2. Cell Cycle/DNA Damage Stem Cell/Wnt PI3K/Akt/mTOR
  3. CDK GSK-3
  4. DIF-3

DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in cells. DIF-3 induces reactive oxygen species (ROS) and autophagy. DIF suppresses the growth of Trypanosoma. cruzi in HT1080 cells. DIF-3 exerts antitumor effects both in vitro and in vivo.

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DIF-3 Chemical Structure

DIF-3 Chemical Structure

CAS No. : 113411-17-9

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Based on 2 publication(s) in Google Scholar

DIF-3 Related Antibodies

Top Publications Citing Use of Products

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GSK-3 GSK-3α GSK-3β

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

DIF-3 is an orally active anticancer agent. DIF-3 reduces the expression levels of cyclin D1 and c-Myc by facilitating their degradation via activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in cells. DIF-3 induces reactive oxygen species (ROS) and autophagy. DIF suppresses the growth of Trypanosoma. cruzi in HT1080 cells. DIF-3 exerts antitumor effects both in vitro and in vivo[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
S2 IC50
4.6 μM
Compound: 2, DIF-3
Immunosuppressive activity in Drosophila S2 cells expressing att-luc reporter gene assessed as inhibition of peptidoglycan-induced attacin production pre-treated for 1.5 hrs before peptidoglycan stimulation for 8 hrs by luciferase reporter gene assay
Immunosuppressive activity in Drosophila S2 cells expressing att-luc reporter gene assessed as inhibition of peptidoglycan-induced attacin production pre-treated for 1.5 hrs before peptidoglycan stimulation for 8 hrs by luciferase reporter gene assay
[PMID: 26122773]
In Vitro

DIF-3 (10-30 μM, 24-48 h) inhibits proliferation in a dose-dependent manner in human colon cancer cells[1].
DIF-3 (30 μM, 24 h) arrests the cell cycle at G0/G1 phase in human colon cancer cells[1].
DIF-3 (10-30 μM, 1-24 h) induces proteolysis of cyclin D1 and c-Myc in human colon cancer cells via activation of GSK-3β[1].
DIF-3 (10-30 μM, 1-24 h) inhibits Wnt/β-catenin signaling pathway-related proteins in human colon cancer cells[1].
DIF-3 (10 μM, 4 h) inhibits lysophosphatidic acide (LPA) stimulated migration of murine osteosarcoma LM8 cells[2].
DIF-3 (20 μM, 0.25-24 h) inhibits mTOR signaling and induces autophagy in K562 CML cells[3].
DIF-3 (20 μM) induces mitochondrial membrane potential (MMP) (0-10 min), a decrease of ATP content (6 h) and an induction of ROS production (0-30 min) in K562 cells[3].
DIF-3 (10 μM, 3 d) suppresses the growth of Trypanosoma. cruzi in HT1080 cells with an IC50 of 3.95 μM[4].

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

DIF-3 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HCT-116, DLD-1
Concentration: 10, 20, 30 μM
Incubation Time: 24, 48 h
Result: Strongly inhibited proliferation in a dose-dependent manner in both cell lines.
HCT-116 cells were more sensitive to DIF-3 than DLD-1 cells.

Cell Cycle Analysis[1]

Cell Line: HCT-116, DLD-1
Concentration: 30 μM
Incubation Time: 24 h
Result: Significantly increased the number of cells in G0/G1 phase and decreased those in S phase in both cell lines.
Also significantly increased the number of cells in G2 phase when HCT-116 cells were employed, this effect was not observed by using DLD-1 cells.

Cell Migration Assay [2]

Cell Line: LM8
Concentration: 10 μM
Incubation Time: 4 h
Result: Suppressed LPA-induced cell migration, whereas did not significantly affected cell migration in the absence of LPA.

Cell Autophagy Assay[3]

Cell Line: K562
Concentration: 20 μM
Incubation Time: 0.25, 0.5, 1, 3, 6, 24 h for mTOR study; 6, 16, 36, 48 h for Cathepsin B activity study
Result: Induced the rapid dephosphorylation of mTOR at Ser2481. Inhibited the mTOR pathway and leads to a rapid and robust conversion of LC3-I to LC3-II.
Increased autophagy was accompanied by the late activation of cathepsin B.

Western Blot Analysis[1]

Cell Line: HCT-116
Concentration: 10, 20, 30 μM
Incubation Time: 1, 3, 6, 12, 24 h
Result: Induced a rapid and marked reduction in the amount of cyclin D1 protein and c-Myc protein in a time and dose-dependent manner.
Had no effect on the expression level of β-catenin (30 μM for 24 h).
Reduced the amount of TCF7L2 which increased gradually over time in control cells, in a time and dose-dependent manner.
Reduction of TCF7L2 was associated with the transcriptional inhibition of cyclin D1 mRNA in HCT-116 cells.

Western Blot Analysis[1]

Cell Line: HCT-116
Concentration: 30 μM
Incubation Time: 1 h
Result: Effects could be attenuated by MG132 (HY-13259) and SB216763 (HY-12012), indicating the involvement of GSK-3β in degradation of cyclin D1 and c-Myc.
In Vivo

DIF-3 (150 mg/kg; p.o.; once a day for 5 days/week over 4 weeks) inhibits oxidative stress (0.2% KBrO3)-induced tumors in Mutyh-/- mice[1].

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

Animal Model: Mutyh-/- mice (KBrO3 dissolved in water at a concentration of 2 g/L was administered to 4-week-old mice for 12 weeks)[1]
Dosage: 150 mg/kg
Administration: Oral gavage (p.o.); once a day for 5 days/week over 4 weeks
Result: Markedly reduced the number of intestinal tumors, especially the number of large tumors with a diameter of >2.0 mm.
No differences in the appearance, activity, body weight, or blood cell counts.
The numbers of TCF7L2-and cyclin D1-positive nuclei in tumors were significantly decreased.
Molecular Weight

272.72

Formula

C13H17ClO4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(CCCCC)C1=C(C=C(C(Cl)=C1O)OC)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 : 100 mg/mL (366.68 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 3.6668 mL 18.3338 mL 36.6676 mL
5 mM 0.7334 mL 3.6668 mL 7.3335 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.

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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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (9.17 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
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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 3.6668 mL 18.3338 mL 36.6676 mL 91.6691 mL
5 mM 0.7334 mL 3.6668 mL 7.3335 mL 18.3338 mL
10 mM 0.3667 mL 1.8334 mL 3.6668 mL 9.1669 mL
15 mM 0.2445 mL 1.2223 mL 2.4445 mL 6.1113 mL
20 mM 0.1833 mL 0.9167 mL 1.8334 mL 4.5835 mL
25 mM 0.1467 mL 0.7334 mL 1.4667 mL 3.6668 mL
30 mM 0.1222 mL 0.6111 mL 1.2223 mL 3.0556 mL
40 mM 0.0917 mL 0.4583 mL 0.9167 mL 2.2917 mL
50 mM 0.0733 mL 0.3667 mL 0.7334 mL 1.8334 mL
60 mM 0.0611 mL 0.3056 mL 0.6111 mL 1.5278 mL
80 mM 0.0458 mL 0.2292 mL 0.4583 mL 1.1459 mL
100 mM 0.0367 mL 0.1833 mL 0.3667 mL 0.9167 mL
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DIF-3 Related Classifications

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  • 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:

DIF-3113411-17-9DIF3DIF 3CDKGSK-3Cyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3cyclin D1c-MycGSK-3βWnt/β-cateninDLD-1 cellsHeLaInhibitorinhibitorinhibit

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