目录号 | 产品详情 | 靶点 | |
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T73456 | |||
DRP1i27是一种有效抑制人源Drp1(动力蛋白相关蛋白1)的化合物。它通过与Drp1的GTPase位点结合,并与Gln34及Asp218形成氢键来发挥作用。DRP1i27主要针对Drp1介导的线粒体裂变细胞系模型,能有效防止模拟缺血再灌注引起的损伤。 | |||
T37671 | |||
N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM). It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors. CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion. | |||
T78371 | |||
Ac2-26 ammonium是一种具抗炎作用的annexin 1 N末端肽。该化合物能够通过伴侣介导的自噬(CMA)机制降低溶酶体中的IKKβ蛋白含量,从而改善肺缺血再灌注损伤,并在哮喘大鼠模型中抑制气道炎症以及高反应性的表现。 | |||
T78562 | |||
FX-06 (Fibrin-derived peptide Bβ15-42)为纤维蛋白Bbeta链衍生的肽类化合物。通过与VE-cadherin结合并阻断白细胞的迁移,FX-06激活了以VE-cadherin为中心的信号通路。该化合物主要应用于缺血/再灌注损伤和登革热休克综合征(DSS)的相关研究。 | |||
T81037 | |||
Tat-HA-NR2B9 是一种包括HIV-1 Tat细胞膜转导结构域片段、流感病毒血凝素(HA)表位标签以及NR2B(NR2B9c) C端9个氨基酸的化学复合物。该化合物能够降低大鼠缺血性脑损伤的梗塞面积,同时促进神经功能的恢复。 | |||
T81485 | |||
Phoenixin-14 (PNX-14) TFA 是具抗焦虑、心脏保护及神经保护效果的穿透大脑屏障神经肽。它通过上调GnRH受体mRNA调控垂体促性腺激素分泌,并促进胰岛素释放。此外,Phoenixin-14 TFA保护小鼠免受缺血/再灌注(IR)伤害,通过降低ROS、提高GSH减缓氧化应激。 | |||
T76024 | |||
IKKγ NBD 抑制肽 TFA 是一种高度特异性的NF-κB 抑制剂。IKKγ NBD 抑制肽 TFA 通过阻断 IKKγ/NEMO 结合域 (NBD) 与 IKKα 和 IKKβ 之间的相互作用,而阻断 TNF-α 诱导的NF-κB 激活。IKKγ NBD 抑制肽 TFA 可显著降低炎症、改善脑缺血所致的神经功能缺损。 | |||
T79372 | Adenosine Receptor | ||
A3AR拮抗剂1(化合物12)是一种选择性的A3AR激动剂,其Ki值为25.8 nM。该化合物能有效促进β-arrestin2的募集,表现出EC50为5.17 nM的高亲和力。A3AR拮抗剂1主要用于炎症性疾病、缺血、癌症、神经性疼痛和肝脏疾病等方面的科研。 | |||
T70763 | |||
KR-67607, also known as NTX-101 is novel selective 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor. KR-67607 decreased 4-hydroxynonenal expression and increased antioxidant and mucus secretion in BAC-treated rat eyes. KR-67607 showed its protective effects against ischemia-reperfusion-induced eye injury. KR-67607 effectively reduced cortisol levels in mouse eyes and maintained the trabecular meshwork (TM) structure in the presence of transient ischemic stress. Furthermore, KR-67607 reversed the elevation of intra-ocular pressure (IOP), suggesting that the TM structure maintained by KR-67607 prevented the excessive rise in IOP that exacerbates glaucoma. | |||
T70063 | |||
GYKI 52466 is an allosteric AMPA receptor antagonist. It selectively inhibits AMPA-induced inward currents (IC50 = 7.5 µM) over NMDA- or GABA-induced inward currents in primary rat hippocampal neurons at 50 µM but also inhibits kainate-induced inward currents in the same cells (IC50 = 11 µM).2 GYKI 52466 (10 µM) reduces the amplitude of spontaneous excitatory postsynaptic currents (EPSCs) in the same cells. It increases the latency to seizure onset and reduces mortality in a rat model of generalized tonic-clonic seizures induced by 4-aminopyridine (4-AP) when administered at doses of 25 and 50 mg/kg. GYKI 52466 (30 mg/kg) prevents neuronal damage in the CA1 region of the hippocampus in a rat model of global ischemia-reperfusion injury induced by four-vessel occlusion. |
目录号 | 产品名/同用名 | 种属 | 表达系统 | ||
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TMPY-04424 | MST3 Protein, Human, Recombinant (His) | Human | Baculovirus Insect Cells | ||
Aberrant STK24 expression was an independent prognostic indicator in lung adenocarcinoma patients. Its dysregulation was associated with its DNA copy number alteration and methylation. STK24/CCM3-regulated exocytosis plays an important role in the protection of kidneys from ischemia-reperfusion injury.
