iBET-BD2

Tocris Bioscience | Catalog # 7458

Potent and selective pan-BD2 inhibitor; orally bioavailable
Tocris Bioscience

Key Product Details

Description

Potent and selective pan-BD2 inhibitor; orally bioavailable

Alternative Names

GSK046
View all Bromodomain Inhibitors »

Product Description

iBET-BD2 is a potent and selective pan-BD2 inhibitor (IC50 values are 49, 98, 214 and 264 nM for BRD4BD2, BRD3BD2, BRDTBD2 and BRD2BD2, respectively). iBET-BD2 is selective for BD2 over BD1 (IC50 values are 10965, 36317, 70558, and >50119 µM for BRD2BD1, BRD3BD1, BRD4BD1, and BRDTBD1, respectively) in a time-resolved FRET (TR-FRET) assay. iBET-BD2 (1 μM) inhibits IFN-γ-induced protein expression of MHC class I in K562 cells. iBET-BD2 reduces the production of anti-KLH IgM antibodies in mice immunized with keyhole limpet hemocyanin (KLH). iBET-BD2 exhibits immunomodulatory activity. iBET-BD2 is orally bioavailable.

Licensing Information

This probe is supplied in conjunction with the Structural Genomics Consortium. For further characterization details, please visit the iBET-BD2 probe summary on the SGC website.

Product Specifications for iBET-BD2

Molecular Weight

414.48

Formula

C23H27FN2O4

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

4-(Acetylamino)-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-[(1S)-1-phenylethoxy]benzamide

CAS Number

2474876-09-8

PubChem ID

146018690

InChI Key

FRBRZGLUFOZRGD-JVPBZIDWSA-N

SMILES

C[C@@H](C1=CC=CC=C1)OC2=C(C(F)=CC(C(N[C@H]3CC[C@@H](CC3)O)=O)=C2)NC(C)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.45 100
Ethanol 41.45 100

Preparing Stock Solutions for iBET-BD2

The following data is based on the product molecular weight 414.48.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.41 mL 12.06 mL 24.13 mL
5 mM 0.48 mL 2.41 mL 4.83 mL
10 mM 0.24 mL 1.21 mL 2.41 mL
50 mM 0.05 mL 0.24 mL 0.48 mL

Calculators

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Background References

References are publications that support the biological activity of the product.

Product Documents for iBET-BD2

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for iBET-BD2

For research use only

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