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| Targets |
FUBP1–IN-1 targets FUSE binding protein 1 (FUBP1), a protein that binds to the far upstream element (FUSE) sequence of the c-myc gene. By inhibiting FUBP1, it disrupts the regulation of c-myc expression. This makes it a valuable tool for studying the role of FUBP1 in cell proliferation, differentiation, and cancer.
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| ln Vitro |
In vitro, FUBP1–IN-1 demonstrates potent inhibition of FUBP1 binding to DNA. Its IC50 of 11.0 µM confirms its activity as a moderate inhibitor. This activity is confirmed in DNA binding assays where it inhibits the interaction between FUBP1 and the FUSE sequence. It is used to study the role of FUBP1 in c-myc regulation.
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| ln Vivo |
In vivo, FUBP1–IN-1 is used as a research tool to study the role of FUBP1 in various physiological and pathological processes. By inhibiting FUBP1, it can affect the expression of c-myc and other target genes. It is used to explore the therapeutic potential of FUBP1 inhibition in cancer, where c-myc is often dysregulated.
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| Enzyme Assay |
The in vitro DNA binding assay for FUBP1–IN-1 involves measuring its ability to inhibit the binding of FUBP1 to the FUSE sequence. Recombinant FUBP1 protein is incubated with a labeled FUSE DNA probe in the presence of varying concentrations of the compound. The amount of protein-DNA complex formed is measured using an electrophoretic mobility shift assay (EMSA) or a fluorescence polarization assay, and the IC50 is calculated.
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| Cell Assay |
In vitro cell culture studies for FUBP1–IN-1 utilize cancer cell lines where c-myc is overexpressed. Cells are treated with the compound, and cell viability is assessed using MTT assays. The expression of c-myc and its target genes is measured by qPCR or Western blotting. The effect on cell proliferation and apoptosis is assessed by flow cytometry.
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| Animal Protocol |
In vivo animal experiments for FUBP1–IN-1 are not extensively documented. However, its effects on c-myc expression and tumor growth could be studied in xenograft models. The compound would be administered, and tumor growth would be monitored. The expression of c-myc and other markers in the tumor tissue would be analyzed.
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| ADME/Pharmacokinetics |
FUBP1–IN-1 has a molecular formula of C19H14F3N3O2S and a molecular weight of 405.39 g/mol. It is a solid compound that is soluble in DMSO (16.67 mg/mL, 41.12 mM). It is typically stored as a powder at -20°C for long-term stability. Its stability is maintained under recommended storage conditions. It has a predicted density of 1.42±0.1 g/cm3.
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| Toxicity/Toxicokinetics |
Toxicological data for FUBP1–IN-1 are limited, as it is a research compound. It is not intended for human use. Comprehensive toxicity studies have not been reported. Standard safety precautions for handling chemical reagents should be followed. Its effects on c-myc expression suggest it could have significant biological effects.
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| References | |
| Additional Infomation |
FUBP1–IN-1 is a research compound with no clinical approval. It is a valuable tool for studying FUBP1 biology and the regulation of c-myc expression. It is used in drug discovery programs to explore the therapeutic potential of FUBP1 inhibition for the treatment of cancer and other diseases where c-myc is dysregulated.
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| Molecular Formula |
C19H14F3N3O2S
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|---|---|
| Molecular Weight |
405.393573284149
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| Exact Mass |
405.075
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| CAS # |
883003-62-1
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| PubChem CID |
2823337
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
4.2
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
541
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C=C(C=C1)C2=NC3=CC(=NN3C(=C2)C(F)(F)F)C4=CC=CS4)OC
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| InChi Key |
CLFOYJSEPPNFQZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H14F3N3O2S/c1-26-14-6-5-11(8-15(14)27-2)12-9-17(19(20,21)22)25-18(23-12)10-13(24-25)16-4-3-7-28-16/h3-10H,1-2H3
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| Chemical Name |
5-(3,4-dimethoxyphenyl)-2-thiophen-2-yl-7-(trifluoromethyl)pyrazolo[1,5-a]pyrimidine
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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 : ~16.67 mg/mL (~41.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.79 mg/mL (4.42 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 17.9 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 | 2.4668 mL | 12.3338 mL | 24.6676 mL | |
| 5 mM | 0.4934 mL | 2.4668 mL | 4.9335 mL | |
| 10 mM | 0.2467 mL | 1.2334 mL | 2.4668 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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