iBET-BD2

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Cat.No. 7458 - iBET-BD2 | C23H27FN2O4 | CAS No. 2474876-09-8
Description: Potent and selective pan-BD2 inhibitor; orally bioavailable
Alternative Names: GSK046
Chemical Name: 4-(Acetylamino)-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-[(1S)-1-phenylethoxy]benzamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (5)

Biological Activity for iBET-BD2

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.

Technical Data for iBET-BD2

M. Wt 414.48
Formula C23H27FN2O4
Storage Store at -20°C
Purity ≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for iBET-BD2

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 will 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

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References for iBET-BD2

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

Gilan et al (2020) Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science 368 387 PMID: 32193360

Preston et al (2020) Design and synthesis of a highly selective and in vivo-capable inhibitor of the second bromodomain of the bromodomain and extra terminal domain family of proteins. J.Med.Chem. 63 9070 PMID: 32691591


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Keywords: iBET-BD2, iBET-BD2 supplier, GSK046, GSK-046, GSK, 046, iBET, BD2, iBETBD2, pan-BD2, selective, inhibitors, inhibits, SGC, Bromodomains, 7458, Tocris Bioscience

Citations for iBET-BD2

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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