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Fig. 1 · Structure
Cat. No.
A11783
CAS No.
1300031-49-5
Formula
C23H21N5O3
Mol. Weight
415.4

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GSK 1210151A (I-BET151)

Cat. No. A11783 CAS 1300031-49-5

BET Bromodomain Inhibitor

Also available in: DFICBY Astrocyte-to-Neuron Reprogramming Kit

GSK1210151A is a novel selective inhibitor of the bromodomain and extra terminal (BET) family proteins BRD2, BRD3, and BRD4.

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Publications for GSK 1210151A

1 publication citing this product

  1. Momeny M, .et al. , Anticancer Drugs, 2018, Nov;29(10):1011-1020 PMID: 30096128
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Biological Activity

Target & Activity

Target Activity Value
BRD3 (Cell-free assay) 0.25 μM
BRD2 (Cell-free assay) 0.5 μM
BRD4 (Cell-free assay) 0.79 μM

Cellular Effect

Cell Line Activity Value Description Reference
HL-60 IC50 195 nM Antiproliferative activity against human HL-60 cells after 72 hrs by cell titer glo assay [PMID: 32691589]
HT-29 IC50 0.945 μM Growth inhibition of human HT-29 cells after 72 hrs by SRB assay [PMID: 25559428]
K562 IC50 > 2000 nM Cytotoxicity against human K562 cells harboring BCR-ABL fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay [PMID: 26080064]
MM1.S IC50 0.299 μM Growth inhibition of human MM1S cells after 72 hrs by SRB assay [PMID: 25559428]
MOLM-13 IC50 228 nM Cytotoxicity against human MOLM13 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay [PMID: 26080064]
MOLM-13 IC50 228 nM Growth inhibition of human MOLM13 cells after 4 days by WST-8 assay [PMID: 28463487]
MV4-11 IC50 0.119 μM Growth inhibition of human MV4-11 cells after 72 hrs by SRB assay [PMID: 25559428]
MV4-11 IC50 126.9 nM Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer glo assay [PMID: 32691589]
MV4-11 IC50 162 nM Cytotoxicity against human MV4-11 cells harboring MLL1 fusion gene assessed as growth inhibition after 4 days by CellTiter-Glo luminescent assay [PMID: 26080064]
MV4-11 IC50 162 nM Growth inhibition of human MV4-11 cells after 4 days by WST-8 assay [PMID: 28463487]
Raji IC50 0.13 μM Inhibition of BRD4 in human Raji cells assessed as reduction of MYC expression after 4 hrs [PMID: 24900758]
THP-1 IC50 134.2 nM Antiproliferative activity against human THP-1 cells after 72 hrs by cell titer glo assay [PMID: 32691589]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1300031-49-5
Applications BET Bromodomain Inhibitor
Formula C23H21N5O3
Molecular Weight 415.4
Synonyms I-BET151
SMILES
CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)[C@H](C)C5=CC=CC=N5)OC

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO >100 mg/mL (240.71 mM)
Water Insoluble
Ethanol 83 mg/mL

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Publications

1 publication citing this product

  1. Momeny M, .et al. , Anticancer Drugs, 2018, Nov;29(10):1011-1020 PMID: 30096128

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