PFI 4

Modify Date: 2024-01-08 20:33:22

PFI 4 Structure
PFI 4 structure
Common Name PFI 4
CAS Number 900305-37-5 Molecular Weight 380.440
Density 1.3±0.1 g/cm3 Boiling Point 512.1±50.0 °C at 760 mmHg
Molecular Formula C21H24N4O3 Melting Point N/A
MSDS Chinese USA Flash Point 263.5±30.1 °C

 Use of PFI 4


PFI-4 is a potent and selective and cell permeable BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. IC50 value: 80 nMTarget: BRPF1in vitro: Disrupts BRPF1 binding to histone H3.3. PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 with a Kd =13 nM as determined by ITC. It reduces recovery time in triple BRD cell construct in FRAP, inhibiting binding to tri-acetylated histone 4 (residues 1-21). It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 μM) and is selective for BRPF1 over BRPF2 and BRPF3. PFI-4 is potent in cells, with an IC50 value of 250 nM.

 Names

Name pfi-4
Synonym More Synonyms

 PFI 4 Biological Activity

Description PFI-4 is a potent and selective and cell permeable BRPF1 bromodomain inhibitor (IC50 = 80 nM). Exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. IC50 value: 80 nMTarget: BRPF1in vitro: Disrupts BRPF1 binding to histone H3.3. PFI-4 is a chemical probe that specifically binds to the bromodomain of BRPF1 with a Kd =13 nM as determined by ITC. It reduces recovery time in triple BRD cell construct in FRAP, inhibiting binding to tri-acetylated histone 4 (residues 1-21). It has much lower affinity for bromodomain 1 of BRD4 (Kd = >50 μM) and is selective for BRPF1 over BRPF2 and BRPF3. PFI-4 is potent in cells, with an IC50 value of 250 nM.
Related Catalog
References

[1]. Demont EH, et al. 1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain. (2014) ACS Med Chem Lett. 5(11):1190-1195.

 Chemical & Physical Properties

Density 1.3±0.1 g/cm3
Boiling Point 512.1±50.0 °C at 760 mmHg
Molecular Formula C21H24N4O3
Molecular Weight 380.440
Flash Point 263.5±30.1 °C
Exact Mass 380.184845
LogP 1.79
Vapour Pressure 0.0±1.3 mmHg at 25°C
Index of Refraction 1.649
Storage condition -20℃

 Safety Information

RIDADR NONH for all modes of transport

 Synonyms

Benzamide, N-[2,3-dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxy-
N-[1,3-Dimethyl-2-oxo-6-(1-pyrrolidinyl)-2,3-dihydro-1H-benzimidazol-5-yl]-2-methoxybenzamide
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