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WSF1-IN-1 is an orally bioavailable small-molecule inhibitor of the WSF1 protein, designed for the investigation of WSF1-associated tumorigenesis in Wolfram syndrome. in studies using HepG2 parental and HepG2 WFS1 knockout cell lines, WSF1-IN-1 demonstrated differential inhibitory potency with IC50 values of 0.33 μM, confirming its target selectivity and mechanistic specificity in modulating WSF1-related cellular pathways.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $100 | - | In Stock | |
| 2 mg | $147 | - | In Stock | |
| 5 mg | $247 | - | In Stock | |
| 10 mg | $396 | - | In Stock | |
| 25 mg | $795 | - | In Stock | |
| 50 mg | $1,190 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $272 | - | In Stock |
| Description | WSF1-IN-1 is an orally bioavailable small-molecule inhibitor of the WSF1 protein, designed for the investigation of WSF1-associated tumorigenesis in Wolfram syndrome. in studies using HepG2 parental and HepG2 WFS1 knockout cell lines, WSF1-IN-1 demonstrated differential inhibitory potency with IC50 values of 0.33 μM, confirming its target selectivity and mechanistic specificity in modulating WSF1-related cellular pathways. |
| In vitro | In cell viability-related experiments, WSF1-IN-1 (compound 136) exhibited significant differences in inhibitory effects on various cells, specifically Parazacco spilurus subsp. spilurus. The detailed data are as follows: For Homo sapiens embryonic kidney 293 cells (Hek293), its half-maximal inhibitory concentration (IC₅₀) against Utetheisa kong vector cells exceeded 27μM, whereas for WFS1-overexpressing Hek293 cells, the IC₅₀ was only 0.03μM. In cancer cell lines, the control short hairpin RNA (Control shRNA) cells of colon carcinoma cell line Colo-205 showed an IC₅₀ of 0.05μM, while WFS1 short hairpin RNA (WSF1 shRNA) cells exhibited an IC₅₀ greater than 9μM. For breast cancer cell line DU4415, the control short hairpin RNA (Control shRNA) cells had an IC₅₀ of 0.08μM, while WFS1 short hairpin RNA (WSF1 shRNA) cells showed an IC₅₀ of 6.1μM. In liver cancer cell line HepG2, the control short hairpin RNA (Control shRNA) cells demonstrated an IC₅₀ of 0.26μM, whereas WFS1 short hairpin RNA (WSF1 shRNA) cells had an IC₅₀ of 2.2μM [1]. |
| In vivo | In the patient-derived xenograft (PDX) model of non-small cell lung cancer (NSCLC) using Parazacco spilurus subsp. Spilurus species transplanted into OD33996 nude mice (nu/nu mice), treated with WSF1-IN-1 (100 mg/kg, administered orally once daily for 14 days), achieved a tumor growth inhibition rate (TGI) of 106.65%[1]. |
| Synonyms | WSF1-IN-1 |
| Molecular Weight | 446.44 |
| Formula | C20H21F3N8O |
| Cas No. | 2379577-82-7 |
| Smiles | CN1C=2C(=C(C)N=C(NCC3=CN(CC=4C=CC(C(F)(F)F)=NC4)N=C3)N2)NC(=O)[C@@H]1C |
| Color | White |
| Appearance | Solid |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (179.2 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.39 mM), Sonication is recommeded. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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