2. Metabolic Enzyme/Protease
  3. Methylenetetrahydrofolate Dehydrogenase (MTHFD)
  4. DS44960156

DS44960156 is a selective MTHFD2 inhibitor with moderate to low blood-brain barrier penetration (IC50=1.6 μM, Ki=1.23 μM). DS44960156 specifically binds to the active site of MTHFD2, disrupts redox homeostasis and blocks serine-mediated one-carbon metabolism, thereby increasing the NAD+/NADH ratio and ROS levels. DS44960156 not only effectively inhibits the proliferation of glioma cells, but also enhances the sensitivity of cells to glutamine starvation-induced death. DS44960156 binds to plasma proteins, shows no mutagenicity, carcinogenicity or acute oral toxicity, and serves as a research agent for glioblastoma multiforme and other cancers.

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DS44960156

DS44960156 Chemical Structure

CAS No. : 2361327-08-2

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

DS44960156 Related Antibodies

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  • Purity & Documentation

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Description

DS44960156 is a selective MTHFD2 inhibitor with moderate to low blood-brain barrier penetration (IC50=1.6 μM, Ki=1.23 μM). DS44960156 specifically binds to the active site of MTHFD2, disrupts redox homeostasis and blocks serine-mediated one-carbon metabolism, thereby increasing the NAD+/NADH ratio and ROS levels. DS44960156 not only effectively inhibits the proliferation of glioma cells, but also enhances the sensitivity of cells to glutamine starvation-induced death. DS44960156 binds to plasma proteins, shows no mutagenicity, carcinogenicity or acute oral toxicity, and serves as a research agent for glioblastoma multiforme and other cancers[1][2][3].

IC50 & Target

IC50: 1.6 μM (MTHFD2), >30 μM (MTHFD1)[1].
In Vitro

DS44960156 inhibits the viability of LN229 glioblastoma cells with an IC50 of 481.2 μM; it also inhibits the viability of U251 glioblastoma cells with an IC50 of 214.9 μM[1].
DS44960156 (500 μM (LN229), 300 μM (U251); 24 h) inhibits the proliferation and promotes the apoptosis of glioblastoma cells; glutamine starvation conditions enhance the antiproliferative and apoptosis-inducing activities of DS44960156, and increase the NAD+/NADH ratio and ROS levels[1].
DS44960156 exhibits favorable druglike properties, including compliance with standard pharmacokinetic rules, low metabolic risk, and low predicted toxicity, with a plasma protein binding rate of 84.75% and a half-life of 0.77 h[2].

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

DS44960156 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: human glioblastoma LN229, U251 cell lines
Concentration: 500 μM (for LN229 cells); 300 μM (for U251 cells)
Incubation Time: 24 h; or 24, 48, 72, 96 h (proliferation measurement post-medium change)
Result: Inhibited proliferation of LN229 and U251 cells under both glutamine-containing and glutamine-free conditions, with significantly greater antiproliferative effects observed under glutamine starvation.
In Vivo

No in vivo animal experiments directly related to DS44960156 are available to date. Its analog DS18561882 exhibits significant in vivo anti-tumor activity with extremely low associated toxicity in a nude mouse MDA-MB-231 triple-negative breast cancer xenograft model after oral administration[4].

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

349.34

Formula

C20H15NO5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C(C(N2CCC(C3=CC=CC=C3O4)=C(C4=O)C2)=O)C=C1
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 : 100 mg/mL (286.25 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 2.8625 mL 14.3127 mL 28.6254 mL
5 mM 0.5725 mL 2.8625 mL 5.7251 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
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Volume
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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: ≥ 2.5 mg/mL (7.16 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (7.16 mM); Suspended solution

    This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

Purity: ≥99.0%

SDS (251 KB)

COA (248 KB) Elemental Analysis Report (106 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, 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 2.8625 mL 14.3127 mL 28.6254 mL 71.5635 mL
5 mM 0.5725 mL 2.8625 mL 5.7251 mL 14.3127 mL
10 mM 0.2863 mL 1.4313 mL 2.8625 mL 7.1564 mL
15 mM 0.1908 mL 0.9542 mL 1.9084 mL 4.7709 mL
20 mM 0.1431 mL 0.7156 mL 1.4313 mL 3.5782 mL
25 mM 0.1145 mL 0.5725 mL 1.1450 mL 2.8625 mL
30 mM 0.0954 mL 0.4771 mL 0.9542 mL 2.3855 mL
40 mM 0.0716 mL 0.3578 mL 0.7156 mL 1.7891 mL
50 mM 0.0573 mL 0.2863 mL 0.5725 mL 1.4313 mL
60 mM 0.0477 mL 0.2385 mL 0.4771 mL 1.1927 mL
80 mM 0.0358 mL 0.1789 mL 0.3578 mL 0.8945 mL
100 mM 0.0286 mL 0.1431 mL 0.2863 mL 0.7156 mL
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DS44960156 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:

DS449601562361327-08-2DS 44960156DS-44960156Methylenetetrahydrofolate Dehydrogenase (MTHFD)glutamine starvationU251 glioblastoma cellsone-carbon metabolismMTHFD2LN229 glioblastoma cellsredox homeostasisglioblastoma multiformeglioma cellsMTHFD1ROS signalingInhibitorinhibitorinhibit

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