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TMPK-00481 | PDGF R beta/CD140b Protein, Cynomolgus, Recombinant (His) | Cynomolgus | HEK293 Cells | ||
Platelet-derived growth factor receptor (PDGFR) signaling is involved in proliferation and survival in a wide array of cell types.PDGFR-β signalling, via TGF-β signalling, may be crucial for restoration of BBB integrity after cerebral ischemia and therefore represents a novel potential therapeutic target.
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TMPJ-01051 | Pleiotrophin/PTN Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
Pleiotrophin (PTN) is a secreted, strongly heparinbinding, developmentally regulated cytokine. PTN is a highly conserved protein,Human, mouse, rat, canine, porcine, equine and bovine PTN share 98% aa sequence identity or greater. PTN and midkine share 50% amino acid (aa) sequence identity, share some functions, and constitute a family. During development, PTN is involved in development of brain, bone, and organs undergoing branching morphogenesis. PTN causes PTPRB dimerization and inactivates its phosphatase activity, which allows increased tyrosine phosphorylation of its substrates. Increased expression of PTN is correlated with neuronal development or stresses such as brain ischemia and Parkinson’s disease.
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TMPK-01168 | LOX-1 Protein, Mouse, Recombinant (His) | Mouse | HEK293 Cells | ||
LOX-1 is a transmembrane glycoprotein that binds to and internalizes ox-LDL.LOX-1 gene deletion in mice and anti-LOX-1 therapy has been shown to decrease inflammation, oxidative stress and atherosclerosis. LOX-1 deletion also results in damage from ischemia, making LOX-1 a promising target of therapy for atherosclerosis and related disorders. In this article we focus on the different mechanisms for regulation, signaling and the various effects of LOX-1 in contributing to atherosclerosis.
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TMPJ-01074 | PKCE Protein, Human, Recombinant (His) | Human | E. coli | ||
Protein Kinase C Epsilon type is a member of the serine- and threonine-specific protein kinase family that can be activated by calcium and the second messenger diacylglycerol. Protein Kinase C Epsilon contains these domains: one AGC-kinase C-terminal domain, one C2 domain, one protein kinase domain and two phorbol-ester/DAG-type zinc fingers. Protein Kinase C Epsilon phosphorylate a variety of protein targets and has been identified to participate in diverse cellular signaling pathways. It has many different cellular functions, such as neuron channel activation, apoptosis, cardioprotection from ischemia, heat shock response, as well as insulin exocytosis. Protein Kinase C Epsilon also serves as the receptor for phorbol esters, a class of tumor promoters.
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TMPJ-01022 | SUMO3 Protein, Human, Recombinant (HEK293, His) | Human | HEK293 Cells | ||
Small ubiquitin-like modifier (SUMO), also known as SUMO homologue and SMT3, is a member of the superfamily of ubiquitin-like polypeptides that become covalently attached to various intracellular target proteins as a way to alter their function, location, and/or half-life. Small ubiquitin-like modifiers include SUMO1, SUMO2, SUMO3, and SUMO4. Except for SUMO4, all other SUMOs are ubiquitously expressed, including in the brain. In human, SUMO2 and SUMO3 are two highly homologous proteins, collectively called SUMO2/3. Several studies suggest that SUMO3 are associated with pathogenesis in several neurological diseases, including Alzheimer's disease, Parkinson's disease, and cerebral ischemia/stroke.
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TMPJ-00082 | NGAL/Lipocalin-2 Protein, Mouse, Recombinant (hFc) | Mouse | HEK293 Cells | ||
Lipocalin-2, also known as Neutrophil Gelatinase-Associated Lipocalin (NGAL), is a secretory protein of the lipocalin superfamily. Lipocalin-2 contains a signal peptide that enables it to be secreted and form complexes with matrix metalloproteinase-9 (MMP-9) through disulfide bonds. Similar to other lipocalin family members, Lipocalin-2 is involved in diverse cellular processes, including the transport of small hydrophobic molecules, protection of MMP-9 from proteolytic degradation, and cell signaling. Furthermore, Lipocalin-2 can tightly bind to bacterial siderophore through a cell surface receptor, possibly serving as a potent bacteriostatic agent by sequestering iron, regulating innate immunity and protecting kidney epithelial cells from ischemia–reperfusion injury. This protein is mainly expressed in neutrophils and in lower levels in the kidney, prostate, and epithelia of the respiratory and alimentary tracts.Recent evidence also suggests its role as a biomarker for renal injury and inflammation.
