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Darbufelone

Catalog No. T10960   CAS 139226-28-1
Synonyms: CI-1004

Darbufelone (CI-1004) is a non-competitive dual inhibitor of PGF2α and LTB4. Dabfilon effectively inhibits PGHS-2 with a Ki of 10 μM and IC50s of 0.19 μM and 20 μM for PGHS-2 and PGHS-1.

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Darbufelone Chemical Structure
Darbufelone, CAS 139226-28-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 62.00
5 mg In stock $ 133.00
10 mg In stock $ 223.00
25 mg In stock $ 490.00
50 mg In stock $ 715.00
100 mg In stock $ 987.00
500 mg In stock $ 1,980.00
1 mL * 10 mM (in DMSO) In stock $ 188.00
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Purity: 99.77%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Darbufelone (CI-1004) is a non-competitive dual inhibitor of PGF2α and LTB4. Dabfilon effectively inhibits PGHS-2 with a Ki of 10 μM and IC50s of 0.19 μM and 20 μM for PGHS-2 and PGHS-1.
Targets&IC50 PGHS1:20 μM , PGHS2:0.19 μM
In vitro Darbufelone (5 - 60 μM) increases the cell growth inhibitory effects in A549, H520 and H460 cell lines with IC50s of 20, 21 and 15 μM[2].
In vivo Darbufelone (80 mg/kg/day) decreases the tumor volumes in a time-dependent manner. Darbufelone (20 or 40 mg/kg/day) dos not show any significant inhibition of tumor weight. At necropsy, Darbufelone (80 mg/kg/day) reduces the tumor weight by 30.2%[2].
Synonyms CI-1004
Molecular Weight 332.46
Formula C18H24N2O2S
CAS No. 139226-28-1

Storage

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

Solubility Information

DMSO: 45 mg/mL (135.35 mM)

TargetMolReferences and Literature

1. Johnson AR, et al. Slow-binding inhibition of human prostaglandin endoperoxide synthase-2 with darbufelone, an isoform-selective antiinflammatory di-tert-butyl phenol. Biochemistry. 2001 Jun 26;40(25):7736-45. 2. Ye X, et al. Darbufelone, a novel anti-inflammatory drug, induces growth inhibition of lung cancer cells both in vitro and in vivo. Cancer Chemother Pharmacol. 2010 Jul;66(2):277-85.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library GPCR Compound Library Bioactive Compounds Library Max ReFRAME Related Library Bioactive Compound Library

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Keywords

Darbufelone 139226-28-1 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor LTR CI1004 CI-1004 CI 1004 inhibitor inhibit

 

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