An inhibitor of DOCK2, DOCK5, and DOCK180
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CPYPP

Item No. 17386

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[3-(2-chlorophenyl)-2-propen-1-ylidene]-1-phenyl-3,5-pyrazolidinedione
CAS Number
310460-39-0
Molecular Formula
C18H13ClN2O2
Formula Weight
324.8
Purity
≥98% (mixture of isomers)
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mM
λmax
247, 362 nm
SMILES
O=C(N(C1=CC=CC=C1)NC/2=O)C2=C/C=C/C3=C(Cl)C=CC=C3
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-
InChi Key
VVZJFICTTKPNCK-XWDZFIQBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $75

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    10 mg

    $143

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    25 mg

    $333

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    50 mg

    $627

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    Product Description

    CPYPP is an inhibitor of the Rac activators dedicator of cytokinesis 2 (DOCK2; IC50 = 22.8 µM for DOCK2 guanine nucleotide exchange factor (GEF) activity), DOCK5, and DOCK180.1,2 It is selective for these DOCK-A subfamily proteins over the DOCK-D subfamily member DOCK9.1 CPYPP (100 µM) prevents chemokine-induced Rac activation in T and B cells. It also inhibits chemokine-induced migration of T and B cells. CPYPP (5 mg/animal, i.p.) reduces migration of T cells to peripheral lymph nodes in mice following adoptive transfer of spleen cells from knock-in mice expressing GFP-tagged DOCK2. It also reduces myeloperoxidase (MPO) activity in lung tissue, LPS-induced cytokine release in serum, and the severity of lung injury in a mouse model of endotoxemia-induced acute lung injury when administered at a dose of 250 mg/kg.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Nishikimi, A., Uruno, T., Duan, X., et al. Blockade of inflammatory responses by a small-molecule inhibitor of the Rac activator DOCK2. Chem. Biol. 19(4), 488-497 (2012).

    2. Ferrandez, Y., Zhang, W., Peurois, F., et al. Allosteric inhibition of the guanine nucleotide exchange factor DOCK5 by a small molecule. Sci. Rep. 7(1), 14409 (2017).

    3. Xu, X., Su, Y., Wu, K., et al. DOCK2 contributes to endotoxemia-induced acute lung injury in mice by activating proinflammatory macrophages. Biochem. Pharmacol. 184, 114399 (2021).