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TMPY-02043 | PARK7/DJ-1 Protein, Human, Recombinant (His) | Human | E. coli | ||
Parkinson's disease locus DJ-1 (PARK7) is a differentially expressed transcript. DJ-1 plays a physiologic role in protection of erythroid cells from oxidant damage, a function unmasked in the context of oxidative stress. PARK7 belongs to the peptidase C56 family of proteins. It acts as a positive regulator of androgen receptor-dependent transcription. It may also function as a redox-sensitive chaperone, as a sensor for oxidative stress, and it apparently protects neurons against oxidative stress and cell death. Mutations in the DJ-1 gene are associated with rare forms of autosomal recessive early-onset Parkinson's disease (PD). DJ-1/p53 interactions contribute to apoptosis resistance in clonal myeloid cells and may serve as a prognostic marker in patients with myelodysplastic syndromes (MDS). DJ-1 regulates redox signaling kinase pathways and acts as a transcriptional regulator of antioxidative gene batteries. Therefore, DJ-1 is an important redox-reactive signaling intermediate controlling oxidative stress after ischemia, upon neuroinflammation, and during age-related neurodegenerative processes. Augmenting DJ-1 activity might provide novel approaches to treating chronic neurodegenerative illnesses such as Parkinson's disease and acute damage such as stroke.
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TMPY-01000 | BVES Protein, Human, Recombinant (GST) | Human | E. coli | ||
Blood vessel epicardial substance (BVES), or POPDC1, is a tight junction-associated transmembrane protein that modulates epithelial-to-mesenchymal transition (EMT) via junctional signaling pathways. BVES plays a protective role both in ulcerative and infectious colitis and identify BVES as a critical protector of colonic mucosal integrity. The Popeye domain containing1, also called Bves (Popdc1/Bves), is a transmembrane protein that functions in muscle regeneration, heart rate regulation, hypoxia tolerance, and ischemia preconditioning. The expression of Popdc1/Bves is elevated in cardiomyocytes maintained in serum free defined medium. Popdc1/Bves plays a role in the preservation of cardiomyocyte viability under serum deficiency through the alteration of Rac1 activity and the regulation of Bnip3 expression by FoxO3 and NFκB transcription factors pointing to Popdc1/Bves as a potential target to enhance heart protection. Blood vessel epicardial substance (BVES) is a tight junction-associated protein that regulates epithelial-mesenchymal states and is underexpressed in epithelial malignancy. Loss of BVES promotes inflammatory tumourigenesis through dysregulation of Wnt signalling and the oncogene c-Myc. BVES promoter methylation status may serve as a CAC biomarker. Blood vessel epicardial substance (BVES/Popdc1) is a junctional-associated transmembrane protein that is underexpressed in a number of malignancies and regulates epithelial-to-mesenchymal transition. BVES is a key regulator of intestinal stem cell programs and mucosal homeostasis.
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TMPY-04408 | CAMKII beta/CAMK2B Protein, Human, Recombinant (His & GST) | Human | Baculovirus Insect Cells | ||
Calcium/calmodulin-dependent protein kinase II beta (CAMK2B) is a member of the serine/threonine protein kinase family and to the Ca(2+)/calmodulin-dependent protein kinase subfamily. CaMKII is an important player in prostate cancer cells ability to escape apoptosis under androgen ablation and facilitate the progression of prostate cancer cells to an androgen independent state. As a multifunctional protein kinase, the loss of activity may play a critical role in initiating the changes leading to ischemia-induced cell death. CaMKII are found to be important for the functions of immune cells. CaMKII can be activated by TLR ligands, and in turn promotes both myeloid differentiating factor 88 and Toll/IL-1 receptor domain-containing adaptor protein-inducing IFN-beta-dependent inflammatory responses by directly activating TAK1 and IRF3. CAMKII has four subunit isoforms (alpha, beta, gamma, delta). It is possible that distinct isoforms of this chain have different cellular localizations and interact differently with calmodulin. The alpha- and beta-isoforms have narrow distributions restricted mainly to neuronal tissues, but the gamma- and delta-isoforms are ubiquitously expressed within neuronal and non-neuronal tissues. CAMK2B is important for controlling the direction of plasticity at the parallel fiber-Purkinje cell synapse. CaMK2 is involved in neuronal survival through the reorganization of the neuroarchitecture and that the regulation of this role is controlled at the level of gene expression. Because CaMK2B influences the expression of many neuroreceptors and influences neural outgrowth and pruning, its altered expression in the cerebral cortex in schizophrenia or depression may contribute to schizophrenia and depression.
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