I-BET151 | 2220

A BET bromodomain inhibitor that interacts with BRD4 and BRD3 BET proteins and displaces them from chromatin; displays highefficacy against human and murine MLL-fusion leukemic cell lines, through the induction of early cell cycle arrest and apoptosis. The mode of action is, at least in part, due to suppressing the transcription of key genes (BCL2, C-MYC and CDK6) that are critical for MLL-fusion leukemia maintenance.

I-BET151 is a BET bromodomain inhibitor that interacts with BRD4 and BRD3 BET proteins and displaces them from chromatin; displays highefficacy against human and murine MLL-fusion leukemic cell lines, through the induction of early cell cycle arrest and apoptosis.

2220 | I-BET151 DataSheet

Alternate Name/Synonyms: GSK1210151A

Appearance: Beige to pale yellow solid

Formulation: N/A

CAS Number: 1300031-49-5

Structure Available?: Yes

Peptide sequence: N/A

Salt Form: No

Molecular Formula: C₂₃H₂₁N₅O₃

Molecular Weight: 415.44

Cell-Permeable?: Yes

Purity: ≥98% by HPLC (≥99.5% optical purity)

Solubilities: DMSO (100 mM) or Ethanol (100 mM)

Handling: Protect from light and moisture

Country of Origin: USA

Tag Line: A BET bromodomain inhibitor

MDL Number: MFCD22124472

PubChem CID: 52912189

SMILES: CC1=C(C(=NO1)C)C2=C(C=C3C(=C2)N=CC4=C3N(C(=O)N4)C(C)C5=CC=CC=N5)OC

InChi: 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