2. Neuronal Signaling Stem Cell/Wnt Apoptosis
  3. γ-secretase Apoptosis
  4. L-685458

L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers.

For research use only. We do not sell to patients.

L-685458 Chemical Structure

L-685458 Chemical Structure

CAS No. : 292632-98-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 666 In-stock
Solution
10 mM * 1 mL in DMSO USD 666 In-stock
Solid
1 mg USD 150 In-stock
5 mg USD 450 In-stock
10 mg USD 700 In-stock
25 mg USD 1300 In-stock
50 mg USD 1900 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

L-685458 Related Antibodies

Top Publications Citing Use of Products

    L-685458 purchased from MedChemExpress. Usage Cited in: Evid Based Complement Alternat Med. 2018 Nov 21;2018:3082507.  [Abstract]

    Protein extracts are immunoblotted to determine the relative expression levels of VEGFR2, Notch1, Jagged1, and Hes1 in the treatment of Ox-LDL, TMP, PF, L-6854598.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    L-685458 is a potent transition state analog (TSA) γ-secretase inhibitor (GSI). L-685458 inhibits amyloid β-protein precursor γ-secretase activity with IC50 of 17 nM, shows greater than 50-100-fold selectivity over other aspartyl proteases tested. L685458 inhibits γ-secretase-mediated cleavage of APP-C99 and Notch-100 with IC50s of 301.3 nM and 351.3 nM, respectively. L-685458 can be used for the research of alzheimer’s disease (AD) and cancers[1][2].

    In Vitro

    L-685458 reduces both Aβ(40) and Aβ(42) peptide formation in 3 different cells. It against Neuro2A h AβPP695, CHO h AβPP695, and SHSY5 spβA4CTF reduction of Aβ(40) with IC50 values of 402 nM, 113 nM and 48 nM, respectively. And the IC50 values are 775 nM, 248 nM, 67 nM, respectively[1].
    L-685458 (5-40 μM; 24 hours) leads to a dramatic downregulation of Hes-1 in 786-O cells[3].
    L-685458 has inhibitory effects in hepatoma cell lines, it against Huh7, HepG2, HLE and SKHep1 cells with IC50 of 12.91 μM, 12.69 μM, 21.76 μM and 12.18 μM, respectively[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    L-685458 Related Antibodies
    In Vivo

    L-685458 (percutaneous administration; 5 mg/kg; 2 weeks) has antitumor effects in mouse hepatoma models. L-685458 inhibits EpCAM production except in necrotic areas. And HES1 staining is also diminished in the nucleus[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: NOD-SCID Mouse Hepatoma Model[4]
    Dosage: 5 mg/kg
    Administration: Percutaneous administration; 5 mg/kg; 2 weeks
    Result: Exhibited anti-tumor activities in vivo.
    Molecular Weight

    672.85

    Formula

    C39H52N4O6
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N)[C@H](CC1=CC=CC=C1)NC([C@H](CC(C)C)NC([C@H](CC2=CC=CC=C2)C[C@@H](O)[C@@H](NC(OC(C)(C)C)=O)CC3=CC=CC=C3)=O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 83.3 mg/mL (123.80 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4862 mL 7.4311 mL 14.8622 mL
    5 mM 0.2972 mL 1.4862 mL 2.9724 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    In Vivo Dissolution Calculator
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    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.37%

    COA (251 KB) LCMS (267 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.4862 mL 7.4311 mL 14.8622 mL 37.1554 mL
    5 mM 0.2972 mL 1.4862 mL 2.9724 mL 7.4311 mL
    10 mM 0.1486 mL 0.7431 mL 1.4862 mL 3.7155 mL
    15 mM 0.0991 mL 0.4954 mL 0.9908 mL 2.4770 mL
    20 mM 0.0743 mL 0.3716 mL 0.7431 mL 1.8578 mL
    25 mM 0.0594 mL 0.2972 mL 0.5945 mL 1.4862 mL
    30 mM 0.0495 mL 0.2477 mL 0.4954 mL 1.2385 mL
    40 mM 0.0372 mL 0.1858 mL 0.3716 mL 0.9289 mL
    50 mM 0.0297 mL 0.1486 mL 0.2972 mL 0.7431 mL
    60 mM 0.0248 mL 0.1239 mL 0.2477 mL 0.6193 mL
    80 mM 0.0186 mL 0.0929 mL 0.1858 mL 0.4644 mL
    100 mM 0.0149 mL 0.0743 mL 0.1486 mL 0.3716 mL
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    L-685458 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    L-685458292632-98-5L-685,458L685458L 685458γ-secretaseApoptosisGamma secretasealzheimer’s diseaseADcancerHES1Inhibitorinhibitorinhibit

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