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  3. JH530

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.

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

JH530

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]

Cellular Effect
Cell Line Type Value Description References
HCC1806 IC50
0.7 μM
Compound: 5c; JH530
Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell proliferation incubated for 24 hrs by SRB assay
Antiproliferative activity against human HCC1806 cells assessed as inhibition of cell proliferation incubated for 24 hrs by SRB assay
[PMID: 37212861]
HCC1937 IC50
1.03 μM
Compound: 5c; JH530
Antiproliferative activity against human HCC1937 cells assessed as inhibition of cell proliferation incubated for 24 hrs by SRB assay
Antiproliferative activity against human HCC1937 cells assessed as inhibition of cell proliferation incubated for 24 hrs by SRB assay
[PMID: 37212861]
MDA-MB-468 IC50
0.92 μM
Compound: 5c; JH530
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 24 hrs by SRB assay
Antiproliferative activity against human MDA-MB-468 cells assessed as inhibition of cell proliferation incubated for 24 hrs by SRB assay
[PMID: 37212861]
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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JH530
Cat. No.:
HY-149847
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