CPYPP

Catalog No.S0899

For research use only.

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

CAS No. 310460-39-0

Purity & Quality Control

Choose Selective DOCK Inhibitors

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

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 Research:

[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 Research:

[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.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 324.76
Formula

C18H13ClN2O2

CAS No. 310460-39-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CC=C(C=C1)N2C(=O)C(=CC=CC3=CC=CC=C3Cl)C(=O)N2

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy CPYPP | CPYPP supplier | purchase CPYPP | CPYPP cost | CPYPP manufacturer | order CPYPP | CPYPP distributor