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Synonyms: SKLB163


| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 1 mg | $137 | In Stock | In Stock | |
| 5 mg | $336 | In Stock | In Stock | |
| 10 mg | $497 | In Stock | In Stock | |
| 25 mg | $793 | In Stock | In Stock | |
| 50 mg | $1,130 | In Stock | In Stock | |
| 100 mg | $1,520 | In Stock | In Stock | |
| 500 mg | $2,970 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $373 | In Stock | In Stock |

| Description | SKLB-163 is a small-molecule inhibitor and a RhoGDI inhibitor with oral bioactivity, cell permeability, and selectivity. This compound induces tumor cell apoptosis, inhibits proliferation and migration, and enhances radiosensitivity by downregulating RhoGDI, activating the JNK-1/caspase-3 pathway, and suppressing Akt and p44/42 MAPK phosphorylation. |
| Targets & IC50 | A431 cells:4.4 μM, HCT116 cells:1.3 μM, A549 cells:4 μM, A375 cells:1.8 μM, BxPC-3 cells:6.6 μM |
| In vitro | Methods: Nasopharyngeal carcinoma (NPC) cells were treated with various concentrations (0–20 μM) of SKLB-163 for 48 h, and changes in cell proliferation, migration, and radiosensitivity were detected. Results: SKLB-163 inhibited proliferation and migration of nasopharyngeal carcinoma (NPC) cells and sensitized the cells to radiation. [1] Methods: A375, SPC-A1, SW620, HeLa, and PC-3 cells were treated with various concentrations (0–20 μM) of SKLB-163 for 48 h to detect cytotoxic effects. A375 cells were treated with various concentrations (0–2.5 μM) of SKLB-163 for 48 h to detect apoptosis and colony formation. Results: SKLB-163 showed cytotoxic effects in A375, SPC-A1, SW620, HeLa, and PC-3 cells, and could induce apoptosis and inhibit colony formation in A375 cells. [2] |
| In vivo | Methods: To detect in vivo antitumor and radiosensitizing effects, SKLB-163 (25–100 mg/kg, gavage, once daily for 30 days) was administered alone in a nasopharyngeal carcinoma mouse model, or combined with radiotherapy (3 Gy radiation once daily for 3 days starting on day 6 of SKLB-163 administration). Results: SKLB-163 alone inhibited tumor growth and ascites formation, and suppressed liver and lung metastasis; combined administration sensitized nasopharyngeal carcinoma tumors to radiation. [1] |
| Synonyms | SKLB163 |
| Molecular Weight | 405.92 |
| Formula | C18H16ClN3O2S2 |
| Cas No. | 1255099-06-9 |
| Smiles | S(CC(NCC1=CC=CC=C1)=O)C2=NC=3C(S2)=CC(NC(CCl)=O)=CC3 |
| Relative Density. | 1.43 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 247.5 mg/mL (609.73 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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