1. Cell Cycle/DNA Damage Epigenetics Apoptosis
  2. Sirtuin Apoptosis
  3. JGB1741

JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research.

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JGB1741

JGB1741 Estructura química

No. CAS : 1256375-38-8

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE JGB1741

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Descripciòn

JGB1741 (ILS-JGB-1741) is a potent and specific SIRT1 activity inhibitor with an IC50 of ∼15 μM. JGB1741 is a weak SIRT2 and SIRT3 inhibitor with an all IC50>100 μM. JGB1741 increases the acetylated p53 levels leading to p53-mediated apoptosis with modulation of Bax/Bcl2 ratio, cytochrome c release and PARP cleavage. JGB1741 has the potential for breast cancer research[1].

IC50 & Target[1]

SIRT1

∼15 μM (IC50)

SIRT2

>100 μM (IC50)

SIRT3

>100 μM (IC50)

In Vitro

JGB1741 (ILS-JGB-1741; 1-10000 nM; 24 h) inhibits MDA-MB 231 cell proliferation[1].
JGB1741 (0.01-1 μM; 24 h) induces apoptosis of MDA-MB 231 cells[1].
JGB1741 (0.01-1 μM; 24 h) shows a cell cycle arrest at G1 phase with more and more cells entering into sub G0/G1 phase[1].
JGB1741 (0.01-1 μM; 24 h) shows an increase in the global acetylation of H3K9, p53 expression and acetylated p53K382 levels[1].

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

Cell Proliferation Assay[1]

Cell Line: K562, HepG2 and MDA-MB 231 cell lines
Concentration: 1, 10, 50, 100, 500, 1000, 10000 nM
Incubation Time: 24 hours
Result: Inhibited MDA-MB 231 cell proliferation more potently with an IC50 of 0.5 μM than K562 and HepG2 cell proliferation (IC50>1 μM).

Apoptosis Analysis[1]

Cell Line: MDA-MB 231 cells
Concentration: 0.01, 0.1, 0.5, 1 μM
Incubation Time:
Result: Showed an increase in the percent apoptotic cells in a dose-dependent fashion with ∼70% apoptosis at 1 μM concentration.

Cell Cycle Analysis[1]

Cell Line: MDA-MB 231 cells
Concentration: 0.01, 0.1, 0.5, 1 μM
Incubation Time:
Result: Showed a cell cycle arrest at G1 phase with more and more cells entering into sub G0/G1 phase, the apoptotic phase, in a dose-dependent fashion.

Western Blot Analysis[1]

Cell Line: MDA-MB 231 cells
Concentration: 0.01, 0.1, 0.5, 1 μM
Incubation Time:
Result: Caused a dose-dependent increase in the global acetylation of H3K9.
Showed an increase in both p53 expression and acetylated p53K382 levels.
Peso molecular

440.56

Fòrmula

C27H24N2O2S

No. CAS
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC1=C(C2=C(C=C1)C=CC=C2)/C=N/C3=C(C4=C(S3)CCCC4)C(NCC5=CC=CC=C5)=O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvente y solubilidad
In Vitro: 

DMSO : 5 mg/mL (11.35 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 2.2698 mL 11.3492 mL 22.6984 mL
5 mM 0.4540 mL 2.2698 mL 4.5397 mL
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 (protect from 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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Pureza y Documentación
Referencias

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 (protect from 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 2.2698 mL 11.3492 mL 22.6984 mL 56.7460 mL
5 mM 0.4540 mL 2.2698 mL 4.5397 mL 11.3492 mL
10 mM 0.2270 mL 1.1349 mL 2.2698 mL 5.6746 mL
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  • 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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Inquiry Information

Nombre del producto:
JGB1741
Cat. No.:
HY-111329
Cantidad:
MCE Japan Authorized Agent: