PLX51107

DESCRIPTION

A BET family protein inhibitor; binds to BD1 in BRD2, BRD3, BRD4, and BRDT (Kds = 1.6, 2.1, 1.7, and 5 nM, respectively), as well as BD2 (Kds = 5.9, 6.2, 6.1, and 120 nM, respectively); binds to bromodomains of CBP and p300 (Kds = ~100 nM for both); inhibits CpG-induced proliferation of primary CLL cells from 0.1-10 µM; inhibits Ba/F3 cell-induced splenomegaly in mice from 0.5-10 mg/kg; reduces tumor volume and increases survival in YUMM3.3 and D4M3.A mouse syngeneic B-RAFV600E mutant melanoma models

DETAILS

Inchi: InChI=1S/C26H22N4O3/c1-15-24(17(3)33-29-15)20-12-23-25(28-13-20)21(18-7-9-19(10-8-18)26(31)32)14-30(23)16(2)22-6-4-5-11-27-22/h4-14,16H,1-3H3,(H,31,32)/t16-/m0/s1
Purity: ≥98%
Raptas: Product Type|Biochemicals|Small Molecule Inhibitors|Chromatin Reader Interactions||Research Area|Epigenetics, Transcription, & Translation|Readers|Bromodomains
Smiles: C[C@@H](C1=NC=CC=C1)N2C=C(C3=CC=C(C(O)=O)C=C3)C4=NC=C(C5=C(C)ON=C5C)C=C42
Inchikey: AMSUHYUVOVCWTP-INIZCTEOSA-N
Cas Number: 1627929-55-8
Formulation: A solid
Storage Temp: -20
Shipping Temp: -20
Formula Markup: C26H22N4O3
Formula Weight: 438.5
Shelf Life Days: 1460