| CAS NO: | 900305-37-5 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 380.44 |
|---|---|
| Formula | C21H24N4O3 |
| CAS No. | 900305-37-5 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 17 mg/mL (44.7 mM) |
| Water: <1 mg/mL | |
| Ethanol: 5 mg/mL (13.1 mM) | |
| Other info | Chemical Name: N-[2,3-Dihydro-1,3-dimethyl-2-oxo-6-(1-pyrrolidinyl)-1H-benzimidazol-5-yl]-2-methoxybenzamide InChi Key: QCIJLRJBZDBVDB-UHFFFAOYSA-N InChi Code: 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) SMILES Code: O=C(NC1=C(N2CCCC2)C=C(N3C)C(N(C)C3=O)=C1)C4=CC=CC=C4OC |
| Synonyms | PFI 4; PFI4; PFI-4. |
| In Vitro | In vitro activity: PFI-4 is cell permeable, and acts by displacing the BRPF1 bromodomain from Histone H3.3. Kinase Assay: 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. Cell Assay: 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. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5 |
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