2. Epigenetics Metabolic Enzyme/Protease
  3. DNA Methyltransferase Pyruvate Kinase
  4. METTL1-WDR4-IN-1

METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m7G methyltransferase activity of the METTL1-WDR4 complex, blocking m7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8+ T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy.

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

METTL1-WDR4-IN-1

METTL1-WDR4-IN-1 Chemical Structure

CAS No. : 374705-10-9

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of METTL1-WDR4-IN-1:

METTL1-WDR4-IN-1 Related Antibodies

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1 Publications Citing Use of MCE METTL1-WDR4-IN-1

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DNA Methyltransferase DNMT1 DNMT3 MGMT

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Description

METTL1-WDR4-IN-1 (Compound 1) is a selective competitive inhibitor of the methyltransferase complex METTL1-WDR4 (IC50 = 144 μM). METTL1-WDR4-IN-1 inhibits the m7G methyltransferase activity of the METTL1-WDR4 complex, blocking m7G modification of PKM mRNA, reducing PKM2 protein expression, disrupting the METTL1/PKM2/H3K9la positive feedback loop, and simultaneously inhibiting PKM2 nuclear translocation-mediated CD155 transcriptional activation. METTL1-WDR4-IN-1 can inhibit tumor cell proliferation, weaken glycolytic metabolism, reverse tumor immune evasion (restoring NK cell and CD8+ T cell function), and regulate RNA epigenetic modification and the tumor immune microenvironment. METTL1-WDR4-IN-1 can be used in immunotherapy research for cancers such as colorectal cancer, and is particularly suitable for use in combination with PKM2 inhibitors to enhance anti-tumor treatment efficacy[1][2].

IC50 & Target

IC50: 144 μM (METTL1-WDR4)[1].
In Vitro

METTL1-WDR4-IN-1, as a METTL1 inhibitor, downregulates METTL1 protein and mRNA expression in HCT-116 and RKO CRC cells, inhibits m7G modification of PKM mRNA, and reduces PKM2 protein levels[2].
METTL1-WDR4-IN-1 inhibits glycolysis in CRC cells, reducing extracellular acidification rate (ECAR) and lactate accumulation, and downregulating H3K9la histone modification levels[2].
METTL1-WDR4-IN-1 inhibits PKM2 nuclear translocation in CRC cells, reduces CD155 transcription and protein expression, and enhances the expression of NK cell activation-related markers CD107a and CD16[2].
METTL1-WDR4-IN-1, in combination with the PKM2 inhibitor Shikonin, synergistically downregulates PKM2, H3K9la, and CD155 expression in CRC cells and synergistically inhibits cell proliferation[2].

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

METTL1-WDR4-IN-1 Related Antibodies
Molecular Weight

241.27

Formula

C8H11N5O2S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

S=C1N=C2C(N1)=C(N)N=CN2CC(CO)O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 55 mg/mL (227.96 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 4.1447 mL 20.7237 mL 41.4473 mL
5 mM 0.8289 mL 4.1447 mL 8.2895 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 (protect from light). 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
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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

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Volume (start)

V1

=
Concentration (final)

C2

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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: ≥ 2.75 mg/mL (11.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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: ≥ 2.75 mg/mL (11.40 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 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
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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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 (protect from light). 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 4.1447 mL 20.7237 mL 41.4473 mL 103.6184 mL
5 mM 0.8289 mL 4.1447 mL 8.2895 mL 20.7237 mL
10 mM 0.4145 mL 2.0724 mL 4.1447 mL 10.3618 mL
15 mM 0.2763 mL 1.3816 mL 2.7632 mL 6.9079 mL
20 mM 0.2072 mL 1.0362 mL 2.0724 mL 5.1809 mL
25 mM 0.1658 mL 0.8289 mL 1.6579 mL 4.1447 mL
30 mM 0.1382 mL 0.6908 mL 1.3816 mL 3.4539 mL
40 mM 0.1036 mL 0.5181 mL 1.0362 mL 2.5905 mL
50 mM 0.0829 mL 0.4145 mL 0.8289 mL 2.0724 mL
60 mM 0.0691 mL 0.3454 mL 0.6908 mL 1.7270 mL
80 mM 0.0518 mL 0.2590 mL 0.5181 mL 1.2952 mL
100 mM 0.0414 mL 0.2072 mL 0.4145 mL 1.0362 mL
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METTL1-WDR4-IN-1 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:

METTL1-WDR4-IN-1374705-10-9DNA MethyltransferasePyruvate KinaseDNMTsDNA MTasesInhibitorinhibitorinhibit

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