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Synonyms:
STAT3-IN-53
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
| Description | STAT3-IN-53 (Compound L20) is a STAT3 inhibitor with a dissociation constant (Kd) of 6.16 μM. It binds directly to the SH2 domain of STAT3, inhibiting phosphorylation at the Y705 site without affecting total STAT3 protein levels. STAT3-IN-53 downregulates the transcription and expression of cyclin-D1 and c-Myc, induces cell cycle arrest, and promotes apoptosis. Additionally, STAT3-IN-53 exhibits anticancer activity against colorectal cancer. |
| Targets & IC50 | STAT3:6.16 μM (Kd) |
| In vitro | STAT3-IN-53 binds directly to recombinant full-length wild-type STAT3 protein with a Kd value of 6.16 μM. In HEK-BLUE-IL6 cells, STAT3-IN-53 effectively inhibits the IL-6/JAK/STAT3 signaling pathway, displaying an IC50 of 0.89 μM. Over 96 hours, STAT3-IN-53 strongly suppresses the proliferation of colorectal cancer cell lines HCT116, HT29, SW480, MC38, and CT26, with the greatest potency against HCT116 cells (IC50 = 0.45 μM). |
| In vivo | STAT3-IN-53 (5-20 mg/kg; intraperitoneal injection; once daily; 12 days) exhibits dose-dependent inhibition of subcutaneous MC38 colon adenocarcinoma growth in C57BL/6J mice. |
| Molecular Weight | 678.73 |
| Formula | C33H33F3N8O3S |
| Cas No. | 3113051-34-3 |
| Smiles | O=C(OCC)C1=NC=CC(=C1)C2=NN=C(S2)NC3=CC=4N=C(C=5C=CC(OC(F)(F)F)=CC5)N(C4C=C3N6CCN(CC)CC6)C7CC7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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.
| Size | Quantity | Unit Price | Amount | Operation |
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