| Identification | Back Directory | [Name]
4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione | [CAS]
310460-39-0 | [Synonyms]
CPYPP
4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
3,5-Pyrazolidinedione, 4-[3-(2-chlorophenyl)-2-propen-1-ylidene]-1-phenyl- | [Molecular Formula]
C18H13ClN2O2 | [MOL File]
310460-39-0.mol | [Molecular Weight]
324.76 |
| Chemical Properties | Back Directory | [density ]
1.405±0.06 g/cm3(Predicted) | [storage temp. ]
Sealed in dry,2-8°C | [solubility ]
DMSO: 50 mM | [form ]
A crystalline solid | [pka]
8.26±0.20(Predicted) | [color ]
Brown to reddish brown |
| Hazard Information | Back Directory | [Uses]
CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2DHR-2 for Rac1 in a dose-dependent manner with an IC50 of 22.8 μM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9[1]. | [in vivo]
When 2.5 mg/kg of CPYPP is administrated intravenously, the plasma concentration of CPYPP is only 2.4 μM at 30 min. However, by intraperitoneally injecting 250 mg/kg of CPYPP into mice, the plasma concentration of CPYPP reached to 11.3 μM at 30 min and 10.9 μM at 1 hr, respectively[1].
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The adoptively transferred spleen cells from mice that has been made by a ‘‘knock-in’’ strategy to express endogenous DOCK2 as a fusion protein with green fluorescent protein (GFP). Intraperitoneal injection of CPYPP (5 mg per mouse) 1 hr before adoptive transfer reduces the percentage of the migrated T cells to <25% of the control level[1]. | [storage]
Store at -20°C | [References]
[1] Nishikimi A, et al. Blockade of inflammatory responses by a small-molecule inhibitor of the Rac activator DOCK2. Chem Biol. 2012 Apr 20;19(4):488-97. DOI:10.1016/j.chembiol.2012.03.008 |
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