HJC0416

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HJC0416 is a potent and orally active STAT3 inhibitor. HJC0416 shows antiprolifeative activity and induces apoptosis. HJC0416 decreases the expression of p-STAT3 (Tyr-705), Cyclin D1 and increases the expression of cleaved caspase-3 protein. HJC0416 shows anti-tumor activity.

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

HJC0416 Chemical Structure

CAS No. : 1617518-22-5

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Other Forms of HJC0416:

HJC0416 hydrochloride Get quote

1 Publications Citing Use of MCE HJC0416

•Cell Mol Gastroenterol Hepatol. 2024 Jun 5:101367. [Abstract]

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STAT3 STAT5 STAT6 STAT1

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

STAT3

Cellular Effect

Cell Line	Type	Value	Description	References
ASPC1	IC₅₀	0.04 μM Compound: 12, HJC0416	Antiproliferative activity against human AsPC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay Antiproliferative activity against human AsPC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay	[PMID: 24904966]
MCF7	IC₅₀	1.76 μM Compound: 12, HJC0416	Antiproliferative activity against ER-positive human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay Antiproliferative activity against ER-positive human MCF7 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay	[PMID: 24904966]
MDA-MB-231	IC₅₀	1.97 μM Compound: 12, HJC0416	Antiproliferative activity against ER-negative and triple-negative human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay Antiproliferative activity against ER-negative and triple-negative human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay	[PMID: 24904966]
PANC-1	IC₅₀	1.88 μM Compound: 12, HJC0416	Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay Antiproliferative activity against human PANC1 cells assessed as inhibition of cell proliferation after 72 hrs by MTS assay	[PMID: 24904966]

In Vitro

HJC0416 (0-10 µM; 48 h) shows antiprolifeative activity and induces apoptosis in MDA-MB-231 cells^[1].
HJC0416 (0-10 µM; 12 h) decreases the expression of p-STAT3 (Tyr-705), Cyclin D1 and increases the expression of cleaved caspase-3 protein^[1].

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

Cell Proliferation Assay^[1]

Cell Line:	MCF-7, MDA-MB-231, AsPC1, Panc-1 cells
Concentration:	0-100 µM
Incubation Time:	72 h
Result:	Showed antiproliferative activity with IC₅₀s 1.76, 1.97, 0.04, 1.88 µM for MCF-7, MDA-MB-231, AsPC1, Panc-1 cells, respectively.

Apoptosis Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	1, 5, 10 µM
Incubation Time:	48 h
Result:	Induced cell apoptosis.

Western Blot Analysis^[1]

Cell Line:	MDA-MB-231 cells
Concentration:	0, 1, 5, 10 µM
Incubation Time:	12 h
Result:	Suppressed the expression of phosphorylated STAT3 at Tyr-705, Cyclin D1, increased the expression of cleaved caspase-3.

In Vivo

HJC0416 (10 mg/kg for i.p.; 100 mg/kg for p.o.; daily for 7 days) reduces the tumor growth with no significant body weight loss in mice^[1].

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

Animal Model:	6 weeks, female nude mice (MDA-MB-231 cells)^[1]
Dosage:	10 mg/kg for i.p.; 100 mg/kg for p.o.
Administration:	I.p. or p.o.; daily for 7 days
Result:	Decreased the tumor volume for 67% as compared to the control mice for i.p.; the growth of xenograft tumors in mice was also significantly reduced at a dose of 100 mg/kg by 46%.

Molecular Weight

392.86

Formula

C₁₈H₁₇ClN₂O₄S

CAS No.

1617518-22-5

SMILES

O=C(NC1=CC=C(C=CS2(=O)=O)C2=C1)C3=CC(Cl)=CC=C3OCCCN

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]. Chen H, et al. Discovery of potent anticancer agent HJC0416, an orally bioavailable small molecule inhibitor of signal transducer and activator of transcription 3 (STAT3). Eur J Med Chem. 2014 Jul 23;82:195-203. [Content Brief]

HJC0416 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HJC04161617518-22-5HJC 0416HJC-0416STATApoptosisantiprolifeativeantitumororally activeapoptosisMDA-MB-231 cellsp-STAT3 (Tyr-705)Cyclin D1cleaved caspase-3Inhibitorinhibitorinhibit

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