Synonym: 7-(3,5-Dimethyl-4-isoxazolyl)-8-(methyloxy)-1-[(1R)-1-(2-pyridinyl)ethyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one; I-BET151
CAS Number: 1300031-49-5
Empirical Formula (Hill Notation): C23H21N5O3
Molecular Weight: 415.44
Linear Formula: C23H21N5O3
Product Type: Chemical
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| assay |
≥98% (HPLC) |
| color |
white to beige |
| form |
powder |
| InChI |
1S/C23H21N5O3/c1-12-21(14(3)31-27-12)16-9-18-15(10-20(16)30-4)22-19(11-25-18)26-23(29)28(22)13(2)17-7-5-6-8-24-17/h5-11,13H,1-4H3,(H,26,29)/t13-/m1/s1 |
| InChI key |
VUVUVNZRUGEAHB-CYBMUJFWSA-N |
| originator |
GlaxoSmithKline |
| Quality Level |
100  |
| relevant disease(s) |
cancer |
| SMILES string |
[n]2(c3c([nH][c]2=O)cnc4c3cc(c(c4)c5c(n[o]c5C)C)OC)[C@H](C)c1ncccc1 |
| solubility |
DMSO: 20 mg/mL, clear |
| storage temp. |
2-8°C |
| Application: |
GSK1210151A or I-BET151 has been used to study its inhibitory effect on BET (bromodomain and extra terminal) recruitment to chromatin in treating MLL (mixed-lineage leukemia)-fusion leukemia. |
| Biochem/physiol Actions: |
GSK1210151A (I-BET151) is an inhibitor of the BET (bromodomain and extra terminal domain protein) family of acetyl-lysine recognizing, chromatin ′adaptor′ proteins. |
| Biochem/physiol Actions: |
GSK1210151A (I-BET151) is an inhibitor of the BET (bromodomain and extra terminal domain protein) family of acetyl-lysine recognizing, chromatin ′adaptor′ proteins. 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) showed good efficacy in 2 MLL animal models. |
| Other Notes: |
GSK1210151A has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the GSK1210151A probe summary  on the Chemical Probes Portal website. |
| Packaging: |
5, 25 mg in glass bottle |
| Symbol |
GHS06 |
| Signal word |
Danger |
| Hazard statements |
H301 |
| Precautionary statements |
P301 + P310 |
| Hazard Codes |
T |
| Risk Statements |
25 |
| Safety Statements |
45 |
| RIDADR |
UN 2811 6.1 / PGIII |
| WGK Germany |
WGK 3 |
| Flash Point(F) |
Not applicable |
| Flash Point(C) |
Not applicable |
| Purity |
≥98% (HPLC) |
| Storage Temp. |
2-8°C |
| UNSPSC |
12352200 |