CPYPP

Catalog No.S0899 Batch:S089901

Technical Data

Formula

C₁₈H₁₃ClN₂O₂

Molecular Weight

324.76

CAS No.

310460-39-0

Solubility (25°C)*

In vitro

DMSO

65 mg/mL (200.14 mM)

Water

Insoluble

Ethanol

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

1.65mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 33 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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

Targets

DOCK2^DHR-2 ^[1]
(Cell-free assay)

22.8 μM

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]

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]

Protocol (from reference)

Cell Assay:^{^[1]}	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.
Animal Study:^{^[1]}	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.

Cell Assay:^{^[1]}

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.

Animal Study:^{^[1]}

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.

References

[1] Akihiko Nishikimi, et al. Chem Biol. 2012 Apr 20;19(4):488-97.

Selleck's CPYPP has been cited by 1 publication

DOCK2 and phosphoinositide-3 kinase δ mediate two complementary signaling pathways for CXCR5-dependent B cell migration [ Front Immunol, 2022, 13:982383]	PubMed: 36341455

DOCK2 and phosphoinositide-3 kinase δ mediate two complementary signaling pathways for CXCR5-dependent B cell migration [ Front Immunol, 2022, 13:982383]

PubMed: 36341455

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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