| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
DIF-3 targets GSK-3β (glycogen synthase kinase-3β), activating it to promote the degradation of cyclin D1 and c-Myc. It also inhibits the Wnt/β-catenin signaling pathway, a key pathway involved in cell proliferation and differentiation. By reducing cyclin D1 and c-Myc expression and inhibiting Wnt signaling, DIF-3 induces cell cycle arrest and inhibits cancer cell proliferation. These mechanisms make DIF-3 a valuable tool for studying cell cycle regulation and Wnt signaling.
|
|---|---|
| ln Vitro |
DIF-3 induces G0/G1 phase cell cycle arrest in mammalian cells. It promotes the degradation of cyclin D1 and c-Myc through activation of GSK-3β. DIF-3 inhibits Wnt/β-catenin signaling pathway-related proteins in DLD-1 cells. These activities lead to inhibition of cancer cell proliferation. Specific IC₅₀ values for various activities are not extensively documented in the literature.
|
| ln Vivo |
In vivo activity data for DIF-3 are limited in the literature. Based on its in vitro anticancer activity and ability to inhibit cell proliferation through GSK-3β activation and Wnt signaling inhibition, it is anticipated to have potential in vivo antitumor efficacy. However, specific animal studies detailing its therapeutic effects and pharmacokinetics are not extensively documented.
|
| Enzyme Assay |
The non-cellular enzyme/receptor binding assay for DIF-3 would typically involve measuring GSK-3β activity using a kinase assay. Recombinant GSK-3β is incubated with a substrate peptide and ATP in the presence of varying concentrations of DIF-3. Phosphorylation of the substrate is measured using radioactive [γ-³²P]-ATP or by using a fluorescent or luminescent detection system. The compound's ability to activate GSK-3β is assessed. Wnt/β-catenin signaling can be evaluated using cell-free reporter assays.
|
| Cell Assay |
In vitro cellular assays for DIF-3 typically use cancer cell lines such as DLD-1 colon cancer cells. Cells are treated with various concentrations of DIF-3 for 24-72 hours. Cell proliferation is assessed using MTT or CCK-8 assays. Cell cycle distribution is analyzed by flow cytometry with propidium iodide staining. Protein expression levels of cyclin D1, c-Myc, GSK-3β, β-catenin, and other signaling proteins are analyzed by Western blotting. Apoptosis is detected by Annexin V/PI staining.
|
| Animal Protocol |
In vivo animal studies for DIF-3 are not extensively documented. Based on its anticancer activity, typical study designs would involve xenograft mouse models bearing human cancer cells such as DLD-1. DIF-3 would be administered orally or intraperitoneally. Tumor growth inhibition, body weight changes, and survival rates would be monitored. Tumor tissues would be analyzed for cell cycle markers and Wnt/β-catenin signaling proteins.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of DIF-3 are not extensively characterized. As a small molecule with molecular weight 272.72, it is expected to have reasonable oral bioavailability. The compound contains a chloro group, which may affect its metabolic stability. Metabolic pathways likely involve phase I oxidation and phase II conjugation. Specific PK parameters such as half-life, Cmax, and protein binding are not well documented.
|
| Toxicity/Toxicokinetics |
Toxicological data for DIF-3 are limited. As a research-grade compound, comprehensive toxicology studies are not available. The compound may cause skin and eye irritation upon contact. Standard laboratory safety precautions should be observed when handling this compound.
|
| References | |
| Additional Infomation |
DIF-3 is a research-grade compound intended for laboratory use only. It is not approved for clinical use as a therapeutic agent. Its primary applications include studying cell cycle regulation and the role of GSK-3β in cancer, investigating Wnt/β-catenin signaling and its role in cancer and development, and exploring the therapeutic potential of differentiation-inducing factors in cancer and regenerative medicine. DIF-3 is also known as Differentiation-inducing factor 3.
|
| Molecular Formula |
C13H17CLO4
|
|---|---|
| Molecular Weight |
272.72468
|
| Exact Mass |
272.082
|
| CAS # |
113411-17-9
|
| PubChem CID |
3081033
|
| Appearance |
White to off-white solid powder
|
| Density |
1.24g/cm3
|
| Boiling Point |
416.9ºC at 760mmHg
|
| Flash Point |
205.9ºC
|
| Vapour Pressure |
1.53E-07mmHg at 25°C
|
| Index of Refraction |
1.551
|
| LogP |
3.522
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
18
|
| Complexity |
272
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
JWBMZIJMSBFBIY-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H17ClO4/c1-3-4-5-6-8(15)11-9(16)7-10(18-2)12(14)13(11)17/h7,16-17H,3-6H2,1-2H3
|
| Chemical Name |
1-(3-chloro-2,6-dihydroxy-4-methoxyphenyl)hexan-1-one
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~366.68 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.3667 mL | 1.8334 mL | 3.6668 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
