2. Metabolic Enzyme/Protease
    Autophagy
  3. NAMPT
    Autophagy
  4. (E)-Daporinad

(E)-Daporinad  (Synonyms: FK866; APO866)

Cat. No.: HY-50876 Purity: 99.72%
COA Handling Instructions

(E)-Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC50 of 0.09 nM.

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

(E)-Daporinad Chemical Structure

(E)-Daporinad Chemical Structure

CAS No. : 658084-64-1

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 81 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 81 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 74 In-stock
Estimated Time of Arrival: December 31
10 mg USD 132 In-stock
Estimated Time of Arrival: December 31
50 mg USD 468 In-stock
Estimated Time of Arrival: December 31
100 mg USD 708 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 21 publication(s) in Google Scholar

Top Publications Citing Use of Products

    (E)-Daporinad purchased from MCE. Usage Cited in: J Cell Physiol. 2019 Apr;234(4):4385-4395.  [Abstract]

    SW620 and HCT116 cells are seeded into a six-well plate for 72 hr, followed by treatment with different concentrations (100 nM and 10 μM) of FK866 for 24 hr.

    (E)-Daporinad purchased from MCE. Usage Cited in: Mol Med Rep. 2017 Oct;16(4):5121-5128.  [Abstract]

    Effects of Emodin, FK866 and DEX on PMN apoptosis in SAP rats. Protein expression levels of Fas, FasL, Bax, cleaved caspase 3 and Bcl xL are detected by western blotting. β actin served as an internal control. Data are presented as the mean±standard deviation.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    (E)-Daporinad (FK866) is an effective inhibitor of nicotinamide phosphoribosyltransferase (NMPRTase; Nampt) with an IC50 of 0.09 nM.

    IC50 & Target

    IC50: 0.09 nM (NMPRTase)
    In Vitro

    Nampt inhibition with (E)-Daporinad (FK866) induces significant NAD+ intracellular reduction and selectively kills MM cells. (E)-Daporinad (FK866)-induced cell death is associated with inhibition of Nampt activity, rather than protein expression, and higher NAD+ baseline levels in MM cells than normal PBMCs confer (E)-Daporinad (FK866) sensitivity. (E)-Daporinad (FK866) abrogates the survival advantage conferred by the bone marrow microenvironment[1]. (E)-Daporinad (FK866) prevents the [Ca2+]i increase induced by different mitogens and reduces the Ca2+ content of TG-responsive Ca2+ stores in Jurkat and in activated PBLs. (E)-Daporinad (FK866) reduces the Ca2+ content of TG-responsive Ca2+ stores in Jurkat cells but not in Bcl2-Jurkat cells[2]. Inhibition of NAMPT by (E)-Daporinad (FK866), or inhibition of SIRT by nicotinamide decreases proliferation and triggered death of 293T cells involving the p53 acetylation pathway[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    (E)-Daporinad (FK866) (30 mg/kg, i.p.) decreases the tumor burden in CB17-SCID mice, and the tumor tissue demonstrates a significant decrease in ERK phosphorylation and proteolytic cleavage of LC3[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    391.51

    Appearance

    Solid

    Formula

    C24H29N3O2
    CAS No.
    SMILES

    O=C(C1=CC=CC=C1)N(CC2)CCC2CCCCNC(/C=C/C3=CC=CN=C3)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (127.71 mM)

    H2O : 1 mg/mL (2.55 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.5542 mL 12.7711 mL 25.5421 mL
    5 mM 0.5108 mL 2.5542 mL 5.1084 mL
    10 mM 0.2554 mL 1.2771 mL 2.5542 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  20% SBE-β-CD in saline

      Solubility: 4 mg/mL (10.22 mM); Clear solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (6.39 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.91%

    COA (242 KB) HNMR (223 KB) LCMS (402 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    MM1S cells (2×104 cells/well) are cultured for 72 and 96 hours in BMSC-coated 96-well plates in the presence or absence of drug. DNA synthesis is measured by (3H)-thymidine uptake, with (3H)-thymidine added (0.5 μCi/well) during the last 8 hours of cultures.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    CB17-SCID mice (28-35 days old) are irradiated (200 cGy), and then inoculated subcutaneously in the right flank with 3×106 MM1S cells in 100 μL RPMI 1640. After detection of tumor (2 weeks after the injection), 7 mice are treated intraperitoneally with either vehicle or (E)-Daporinad (FK866) (30 mg/kg body weight) twice a day for 4 days, repeated weekly over 3 weeks. Caliper measurements of the longest perpendicular tumor diameters are performed twice a week to estimate the tumor volume using the following formula: length×width2×0.5. Tumor growth inhibition (TGI) is calculated. Animals are killed when tumors reach 2 cm3 or the mice appear moribund. Survival is evaluated from the first day of treatment until death.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

    (E)-Daporinad658084-64-1FK866 APO866FK 866FK-866APO866APO 866APO-866NAMPTAutophagyNicotinamide phosphoribosyl transferasePBEFVisfatinpre-B cell-enhancing factorPre-B cell colony enhancing factorInhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Salutation

    Applicant Name *

    		 

    Email address *

    Phone number *

    		 

    Organization name *

    Department *

    		 

    Requested quantity *

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    (E)-Daporinad
    Cat. No.:
    HY-50876
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email address *

    Phone number

    		 

    Department *

    Organization name *

    		 

    Country or Region *

    Remarks

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.