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Inolitazone

Catalog No. T15581   CAS 223132-37-4
Synonyms: RS5444, Efatutazone, CS-7017

Inolitazone (RS5444) a high-affinity PPARγ agonist. Inolitazone exhibits IC50 for growth inhibition is ~0.8 nM in vitro.

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Inolitazone Chemical Structure
Inolitazone, CAS 223132-37-4
Pack Size Availability Price/USD Quantity
1 mg In stock $ 113.00
5 mg In stock $ 267.00
10 mg In stock $ 427.00
25 mg In stock $ 693.00
50 mg In stock $ 987.00
100 mg In stock $ 1,350.00
500 mg In stock $ 2,690.00
1 mL * 10 mM (in DMSO) In stock $ 338.00
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Purity: 99.58%
Purity: 98.00%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Inolitazone (RS5444) a high-affinity PPARγ agonist. Inolitazone exhibits IC50 for growth inhibition is ~0.8 nM in vitro.
In vitro Inolitazone (10 nM) inhibits the growth of DRO cells through a PPARγ-dependent mechanism[1]. Inolitazone upregulates the cell cycle kinase inhibitor, p21WAF1/CIP1. Inolitazone (10 nM) activates PPARγ:RXRα-dependent transcription utilizing a PPRE response element fused to a luciferase reporter gene (PPRE3-tk-luc). Inolitazone specifically activates PPARγ, but not PPARα or PPARδ. Inolitazone (10 nM) 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[2].
In vivo In athymic nude mice prior to DRO tumor cell implantation, Inolitazone inhibits tumor growth in a dose responsive fashion. 0.025% Inolitazone inhibits growth on day 32 by 94.4%. In the 0.0025% treatment group, tumor growth is inhibited by 62.3% while the 0.00025% dose demonstrated no growth inhibitory activity as compared to control. Inolitazone treated animals demonstrate tumor growth inhibition of 68.9% in DRO tumors and 48.3% in ARO tumors on day 35. Inolitazone plus Paclitaxel demonstrate additive antiproliferative activity in cell culture and minimal ATC tumor growth[1].
Synonyms RS5444, Efatutazone, CS-7017
Molecular Weight 502.58
Formula C27H26N4O4S
CAS No. 223132-37-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 55 mg/mL (109.43 mM)

TargetMolReferences and Literature

1. 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. 2. 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Transcription Factor-Targeted Compound Library Drug Repurposing Compound Library Anti-Cancer Compound Library Metabolism Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compound Library Clinical Compound Library

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Keywords

Inolitazone 223132-37-4 DNA Damage/DNA Repair Metabolism PPAR Peroxisome proliferator-activated receptors RS5444 RS 5444 Efatutazone RS-5444 CS 7017 CS-7017 Inhibitor inhibit CS7017 inhibitor

 

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