[CAS NO. 310460-39-0] CPYPP
PRODUCTS SPECIFICATIONS [310460-39-0]
DESCRIPTION [310460-39-0]
Overview
| MDL | MFCD00980987 |
|---|---|
| Molecular Weight | 324.76 |
| Molecular Formula | C18H13ClN2O2 |
| SMILES | O=C(/C1=C\C=C\C2=CC=CC=C2Cl)NN(C3=CC=CC=C3)C1=O |
2 Publications Citing Use of MCE
Summary
CPYPP is a DOCK2-Rac1 interaction inhibitor. CPYPP binds to DOCK2 DHR-2 domain and inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2 DHR-2 for Rac1 in a dose-dependent manner with an IC 50 of 22.8 µM. CPYPP also inhibits DOCK180 and DOCK5 and less inhibits DOCK9 [1] .
IC50 & Target
IC50: 22.8 µM (GEF activity of DOCK2 DHR-2 for Rac1)
In Vitro
CPYPP binds to DOCK2 DHR-2 domain in a reversible manner and inhibited its catalytic activity in vitro. When lymphocytes are treated with CPYPP, both chemokine receptor- and antigen receptor-mediated Rac activation are blocked, resulting in marked reduction of chemotactic response and T cell activation
[1]
.
Although overexpression of DOCK2 induces Rac activation in HEK293T cells, this activation is markedly suppressed by treating the cells with CPYPP at 100 µM for 1 hr before assay
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]
.
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 25 mg/mL ( 76.98 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 3.0792 mL | 15.3960 mL | 30.7920 mL |
| 5 mM | 0.6158 mL | 3.0792 mL | 6.1584 mL |
| 10 mM | 0.3079 mL | 1.5396 mL | 3.0792 mL |
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1.
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2.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (7.70 mM); Clear solution