JY-2
Based on 2 publication(s) in Google Scholar
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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- Purity: 99.75%
- CAS No.: 339103-05-8
- 화학식: C13H7Cl2N3O
- 분자량:292.12
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) JY-2
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Biological Activity
22 μM (FoxO1 transcriptional activity)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
1.7 μM
Compound: 7f
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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
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[PMID: 23046966] |
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.
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Cell Line:HepG2 and INS-1 cells
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Concentration:10, 50 and 100 μM
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Incubation Time:24 h
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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).
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Cell Line:HepG2 cells
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Concentration:10, 50 and 100 μM
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Incubation Time:4 h; in the presence of PA (500μM)
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Result:Increased p-FoxO1 levels in the whole cell lysate with a concurrent reduction in nuclear FoxO1 levels.
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.
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Animal Model:C57BL/6J mice[1]
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Dosage:50, 100, 200 mg/kg
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Administration:Oral, three times for two days (9:00 AM, 7:00 PM, 9:00 AM on the next day)
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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.
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Animal Model:db/db mice and C57BL/6J mice, high fat-diet-induced obese diabetic (DIO) model[1]
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Dosage:50, 100 mg/kg
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Administration:Oral, once daily for 4 weeks
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Result:Decreased the levels of fasting blood glucose, improved glucose tolerance. The expression of ColIV, a fibrosis marker, was also lowered.
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Animal Model:C57BL/6J mice[1]
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Dosage:20 mg/kg or 50 mg/kg
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Administration:IV or PO (Pharmacokinetic Analysis)
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Result:Showed an overall good pharmacokinetic profile.
Chemical Information
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CAS No. 339103-05-8
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Appearance Solid
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분자량 292.12
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화학식 C13H7Cl2N3O
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Color White to off-white
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SMILES
ClC1=CC(Cl)=C(C2=NC(C3=CC=CC=N3)=NO2)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Cell Death Dis
CRLF1 bridges AKT and mTORC2 through SIN1 to inhibit pyroptosis and enhance chemo-resistance in ovarian cancer. [Abstract]2024 Sep 10;15(9):662. PMID: 39256356 -
Int J Chron Obstruct Pulmon Dis
Azithromycin Mitigates Tobacco Smoke-Induced Lung Senescence by Modulating the FOXO3A/CCND1 Signaling Pathway. [Abstract]2025 Nov 11:20:3631-3645. PMID: 41244262
용액&용해도
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. 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 |