1. Cell Cycle/DNA Damage Metabolic Enzyme/Protease Apoptosis
  2. HSP Apoptosis
  3. JG-231

JG-231 is an allosteric inhibitor of heat shock protein 70 (Hsp70). JG - 231 inhibits the binding of Hsp70 and BAG family proteins, including inhibition of Hsp70 and BAG1 with a Ki of 0.11 μM. JG-231 inhibits proliferation of tumor cells and induces apoptosis. JG-231 has antitumor activity.

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

JG-231 Chemical Structure

JG-231 Chemical Structure

CAS No. : 1627126-59-3

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Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 1 publication(s) in Google Scholar

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Description

JG-231 is an allosteric inhibitor of heat shock protein 70 (Hsp70). JG - 231 inhibits the binding of Hsp70 and BAG family proteins, including inhibition of Hsp70 and BAG1 with a Ki of 0.11 μM. JG-231 inhibits proliferation of tumor cells and induces apoptosis. JG-231 has antitumor activity[1][2].

IC50 & Target[2]

HSP70

 

Cellular Effect
Cell Line Type Value Description References
MCF7 IC50
0.12 μM
Compound: 42; JG-231
Antiproliferative activity against human MCF7 cells by MTT assay
Antiproliferative activity against human MCF7 cells by MTT assay
[PMID: 29953808]
MDA-MB-231 IC50
0.25 μM
Compound: 42; JG-231
Antiproliferative activity against human MDA-MB-231 cells by MTT assay
Antiproliferative activity against human MDA-MB-231 cells by MTT assay
[PMID: 29953808]
MEF IC50
2.5 μM
Compound: 42; JG-231
Antiproliferative activity against MEF cells by MTT assay
Antiproliferative activity against MEF cells by MTT assay
[PMID: 29953808]
In Vitro

JG-231 (0.31-5 μM; 4-10 days) inhibits cell ball growth in 3D cultured TT and MZ-CRC-1 cells in a dose- and time-dependent manner[1].
JG-231 (0-10 μM; 12-24 h) disrupts the interaction between Hsp70 and BAG3, affects the signaling pathway related to Hsp70, and induces cell apoptosis in MCF-7 cells[2].

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

Western Blot Analysis[2]

Cell Line: MCF-7
Concentration: 0.1, 0.5, 1, 5 and 10 μM
Incubation Time: 24 h
Result: Reduced the levels of Akt, c-Raf , CDK4, IAP-1 and HuR.
Did not change the levels of Hsp72 and Hsp90.
In Vivo

JG-231 (4 mg/kg; intraperitoneal injection; three times a week for 4 weeks) has an antitumor effect in a mouse model of breast cancer xenotransplantation[2].
Pharmacokinetic Analysis in Mice[1]

Route Dose (mg/kg) Cmax (nM) Tmax (h) t1/2 (h) AUC0-∞ (nM·h)
i.p. 5 159 2 21.6 3401

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

Animal Model: Four-week-old female athymic mice (Charles River) bearing xenografted MDA-MB-231 cells[2]
Dosage: 4 mg/kg
Administration: Intraperitoneal injection (i.p.); 3 days a week for 4 weeks
Result: Inhibited tumor growth.
Did not significantly change the weight of mice.
Molecular Weight

619.47

Formula

C22H18BrCl2N3OS4

CAS No.
Appearance

Solid

Color

Orange to reddish brown

SMILES

O=C1N(CC)/C(S/C1=C2SC3=CC(Cl)=CC=C3N/2C)=C/C4=[N+](CC5=CC=C(Br)S5)C=CS4.[Cl-]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 2 mg/mL (3.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6143 mL 8.0714 mL 16.1428 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6143 mL 8.0714 mL 16.1428 mL 40.3571 mL
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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.

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Product Name:
JG-231
Cat. No.:
HY-124611
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