| 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 |
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| Other Sizes |
Purity: ≥98%
| Targets |
F1063-0967 selectively targets dual-specificity phosphatase 26 (DUSP26), a member of the protein tyrosine phosphatase (PTP) superfamily that negatively regulates the mitogen-activated protein kinase (MAPK) signaling pathway. By inhibiting DUSP26, F1063-0967 blocks its phosphatase activity, thereby reactivating MAPK signaling and promoting apoptosis in cancer cells that overexpress DUSP26.
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| ln Vitro |
F1063-0967 is an IC50 of 11.62 μM for dual-specificity phosphatase 26 (DUSP26) inhibitors. F1063-0967 strongly promotes apoptosis in IMR32 cells at concentrations greater than 0.1 μM. With an IC50 value of 4.13 μM, F1063-0967 causes apoptosis in the IMR-32 cell line. F1063-0967 exhibits negligible inhibitory effect on the SH-SY5Y cell line and no effect on the HL7702 cell line [1].
In vitro, F1063-0967 inhibits DUSP26 with an IC₅₀ of approximately 11.6 µM. Its inhibitory activity against DUSP26 is higher than that of NCS87877 (IC₅₀ = 16.67 μM) but lower than that of ethyl-3,4-dephostatin (IC₅₀ = 6.8 μM). The compound induces apoptosis in IMR-32 neuroblastoma cells with an IC₅₀ of 4.13 µM, as shown by MTT assay. It shows no effect on normal HL7702 cells and exhibits minimal toxicity toward SH-SY5Y cells. |
| ln Vivo |
In vivo activity for F1063-0967 has not been fully characterized and is listed as "TBD" (To Be Determined) in available datasheets. As a research compound, its pharmacokinetic and pharmacodynamic properties in animal models remain to be established.
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| Enzyme Assay |
Non-cellular enzyme assays for F1063-0967 involve assessing its inhibition of DUSP26 using purified recombinant enzyme. The phosphatase activity is measured using a synthetic substrate such as p-nitrophenyl phosphate (pNPP) or a phosphopeptide substrate. The enzyme is incubated with varying concentrations of F1063-0967, and the release of phosphate is monitored spectrophotometrically. IC₅₀ values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for F1063-0967 involve treating neuroblastoma cell lines such as IMR-32 with the compound and assessing cell viability and apoptosis. Cells are treated with varying concentrations of F1063-0967 for specified time periods. Cell viability is measured using MTT or CellTiter-Glo® assays. Apoptosis is assessed by flow cytometry using Annexin V/PI staining or by measuring caspase activity. The compound's selective cytotoxicity toward DUSP26-overexpressing cells is evaluated by comparing effects on cancer cell lines versus normal cell lines such as HL7702.
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| Animal Protocol |
In vivo animal experiments for F1063-0967 have not been extensively documented. As a research compound targeting DUSP26, potential studies would involve administration to mouse xenograft models of neuroblastoma or other DUSP26-overexpressing tumors. Endpoints would include tumor growth inhibition, assessment of DUSP26 inhibition in tumor tissue, and evaluation of pharmacodynamic markers such as MAPK pathway activation. Pharmacokinetic studies would characterize absorption, distribution, metabolism, and excretion.
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| ADME/Pharmacokinetics |
F1063-0967 has a molecular weight of 484.59 and a molecular formula of C24H24N2O5S2. It is a solid powder with a purity of >98%. The compound is soluble in DMSO. For short-term storage (days to weeks), it should be kept dry, dark, and at 0-4°C; for long-term storage (months to years), it should be stored at -20°C. The compound has a shelf life of >2 years if stored properly.
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| Toxicity/Toxicokinetics |
F1063-0967 is a research compound for laboratory use only and is not intended for human therapeutic or diagnostic use. In preclinical studies, it has shown selective cytotoxicity toward DUSP26-overexpressing tumor cells while sparing normal cells. Standard laboratory safety precautions should be followed when handling the compound. It may cause skin, eye, and respiratory irritation.
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| References | |
| Additional Infomation |
F1063-0967 (CAS 613225-56-2) is a novel inhibitor of dual-specificity phosphatase 26 (DUSP26) with an IC₅₀ of 11.62 µM. It induces apoptosis in IMR-32 neuroblastoma cells with an IC₅₀ of 4.13 µM. The compound was identified through a hybrid virtual screening approach. F1063-0967 is a valuable tool for studying DUSP26 function in oncogenic signaling and neuroblastoma pathogenesis. It is available from various commercial suppliers for research applications.
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| Molecular Formula |
C24H24N2O5S2
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|---|---|
| Molecular Weight |
484.585
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| Exact Mass |
484.112
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| Elemental Analysis |
C, 59.49; H, 4.99; N, 5.78; O, 16.51; S, 13.23
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| CAS # |
613225-56-2
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| Related CAS # |
613225-56-2;
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| PubChem CID |
5895168
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.704
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| LogP |
5.03
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
779
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1/C(=C\C2C=CC(C)=CC=2)/C(N(C1=S)CCCCCC(NC1C=CC(C(=O)O)=C(C=1)O)=O)=O
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| InChi Key |
RNICWTYEMLCCAS-MOSHPQCFSA-N
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| InChi Code |
InChI=1S/C24H24N2O5S2/c1-15-6-8-16(9-7-15)13-20-22(29)26(24(32)33-20)12-4-2-3-5-21(28)25-17-10-11-18(23(30)31)19(27)14-17/h6-11,13-14,27H,2-5,12H2,1H3,(H,25,28)(H,30,31)/b20-13-
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| Chemical Name |
2-hydroxy-4-[6-[(5Z)-5-[(4-methylphenyl)methylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]hexanoylamino]benzoic acid
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| Synonyms |
F1063-0967; F1063 0967; F10630967; F-10630967; F 10630967;
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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 : ~100 mg/mL (~206.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.16 mM) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0636 mL | 10.3180 mL | 20.6360 mL | |
| 5 mM | 0.4127 mL | 2.0636 mL | 4.1272 mL | |
| 10 mM | 0.2064 mL | 1.0318 mL | 2.0636 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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