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Submit ReviewL-685,458
说明： Potent and selective γ-secretase inhibitor
别名： L 458,γ-Secretase Inhibitor X
化学名： (5S)-(tert-Butoxycarbonylamino)-6-phenyl-(4R)-hydroxy-(2R)-benzylhexanoyl)-L-leucy-L-phenylalaninamide
纯度： ≥97% (HPLC)
生物活性 for L-685,458
L-685,458 is a potent and selective γ-secretase inhibitor (IC50 = 17 nM) that displays > 50-fold selectivity over a range of aspartyl, serine and cysteine proteases. L-685,458 binds with high affinity to the related aspartyl protease, signal peptide peptidase (SPP; KD = 5.1 nM), and inhibits SPP expressed in HEK293 cells (IC50 = 10 μM). L-685,458 exhibits equal potency for inhibition of Aβ40 and Aβ42 peptides (IC50 values are 48 and 67 nM respectively in human neuroblastoma cells). It also regulates CXCR4 and VEGFR2 expression through inhibition of Notch signaling in vitro.
技术数据 for L-685,458
| 分子量 | 672.85 |
| 公式 | C39H52N4O6 |
| 储存 | Store at -20°C |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 292632-98-5 |
| PubChem ID | 5479543 |
| InChI Key | MURCDOXDAHPNRQ-ZJKZPDEISA-N |
| Smiles | O[C@H](C[C@@H](CC1=CC=CC=C1)C(N[C@@H](CC(C)C)C(N[C@@H](CC3=CC=CC=C3)C(N)=O)=O)=O)[C@H](CC2=CC=CC=C2)NC(OC(C)(C)C)=O |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for L-685,458
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 10.09 | 15 |
制备储备液 for L-685,458
以下数据基于产品分子量 672.85。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| 浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.15 mM | 9.91 mL | 49.54 mL | 99.08 mL |
| 0.75 mM | 1.98 mL | 9.91 mL | 19.82 mL |
| 1.5 mM | 0.99 mL | 4.95 mL | 9.91 mL |
| 7.5 mM | 0.2 mL | 0.99 mL | 1.98 mL |
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产品说明书 for L-685,458
参考文献 for L-685,458
参考文献是支持产品生物活性的出版物。
Shearman et al (2000) L-685,458, an aspartyl protease transition state mimic, is a potent inhibitor of amyloid-β-protein precursor γ-secretase activity. Biochemistry 39 8698 PMID: 10913280
Williams et al (2006) Up-regulation of the Notch ligand delta-like 4 inhibits VEGF-induced endothelial cell function. Blood 107 931 PMID: 16219802
Williams et al (2008) Regulation of CXCR4 by the Notch ligand delta-like 4 in endothelial cells. Cancer Res. 68 1889 PMID: 18339870
Iben et al (2007) Signal peptide peptidase and gamma-secretase share equivalent inhibitor binding pharmacology. J.Biol.Chem. 282 36829 PMID: 17932033
If you know of a relevant reference for L-685,458, please let us know.
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关键词: L-685,458, L-685,458 supplier, L458, Potent, selective, γ-secretase, gamma-secretase, inhibitors, inhibits, Aβ4, beta40, β42, beta42, Proteinases, Proteases, b-amyloid, β-Amyloid, beta-Amyloid, Precursor, Protein, APP, beta, L685458, amyloidbeta, amyloidb, amyloidβ, inhibitor, X, SPP, SP, L, 458, gamma-Secretase, Inhibitor, Gamma-Secretase, Amyloid, Beta, Peptides, Other, 2627, Tocris Bioscience
8 篇 L-685,458 的引用文献
引用文献是使用了 Tocris 产品的出版物。 L-685,458 的部分引用包括：
Kaylan et al (2018) Spatial patterning of liver progenitor cell differentiation mediated by cellular contractility and Notch signaling. Elife 7 PMID: 30589410
Chai et al (2017) HIV-1 counteracts an innate restriction by amyloid precursor protein resulting in neurodegeneration. Nat Commun 8 1522 PMID: 29142315
Ran et al (2015) Differential Inhibition of Signal Peptide Peptidase Family Members by Established γ-Secretase Inhibitors. PLoS One 10 e0128619 PMID: 26046535
Mentrup et al (2022) Phagosomal signalling of the C-type lectin receptor Dectin-1 is terminated by intramembrane proteolysis. Nat.Commun. 13 1880 PMID: 35388002
Ran et al (2014) γ-Secretase processing and effects of γ-secretase inhibitors and modulators on long Aβ peptides in cells. J Biol Chem 289 3276 PMID: 24352661
Origlia et al (2014) RAGE inhibition in microglia prevents ischemia-dependent synaptic dysfunction in an amyloid-enriched environment. J Neurosci 34 8749 PMID: 24966375
Greife et al (2014) Canonical Notch signalling is inactive in urothelial carcinoma. BMC Cancer 14 628 PMID: 25167871
Liu et al (2018) APP upregulation contributes to retinal ganglion cell degeneration via JNK3. Cell Death Differ 25 661 PMID: 29238071
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