iBET-BD2
Tocris Bioscience, part of Bio-Techne | Catalog # 7458
Potent and selective pan-BD2 inhibitor; orally bioavailable
Key Product Details
Description
Potent and selective pan-BD2 inhibitor; orally bioavailable
Alternative Names
GSK046
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
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Preston 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. 2020 PMID: 32691591
- Gilan Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation. Science 2020 PMID: 32193360
Product Specific Notices for iBET-BD2
For research use only
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