AdipoGen Life Sciences

PFI-4

Product Code:
 
SYN-3047
Product Group:
 
Inhibitors and Activators
Regulatory Status:
 
RUO
Storage:
 
+4°C
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Chemical Structure
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Chemical Structure

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Further Information

Alternate Names/Synonyms:
N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxy benzamide
Appearance:
Solid.
CAS:
900305-37-5
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C21H24N4O3/c1-23-17-12-15(22-20(26)14-8-4-5-9-19(14)28-3)16(25-10-6-7-11-25)13-18(17)24(2)21(23)27/h4-5,8-9,12-13H,6-7,10-11H2,1-3H3,(H,22,26)
InChiKey:
QCIJLRJBZDBVDB-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 900305-37-5. Formula: C21H24N4O3. MW: 380.5. Potent and selective BRPF1 bromodomain inhibitor, with an IC50 of 80nM. PFI-4 exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. PFI-4 specifically binds to the bromodomain of BRPF1 (Kd = 13nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21). PFI-4 is potent in cells, with an IC50 value of 250nM.
Molecular Formula:
C21H24N4O3
Molecular Weight:
380.5
Package Type:
Plastic Vial
Product Description:
Potent and selective BRPF1 bromodomain inhibitor, with an IC50 of 80nM. PFI-4 exhibits >100-fold selectivity for BRPF1 over a panel of other bromodomains including BRPF2 (BRD1), BRPF3 and BRD4. PFI-4 specifically binds to the bromodomain of BRPF1 (Kd = 13nM), inhibiting binding to tri-acetylated histone 4 (residues 1-21). PFI-4 is potent in cells, with an IC50 value of 250nM.
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.

References

1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain: E.H. Demont, et al.; ACS Med. Chem. Lett. 5, 1190 (2014)