DOCK2-IN-1

• CAT Number: I041697
• CAS Number: 4590-86-7
• Molecular Formula: C16H11ClN2O2
• Molecular Weight: 298.72
• Purity: ≥95%
• Synonyms: (4E)-4-[(2-chlorophenyl)methylidene]-1-phenylpyrazolidine-3,5-dione
• InChI: InChI=1S/C16H11ClN2O2/c17-14-9-5-4-6-11(14)10-13-15(20)18-19(16(13)21)12-7-2-1-3-8-12/h1-10H,(H,18,20)/b13-10+
• InChIKey: VEBASGXAFMQOLL-JLHYYAGUSA-N
• SMILES: C1=CC=C(C=C1)N2C(=O)C(=CC3=CC=CC=C3Cl)C(=O)N2

DOCK2-IN-1 (compound 3), a CPYPP (HY-110100) analogue, is an inhibitor of DOCK2 as well (IC50=19.1 μM). DOCK2-IN-1 binds to DOCK2 DHR-2 domain in a reversible manner to inhibits its catalytic activity. DOCK2-IN-1 blocks the activation of both chemokine receptor- and antigen receptor-mediated Rac in lymphocytes. DOCK2-IN-1 significantly suppresses chemotactic response and T cell activation[1].

Reference

[1]. Nishikimi A, et al. Blockade of inflammatory responses by a small-molecule inhibitor of the Rac activator DOCK2. Chem Biol. 2012 Apr 20;19(4):488-97.
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