GLPBio

CPYPP

Catalog No.: GC50065Purity:>98.00%
COASDSData Sheet
CPYPP bound to DOCK2 DHR-2 domain (DOCK2DHR-2) in a reversible manner and inhibited its catalytic activity.

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CPYPP
Cas No.: 310460-39-0
10 mgIn Stock
$135.00
1
50 mgIn Stock
$441.00
1
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Description

CPYPP bound to DOCK2 DHR-2 domain (DOCK2DHR-2) in a reversible manner and inhibited its catalytic activity[1].

CPYPP inhibited the guanine nucleotide exchange factor (GEF) activity of DOCK2DHR-2 for Rac1 in a dose-dependent manner, with a half-maximal inhibitory concentration (IC50) of 22.8 ± 2.4 µM. This inhibitory activity was independent on length of preincubation time, ranging from 2 min to 30 min. In addition, CPYPP was nontoxic when applied to spleen cells or thymoma cells (BW5147α-β-) at 100 µM for 3 hr or 3 days, respectively [1]. Pre-treatment of human neutrophils with CPYPP, a small molecule inhibitor of the DHR-2 domain of DOCK proteins and thus of the Rac GEF activity of human DOCK2 and DOCK5, significantly impaired neutrophil chemotaxis and ROS production [2].

CPYPP effectively decreased the secretion and gene expression of TNF-α, IL-1β and IL-6 in the lungs, suggested effects of DOCK2 on endotoxemia-induced inflammatory responses in mice. CPYPP remarkably inhibited the infiltration of total cells, macrophages and neutrophils into the bronchoalveolar lavage fluid [3]. A reseach found out that a joint usage of both CPYPP and C25-140 revealed a better consequence compared to monotherapy against hepatic I/R injury [4].

References:
[1]. Nishikimi?A, Uruno?T, Duan?X, Cao?Q, Okamura?Y, Saitoh?T, et al.?Blockade of inflammatory responses by a small-molecule inhibitor of the Rac activator DOCK2. Chem Biol?2012;19:488-97.
[2]. Moens, L., Gouwy, M., Bosch, B. et al. 2019. Human DOCK2 deficiency: report of a novel mutation and evidence for neutrophil dysfunction. J. Clin. Immunol. 39:298.
[3]. Xu, X., Su, Y., Wu, K., Pan, F. & Wang, A. DOCK2 contributes to endotoxemia-induced acute lung injury in mice by activating proinflammatory macrophages. Biochem. Pharmacol. 181, 114399 (2021).
[4]. Zuotian Huang, Junliang Pua, Yunhai Luo, et al. FAM49B, restrained by miR-22, relieved hepatic ischemia/reperfusion injury by inhibiting TRAF6/IKK signaling pathway in a Rac1-dependent manner. Molecular Immunology.143, 2022, 135-146.

Protocol

Cell experiment [1]:

Cell lines

Spleen cells of BALB/c mice

Preparation Method

Spleen cells of BALB/c mice (1 × 107/ml) were incubated in RPMI1640 medium supplemented with 0.5% BSA or 10% FCS in the presence or absence of 100 µM CPYPP. 1 or 5 hr of incubation at 37°C.

Reaction Conditions

100µM for 1 hour or 5 hours

Applications

CPYPP was nontoxic when applied to spleen cells at 100 µM .
Animal experiment [2]:

Animal models

male C57BL/6J mice

Preparation Method

Mice were randomized into four groups (n = 6): the saline + vehicle group, LPS + vehicle group, saline + CPYPP group, and LPS + CPYPP group. ALI was induced by intraperitoneal (i.p.) injection of LPS (10 mg/kg) body weight; The mice in the LPS + vehicle and LPS + CPYPP groups received CPYPP (250 mg/kg) or an equivalent volume of vehicle via i.p. injection 10 min after LPS administration. The mice in the saline + vehicle and saline + CPYPP groups received CPYPP (250 mg/kg) or an equivalent volume of vehicle via i.p. injection 10 min after saline administration.

Dosage form

Intraperitoneal injection, 250 mg/kg

Applications

CPYPP-treated mice had decreased lung injury scores compared with vehicle-treated mice. Furthermore, CPYPP-treated mice exhibited significantly decreased MPO activity and W/D ratios, which indicated decreased pulmonary edema.

References:

[1]: Nishikimi?A, Uruno?T, Duan?X, Cao?Q, Okamura?Y, Saitoh?T, et al.?Blockade of inflammatory responses by a small-molecule inhibitor of the Rac activator DOCK2. Chem Biol?2012;19:488-97.
[2]: Xu, X., Su, Y., Wu, K., Pan, F. & Wang, A. DOCK2 contributes to endotoxemia-induced acute lung injury in mice by activating proinflammatory macrophages. Biochem. Pharmacol. 181, 114399 (2021).

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
310460-39-0
SMILES
O=C(N(C3=CC=CC=C3)NC2=O)/C2=C\C=C\C1=C(Cl)C=CC=C1
Molecular Formula
C18H13ClN2O2
Molecular Weight
324.76
Solubility
DMSO: 50 mM
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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