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PFI-1

Catalog No.: 17030704
Cas No.: 1403764-72-6
Purity : 98% 
17030704 - PFI-1 | CAS 1403764-72-6

Catalog number : 17030704

CAS number : 1403764-72-6

Molecular Formula : C16H17N3O4S 

Molecular Weight : 347.39 

Iupac Chemical Name : 2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide 

Smile : COC1=C(C=CC=C1)S(=O)(=O)NC=1C=C2CN(C(NC2=CC1)=O)C

InChiKey : TXZPMHLMPKIUGK-UHFFFAOYSA-N

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SynonymsPFI1; PFI 1; PFI-1 
Molecular FormulaC16H17N3O4S 
Molecular Weight347.39 
Appearanceoff-white solid 
Purity98% 
SolubilitySoluble in DMSO 
Storage3 years -20ºCpowder 
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. 
SmileCOC1=C(C=CC=C1)S(=O)(=O)NC=1C=C2CN(C(NC2=CC1)=O)C
InChiKeyTXZPMHLMPKIUGK-UHFFFAOYSA-N
InChiInChI=1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20)
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PFI-1 is a potent and highly selective protein interaction Inhibitor, which targets BET bromodomain. PFI-1 that efficiently blocks the interaction of BET BRDs with acetylated histone tails. Co-crystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2. PFI-1 has antiproliferative effects on leukaemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell cycle arrest, down-regulation of MYC expression as well as induction of apoptosis and induces differentiation of primary leukaemic blasts. 

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