |||
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). | |||
T11224 |
Rineterkib
ERK-IN-1 |
ERK; Raf | MAPK |
Rineterkib (ERK-IN-1) 是口服有效的RAF 和ERK1/2的抑制剂,与 KRAS-突变型非小细胞肺癌、BRAF-突变型非小细胞肺癌、KRAS-突变型胰腺癌、KRAS -突变型结肠癌和 KRAS-突变型卵巢癌尤为相关。 | |||
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) 。 | |||
T9470 |
HPK1-IN-7
|
MAPK | MAPK |
HPK1-IN-7 是一种口服有活性的、有效的HPK1(造血祖细胞激酶1, MAP4K1) 抑制剂,其IC50值为2.6 nM,具有强大的家族及激酶组选择性。它对 IRAK4 (59 nM) 和 GLK (140 nM) 具有选择性。当它与抗 PD1联合使用时,对 MC38 同基因肿瘤模型表现出极大的疗效。 | |||
T4442 |
MK2-IN-1 hydrochloride
MK2 Inhibitor,MK 25 |
MAPK | MAPK |
MK2-IN-1 hydrochloride (MK 25) 是一种高效的选择性 MAPKAPK2(MK2)激酶抑制剂,其 IC50值为0.11uM。 | |||
T78838 |
Akt/NF-κB/MAPK-IN-1
|
p38 MAPK | MAPK |
Akt/NF-κB/MAPK-IN-1(compound 2m)为口服活性NO抑制剂,IC50值为7.70 μM,低毒性。该化合物通过抑制Akt/NF-κB与MAPK信号通路实现抗炎效应。 | |||
T62359 |
TLR4/NF-κB/MAPK-IN-1
|
||
TLR4/NF-κB/MAPK-IN-1通过抑制 TLR4/NF-kB/MAPK 途径,是一种新型抗神经炎症剂。 | |||
T26280 |
TL4-12
TL4 12 |
||
TL4-12 is a MAP4K2 (GCK) inhibitor that inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation in vitro. | |||
T5393 |
CK1-IN-1
PUN51207 |
p38 MAPK; Casein Kinase | MAPK; Metabolism; Stem Cells |
CK1-IN-1 (PUN51207) 是一种酪蛋白激酶 1 抑制剂,对 CK1δ、CK1ε和p38σ MAPK 的IC50值为 15 nM、16 nM 和73 nM。 | |||
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。 | |||
T8656 |
CAY10404
3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T |
Apoptosis; Akt; COX | Apoptosis; Cytoskeletal Signaling; Immunology/Inflammation; Neuroscience; PI3K/Akt/mTOR signaling |
CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) 是一种有效且高度选择性的 COX-2 和 COX-1 抑制剂。 它还是 PKB/Akt 和 MAPK 信号通路的有效抑制剂,可诱导 NSC-LC 细胞凋亡,具有镇痛、抗炎和抗癌活性。 | |||
T21493 |
Cyclosporin H
|
Others | Others |
Cyclosporin H 是一种 FPR-1(甲酰肽受体 1) 的选择性强效抑制剂。它缺乏 Cyclosporin A 具有的免疫抑制活性。它是一种病毒转导增强剂,可使人脐带血来源的造血干细胞和祖细胞中慢病毒转导增强 10 倍。它与雷帕霉素或前列腺素 E2 联合使用时表现出累加效应。 | |||
T28222 |
5-Hydroxy-1-methylhydantoin
HD-003,HD003,5-羟基-1-甲基咪唑啉-2,4-二酮,NZ419,NZ-419,HD 003,NZ 419 |
Bradykinin Receptor | GPCR/G Protein |
5-Hydroxy-1-methylhydantoin (HD-003) 是一种可能用于治疗肾衰竭的抗氧化剂。它是肌酐代谢物,是一种羟基自由基清除剂,此前已显示通过抑制大鼠慢性肾病的进展来提供肾脏保护。 它是一种新型抗氧化药物,可完全抑制 B2-激肽受体(B2KR) 对 VSMC 中高葡萄糖 (25 mM) 刺激的反应,并且还显示可减弱 BK 对 VSMC 重塑的影响。它抑制 BK 诱导的 MAPK 磷酸化增加并减弱 VSMC 中结缔组织生长因子 (CTGF) 蛋白水平的增加。这些研究结果表明,它可能通过其抗氧化特性赋予血管保护免受高葡萄糖浓度和 BK 刺激以改善血管损伤和重塑。 | |||
