OXF BD 02

Selective BRD4(1) inhibitor CAS# 1429129-68-9

OXF BD 02

2D Structure

Catalog No. BCC5598----Order now to get a substantial discount!

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OXF BD 02: 5mg $127 In Stock
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OXF BD 02

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Chemical Properties of OXF BD 02

Cas No. 1429129-68-9 SDF Download SDF
PubChem ID 56929801 Appearance Powder
Formula C18H17NO3 M.Wt 295.33
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 100 mM in DMSO and to 10 mM in ethanol with gentle warming
Chemical Name 3-(3,5-dimethyl-1,2-oxazol-4-yl)-5-[hydroxy(phenyl)methyl]phenol
SMILES CC1=C(C(=NO1)C)C2=CC(=CC(=C2)O)C(C3=CC=CC=C3)O
Standard InChIKey FEQUIPXIENTMJN-UHFFFAOYSA-N
Standard InChI InChI=1S/C18H17NO3/c1-11-17(12(2)22-19-11)14-8-15(10-16(20)9-14)18(21)13-6-4-3-5-7-13/h3-10,18,20-21H,1-2H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of OXF BD 02

DescriptionSelective inhibitor of the first bromodomain of BRD4 (BRD4(1)) (IC50 = 382 nM). Exhibits 2-3-fold selectivity for BRD4(1) over the CBP bromodomain and has little affinity for a range of other bromodomains. Reduces viability of lung adenocarcinoma cell lines and attenuates proliferation of MV-4-11 leukemia cells. Cell permeable.

OXF BD 02 Dilution Calculator

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OXF BD 02 Molarity Calculator

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Preparing Stock Solutions of OXF BD 02

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.386 mL 16.9302 mL 33.8604 mL 67.7209 mL 84.6511 mL
5 mM 0.6772 mL 3.386 mL 6.7721 mL 13.5442 mL 16.9302 mL
10 mM 0.3386 mL 1.693 mL 3.386 mL 6.7721 mL 8.4651 mL
50 mM 0.0677 mL 0.3386 mL 0.6772 mL 1.3544 mL 1.693 mL
100 mM 0.0339 mL 0.1693 mL 0.3386 mL 0.6772 mL 0.8465 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on OXF BD 02

Optimization of 3,5-dimethylisoxazole derivatives as potent bromodomain ligands.[Pubmed:23517011]

J Med Chem. 2013 Apr 25;56(8):3217-27.

The bromodomain protein module, which binds to acetylated lysine, is emerging as an important epigenetic therapeutic target. We report the structure-guided optimization of 3,5-dimethylisoxazole derivatives to develop potent inhibitors of the BET (bromodomain and extra terminal domain) bromodomain family with good ligand efficiency. X-ray crystal structures of the most potent compounds reveal key interactions required for high affinity at BRD4(1). Cellular studies demonstrate that the phenol and acetate derivatives of the lead compounds showed strong antiproliferative effects on MV4;11 acute myeloid leukemia cells, as shown for other BET bromodomain inhibitors and genetic BRD4 knockdown, whereas the reported compounds showed no general cytotoxicity in other cancer cell lines tested.

3,5-dimethylisoxazoles act as acetyl-lysine-mimetic bromodomain ligands.[Pubmed:21851057]

J Med Chem. 2011 Oct 13;54(19):6761-70.

Histone-lysine acetylation is a vital chromatin post-translational modification involved in the epigenetic regulation of gene transcription. Bromodomains bind acetylated lysines, acting as readers of the histone-acetylation code. Competitive inhibitors of this interaction have antiproliferative and anti-inflammatory properties. With 57 distinct bromodomains known, the discovery of subtype-selective inhibitors of the histone-bromodomain interaction is of great importance. We have identified the 3,5-dimethylisoxazole moiety as a novel acetyl-lysine bioisostere, which displaces acetylated histone-mimicking peptides from bromodomains. Using X-ray crystallographic analysis, we have determined the interactions responsible for the activity and selectivity of 4-substituted 3,5-dimethylisoxazoles against a selection of phylogenetically diverse bromodomains. By exploiting these interactions, we have developed compound 4d, which has IC(50) values of <5 muM for the bromodomain-containing proteins BRD2(1) and BRD4(1). These compounds are promising leads for the further development of selective probes for the bromodomain and extra C-terminal domain (BET) family and CREBBP bromodomains.

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