I-BRD9 |
| Catalog No.GC12588 |
BRD9 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1714146-59-4
Sample solution is provided at 25 µL, 10mM.
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pIC50: 7.3
I-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].
In vivo: So far, there is no animal in vivo data reported for I-BRD9.
Clinical trial: Up to now, I-BRD9 is still in the preclinical development stage.
Reference:
[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.
| Cas No. | 1714146-59-4 | SDF | |
| Chemical Name | 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 | ||
| Canonical SMILES | N=C(C(S1)=CC2=C1C(C3=CC=CC(C(F)(F)F)=C3)=CN(CC)C2=O)NC(CC4)CCS4(=O)=O | ||
| Formula | C22H22F3N3O3S2 | M.Wt | 497.55 |
| Solubility | DMF: 30 mg/mL,DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL,DMSO: 25 mg/mL | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0098 mL | 10.0492 mL | 20.0985 mL |
| 5 mM | 0.402 mL | 2.0098 mL | 4.0197 mL |
| 10 mM | 0.201 mL | 1.0049 mL | 2.0098 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 38 reference(s) in Google Scholar.)
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