Submit a Review & Earn an Amazon Gift Card
You can now submit reviews for your favorite Tocris products. Your review will help other researchers decide on the best products for their research. Why not submit a review today?!
Submit ReviewiBET-BD2
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)
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.
Compound Libraries for iBET-BD2
iBET-BD2 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.
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.
| 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 |
Molarity Calculator
Molarity Calculator
Calculate the mass, volume, or concentration required for a solution.
Reconstitution Calculator
Reconstitution Calculator
Dilution Calculator
Dilution Calculator
Calculate the dilution required to prepare a stock solution.
Product Datasheets for iBET-BD2
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
If you know of a relevant reference for iBET-BD2, please let us know.
View Related Products by Target
View Related Products by Product Action
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
Citations are publications that use Tocris products.
Currently there are no citations for iBET-BD2. Do you know of a great paper that uses iBET-BD2 from Tocris? Please let us know.
Reviews for iBET-BD2
There are currently no reviews for this product. Be the first to review iBET-BD2 and earn rewards!
Have you used iBET-BD2?
Submit a review and receive an Amazon gift card.
$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image
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!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Stem Cell Research Product Guide
This product guide provides a background to the use of small molecules in stem cell research and lists over 200 products for use in:
- Self-renewal and Maintenance
- Differentiation
- Reprogramming
- Organoid Generation
- GMP and Ancillary Material Grade Products
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer Poster
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.