[CAS NO. 1300031-52-0] GSK1324726A (I-BET726)
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PRODUCTS SPECIFICATIONS [1300031-52-0]
Store
Catalog
SLK-S7620
Brand
Selleck
CAS
1300031-52-0
DESCRIPTION [1300031-52-0]
Overview
| MDL | MFCD28144683 |
|---|---|
| Molecular Weight | 434.91 |
| Molecular Formula | C25H23ClN2O3 |
| SMILES | O=C(O)C1=CC=C(C2=CC3=C(N(C(C)=O)[C@@H](C)C[C@H]3NC4=CC=C(Cl)C=C4)C=C2)C=C1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2993 mL | 11.4966 mL | 22.9933 mL |
| 5 mM | 0.4599 mL | 2.2993 mL | 4.5987 mL |
| 10 mM | 0.2299 mL | 1.1497 mL | 2.2993 mL |
| 50 mM | 0.0460 mL | 0.2299 mL | 0.4599 mL |
Description
GSK1324726A (I-BET726) is a highly selective inhibitor of family proteins with of 41 nM, 31 nM, and 22 nM for BRD2, BRD3, and BRD4, respectively.
In vitro
In neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN.
In vivo
In the mouse SK–N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. In a mouse septic shock model, GSK1324726A (10 mg/kg i.v.) shows potent anti-inflammatory effects, and prevents death of diseased animals.
References
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