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
|Source||Cell Stem Cell (2015). Figure 2. GSK1210151A|
|Method||Efficiently Generating CiNs|
|Cell Lines||TUJ1-stained cells|
|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|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 80 mg/mL|
|Related Epigenetic Reader Domain Products|
GNE-064 is an orally administered brominated structural inhibitor of SMARCA2/4 and PBRM1 and is being developed as a tool compound.GNE-064 inhibits SMARCA4 with an IC50 value of 0.035 μM and also SMARCA2 with an EC50 value of 0.10 μM.
GSK232 is a highly selective inhibitor of cell permeation of non-BET CECR2 brominated structures with >500-fold selectivity for BET family brominated structures.
GSK852 is a very potent selective BET inhibitor of BD2 (pIC50 = 7.9).
The menin-MLL inhibitor M-1121 is a covalent protein-protein interaction inhibitor with oral activity that achieves complete and durable tumor regression.
Inobrodib (CCS1477) is an orally active, potent and selective p300/CBP inhibitor. inobrodib binds to p300 and CBP with Kd values of 1.3 and 1.7 nM and has a 170/130 fold selectivity compared to BRD4 with a Kd of 222 nM. ccs1477 acts by inhibiting CCS1477 acts by inhibiting the expression and function of androgen receptor (AR) and by inhibiting c-Myc.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.