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JH530 is an effective methuosis inducer that inhibits the triple-negative breast cancer (TNBC) cells proliferation by causing intracellular complete vacuolization. JH530 has anti-tumor activity and can be used for cancer research.

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JH530 Chemical Structure

JH530 Chemical Structure

CAS No. : 2928616-74-2

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Description

JH530 is an effective methuosis inducer that inhibits the triple-negative breast cancer (TNBC) cells proliferation by causing intracellular complete vacuolization. JH530 has anti-tumor activity and can be used for cancer research[1].

IC50 & Target

Methuosis[1]

In Vitro

JH530 (compound 5c) (1 μM or 2 μM; 24 hours) causes notable cellular morphological changes in HCC1806 cells, characterized by the accumulation of intracellular vacuoles, and scarcely affected the morphology of 184B5 cells and cell viability[1].
JH530 (0.5, 1.0, 1.5μM; 24 hours) causes cell death by methuosis[1].
JH530 (1 μM; 24 hours) effectively suppresses the proliferation of TNBC cells invitro[1].
JH530 (1.5 μM; 24 hours) causes the increase of Rab7 and Lamp1 expression in HCC1806 and MDA-MB-468[1].

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

Cell Proliferation Assay[1]

Cell Line: HCC1806, HCC1937, MDA-MB-468 cells
Concentration: 1 μM
Incubation Time: 24 hours
Result: Expressed remarkable anti-proliferative activities invitro, with the IC50s were 0.70 μM, 0.92 μM, and 1.03 μM for three TNBC cells HCC1806, MDA-MB-468, and HCC1937, respectively.

Cell Viability Assay[1]

Cell Line: HCC1806, 184B5
Concentration: 1 μM or 2 μM
Incubation Time: 24 hours
Result: Exhibited notable cellular morphological changes at 1 μM, characterized by the accumulation of intracellular vacuoles in HCC1806 cells.
Scarcely affected the morphology of 184B5 cells and cell viability.

Western Blot Analysis[1]

Cell Line: HCC1806; MDA-MB-468
Concentration: 0, 0.5, 1.0, 1.5 μM
Incubation Time: 24 hours
Result: Dose-dependently induced the increase of Rab7 and Lamp1 expression, and causes cell death by methuosis.

Immunofluorescence[1]

Cell Line: HCC1806, HCC1937, MDA-MB-468 cells
Concentration: 1.5 μM
Incubation Time: 24 hours
Result: Induced the increase of Rab7 and Lamp1 expression in HCC1806 and MDA-MB-468.
Induced the accumulation of vacuoles in most of the cell.
In Vivo

JH530 (compound 5c ) (2.5 mg/kg or 5.0 mg/kg; i.p.; once every 2 days for two week) elicites tumor regression and well tolerated with treatment doses without causing a noticeable weight decrease[1].

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

Animal Model: HCC1806 cell xenograft mouse model [1]
Dosage: 2.5 mg/kg, 5.0 mg/kg
Administration: Intraperitoneal injection (i.p.); once every 2 days
Result: Inhibits HCC1806 tumor weight at 2.5 mg/kg significantly, while exhibit more apparent tumor suppressive effects at 5 mg/kg[1].
Molecular Weight

530.44

Formula

C22H24BrN7O2S

CAS No.
SMILES

O=C(C1=CC=CC(Br)=N1)NC2=C(OC)C=C(NC3=NC(N4CCNCC4)=NC=C3SC)C=C2

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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
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    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.

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JH530
Cat. No.:
HY-149847
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