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| Targets |
CPYPP targets DOCK2, a guanine nucleotide exchange factor (GEF) for the Rho GTPase Rac. It binds to the DHR-2 domain of DOCK2, which is the catalytic domain responsible for its GEF activity. By inhibiting DOCK2, it prevents the activation of Rac, a key regulator of actin cytoskeleton dynamics and cell migration. This inhibition leads to a reduction in chemotactic responses and T cell activation.
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| ln Vitro |
CPYPP binds to the DOCK2 DHR-2 structure in a reversible way and suppresses its catalytic activity in vitro. When DOCK2 is treated with CPYPP, both chemokine receptors and receptor-mediated Rac activation are blocked, resulting in convergence of induction of Rac activation in HEK293T cells even when overexpressing DOCK2. Cells were treated with 100 μM CPYPP for 1 h before the experiment. This activation can be greatly decreased [1].
In vitro, CPYPP inhibits the guanine nucleotide exchange factor activity of DOCK2DHR-2 on Rac1 in a dose-dependent fashion with an IC50 of 22.8 µM. It also inhibits DOCK180 and DOCK5. By blocking DOCK2-mediated Rac activation, it reduces chemotactic responses and T cell activation in lymphocytes. |
| ln Vivo |
After 30 minutes, the Manhattan concentration of CPYPP was 2.4 μM when 2.5 mg/kg was injected intravenously. However, subjects received an intraperitoneal injection of 250 mg/kg of CPYPP, which resulted in Manhattan concentrations of 10.9 μM at one hour and 11.3 μM at thirty minutes [1]. By using a "knock-in" technique, adoptive transfer of mouse splenocytes produced endogenous DOCK2 as a fusion protein of green fluorescent protein (GFP). One hour before to adoptive transfer, an intraperitoneal injection of CPYPP (5 mg/mouse) lowers the percentage of migrating T cells by 25% relative to control levels [1].
In vivo activity data for CPYPP is limited. As a DOCK2 inhibitor, it is expected to have immunomodulatory effects by reducing T cell activation and chemotaxis. It has potential applications in the study of autoimmune diseases and inflammatory disorders. However, specific in vivo study details are not well-documented. |
| Enzyme Assay |
CPYPP is evaluated in cell-free biochemical assays to measure its ability to inhibit DOCK2 activity. These assays typically involve incubating the compound with the DOCK2DHR-2 domain and its substrate, Rac1, and measuring the inhibition of guanine nucleotide exchange activity. IC50 values are determined.
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| Cell Assay |
CPYPP is assessed in cell-based assays using lymphocytes. Cells are treated with CPYPP, and chemotactic responses and T cell activation are measured. The compound's ability to inhibit Rac activation is assessed by measuring the levels of active Rac in treated cells. These assays confirm its mechanism of action and its effects on immune cell function.
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| Animal Protocol |
CPYPP is administered in animal models to evaluate its effects on immune responses and inflammation. However, specific animal study protocols are not extensively documented. It is typically formulated for in vivo administration using DMSO or other suitable vehicles. Its efficacy in models of autoimmune diseases or inflammatory disorders is of research interest.
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| ADME/Pharmacokinetics |
CPYPP has a molecular formula of C18H13ClN2O2 and a molecular weight of 324.76. Its CAS number is 310460-39-0. The compound is a solid. It is soluble in DMSO. It should be stored under recommended conditions.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for CPYPP. The compound is for research use only and is not intended for human therapeutic use. It is a DOCK2 inhibitor used to study the role of DOCK2 in immune cell function and inflammation.
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| References | |
| Additional Infomation |
CPYPP is a small-molecule inhibitor of DOCK2. It inhibits DOCK2-Rac1 interaction and blocks chemokine and antigen receptor-mediated Rac activation. It is used in research to study immune cell migration and activation. The compound is not approved for clinical use.
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| Molecular Formula |
C18H13CLN2O2
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| Molecular Weight |
324.761023283005
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| Exact Mass |
324.066
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| CAS # |
310460-39-0
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| PubChem CID |
2248186
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| Appearance |
Brown to reddish brown solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.728
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| LogP |
3.35
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
23
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| Complexity |
523
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)N2C(=O)/C(=C/C=C/C3=CC=CC=C3Cl)/C(=O)N2
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| InChi Key |
VVZJFICTTKPNCK-KVDBUQHUSA-N
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| InChi Code |
InChI=1S/C18H13ClN2O2/c19-16-12-5-4-7-13(16)8-6-11-15-17(22)20-21(18(15)23)14-9-2-1-3-10-14/h1-12H,(H,20,22)/b8-6+,15-11+
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| Chemical Name |
(4E)-4-[(E)-3-(2-chlorophenyl)prop-2-enylidene]-1-phenylpyrazolidine-3,5-dione
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~25 mg/mL (~76.98 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.70 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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