Cat. No.: HY-189636

Antiproliferative agent-83

Antiproliferative agent-83 is an orally active STAT3 inhibitor (K_d = 5.63 μM) with antiproliferative activity against Huh-7 cells (IC₅₀ = 1.30 μM). Antiproliferative agent-83 inhibits dual phosphorylation of STAT3 at tyrosine and serine residues, blocking nuclear translocation and downstream transcriptional activation. Antiproliferative agent-83 induces apoptosis, ROS accumulation, and mitochondrial depolarization. Antiproliferative agent-83 suppresses tumor growth in a hepatocellular carcinoma xenograft mouse model. Antiproliferative agent-83 can be used for research on hepatocellular carcinoma.

For research use only. We do not sell to patients.

Formula: C₃₂H₃₀N₄O₅S
Molecular Weight:582.67

Storage:

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

Antiproliferative agent-83 Chemical Structure

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

STAT3

5.63 μM (Kd)

Caspase 3

Bax

Bcl-2

All STAT Isoforms :

All Caspase Isoforms :

All Bcl-2 Family Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Huh-7	IC50	1.30 μM	Antiproliferative activity against human Huh-7 cells assessed as viability reduction after 48 hrs incubation by MTT assay. Antiproliferative activity against human Huh-7 cells assessed as viability reduction after 48 hrs incubation by MTT assay.	42673832
HepG2	IC50	0.45 μM	Antiproliferative activity against human HepG2 cells assessed as viability reduction after 48 hrs incubation by MTT assay. Antiproliferative activity against human HepG2 cells assessed as viability reduction after 48 hrs incubation by MTT assay.	42673832
HCT-116	IC50	1.50 μM	Antiproliferative activity against human HCT116 cells assessed as viability reduction after 48 hrs incubation by MTT assay. Antiproliferative activity against human HCT116 cells assessed as viability reduction after 48 hrs incubation by MTT assay.	42673832
MCF7	IC50	0.93 μM	Antiproliferative activity against human MCF-7 cells assessed as viability reduction after 48 hrs incubation by MTT assay. Antiproliferative activity against human MCF-7 cells assessed as viability reduction after 48 hrs incubation by MTT assay.	42673832
MDA-MB-231	IC50	3.39 μM	Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction after 48 hrs incubation by MTT assay. Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction after 48 hrs incubation by MTT assay.	42673832
HK-2	IC50	2.01 μM	Antiproliferative activity against human HK-2 cells assessed as viability reduction after 48 hrs incubation by MTT assay. Antiproliferative activity against human HK-2 cells assessed as viability reduction after 48 hrs incubation by MTT assay.	42673832
AML12	IC50	4.51 μM	Antiproliferative activity against mouse AML12 cells assessed as viability reduction after 48 hrs incubation by MTT assay. Antiproliferative activity against mouse AML12 cells assessed as viability reduction after 48 hrs incubation by MTT assay.	42673832

In Vitro

Anti-cancerOthersApoptosisMitochondrial FunctionOxidative Stress

Anti-cancer

Antiproliferative agent-83 (compound 18) exhibits potent antiproliferative activity in Huh-7, HepG2, HCT116, MCF-7, MDA-MB-231, HK-2, and AML12 cells, with an IC₅₀ of 1.30 μM against Huh-7^[1].
Antiproliferative agent-83 (0.5-2 μM; 48 h, followed by 10-14 days of culture) inhibits colony formation in Huh-7 cells^[1].
Antiproliferative agent-83 (2-4 μM; 24-72 h) reduces wound healing in Huh-7 cells^[1].

Others

Antiproliferative agent-83 (0.3125-10 μM; 60 s) directly binds STAT3 in SPR with a K_D of 5.63 μM^[1].
Antiproliferative agent-83 (0.5-2 μM; 24 h) selectively inhibits dual phosphorylation of STAT3 at Tyr705 and Ser727 in Huh-7 and HepG2 cells, without affecting total STAT3 or STAT1/STAT5 phosphorylation^[1].
Antiproliferative agent-83 (2 μM; 24 h; heating at 40-60 °C for 3 min) binds to STAT3 in Huh-7 cells, producing thermal stabilization over the 40-60 °C range^[1].
Antiproliferative agent-83 (1 μM; 6 h) blocks IL-6-induced nuclear translocation of p-STAT3 (Tyr705) in Huh-7 cells^[1].

Anti-cancer

Apoptosis

Antiproliferative agent-83 (4 μM; 24 h; alone at 2 μM or in combination with 5 mM NAC (HY-B0215); 24 h) induces apoptosis in Huh-7 cells, and this apoptosis can be reversed by NAC^[1].
Antiproliferative agent-83 (2 μM; 24 h) upregulates cleaved caspase-3 and Bax and downregulates Bcl-2 in Huh-7 cells^[1].