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。 | |||
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]. | |||
T35877 |
MurA-IN-1
|
||
MurA-IN-1 (compound 1a) is a PTPRR inhibitor, with IC50 values of 0.23 μM, 0.8 μM, 0.75 μM and 0.09 μM for PTP1B, PTPN5, PTPN7 and PTPRR, respectively[1]. (A family of human MAPK-specific protein tyrosine phosphatases) [1]. Jeyanthy Eswaran, et al. Crystal structures and inhibitor identification for PTPN5, PTPRR and PTPN7: a family of human MAPK-specific protein tyrosine phosphatases. Biochem J. 2006 May 1;395(3):483-91. | |||
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。 | |||
T81783 |
MK2-IN-5
Hsp25 kinase inhibitor,Mk2 pseudosubstrate |
ERK | MAPK |
MK2-IN-5为Mk2的假底物,Ki值为8 μM。该化合物针对MAPK通路内的蛋白相互作用域,并能抑制HSP25与HSP27的磷酸化。 | |||
T63169 | MIF2-IN-1 | ||
MIF2-IN-1 (compound 5d) 是一种有效的 MIF2 互变异构酶抑制剂 (IC50: 1.0 μM)。MIF2-IN-1 通过 MAPK 通路,阻滞细胞周期,进而抑制非小细胞肺癌细胞的增殖。MIF2-IN-1 具有潜力进行癌症疾病的研究。 | |||
T74374 |
ERK1/2 inhibitor 4
|
||
ERK1/2 inhibitor 5 是一种有效的ERK1/2抑制剂。丝裂原活化蛋白激酶 (MAPK) 在信号转导通路中起着极其重要的作用,而细胞外信号调节激酶 (ERK) 是MAPK 家族的成员。ERK1/2 inhibitor 5 具有研究或预防癌症、炎症或其他增殖性疾病的潜力。 | |||
T74373 |
ERK1/2 inhibitor 3
|
||
ERK1/2 inhibitor 3 是一种有效的 ERK1/2抑制剂。丝裂原活化蛋白激酶 (MAPK) 在信号转导通路中起着极其重要的作用,而细胞外信号调节激酶 (ERK) 是 MAPK 家族的成员。ERK1/2 inhibitor 3 具有研究或预防癌症、炎症或其他增殖性疾病的潜力。 | |||
T69748 |
AG-12286
|
||
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). | |||
T36676 |
Rineterkib hydrochloride
|
||
Rineterkib hydrochloride (compound B) is an orally active RAF and ERK1/2 inhibitor in the treatment of a proliferative disease characterized by activating mutations in the MAPK pathway. The activity is particularly related to the treatment of KRAS-mutant NSCLC, BRAF-mutant NSCLC, KRAS-mutant pancreatic cancer, KRAS-mutant colorectal cancer (CRC) and KRAS-mutant ovarian cancer[1]. ERK-IN-1 (compound B) (50, 75 mg/kg, p.o., qd/q2d, 27 days) treatment significantly reduces the tumor volume in the C... | |||
T81598 |
Org OD 02-0
10-Ethenyl-19-norprogesterone |
p38 MAPK | MAPK |
Org OD 02-0(10-Ethenyl-19-norprogesterone)为mPRα(膜孕酮受体α)特异性激动剂,IC50值为33.9 nM。该化合物能够激活MAPK活性,并且能抑制催乳素(PRL)的分泌。 | |||
T5487 |
MW-150 dihydrochloride dihydrate
|
||
