4-(3-(2-Chlorophenyl)allylidene)-1-phenylpyrazolidine-3,5-dione

Name	CPYPP
Synonyms	CPYPP 4-(3-(2-Chlorophenyl)allylidene)-1-phenylpyrazolidine-3,5-dione 4-[3-(2-Chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione 3,5-Pyrazolidinedione, 4-[3-(2-chlorophenyl)-2-propen-1-ylidene]-1-phenyl-
CAS	310460-39-0

Molecular Formula	C18H13ClN2O2
Molar Mass	324.76
Density	1.405±0.06 g/cm3(Predicted)
pKa	8.26±0.20(Predicted)
Storage Condition	2-8°C
MDL	MFCD00980987
In vitro study	CPYPP binds to DOCK2 DHR-2 domain in a reversible manner and inhibited its catalytic activity in vitro. When lymphocytes are treated with CPYPP, both chemokine receptor- and antigen receptor-mediated Rac activation are blocked, resulting in marked reduction of chemotactic response and T cell activation. Although overexpression of DOCK2 induces Rac activation in HEK293T cells, this activation is markedly suppressed by treating the cells with CPYPP at 100 µM for 1 hr before assay.
In vivo study	When 2.5 mg/kg of CPYPP is administrated intravenously, the plasma concentration of CPYPP is only 2.4 µM at 30 min. However, by intraperitoneally injecting 250 mg/kg of CPYPP into mice, the plasma concentration of CPYPP reached to 11.3 µM at 30 min and 10.9 µM at 1 hr, respectively. The adoptively transferred spleen cells from mice that has been made by a ‘‘knock-in’’ strategy to express endogenous DOCK2 as a fusion protein with green fluorescent protein (GFP). Intraperitoneal injection of CPYPP (5 mg per mouse) 1 hr before adoptive transfer reduces the percentage of the migrated T cells to <25% of the control level.

biological activity	CPYPP is a DOCK2-Rac1 interacting inhibitor. CPYPP binds to the DOCK2DHR-2 domain and inhibits DOCK2DHR-2 of the guanine nucleotide exchange factor activity against Rac1 in a dose-dependent manner with an IC50 of 22.8 μm. CPYPP also inhibits DOCK180 and DOCK5, with less inhibitory activity against dock9.
Target	IC50: 22.8 µm (GEF activity of DOCK2 DHR-2 for Rac1)

Last Update：2024-04-09 21:32:11

Spot supply

Product Name: CPYPP Visit Supplier Webpage Request for quotation
CAS: 310460-39-0
Tel: 609-228-6898
Email: sales@medchemexpress.com
　　　　 tech@medchemexpress.com
Mobile: 609-228-6898

Spot supply

Product Name: CPYPP Visit Supplier Webpage Request for quotation
CAS: 310460-39-0
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922

Wechat: 18621343501
WhatsApp: +86-18621343501

Spot supply

Product Name: CPYPP Visit Supplier Webpage Request for quotation
CAS: 310460-39-0
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328

WhatsApp: +86-18821248368

Spot supply

Product Name: CPYPP Visit Supplier Webpage Request for quotation
CAS: 310460-39-0
Tel: 609-228-6898
Email: sales@medchemexpress.com
　　　　 tech@medchemexpress.com
Mobile: 609-228-6898

Spot supply

Product Name: CPYPP Visit Supplier Webpage Request for quotation
CAS: 310460-39-0
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922

Wechat: 18621343501
WhatsApp: +86-18621343501

Spot supply

Product Name: CPYPP Visit Supplier Webpage Request for quotation
CAS: 310460-39-0
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328

WhatsApp: +86-18821248368

View History

4-(3-(2-Chlorophenyl)allylidene)-1-phenylpyrazolidine-3,5-dione Request for Quotation