Mitochondrial Function

Antiproliferative agent-83 (0.5-4 μM; 24 h) inhibits ATP production in Huh-7 cells with an IC₅₀ of 1.55 μM^[1].

Oxidative Stress

Antiproliferative agent-83 (0.25-1 μM; 24 h; 0.5 μM combined with 5 mM NAC; 24 h) increases ROS in Huh-7 cells, and this increase can be reversed by NAC^[1].
Antiproliferative agent-83 (0.5-2 μM; 24 h) induces mitochondrial depolarization^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

Huh-7 cells
Concentration:

0.5, 1, 2 μM
Incubation Time:

48 h; 10-14 days culture
Result:

Suppressed colony formation in a dose-dependent manner.

Cell Migration Assay ^[1]

Cell Line:

Huh-7 cells
Concentration:

2, 4 μM
Incubation Time:

0, 24, 48, 72 h
Result:

Reduced wound healing in Huh-7 cells.

Apoptosis Analysis^[1]

Cell Line:

Huh-7 cells
Concentration:

1, 2, 4 μM
2 μM alone or with 5 mM NAC (HY-B0215)
Incubation Time:

24 h
Result:

Triggered a prominent increase in apoptotic Huh-7 cells, with apoptotic cells reaching 53.6% at 4 μM.
Produced an apoptotic rate of 32.1% in the NAC rescue experiment, which decreased to 10.23% upon co-incubation with 5 mM NAC; control was 6.05%.

Western Blot Analysis^[1]

Cell Line:

Huh-7 and HepG2 cells
Concentration:

0.5, 1, 2 μM (Huh-7 and HepG2)
2 μM alone or with 5 mM NAC (Huh-7 NAC rescue)
Incubation Time:

24 h
Result:

Exerted prominent inhibitory effects on dual STAT3 phosphorylation at Tyr705 and Ser727 in both Huh‑7 and HepG2 cells, while producing no obvious effect on total STAT3 expression.
Showed negligible impacts on STAT1, p-STAT1 (Tyr701), STAT5, and p-STAT5 (Tyr694).
NAC did not restore compound 18-mediated downregulation of p-STAT3 (Ser727).

Immunofluorescence^[1]

Cell Line:

Huh-7 cells
Concentration:

1 μM
IL-6 50 ng/mL
Incubation Time:

6 h (preincubation)
30 min (IL-6 stimulation)
Result:

Displayed intense nuclear fluorescence of p-STAT3 (Tyr705); this nuclear translocation was markedly suppressed in cells.

Western Blot Analysis^[1]

Cell Line:

Huh-7 cells
Concentration:

0.5, 1, 2 μM
Incubation Time:

24 h
Result:

Upregulated cleaved caspase-3 and Bax and downregulates Bcl-2 in Huh-7 cells.

Parmacokinetics

Species	Dose	Route	T_1/2	AUC_0-t	AUC_0-∞	C_max	T_max
Rat^[1]	5 mg/kg	i.p.	10.32 h	3632.93 ng·h/mL	4370.79 ng·h/mL	406.91 ng/mL	0.87 h
Rat^[1]	5 mg/kg	p.o.	6.11 h	686.89 ng·h/mL	699.80 ng·h/mL	190.24 ng/mL	0.76 h

In Vivo

Anti-cancer

Antiproliferative agent-83 (compound 18) (5-7.5 mg/kg; intraperitoneal injection; once every 3 days; for 13 days) inhibited the growth of Huh-7 xenograft tumors in nude mice, with a tumor inhibition rate of 55.08%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

BALB/c-nude (male, 5-6 weeks, 18-20 g, injected with Huh-7 cells (3 × 10⁶ cells/mouse))^[1]
Dosage:

5 mg/kg; 7.5 mg/kg
Administration:

intraperitoneal injection; every 3 days; for 13 days
Result:

In the Huh-7 xenograft nude mouse model, Antiproliferative agent-83 produced tumor inhibition rate (TIR) values of 54.43% at 5 mg/kg and 55.08% at 7.5 mg/kg.
Only a minimal difference in TIR was observed between the two doses of Antiproliferative agent-83.

Related Protocols :

Chemical Information

Molecular Weight 582.67
Formula C₃₂H₃₀N₄O₅S
SMILES

O=C(C)C1=NC(C(N2CCC3(CCN(C(C4=CC5=C(C=CC=C5)S4(=O)=O)=O)CC3)CC2)=O)=CC6=C1NC7=C6C=CC=C7
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

Handling Instructions (2659 KB)

References

[1]. Jian Z, et al. Discovery of β-carboline derivatives as potent STAT3 dual phosphorylation inhibitor for hepatocellular carcinoma treatment. European journal of medicinal chemistry. 2026 Aug 27;319:119276.

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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.

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Antiproliferative agent-83

All STAT Isoforms

All Caspase Isoforms

All Bcl-2 Family Isoforms