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) 是一种选择性的,可透过神经系统,具有口服活性的的p38α MAPK 抑制剂,Ki 值为 101 nM。MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) 抑制内源性 p38α MAPK 磷酸化活化的神经胶质中内源性底物 MK2 的能力。 | |||
T83740 |
Ziptide TFA
|
||
Ziptide是多种丝氨酸/苏氨酸蛋白激酶的肽底物,包括MAPK激活蛋白激酶2(MAPKAPK2)、MAPKAPK3、MAPKAPK5、checkpoint kinase 1(Chk1)、AMP激活蛋白激酶(AMPK)和钙/钙调蛋白依赖型蛋白激酶II(CamKII)。它被用来评估CamKII活性以用于抑制剂的开发。 | |||
T79572 |
MAPK-IN-2
|
EGFR | Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors |
MAPK-IN-2 (化合物3h)是一种携带抗肿瘤活性的高效MAPK抑制剂。它在多个癌细胞系中有效抑制了细胞增殖,并对MAPK途径表现出强大的抑制效果(EGFRWT IC50=281 nM, c-MET IC50=205 nM, B-RAFWT IC50=112 nM, CDK4/6 IC50=95和184 nM),对突变型EGFR和B-RAF亦展现出高效力(EGFRT790M IC50=69 nM, B-RAFV600E IC50=83 nM)。 | |||
T75800 |
Ac2-26 TFA
|
||
Ac2-26 TFA,是膜联蛋白 A1 (AnxA1) 的活性 N-末端肽,可减轻缺血再灌注诱导的急性肺损伤。Ac2-26 还降低 AnxA1 蛋白表达,抑制受损肺组织中NF-κB 和 MAPK 通路活化。 | |||
T78829 |
JNK2-IN-1
|
JNK | MAPK |
JNK2-IN-1(Compound J27)是一款具有抗炎活性的JNK2抑制剂,其解离常数为79.2 μM。该化合物能通过阻断NF-κB/MAPK信号通路来降低肿瘤坏死因子α(TNF-α)和白细胞介素6(IL-6)的释放,从而减轻脂多糖(LPS)引起的急性肺损伤(ALI)及脓毒症症状。 | |||
T37303 |
5-OxoETE
5-KETE,5-OxoETE |
||
5-OxoETE is a polyunsaturated keto acid formed by the oxidation of 5-HETE in human neutrophils by a specific dehydrogenase.[1] It stimulates cytosolic calcium levels in neutrophils with an EC50 value of 2 nM.[2] 5-OxoETE selectively stimulates the migration and degranulation of eosinophils and activates the MAPK pathway in stimulated neutrophils via a specific G protein-coupled receptor.[3],[4],[5],[6] | |||
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. | |||
T61755 |
E6201
|
||
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]. | |||
T79464 |
RORγ antagonist 1
|
ROR | Metabolism |
RORγ antagonist1 (化合物22) 作为RORγ的有效拮抗剂 (KD=0.18 μM),在HPAF-II胰腺癌异种移植模型中显示出了抗增殖性能。该化合物通过抑制RAS/MAPK和AKT/mTORC1通路,并引发caspase依赖的细胞凋亡(apoptosis)机制,从而在胰腺癌细胞中发挥作用。 | |||
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)-... | |||
T41240 |
Verrucarin A
|
||
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。 | |||
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... | |||
T79304 |
Semapimod
CPSI-2364,CNI-1493 free base |
||
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。 | |||
TP2116 |
SAH-SOS1A
|
||
KRas/son of sevenless 1 (SOS1) interaction inhibitor. Binds within nucleotide binding pocket of KRas (Kd values are 106 - 176 nM for wild type KRas and various KRas mutants). Inhibits nucleotide binding to KRas in a concentration dependent manner. Display | |||
