Home GPCR & G Protein DOCK inhibitor CPYPP For research use only.

CPYPP

CPYPP is an inhibitor of dedicator of cytokinesis 2 (DOCK2). CPYPP inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2DHR-2 for Rac1 in a dose-dependent manner with IC50 of 22.8 μM. CPYPP also inhibits DOCK180, DOCK5 and less DOCK9.

CPYPP Chemical Structure

CPYPP Chemical Structure

CAS: 310460-39-0

Selleck's CPYPP has been cited by 1 publication

Purity & Quality Control

Batch: S089901 DMSO] 65 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 98.56%
98.56

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Biological Activity

Description CPYPP is an inhibitor of dedicator of cytokinesis 2 (DOCK2). CPYPP inhibits the guanine nucleotide exchange factor (GEF) activity of DOCK2DHR-2 for Rac1 in a dose-dependent manner with IC50 of 22.8 μM. CPYPP also inhibits DOCK180, DOCK5 and less DOCK9.
Targets
DOCK2DHR-2 [1]
(Cell-free assay)
22.8 μM
In vitro
In vitro

CPYPP, a small-molecule inhibitor of DOCK2, binds to DOCK2 DHR-2 domain in a reversible manner and inhibits its catalytic activity, and blocks both chemokine receptor- and antigen receptor-mediated Rac activation resulting in marked reduction of chemotactic response and T cell activation in lymphocytes.[1]
Cell Research Cell lines HEK293T cells
Concentrations 100 µM
Incubation Time 1 h
Method

Before assays, cells were stimulated with CCL21 (1 µg/ml), CXCL13 (1 µg/ml),  anti-CD3ε antibody (145-2c11; 10 µg/ml) followed by crosslinking with antihamster IgG (10 µg/ml), or CpG-A (3 µM). Aliquots of the cell extracts were kept for total lysate controls, and the remaining extracts were incubated with GST-fusion Rac-binding domain of PAK1 at 4 ℃ for 60 min. The bound proteins and the same amounts of total lysates were analyzed by SDSPAGE, and blots were probed with anti-Rac antibody.
In Vivo
In vivo

Intraperitoneal injection of CPYPP 1 hr before adoptive transfer reduces the percentage of the migrated T cells to <25% of the control level.[1]
Animal Research Animal Models C57BL/6 mice transferred with spleen cells from DOCK-GFP knock-in mice
Dosages 100 µL (i.p.) or 50 µL (i.v.)
Administration i.p., i.v.

Chemical Information & Solubility

Molecular Weight 324.76 Formula

C18H13ClN2O2
CAS No. 310460-39-0 SDF --
Smiles C1=CC=C(C=C1)N2C(=O)C(=CC=CC3=CC=CC=C3Cl)C(=O)N2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 65 mg/mL ( (200.14 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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