GSK1210151A (I-BET151) is a novel BET bromodomain inhibitor which blocks recruitment of BET to chromatin. GSK1210151A exhibits potent selectivity over an extensive range of diverse protein types such as COX-2, P450, Aurora B, GSK3β, PI3K-γ, GPCR, ion channels and transporters. GSK1210151A displaces BRD3 and BRD4, PAFc and SEC components from chromatin resulting in inhibition of transcription at key genes (BCL2, C-MYC and CDK6) involved in the initiation of mixed lineage leukemia (MLL). GSK1210151A (I-BET151) induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro with IC50 values of 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively. GSK1210151A reduces BCL2 expression in NOMO1 cells. In vivo, GSK1210151A (I-BET151) improves survival and shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine.
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
GSK1210151A purchased from AbMole
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Source | Cell Stem Cell (2015). Figure 2. GSK1210151A |
| Method | Efficiently Generating CiNs | |
| Cell Lines | TUJ1-stained cells | |
| Concentrations | 100 μm | |
| Incubation Time | 14 days | |
| Results | We found that an additional small molecule, I-BET151, dramatically enhanced the reprogramming rate (with a 90% TUJ1-positive cell yield) and neurite outgrowth of the iNs |
| Molecular Weight | 415.44 |
| Formula | C23H21N5O3 |
| CAS Number | 1300031-49-5 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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