L-685,458

Pricing Availability   Qty
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)
说明书
引用文献 (8)
评论
文献 (2)

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.

选择批次从而根据批次分子量重新计算:
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

分析证书/产品说明书
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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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查看全部 γ-Secretase Inhibitors

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:

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


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