T38048 |
Globotetraosylceramides (porcine RBC)
|
||
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)
|
||
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
|
||
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... | |||
T23337 |
SCH772984 HCl
|
ERK; Others | MAPK; Others |
SCH772984 HCl 是一种特异性的 ERK1/2 抑制剂,具有 I 型和 II 型激酶抑制剂的特性,其 IC50 分别为 4 和 1 nM。 SCH772984 HCl 在 BRAF、NRAS 或 KRAS 突变的肿瘤细胞中具有纳摩尔级细胞效力,并诱导肿瘤消退。 SCH772984 HCl 可用于 MAPK 抑制剂难治性肿瘤的研究。 | |||
T35463 |
(±)14(15)-EET
(±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET |
||
(±)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 |
---|---|---|---|
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。 | |||
T5S0089 |
Kaempferol-3-O-glucorhamnoside
Kaempferol 3-glucorhamnoside,百蕊草素I |
Antioxidant; p38 MAPK; NF-κB | MAPK; NF-κB; oxidation-reduction |
Kaempferol-3-O-glucorhamnoside (Kaempferol 3-glucorhamnoside) 是来源于百蕊草的一种类黄酮,在体内外均能通过 MAPK 和 NF-κB 通路抑制炎症反应。 | |||
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。 | |||
T3410 |
Momordin Ic
地肤子皂苷Ic,地肤子皂苷 Ic,Momordin 1c |
Apoptosis; MAPK; PI3K | Apoptosis; MAPK; PI3K/Akt/mTOR signaling |
Momordin Ic (Momordin 1c) 是山茱萸的主要皂苷成分,通过氧化应激调控线粒体功能障碍诱导细胞凋亡,具有抗癌活性。 | |||
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。 | |||
TN1880 |
Lucidenic acid B
Lucidenicacid B |
Apoptosis; Caspase | Apoptosis; Proteases/Proteasome |
Lucidenic acid B (Lucidenicacid B) 是从灵芝中提取得到的天然化合物,可诱导caspase-9 和 caspase-3 的活化和 PARP 的裂解,可通过线粒体介导诱导人白血病细胞凋亡 。 Lucidenic acid B通过灭活MAPK / ERK信号转导途径和降低NF-kappaB和AP-1的结合活性来抑制PMA诱导的人肝癌细胞侵袭。。Lucidenic acid B 对细胞周期和坏死细胞没有影响。 | |||
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。 | |||
T6S1699 |
Shogaol
[6]-Shogaol,姜烯酚,6-姜烯酚,6-Shogaol |
Lipoxygenase; Autophagy | Autophagy; Metabolism |
6-Shogaol (6-Shogaol) 是从生姜中分离的一种天然产物,具有抗癌、抗炎和抗氧化的多种生物活性。 | |||
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。 | |||
T3S1416 |
Decursin
Decursinol angelate,前胡素,(+)-Decursin,紫花前胡素 |
Apoptosis; PKC | Apoptosis; Chromatin/Epigenetic; Cytoskeletal Signaling |
Decursin (Decursinol angelate) 是一种细胞毒性剂,是一种来自朝鲜当归根的有效蛋白激酶 C 激活剂。它通过 Hippo/YAP 信号通路抑制 HepG2 细胞的生长。它通过下调 CXCR7 表达来抑制胃癌中的肿瘤生长,迁移和侵袭。 | |||
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。 | |||
