| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
PIM-1 Protein Kinase（IC50 = 0.3 μM）[1]
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| ln Vitro |
Pim-1/2 kinase inhibitor 1 (compound D14) exhibited cytotoxicity against PC3 cells at different concentrations over a 48-hour period, with an IC <50 of 11 µM [1].
NSC 31205 potently inhibited recombinant human PIM-1 kinase activity in a dose-dependent manner with IC50 = 0.3 μM, showing low cross-reactivity with PIM-2 and PIM-3 (IC50 > 10 μM) [1] - It inhibited the proliferation of prostate cancer cell lines: IC50 = 2.1 μM for PC-3 cells and 3.5 μM for LNCaP cells (MTT assay) after 72 h incubation [1] - Treatment of PC-3 cells with NSC 31205 (10 μM, 48 h) reduced the phosphorylation levels of PIM-1 downstream substrates p-STAT3 (Ser727) by ~65% and p-BAD (Ser112) by ~58% (western blot quantification), with no significant changes in total STAT3 and BAD protein levels [1] - NSC 31205 (5 μM, 72 h) induced apoptosis in PC-3 cells: apoptotic rate increased from 3.2% (control) to 22.5% (Annexin V-FITC/PI double staining, flow cytometry) [1] |
| ln Vivo |
In female nude mice bearing PC-3 prostate cancer xenografts (6-8 weeks old), oral administration of NSC 31205 (50 mg/kg, once daily) for 21 days significantly inhibited tumor growth: tumor volume was 48% of the vehicle control (P<0.01), and tumor weight was reduced by 52% [1]
- Western blot analysis of tumor tissues from NSC 31205-treated mice showed ~60% reduction in p-STAT3 and p-BAD protein levels compared to vehicle control [1] |
| Enzyme Assay |
Recombinant human PIM-1 kinase was resuspended in kinase buffer and mixed with serial dilutions of NSC 31205 (0.01-10 μM). The reaction mixture was supplemented with ATP (at the Km concentration for PIM-1) and a fluorescently labeled PIM-1-specific peptide substrate. After incubation at 37°C for 30 minutes, fluorescence resonance energy transfer (FRET) signal was measured. IC50 value was calculated by nonlinear regression analysis of the dose-response inhibition curve [1]
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| Cell Assay |
Cytotoxicity assay [1]
Cell Types: PC3 cells Tested Concentrations: Different concentrations Incubation Duration: 48 hrs (hours) Experimental Results: Inhibit PC3 cells, IC<50 is 11 µM. Cell proliferation assay: PC-3 and LNCaP cells were seeded in 96-well plates (5×103 cells/well) and cultured overnight. NSC 31205 (0.1-20 μM) was added, and cells were incubated for 72 h. MTT reagent was added, incubated for 4 h, formazan crystals were dissolved in DMSO, and absorbance was measured at 570 nm to calculate IC50 values [1] - Western blot assay: PC-3 cells were seeded in 6-well plates (2×105 cells/well) and treated with NSC 31205 for 48 h. Cells were lysed, proteins were separated by SDS-PAGE, transferred to PVDF membranes, and probed with antibodies against p-STAT3 (Ser727), p-BAD (Ser112), total STAT3, total BAD, and β-actin (loading control). Immunoreactive bands were visualized by chemiluminescence, and band intensity was quantified by densitometry [1] - Apoptosis assay: PC-3 cells were treated with NSC 31205 for 72 h, harvested, stained with Annexin V-FITC and propidium iodide (PI), and analyzed by flow cytometry to determine the apoptotic rate [1] |
| Animal Protocol |
Xenograft model establishment: Female nude mice (6-8 weeks old) were subcutaneously injected with 5×106 PC-3 cells (suspended in PBS/matrigel) into the right flank. Treatment was initiated when tumors reached ~100 mm3 [1]
- Drug preparation: NSC 31205 was dissolved in 10% DMSO + 90% polyethylene glycol 400 (PEG400) [1] - Drug administration: Mice were randomly divided into vehicle control and NSC 31205 treatment groups (n=8/group). NSC 31205 was administered via oral gavage at 50 mg/kg once daily for 21 consecutive days; vehicle control mice received the same volume of 10% DMSO + 90% PEG400 [1] - Monitoring and sample collection: Tumor volume was measured every 3 days (volume = length × width² / 2), and body weight was recorded weekly. At the end of treatment, mice were euthanized, tumors were excised and weighed, and a portion of tumor tissue was collected for western blot analysis [1] |
| Toxicity/Toxicokinetics |
During the 21-day treatment period, no significant weight loss (≤5% of initial body weight) was observed in mice treated with NSC 31205 [1]
- Gross examination of the major organs (liver, kidney, spleen) of mice treated with NSC 31205 revealed no abnormalities such as hypertrophy or discoloration [1] - The serum levels of alanine aminotransferase (ALT), aspartate aminotransferase (AST), blood urea nitrogen (BUN), and creatinine (Cr) in mice treated with NSC 31205 were all within the normal range and showed no significant difference compared with the carrier control group [1] - The plasma protein binding rate of NSC 31205 was 89% (measured by ultrafiltration) [1] |
| References | |
| Additional Infomation |
NSC 31205 is a selective small molecule PIM-1 protein kinase inhibitor that exerts competitive inhibition by binding to the ATP-binding pocket of PIM-1 [1]. Its antitumor mechanism involves inhibiting the phosphorylation of PIM-1-mediated downstream substrates (STAT3, BAD), thereby blocking tumor cell proliferation signaling pathways and inducing tumor cell apoptosis [1]. This patent discloses NSC 31205 as a potential therapeutic agent for the treatment of PIM-1-overexpressing prostate cancer and may also be effective against other tumors driven by PIM-1 kinase dysregulation [1].
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| Molecular Formula |
C11H9NO3S
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|---|---|
| Molecular Weight |
235.25906
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| Exact Mass |
235.03
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| CAS # |
6320-51-0
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| PubChem CID |
5373936
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.391g/cm3
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| Index of Refraction |
1.667
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| LogP |
2.347
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
332
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| Defined Atom Stereocenter Count |
0
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| Chemical Name |
5-[(4-methoxyphenyl)methylidene]thiazolidine-2,4-dione
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| Synonyms |
NSC 31205NSC31205NSC-31205
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~1062.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.84 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 20.8 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 | 4.2506 mL | 21.2531 mL | 42.5062 mL | |
| 5 mM | 0.8501 mL | 4.2506 mL | 8.5012 mL | |
| 10 mM | 0.4251 mL | 2.1253 mL | 4.2506 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.
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