I-BRD9
- Product Name
- I-BRD9
- CAS No.
- 1714146-59-4
- Chemical Name
- I-BRD9
- Synonyms
- I-BRD9;GSK602;CS-2328;I-BRD9;I-BRD-9;I-brd9 GSK602;N-(1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)-5-ethyl-4-oxo-7-(3-(trifluoromethyl)phenyl)-4,5-di;N-(1,1-Dioxidotetrahydro-2H-thiopyran-4-yl)-5-ethyl-4-oxo-7-(3-(trifluoromethyl)phenyl)-4,5-dihydrothieno[3,2-c]pyridine-2-carboximidamide;5-Ethyl-4,5-dihydro-4-oxo-N-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-7-[3-(trifluoromethyl)phenyl]thieno[3,2-c]pyridine-2-carboximidamide;Thieno[3,2-c]pyridine-2-carboximidamide, 5-ethyl-4,5-dihydro-4-oxo-N-(tetrahydro-1,1-dioxido-2H-thiopyran-4-yl)-7-[3-(trifluoromethyl)phenyl]-
- CBNumber
- CB83122929
- Molecular Formula
- C22H22F3N3O3S2
- Formula Weight
- 497.55
- MOL File
- 1714146-59-4.mol
I-BRD9 Property
- Boiling point:
- 683.9±65.0 °C(Predicted)
- Density
- 1.50±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- crystalline solid
- pka
- 9.35±0.40(Predicted)
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- 17749
- Product name
- I-BRD9
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $73
- Updated
- 2024/03/01
- Product number
- 17749
- Product name
- I-BRD9
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $144
- Updated
- 2024/03/01
- Product number
- 17749
- Product name
- I-BRD9
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $231
- Updated
- 2024/03/01
- Product number
- 17749
- Product name
- I-BRD9
- Purity
- ≥98%
- Packaging
- 50mg
- Price
- $967
- Updated
- 2024/03/01
- Product number
- 5591
- Product name
- I-BRD9
- Purity
- ≥98%(HPLC)
- Packaging
- 10
- Price
- $225
- Updated
- 2021/12/16
I-BRD9 Chemical Properties,Usage,Production
Description
I-BRD9 is a selective cellular chemical probe for bromodomain-containing protein 9 (BRD9). I-BRD9 has a pIC50 value of 7.3 for BRD9 inhibitor, with greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 is also shows a greater than 70-fold selectivity against a panel of 34 bromodomains. I-BRD9 downregulates CLEC1, DUSP6, FES and SAMSN1 genes in Kasumi-1 cells.
Uses
I-BRD9 is a bromodomain-containing protein 9 (BRD9) inhibitor which belong to class of (BET) inhibitors that have shown potent anti-inflammatory and anticancer properties.
Biological Activity
pic50: 7.3i-brd9 is a brd9 inhibitor.brd9 is identified as a bromodomain containing protein forming a small sub-branch of the bromodomain family tree. human brd9 has a single bromodomain and contains five isoforms which are produced by alternative splicing.
in vitro
in previous study, the i-brd9 development was driven by iterative medicinal chemistry, using structure based design to result in nanomolar potency at brd9, over 700-fold selectivity against the bet family as well as more than 70-fold to a panel of 34 bromodomains. in kasumi-1 cells, i-brd9 could downregulate dusp6, clec1, samsn1 and fes genes. moreover, i-brd9 was used to expore genes regulated by brd9 in kasumi-1 cells involved in immune response and oncology pathways. in addition, when brd4 was used as a representative member of the bet family for initial selectivity screening, i-brd9 was found to have a pic50 of 5.3 against this protein. i-brd9 thus represented the first available selective tool compound to investigate the cellular phenotype of the inhibition of brd9 bromodomain [1].
storage
Store at -20°C
References
[1] theodoulou nh et al. discovery of i-brd9, a selective cell active chemical probe for bromodomain containing protein 9 inhibition. j med chem. 2016 feb 25;59(4):1425-39.
I-BRD9 Preparation Products And Raw materials
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