2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. M435-1279

M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1.

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

M435-1279 Chemical Structure

M435-1279 Chemical Structure

CAS No. : 1359431-16-5

Size Price Stock Quantity
5 mg USD 150 In-stock
10 mg USD 235 In-stock
25 mg USD 450 In-stock
50 mg USD 750 In-stock
100 mg USD 1200 In-stock
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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

M435-1279 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

M435-1279 is a UBE2T inhibitor. M435-1279 inhibits the Wnt/β-catenin signaling pathway hyperactivation through blocking UBE2T-mediated degradation of RACK1[1].

IC50 & Target

UBE2T

 

In Vitro

M435-1279 (0, 2, 4, 8, 16, 31 μM; 48 h) significantly inhibits the growth of HGC27, AGS, and MKN45 cells[1].
M435-1279 (0, 4, 8, 12, 16, 20 μM) inhibits the cell viability with IC50s of 16.8, 11.88, 6.93, 7.76 μM of GES-1, HGC27, MKN45, AGS cells, respectively[1].
M435-1279 (31 nM to 500 μM) binds to UBE2T with a KD value of 50.5 μM[1].
M435-1279 (11.88 μM; 48 h) inhibits the ubiquitination of RACK1 and the hyperactivation of the Wnt/β-catenin pathway[1].

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

M435-1279 Related Antibodies

Cell Viability Assay[1]

Cell Line: HGC27, AGS, and MKN45 cells
Concentration: 0, 2, 4, 8, 16, 31 μM
Incubation Time: 48 h
Result: Inhibited the cell growth.

Cell Viability Assay[1]

Cell Line: HGC27, AGS, and MKN45 cells
Concentration: 0, 4, 8, 12, 16, 20 μM
Incubation Time:
Result: Inhibited the cell viability with IC50s of 16.8, 11.88, 6.93, 7.76 μM in GES-1, HGC27, MKN45, AGS cells, respectively.
In Vivo

M435-1279 (5 mg/kg/day; intratumor injection for 18 days) slows the tumor growth[1].
M435-1279 induces higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors[1].

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

Animal Model: BALB/C nude mice CDX model (MKN45 tumor size: 75–100 mm3)[1]
Dosage: 5 mg/kg/day
Administration: Intratumor injection for 18 days
Result: Slowed the tumor growth.
Induced higher RACK1 proteins expression, and lower Ki-67 and β-catenin proteins expression in intratumor tumors.
Molecular Weight

419.47

Formula

C18H17N3O5S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=C(O)C2=C(SC3=C2CCCC3)NC1=O)NC4=CC=C(S(=O)(N)=O)C=C4
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 : 50 mg/mL (119.20 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 2.3840 mL 11.9198 mL 23.8396 mL
5 mM 0.4768 mL 2.3840 mL 4.7679 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
=
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

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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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.96 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 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).

*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

Purity: 98.43%

COA (254 KB) HNMR (131 KB) LCMS (97 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 (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 2.3840 mL 11.9198 mL 23.8396 mL 59.5990 mL
5 mM 0.4768 mL 2.3840 mL 4.7679 mL 11.9198 mL
10 mM 0.2384 mL 1.1920 mL 2.3840 mL 5.9599 mL
15 mM 0.1589 mL 0.7947 mL 1.5893 mL 3.9733 mL
20 mM 0.1192 mL 0.5960 mL 1.1920 mL 2.9800 mL
25 mM 0.0954 mL 0.4768 mL 0.9536 mL 2.3840 mL
30 mM 0.0795 mL 0.3973 mL 0.7947 mL 1.9866 mL
40 mM 0.0596 mL 0.2980 mL 0.5960 mL 1.4900 mL
50 mM 0.0477 mL 0.2384 mL 0.4768 mL 1.1920 mL
60 mM 0.0397 mL 0.1987 mL 0.3973 mL 0.9933 mL
80 mM 0.0298 mL 0.1490 mL 0.2980 mL 0.7450 mL
100 mM 0.0238 mL 0.1192 mL 0.2384 mL 0.5960 mL
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M435-1279 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:

M435-12791359431-16-5E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseHGC27AGSMKN45 cellCDX modelRACK1Inhibitorinhibitorinhibit

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