| Field | Specification |
|---|---|
| Alternative names | PK4C9 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C21H14N4O3 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Homocarbonyltopsentin (PK4C9) is a small-molecule compound that binds TSL2, engaging pentaloop conformations of TSL2 and promoting a shift toward triloop conformations that display enhanced SMN2 exon 7 (E7) splicing, with an EC50 of 16 μM[1]. It is supplied as a white to yellow solid (C21H14N4O3, MW 370.36) at 99.82% purity.
Physical & Chemical Properties
| CAS Number | 172286-77-0 |
|---|---|
| Molecular Formula | C21H14N4O3 |
| Molecular Weight | 370.36 g/mol |
| Purity | 99.82% |
| Appearance | Solid |
| Color | White to yellow |
| SMILES | O=C(C1=NC=C(C(C2=CNC3=C2C=CC=C3)=O)N1)C4=CNC5=C4C=CC(O)=C5 |
| Signaling Pathway | Cell Cycle/DNA Damage |
| Solubility | In Vitro: DMSO: 100 mg/mL (270.01 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (270.01 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 2.08 mg/mL (5.62 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 2.08 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (20.8 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Data provided by the manufacturer.
In Vitro
Homocarbonyltopsentin (PK4C9) (10-40 μM; 24 hours) decreases the expression of E7-excluding SMN2 isoforms by up to 5.2-fold and increases E7-including isoforms by up to three-fold in GM03813C cells[1]. Compared with DMSO-treated GM03813C cells, Homocarbonyltopsentin (PK4C9) (40 μM; 24 hours) raised SMN protein expression 1.5-fold[1].
RT-PCR[1]
| Cell Line | GM03813C (SMA) cells; GM03814B fibroblasts cells |
|---|---|
| Concentration | 10-40 μM |
| Incubation Time | 24 hours |
| Result | E7 inclusion reached a maximum of 91% (25% increase, DMSO-treated cells). |
Western Blot Analysis[1]
| Cell Line | GM03813C (SMA) cells; GM03814B fibroblasts cells |
|---|---|
| Concentration | 40 μM |
| Incubation Time | 24 hours |
| Result | Increased SMN protein in SMA cells. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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