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Cat. No.: HY-189287

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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.

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화학식: C₁₆H₁₈N₂O₄
분자량:302.33

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

STAT3 antagonist-1 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

STAT3

All STAT Isoforms :

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 Viability Assay^[1]

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.

Western Blot Analysis^[1]

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 Autophagy Assay^[1]

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.

Related Protocols :

Chemical Information

분자량 302.33
화학식 C₁₆H₁₈N₂O₄
SMILES

OC1=C(OC)C=CC(/C=N/NC2=CC=C(OC)C(OC)=C2)=C1
선적

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Yang HY, et al. Discovery of hydrazone derivatives as novel STAT3 antagonists against pancreatic and colorectal cancers. Bioorganic chemistry. 2026 Oct 05;181:110293.

Calculators

몰농도 계산기

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Mass Mass

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Molecular Weight Molecular Weight

농도 희석 계산기

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Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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