STAT3 antagonist-1
STAT3 antagonist-1 is a selective STAT3 antagonist. STAT3 antagonist-1 induces Autophagy-associated cell death. STAT3 antagonist-1 inhibits cancer stemness and epithelial-mesenchymal transition. STAT3 antagonist-1 can be used for research on pancreatic cancer and colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C16H18N2O4
- Molecular Weight:302.33
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
STAT3 |
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| MIA PaCa-2 | GI50 |
34.4 μM
|
Growth inhibition against human MIA PaCa-2 pancreatic ductal adenocarcinoma cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Growth inhibition against human MIA PaCa-2 pancreatic ductal adenocarcinoma cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
|
42551351 |
| MIA PaCa-2 | GI50 |
8.2 μM
|
Growth inhibition against human MIA PaCa-2 pancreatic ductal adenocarcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Growth inhibition against human MIA PaCa-2 pancreatic ductal adenocarcinoma cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
42551351 |
| MIA PaCa-2 | GI50 |
0.85 μM
|
Growth inhibition against human MIA PaCa-2 pancreatic ductal adenocarcinoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Growth inhibition against human MIA PaCa-2 pancreatic ductal adenocarcinoma cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
42551351 |
| HCT-116 | GI50 |
51.5 μM
|
Growth inhibition against human HCT 116 colorectal cancer cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
Growth inhibition against human HCT 116 colorectal cancer cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay.
|
42551351 |
| HCT-116 | GI50 |
20.5 μM
|
Growth inhibition against human HCT 116 colorectal cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Growth inhibition against human HCT 116 colorectal cancer cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
|
42551351 |
| HCT-116 | GI50 |
4.4 μM
|
Growth inhibition against human HCT 116 colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
Growth inhibition against human HCT 116 colorectal cancer cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay.
|
42551351 |
In Vitro
STAT3 antagonist-1 (Compound P42) (10-50 μM) selectively targets the STAT3 SH2 domain over the DNA-binding domain, as demonstrated by potent inhibition in the STAT3127-688:phosphopeptide FP assay (85% at 10 μM) with a selectivity ratio of 5.00[1].
STAT3 antagonist-1 (24-72 h) exhibits potent growth inhibition in KRAS-mutant MIA PaCa-2 (GI50 ~0.85 μM at 72 h) and HCT 116 (GI50 ~4.4 μM at 72 h) cancer cell lines[1].
STAT3 antagonist-1 (10 μM; 72 h) exhibits selective cytotoxicity toward cancer cell lines at 10 μM, with the highest growth inhibition in MIA PaCa-2 (75%), DLD-1 (77%), and HCT 116 (62%), and minimal effect on non-cancerous MC3T3-E1 cells[1].
STAT3 antagonist-1 (0.1-10 μM; 24-48 h) inhibits STAT3 phosphorylation in MIA PaCa-2 and HCT 116 cells without affecting the total protein levels of upstream kinases JAK2 and SRC[1].
STAT3 antagonist-1 (0.3-30 μM; 24-48 h) induces autophagy-associated cell death in MIA PaCa-2 and HCT 116 cells[1].
STAT3 antagonist-1 (0.3-30 μM; 24-48 h) activates autophagy in MIA PaCa-2 and HCT 116 cells, characterized by increased LC3II/I ratios and decreased p62 levels[1].
STAT3 antagonist-1 (0.3-30 μM) abrogates cancer stemness potential in MIA PaCa-2 and HCT 116 cells by inhibiting colony formation[1].
STAT3 antagonist-1 (0.3-3 μM) down-regulates EMT/stemness markers SNAIL and ZEB1 in MIA PaCa-2 and HCT 116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:MIA PaCa-2, AsPC-1, DLD-1, HCT 116, and MC3T3-E1
-
Concentration:10 μM
-
Incubation Time:72 h
-
Result:Showed 75% growth inhibition in MIA PaCa-2, 62% in HCT 116, 77% in DLD-1, and 22% in AsPC-1.
In non-cancerous MC3T3-E1 cells, GI values were estimated to be >100 μM at 24 h, >100 μM at 48 h, and 30-100 μM at 72 h.
-
Cell Line:MIA PaCa-2 and HCT 116
-
Concentration:0.1, 1, and 10 μM
-
Incubation Time:24 h (MIA PaCa-2); 48 h (HCT 116)
-
Result:In MIA PaCa-2 cells, down-regulated p-STAT3 activity without affecting JAK2 and SRC.
Significantly abrogated p-STAT3 at as low as 1 μM.
Inhibited total STAT3 significantly at 10 μM.
In HCT 116 cells, inhibited STAT3 phosphorylation without affecting JAK2 and SRC.
-
Cell Line:MIA PaCa-2 and HCT 116
-
Concentration:0.3, 3, and 30 μM (MIA PaCa-2); 0.3 and 3 μM (HCT 116)
-
Incubation Time:24 h (MIA PaCa-2); 48 h (HCT 116)
-
Result:Induced significant autophagy at 0.3-30 μM in MIA PaCa-2 cells after 24 h.
Induced consistent autophagy at 0.3 and 3 μM in HCT 116 cells after 48 h.
Chemical Information
-
Molecular Weight 302.33
-
Formula C16H18N2O4
-
SMILES
OC1=C(OC)C=CC(/C=N/NC2=CC=C(OC)C(OC)=C2)=C1
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
STAT3 antagonist-1 Related Classifications
HY-189287 Related Classifications
Powered by Bioz