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抑制剂 & 化合物

3

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Cat. No. Product Name Target Signaling Pathways
T70638 p38-α MAPK-IN-5

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。
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。
T27627 Iroxanadine

BRX005,BRX-235,BRX-005,BRX235,BRX 005,BRX 235

p38 MAPK MAPK
Iroxanadine (BRX-005) 是一种新型小分子MAPK p38 抑制剂,诱导p38 SAPK 的磷酸化,在用去氧肾上腺素预先收缩的豚鼠肺动脉制剂中诱导浓度依赖性松弛,可用于治疗动脉粥样硬化、糖尿病血管病,微血管心绞痛和外周动脉疾病等血管疾病。
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)-...
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...
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-5
Cat.No: T70638
Synonym:
Target:
SR-318
Cat.No: T12997
Synonym:
Target: p38 MAPK, TNF
Iroxanadine
Cat.No: T27627
Synonym: BRX005,BRX-235,BRX-005,BRX235,BRX 005,BRX 235
Target: p38 MAPK
ML 3403
Cat.No: T37590
Synonym:
Target:
Tpl2 Kinase Inhibitor (hydrochloride)
Cat.No: T35536
Synonym:
Target:
(±)14(15)-EET
Cat.No: T35463
Synonym: (±)14,15-EET,(±)14,15-EpETrE,(±)14(15)-EET
Target:
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。
T3676 Sesamol

1,3-Benzodioxol-5-ol,3,4-Methylenedioxyphenol,芝麻酚

Apoptosis; AMPK Apoptosis; Chromatin/Epigenetic; PI3K/Akt/mTOR signaling
Sesamol (1,3-Benzodioxol-5-ol) 是芝麻油的主要成分,具有抗氧化和抗肿瘤活性。它是一种自由基清除剂,在 DPPH 实验中,IC50为 5.95±0.56 μg/mL。
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。

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
Sesamol
Cat.No: T3676
Synonym: 1,3-Benzodioxol-5-ol,3,4-Methylenedioxyphenol,芝麻酚
Target: Apoptosis, AMPK
Sauchinone
Cat.No: T6S1572
Synonym:
Target: ERK, p38 MAPK, NF-κB
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