2. Metabolic Enzyme/Protease
  3. FOXO
  4. JY-2

JY-2 is a moderately selective and orally active Forkhead transcription factor forkhead box O1 (FoxO1) inhibitor that inhibits FoxO1 transcriptional activity with an IC50 of 22 μM. JY-2 shows moderate inhibition against FoxO3a and FoxO4. JY-2 shows anti-diabetic activity.

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JY-2

JY-2 Chemical Structure

CAS No. : 339103-05-8

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10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

JY-2 Related Antibodies

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Description

JY-2 is a moderately selective and orally active Forkhead transcription factor forkhead box O1 (FoxO1) inhibitor that inhibits FoxO1 transcriptional activity with an IC50 of 22 μM. JY-2 shows moderate inhibition against FoxO3a and FoxO4. JY-2 shows anti-diabetic activity[1].

IC50 & Target

22 μM (FoxO1 transcriptional activity)[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
1.7 3
Compound: 7f
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
[PMID: 23046966]
HEK293 IC50
1.7 3
Compound: 7f
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
[PMID: 23046966]
HEK293 IC50
1.7 3
Compound: 7f
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
Negative allosteric modulation of human recombinant mGluR5 expressed in HEK293 cells expressing GLAST assessed as inhibition of DHPG-induced intracellular Ca2+ level after 30 mins by FLIPR assay
[PMID: 23046966]
In Vitro

JY-2 (10-100 μM; 24 h) reduces palmitic acid (PA; HY-N0830)-induced lipotoxicity in HepG2 and INS-1 cells[1].

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

JY-2 Related Antibodies

Real Time qPCR[1]

Cell Line: HepG2 and INS-1 cells
Concentration: 10, 50 and 100 μM
Incubation Time: 24 h
Result: Reduced palmitic acid (PA)-induced G6Pase and PEPCK mRNA expression. Inhibited PA-induced lipid accumulation. Reduced PA-induced mRNA expression of ER stress markers (ATF3, CHOP and GRP78).

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 10, 50 and 100 μM
Incubation Time: 4 h; in the presence of PA (500μM)
Result: Increased p-FoxO1 levels in the whole cell lysate with a concurrent reduction in nuclear FoxO1 levels.
In Vivo

JY-2 (50-200 mg/kg; oral; 3 times for two days or daily for 4 weeks) shows anti-diabetic effects in mice[1].
Pharmacokinetic parameters of JY-2[1]

Parameters i.v. (20 mg/kg) p.o. (50 mg/kg)
AUCall (ng·h/mL) 5017 ± 1038 12270 ± 2775
AUCinf.obs (ng·h/mL) 5030 ± 1037 12400 ± 2753
Cmax (ng/mL) 10790 ± 3269 6826 ± 2342
Tmax (h) 0.1 ± 0.1 0.8 ± 0.7
T1/2 (h) 0.8 ± 0.2 1.3 ± 0.4
MRTinf.obs (h) 0.7 ± 0.1 2.0 ± 0.1
F (%) 97.8

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

Animal Model: C57BL/6J mice[1]
Dosage: 50, 100, 200 mg/kg
Administration: Oral, three times for two days (9:00 AM, 7:00 PM, 9:00 AM on the next day)
Result: Improved glucose tolerance. Significantly reduced the expression of G6Pase and PEPCK mRNA in the liver. Enhanced mRNA expression of insulin and PDX-1 in the pancreas.
Animal Model: db/db mice and C57BL/6J mice, high fat-diet-induced obese diabetic (DIO) model[1]
Dosage: 50, 100 mg/kg
Administration: Oral, once daily for 4 weeks
Result: Decreased the levels of fasting blood glucose, improved glucose tolerance. The expression of ColIV, a fibrosis marker, was also lowered.
Animal Model: C57BL/6J mice[1]
Dosage: 20 mg/kg or 50 mg/kg
Administration: IV or PO (Pharmacokinetic Analysis)
Result: Showed an overall good pharmacokinetic profile.
Masse moléculaire

292.12

Formule

C13H7Cl2N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC(Cl)=C(C2=NC(C3=CC=CC=N3)=NO2)C=C1
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (342.33 mM; ultrasonic and warming and heat to 60°C; 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 3.4233 mL 17.1163 mL 34.2325 mL
5 mM 0.6847 mL 3.4233 mL 6.8465 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. 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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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Working solution concentration: mg/mL
Pureté et documentation

Purity: 99.75%

SDS (393 KB)

COA (250 KB) HNMR (247 KB) LCMS (94 KB)

Instruction de manipulation (2659 KB)
Références

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. 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 3.4233 mL 17.1163 mL 34.2325 mL 85.5813 mL
5 mM 0.6847 mL 3.4233 mL 6.8465 mL 17.1163 mL
10 mM 0.3423 mL 1.7116 mL 3.4233 mL 8.5581 mL
15 mM 0.2282 mL 1.1411 mL 2.2822 mL 5.7054 mL
20 mM 0.1712 mL 0.8558 mL 1.7116 mL 4.2791 mL
25 mM 0.1369 mL 0.6847 mL 1.3693 mL 3.4233 mL
30 mM 0.1141 mL 0.5705 mL 1.1411 mL 2.8527 mL
40 mM 0.0856 mL 0.4279 mL 0.8558 mL 2.1395 mL
50 mM 0.0685 mL 0.3423 mL 0.6847 mL 1.7116 mL
60 mM 0.0571 mL 0.2853 mL 0.5705 mL 1.4264 mL
80 mM 0.0428 mL 0.2140 mL 0.4279 mL 1.0698 mL
100 mM 0.0342 mL 0.1712 mL 0.3423 mL 0.8558 mL
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JY-2 Related Classifications

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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.

Keywords:

JY-2339103-05-8JY2JY 2FOXOForkhead box OlipotoxicityHepG2INS-1ColIVG6PasePEPCKATF3CHOPGRP78Inhibitorinhibitorinhibit

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