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Search Results for " p38-a mapk-in-1 "

15

抑制剂 & 化合物

7

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
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).
T26280	TL4-12 TL4 12
	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。
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).
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)-...
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].
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。
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...
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...

化合物

p38-α MAPK-IN-1

Cat.No: T12347

Target: p38 MAPK, Autophagy

NF-κB/MAPK-IN-1

Cat.No: T63119

Target: NF-κB, MAPK

Cat.No: T6934

Synonym: ARRY-614

Target: Tie-2, p38 MAPK, Autophagy

p38 MAPK-IN-1

Cat.No: T16424

Target: p38 MAPK

Cat.No: T26280

Synonym: TL4 12

p38 MAPK-IN-3

Cat.No: T61803

p38-α MAPK-IN-4

Cat.No: T61091

Cat.No: T69748

Cat.No: T37590

Cat.No: T61755

Cat.No: T41240

Globotetraosylceramides (porcine RBC)

Cat.No: T38048

Tpl2 Kinase Inhibitor (hydrochloride)

Cat.No: T35536

Cat.No: T68321

Cat.No: T35463

Synonym: (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET

Cat. No.	Product Name	Target	Signaling Pathways
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。
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。
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-ÎºB and p38 MAPK pathways, it may block the phosphorylation of mitogen-activated protein kinase (MAPK) molecule p38, apoptosis signal-regu

天然产物

Dehydrocorydaline

Cat.No: T5S2358

Synonym: Dehydrocorydalin,脱氢紫堇碱,13-Methylpalmatine

Target: BCL, PARP, p38 MAPK, Caspase, Parasite, Autophagy

Cat.No: T2768

Synonym: 柴胡皂苷A,柴胡皂苷 A

Target: NF-κB, Antibacterial, Liver X Receptor

Cat.No: TN5888

Target: Others

Cat.No: T3S0737

Synonym: 2'-羟基-4,4',6'-三甲氧基查耳酮,Flavokavain A

Target: Apoptosis, p38 MAPK

Caffeic Acid Phenethyl Ester

Cat.No: T6429

Synonym: Phenylethyl Caffeate,咖啡酸苯乙酯,CAPE

Target: Apoptosis, NF-κB

Cat.No: T6S1572

Target: ERK, p38 MAPK, NF-κB

Cat.No: TN4635

Target: NADPH-oxidase, Beta Amyloid, ASK, IκB/IKK, p38 MAPK, TNF, NOS, NF-κB, COX, Prostaglandin Receptor

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