Inolitazone
Based on 5 publication(s) in Google Scholar
Inolitazone a novel high-affinity PPARγ agonist that is dependent upon PPARγ for its biological activity with IC50 of 0.8 nM for growth inhibition.
For research use only. We do not sell to patients.
- CAS No.: 223132-37-4
- Formula: C27H26N4O4S
- Molecular Weight:502.58
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Inolitazone
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Biological Activity
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PPARγ |
Inolitazone (RS5444) upregulates the cell cycle kinase inhibitor, p21 WAF1/CIP1. Silencing p21 WAF1/CIP1 rendered cells insensitive to Inolitazone. A 10 nM dose of Inolitazone activates PPARγ:RXRα-dependent transcription as demonstrated in a transient transfection assay utilizing a PPRE response element fused to a luciferase reporter gene (PPRE3-tk-luc). DRO cells are treated in culture with Inolitazone, Rosiglitazone, or Troglitazone at the indicated concentrations. DRO cells are transiently transfected with PPRE3-tk-luc to examine effective concentrations at which EC50 occurs. The EC50s are 1 nM (Inolitazone), 65 nM (Rosiglitazone) and 631 nM (Troglitazone). Similarly, the calculated inhibitory concentration at IC50 is 0.8 nM for Inolitazone, 75 nM for Rosiglitazone, and 1412 nM for Troglitazone. Inolitazone specifically activates PPARγ, but not PPARα or PPARδ. Exposure of 10 nM Inolitazone following transient transfection with the appropriate PPAR isoform (γ, α, or δ) and PPAR response element linked to a luciferase reporter in RIE rat small intestinal cell line, which does not express PPARs, yields increased luciferase activity only in the presence of PPARγ and PPRE3-tk-luc[1]. DRO cells are growth inhibited by 10 nM Inolitazone (RS5444) through a PPARγ-dependent mechanism[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 223132-37-4
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Molecular Weight 502.58
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Formula C27H26N4O4S
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SMILES
O=C(N1)SC(CC2=CC=C(OCC3=NC4=CC=C(OC5=CC(C)=C(N)C(C)=C5)C=C4N3C)C=C2)C1=O
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Synonyms
Efatutazone; CS-7017; RS5444
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (5)
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Journal Impact Factor
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Most Recent
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Int J Oncol
2018 Jun;52(6):1991-2000. PMID: 29620161 -
Front Microbiol
Troglitazone Impedes the Oligomerization of Sodium Taurocholate Cotransporting Polypeptide and Entry of Hepatitis B Virus Into Hepatocytes. [Abstract]2019 Jan 8:9:3257. PMID: 30671048 -
Cancer Med
Efatutazone and T0901317 exert synergistically therapeutic effects in acquired gefitinib-resistant lung adenocarcinoma cells. [Abstract]2018 May;7(5):1955-1966. PMID: 29573196
Inolitazone purchased from MedChemExpress. Usage Cited in: Cancer Med. 2018 May;7(5):1955-1966. [Abstract]
Protein expression in cells incubated with 40 μM Efatutazone for 12, 24, and 48 h.
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Exp Cell Res
PPARγ agonist efatutazone and gefitinib synergistically inhibit the proliferation of EGFR-TKI-resistant lung adenocarcinoma cells via the PPARγ/PTEN/Akt pathway. [Abstract]2017 Dec 15;361(2):246-256. PMID: 29080795
Inolitazone purchased from MedChemExpress. Usage Cited in: Exp Cell Res. 2017 Dec 15;361(2):246-256. [Abstract]
Western blot analysis for p21, p-p21, Cyclin D1. Bcl-2, Caspase 3, Cleaved Caspase 3, Caspase 9, Cleaved Caspase 9 and Bax in HCC827-GR and PC-9-GR cells treated with control, Efatutazone alone, Gefitinib alone, or Efatutazone combined with gefitinib for 48 h.
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Protocol
DRO90-1 (DRO) and ARO81 (ARO) cells are plated in 12-well culture plates in triplicate for each condition at an initial concentration of 2×104 cells/well. After overnight incubation, cells are treated with either Inolitazone, Rosiglitazone, Troglitazone, GW9662, or Paclitaxel diluted in DMSO at concentrations indicated in figure legends. All cells receive identical volumes of DMSO and are exposed to each drug for 6 days with medium and drug changed every 48 h. After 6 days, cells are washed with PBS, trypsinized and counted by Beckman Coulter Counter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Suspensions of 1×106/0.1 mL DRO or ARO cells in RPMI medium are injected subcutaneously in one flank of 3-4 week athymic female nude mice. Mice are changed to specialized diets either 1 week prior or 1 week after tumor implantation and randomly assigned to experimental or control groups with 10 mice per group. Diets consisted either placebo, 0.00025%, 0.0025%, or 0.025% Inolitazone formulated into the diet. Mice weighed between 20-25 g and consume on average 4 g of food per day. For combinatorial studies either placebo, 10 mg/kg or 15 mg/kg paclitaxel is injected i.p. twice weekly. Tumors are measured every 3-4 days for 35 days with calipers and tumor volumes are calculated by the formula: 0.5236(a×b×c), where a is the shortest diameter, b is the diameter perpendicular to a and c is the diameter height.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
References
[1]. Copland JA, et al. Novel high-affinity PPARgamma agonist alone and in combination with paclitaxel inhibits human anaplastic thyroid carcinoma tumor growth via p21WAF1/CIP1. Oncogene. 2006 Apr 13;25(16):2304-17. [Content Brief]
[2]. Marlow LA, et al. Reactivation of suppressed RhoB is a critical step for the inhibition of anaplastic thyroid cancer growth. Cancer Res. 2009 Feb 15;69(4):1536-44. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)