| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C18H14N4OS |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
ABC1183 is an orally active, selective, dual inhibitor of GSK3 and CDK9. It inhibits GSK3β, GSK3α and CDK9/cyclin T1, with IC50 values of 657 nM, 327 nM and 321 nM, respectively, and it has anti-inflammatory and anti-tumor activities[1]. It is supplied as a light yellow to yellow solid (C18H14N4OS, MW 334.39) at 99.62% purity.
Physical & Chemical Properties
| CAS Number | 1042735-18-1 |
|---|---|
| Molecular Formula | C18H14N4OS |
| Molecular Weight | 334.39 g/mol |
| Purity | 99.62% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | N#CC1=CC=C(C(C2=C(N)N=C(NC3=CC=C(C)C=C3)S2)=O)C=C1 |
| Target | CDK9- Cyclin T1, GSK-3α, GSK-3β |
| Signaling Pathway | PI3K/Akt/mTOR; Stem Cell/Wnt; Cell Cycle/DNA Damage |
| Solubility | In Vitro: DMSO: 125 mg/mL (373.82 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, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
CDK9- Cyclin T1 321 nM (IC50) |
GSK-3α 327 nM (IC50) |
GSK-3β 657 nM (IC50) |
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 | 125 mg/mL (373.82 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
Data provided by the manufacturer.
In Vitro
ABC1183 at 3 μM for 24 h can halt cell cycle progression and so can influence cell proliferation[1].
Cell Cycle Analysis[1]
| Cell Line | LNCaP human prostate cancer cells |
|---|---|
| Concentration | 3 μM |
| Incubation Time | 24 hours |
| Result | Significantly reduced cells in the G1 and S phases and increased cells in the G2/M and sub-G1 cycle phases. |
In Vivo
In male C57BL/6 mice, ABC1183 (oral gavage, 5 or 50 mg/kg) inhibits tumor proliferation by negatively regulating cell growth and pro-inflammatory signalling[1].
| Animal Model | Male C57BL/6 mice with melanoma B16[1] |
|---|---|
| Dosage | 5 mg/kg |
| Administration | Oral gavage; 5 times per week; 22 days |
| Result | Reduced tumor size and no observed toxicity. Decreased the expression levels of GSK3 α /β, pSer21/9 and GS pSer641 but no change of total GS expression. |
| Animal Model | Male C57BL/6 mice infected crohn’s disease[1] |
|---|---|
| Dosage | 50 mg/kg |
| Administration | Oral gavage; everyday; 3 days |
| Result | Reduced TNF-α by 65%, IL-6 by 30% and IL-1β by 45%. |
| Animal Model | Male C57BL/6 mice with ulcerative colitis[1] |
|---|---|
| Dosage | 50 mg/kg |
| Administration | Oral gavage; once daily; 6 days |
| Result | Increased the expression of the anti-inflammatory factor IL-10, while decreasing the pro-inflammatory factor IL-6. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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