GSK1210151A

SIGMA/SML0666 - ≥98% (HPLC)

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

Catalog Number	PKG Qty.	Price


45-SML0666-5MG	5 mg	$171.00 1/EA	Add To Favorites
45-SML0666-25MG	25 mg	$683.00 1/EA	Add To Favorites

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Properties
Descriptions
Safety Info.
Basic Data

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

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