2. MAPK/ERK Pathway Cell Cycle/DNA Damage Apoptosis Protein Tyrosine Kinase/RTK
  3. MNK Eukaryotic Initiation Factor (eIF) Apoptosis FLT3 DYRK
  4. DS12881479

DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC50 value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia.

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

DS12881479

DS12881479 Chemical Structure

CAS No. : 2373065-59-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
1 mg In-stock
5 mg In-stock
10 mg In-stock
25 mg In-stock
50 mg   Get quote  
100 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

DS12881479 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE DS12881479

View All MNK Isoform Specific Products:

View All Isoforms
MNK1 MNK2 MNK

View All DYRK Isoform Specific Products:

View All Isoforms
DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DS12881479 is a selective non-ATP-competitive MNK1 inhibitor with an IC50 value of 387 nM. DS12881479 stabilizes MNK1 in its autoinhibited DFD-out conformation, blocks eIF4E phosphorylation, suppresses tumor cell proliferation and induces weak apoptosis. DS12881479 also inhibits FLT3 and DYRK1a kinase activity at high concentrations. DS12881479 can be used for the research of cancer, such as leukemia[1][2].

IC50 & Target[1]

MNK1

387 nM (IC50)

eIF4E

 

DYRK1A

 

In Vitro

DS12881479 potently inhibits recombinant MNK1 kinase activity with an IC50 of 387 ± 94 nM[1].
DS12881479 (72-120 h) inhibits proliferation of MV4-11, MOLM-13, and MM.1S cancer cells with IC50 values of 3.32 ± 0.66 μM, 12.08 ± 0.92 μM, and 5.32 ± 1.38 μM, respectively, and lacks activity against MDA-MB-231 cells (IC50 >20 μM)[1].
DS12881479 (300-1000 nM; 24 h) inhibits eIF4E phosphorylation in MV4-11 cells without degrading MNK1 or MNK2 protein[1].
DS12881479 (300 nM; 24 h) weakly induces apoptosis in MV4-11 cells, with a total apoptotic rate of 13.9%[1].
DS12881479 potently inhibits inactive human Mnk1 with an IC50 of 21 nM, and shows weaker inhibition of active human Mnk1 with an IC50 of 416 nM[2].
DS12881479 (5 μM) inhibits only FLT3 and DYRK1a by over 50%, demonstrating good selectivity for human Mnk1 over most other tested active kinases[2].

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

DS12881479 Related Antibodies

Western Blot Analysis[1]

Cell Line: MV4-11 cells
Concentration: 300 nM, 1000 nM
Incubation Time: 24 h
Result: Reduced p-eIF4E levels in a concentration-dependent manner.
Did not reduce MNK1 or MNK2 protein levels.

Apoptosis Analysis[1]

Cell Line: MV4-11 cells
Concentration: 300 nM
Incubation Time: 24 h
Result: Induced 13.9% total apoptosis in MV4-11 cells, with a low level of late apoptosis.
In Vivo

DS12881479 (20 mg/kg; i.p.; daily; 16 days) inhibits tumor growth in MV4-11 xenograft mice[1].

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

Animal Model: NOD-PrkdcscidIl2rgem1/Smoc mice (female, 5 weeks old, acute myeloid leukemia xenograft model with MV4-11 cells)[1]
Dosage: 20 mg/kg
Administration: i.p.; daily; 16 days
Result: Achieved a tumor growth inhibition rate of 28%.
Reduced p-eIF4E levels.
Showed no significant difference in body weight and ALT, TBIL, ALP, TBA, UA, CR compared with the vehicle control group.
Molecular Weight

301.41

Formula

C16H19N3OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1CCN(C)CC1)NC2=NC=C(C3=CC=CC=C3)S2
Shipping

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

DMSO : 250 mg/mL (829.43 mM; Need ultrasonic; 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 3.3177 mL 16.5887 mL 33.1774 mL
5 mM 0.6635 mL 3.3177 mL 6.6355 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

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

    Solubility: ≥ 2.08 mg/mL (6.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (6.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3177 mL 16.5887 mL 33.1774 mL 82.9435 mL
5 mM 0.6635 mL 3.3177 mL 6.6355 mL 16.5887 mL
10 mM 0.3318 mL 1.6589 mL 3.3177 mL 8.2943 mL
15 mM 0.2212 mL 1.1059 mL 2.2118 mL 5.5296 mL
20 mM 0.1659 mL 0.8294 mL 1.6589 mL 4.1472 mL
25 mM 0.1327 mL 0.6635 mL 1.3271 mL 3.3177 mL
30 mM 0.1106 mL 0.5530 mL 1.1059 mL 2.7648 mL
40 mM 0.0829 mL 0.4147 mL 0.8294 mL 2.0736 mL
50 mM 0.0664 mL 0.3318 mL 0.6635 mL 1.6589 mL
60 mM 0.0553 mL 0.2765 mL 0.5530 mL 1.3824 mL
80 mM 0.0415 mL 0.2074 mL 0.4147 mL 1.0368 mL
100 mM 0.0332 mL 0.1659 mL 0.3318 mL 0.8294 mL
  • 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.

DS12881479 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:

DS128814792373065-59-7DS 12881479DS-12881479MNKEukaryotic Initiation Factor (eIF)ApoptosisFLT3DYRKMitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Dual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseeIF4Ehuman MNK1DYRK1aleukemiamultiple myelomaMV4-11MOLM-13MM.1SMNK1Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
DS12881479
Cat. No.:
HY-148105
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

SAFETY DATA SHEET (SDS)

English - EN (393 KB) Français - FR (393 KB) Deutsch - DE (393 KB) Norwegian - NO (393 KB) Español - ES (393 KB) Swedish - SV (393 KB) Italian - IT (393 KB) Korean - KR (393 KB) Portuguese - PT (393 KB)

Request for HNMR Report

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