PFI-3|PFI3|bromodomain inhibitor

Cas No.:	1819363-80-8
Chemical Name:	(E)-1-(2-Hydroxyphenyl)-3-((1R,4R)-5-(pyridin-2-yl)-2,5-diazabicyclo[2.2.1]heptan-2-yl)prop-2-en-1-one
Synonyms:	PFI3, PFI 3
SMILES:	C1[C@@H]2CN([C@H]1CN2C3=CC=CC=N3)/C=C/C(=O)C4=CC=CC=C4O
Formula:	C₁₉H₁₉N₃O₂
M.Wt:	321.37
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

PFI-3 is a selective, potent and cell-permeable SMARCA2/4 bromodomain inhibitor with a Kd of 89 nM.

In Vitro:

PFI-3 is a potent, cell-permeable probe capable of displacing ectopically expressed, GFP-tagged SMARCA2-bromodomain from chromatin. PFI-3 binds avidly to both SMARCA2 and SMARCA4 bromodomains (BROMOScan Kd's between 55 and 110 nM) consistent with the binding constant (Kd=89 nM) measured by isothermal titration calorimetry. PFI-3 does not phenocopy the growth inhibitory effects of SMARCA2 knockdown in lung cancer[1]. Exposure of embryonic stem cells to PFI-3 leads to deprivation of stemness and deregulates lineage specification. Furthermore, differentiation of trophoblast stem cells in the presence of PFI-3 is markedly enhanced[2]. PFI-3 binds to certain family VIII bromodomains while displaying significant, broader bromodomain family selectivity. The high specificity of PFI-3 for family VIII is achieved through a novel bromodomain binding mode of a phenolic headgroup that leads to the unusual displacement of water molecules that are generally retained by most other bromodomain inhibitors reported to date[3].

Cat. No.	Product name	Field of application
DC70466	GSK549	GSK549 (GSK-549) is a potent, highly selective, BD2 domain-selective BET inhibitor with pIC50 of 7.8 (BRD4 BD2), 1150-fold selectivity over BD1.
DC11261	ZL0420	ZL0420 is a potent, highly selective BRD4 inhibitor with IC50 of 27 and 32 nM for BRD4-BD1 and BRD4-BD2, respectively.
DC8261	(-)-JQ-1	The (-)-JQ1 stereoisomer has no appreciable affinity to BET bromodomains，it is the negative control of +JQ-1.
DC8320	RVX-208	RVX-208(RVX 000222) is a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo; is a BET bromodomain antagonist.
DC10786	PLX51107	PLX51107 is a novel BET inhibitor with a unique binding mode in the acetylated lysine binding pocket of BRD4 that differentiates it from other compounds under investigation.
DC8291	PFI-4	PFI-4 is a potent and selective BRPF1 bromodomain inhibitor (IC50 = 80 nM).
DC7649	PFI-3	PFI-3 is a novel potent, selective and cell permeable inhibitor of SMARCA4 and PB1(5) bromodomains with IC50 ~ 89 nM and 48 nM respectively.
DC9305	PF-CBP1(PF-06670910) hydrochloride	PF-CBP1 is potent and highly-selective inhibitor of the bromodomain of CREB binding protein (CBP BRD) that down regulates targets of CBP in macrophages primary neurons.
DC7850	OF-1	OF-1 is a potent inhibitor of BRPF1B and BRPF2 bromodomain with Kd of 100 nM and 500 nM, respectively.
DC9758	NI-57	NI-57 is a potent inhibitor of the bromodomains of BRPF proteins that binds to BRPF1B, BRPF2, and BRPF3 with Kd values of 31, 108, and 408 nM, respectively, as determined by isothermal titration calorimetry.