WP1066 (Synonyms: STAT Inhibitor III) |
Catalog No.GC15980
One-Click Copy Product Info
|
WP1066 is a reversible competitive inhibitor of STAT3 (Signal Transducer and Activator of Transcription 3), with an IC50 of approximately 2.5µM for the inhibition of STAT3 Tyr705 phosphorylation. WP1066 is commonly used in the research of malignant tumors (such as glioma, hepatocellular carcinoma, and breast cancer) and inflammation-related diseases.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 857064-38-1
Sample solution is provided at 25 µL, 10mM.
WP1066 is a reversible competitive inhibitor of STAT3 (Signal Transducer and Activator of Transcription 3), with an IC50 of approximately 2.5µM for the inhibition of STAT3 Tyr705 phosphorylation[1]. WP1066 is commonly used in the research of malignant tumors (such as glioma, hepatocellular carcinoma, and breast cancer) and inflammation-related diseases[2]. WP1066 specifically occupies the SH2 domain pocket of STAT3 through hydrogen bonds and hydrophobic interactions. Its binding can directly block the dimerization process of STAT3[3], thereby inhibiting its nuclear translocation and the transcriptional activation of downstream target genes. This ultimately suppresses tumor cell proliferation, induces tumor cell apoptosis, and reduces the release of inflammatory factors[4].
In vitro, pre-treatment of human oral squamous cell carcinoma Tca8113 and Tca8113/DDP cells with WP1066 (5µM) for 24 hours, followed by treatment with cisplatin (DDP, 0.1–16mg/ml) for 48 hours, significantly inhibits cell proliferation, migration, and invasion capabilities, while reducing STAT3 phosphorylation and miR-21 expression[5]. Treatment of STSW-01 and STSW-01-LUC cells with WP1066 (1.5–3.0µM) for 24 hours significantly decreases STAT3 phosphorylation levels and induces the expression of cell death markers, including necrosis-related protein pMLKL (Ser358) and apoptosis-related protein caspase 3/7[6].
In vivo, WP1066 (40mg/kg) is administered locally, three times per week, to treat a TSCCA xenograft nude mouse model. WP1066 significantly inhibits the increase in tumor volume, reduces tumor cell proliferation and invasion capabilities, and induces tumor cell apoptosis[7]. WP1066 (10–20mg/kg) is administered intraperitoneally, three times per week, to treat gp130757FF mice from 8 weeks of age until 10 weeks of age. WP1066 significantly reduces gastric tumor volume, decreases tumor cell proliferation, and increases tumor cell apoptosis[8].
References:
[1] Horiguchi A, Asano T, Kuroda K, et al. STAT3 inhibitor WP1066 as a novel therapeutic agent for renal cell carcinoma. Br J Cancer. 2010 May 25;102(11):1592-9.
[2] Yang J, Li N, Zhao X, et al. WP1066, a small molecule inhibitor of STAT3, chemosensitizes paclitaxel-resistant ovarian cancer cells to paclitaxel by simultaneously inhibiting the activity of STAT3 and the interaction of STAT3 with Stathmin. Biochem Pharmacol. 2024 Mar;221:116040.
[3] Tsurumaki H, Katano H, Sato K, et al. WP1066, a small molecule inhibitor of the JAK/STAT3 pathway, inhibits ceramide glucosyltransferase activity. Biochem Biophys Res Commun. 2017 Sep 16;491(2):265-270.
[4] Tsujita Y, Horiguchi A, Tasaki S, et al. STAT3 inhibition by WP1066 suppresses the growth and invasiveness of bladder cancer cells. Oncol Rep. 2017 Oct;38(4):2197-2204.
[5] Zhou X, Ren Y, Liu A, et al. WP1066 sensitizes oral squamous cell carcinoma cells to cisplatin by targeting STAT3/miR-21 axis. Sci Rep. 2014 Dec 17;4:7461.
[6] Allaf A, Victoria B, Rosario R, et al. WP1066 induces cell death in a schwannomatosis patient-derived schwannoma cell line. Cold Spring Harb Mol Case Stud. 2022 Jun 22;8(4):a006178.
[7] Zhou X, Ren Y, Liu A, et al. STAT3 inhibitor WP1066 attenuates miRNA-21 to suppress human oral squamous cell carcinoma growth in vitro and in vivo. Oncol Rep. 2014 May;31(5):2173-80.
[8] Judd LM, Menheniott TR, Ling H, et al. Inhibition of the JAK2/STAT3 pathway reduces gastric cancer growth in vitro and in vivo. PLoS One. 2014 May 7;9(5):e95993.
| Cell experiment [1]: | |
Cell lines | STSW-01 cells (human schwannoma cell line derived from a schwannomatosis patient) |
Preparation Method | STSW-01 cells were cultured in Schwann cell media (SCM) containing HEPES buffer and bicarbonate buffered basal medium with 5% FBS, penicillin/streptomycin, and a proprietary supplement mix. Cells were maintained at 37°C with 5% CO₂. Cells were treated with WP1066 at a concentration of 1.5–3.0µM for 24 hours. |
Reaction Conditions | 1.5–3.0µM; 24 hours |
Applications | WP1066 significantly reduced cell viability and STAT-3 phosphorylation in STSW-01 cells. WP1066 also induced expression of markers for both necroptosis (pMLKL) and caspase-dependent cell death (cleaved caspase 3/7) |
| Animal experiment [2]: | |
Animal models | Nude mice |
Preparation Method | Nude mice were subcutaneously implanted with TSCCA cells to establish a xenograft tumor model. When tumors reached approximately 10mm in length, mice were divided into three groups: control, DMSO-treated (local injection, once every 3 days for 21 days), and WP1066-treated (40mg/kg, local injection) |
Dosage form | 40mg/kg; local injection |
Applications | WP1066 treatment significantly reduced tumor volume compared to control and DMSO-treated groups. Histological analysis showed decreased microvessel density, chromatin staining, and increased apoptotic nuclei in WP1066-treated tumors. Expressions of STAT3, p-STAT3, Ki67, Bcl-2, and MMP-2 were downregulated, while PTEN, PDCD4, and TIMP-3 were upregulated in WP1066-treated tumors. |
References: | |
| Cas No. | 857064-38-1 | SDF | |
| Synonyms | STAT Inhibitor III | ||
| Chemical Name | (E)-3-(6-bromopyridin-2-yl)-2-cyano-N-[(1S)-1-phenylethyl]prop-2-enamide | ||
| Canonical SMILES | CC(C1=CC=CC=C1)NC(=O)C(=CC2=NC(=CC=C2)Br)C#N | ||
| Formula | C17H14BrN3O | M.Wt | 356.22 |
| Solubility | ≥ 17.8 mg/mL in DMSO, ≥ 24.6 mg/mL in EtOH with ultrasonic and warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8073 mL | 14.0363 mL | 28.0725 mL |
| 5 mM | 561.5 μL | 2.8073 mL | 5.6145 mL |
| 10 mM | 280.7 μL | 1.4036 mL | 2.8073 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)