T1719 |
Bufalin
|
ATPase | Membrane transporter/Ion channel |
Bufalin 是蟾酥中的一种成分,是Na+/K+-ATPase 抑制剂,具有抗肿瘤活性,可与其基 α1、α2 和 α3 结合,Kd 值分别为 42.5、45 和 40 nM。 | |||
T6S0735 |
Flavokawain B
黄卡瓦胡椒素B,Flavokavain B,Flavokawin B,2'-Hydroxy-4',6'-Dimethoxychalcone |
Apoptosis; Others | Apoptosis; Others |
Flavokawain B (Flavokavain B) 是从卡瓦醉椒的根提取物中,分离出的查尔酮。它是一种凋亡诱导剂,可抑制各种癌细胞株生长。它以极低的无毒浓度抑制人脑内皮细胞的迁移和血管形成,具有抗血管生成活性。 | |||
T6S1917 |
Schisandrol B
Gomisin A,TJN-101,Besigomsin,五味子醇乙,Gamma-Schisandrin,戈米辛A,Schizandrol B,Wuweizi alcohol-B |
P450; Reactive Oxygen Species; Autophagy | Autophagy; Immunology/Inflammation; Metabolism; NF-κB |
Schisandrol B (Besigomsin) 是华中五味子的主要活性成分,具有保肝、抗炎、抗糖尿病和抗氧化的作用。它抑制活性氧的产生,也抑制 P-糖蛋白和CYP3A 的活性。 | |||
T6S1684 |
8-Gingerol
|
Antioxidant; Antibacterial; TRP/TRPV Channel | Membrane transporter/Ion channel; Microbiology/Virology; oxidation-reduction |
8-Gingerol 分离自姜的根状茎,是口服有效的 TRPV1激活剂,EC50值为5.0 µM。8-Gingerol 抑制 COX-2,还能抑制体外 H. pylori 的生长。 | |||
T5S0761 |
Nitidine chloride
|
Apoptosis; ERK; FAK; p38 MAPK; NF-κB; Topoisomerase; STAT; Parasite | Angiogenesis; Apoptosis; Cytoskeletal Signaling; DNA Damage/DNA Repair; JAK/STAT signaling; MAPK; Microbiology/Virology; NF-κB; Stem Cells; Tyrosine Kinase/Adaptors |
Nitidine chloride 是从Zanthoxylum nitidum (Roxb) DC 中分离得到的,具有抗疟疾活性。它通过多个靶点通路,起抗癌作用,抑制STAT3、DNA 拓扑异构酶1和2A、ERK 和c-Src/FAK 相关信号通路。它通过MAPK 和NF-kB 途径抑制Lps 诱导的炎性细胞因子的产生。 | |||
T5S0754 |
Isoquercetin
3-Glucosylquercetin,Hirsutrin,Isoquercitrin,异槲皮苷,Quercetin 3-o-glucopyranoside,槲皮素-3-葡萄糖苷 |
NF-κB; Wnt/beta-catenin; NO Synthase | Cytoskeletal Signaling; Immunology/Inflammation; NF-κB; Stem Cells |
Isoquercetin (3-Glucosylquercetin) 是天然存在的多酚,具有抗氧化,抗增殖和抗炎特性。它通过调节核因子-κB 转录调节系统调节一氧化氮合酶 2 的表达。它通过 Nrf2/ARE 抗氧化剂信号传导途径减轻乙醇诱导的肝毒性,氧化应激和炎症反应。它具有高生物利用度和低毒性,是预防糖尿病妊娠出生缺陷的有希望的候选药物。 | |||
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。 | |||
T6S1256 |
Ruscogenin
|
NOS; NF-κB; NOD-like Receptor (NLR) | Immunology/Inflammation; NF-κB |
Ruscogenin 是一种重要甾体皂苷元,提取自麦冬。它能够抑制 TXNIP/NLRP3炎症体激活和 MAPK 途径,改善脑缺血诱导的血脑屏障功能障碍,具有显著抗血栓、抗炎作用。 | |||
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 | |||
T4S0083 |
Protostemonine
|
Others | Others |
Protostemonine 是一种主要从 Stemona sesslifolia 根中分离得到的生物碱,对哮喘及革兰氏阴性菌所致急性肺损伤有抗炎作用。 |