The B/B Homodimerizer (AP20187) is a synthetic, cell-permeable ligand that can be used to induce homodimerization of fusion proteins containing the DmrB domain. The B/B Homodimerizer has been tested in vitro and in mice. It is nontoxic. We suggest testing various B/B Homodimerizer concentrations within the recommended range (0.01–100 nM for in vitro use or 0.005–10 mg/kg in mice) in order to obtain a complete dose-response profile. The homodimerizer has been widely used to study signal transduction pathways (by inducing oligomerization of cell surface receptor proteins), but it can be used to induce the activity/re-localization of any protein that is affected by oligomerization. The B/B Homodimerizer is identical to the AP20187 ligand, which was previously supplied by ARIAD Pharmaceuticals, Inc.
B/B Washout Ligand—for use with the iDimerize Inducible Homodimer Systems
B/B Washout Ligand is a membrane-permeant ligand that dissociates protein interactions induced by the B/B Homodimerizer (T1/2 of ~10 minutes after adding it to target cells treated with B/B Homodimerizer).
A/C Heterodimerizer (AP21967)—for use with the iDimerize Inducible Heterodimer & Inducible Expression Systems
The A/C Heterodimerizer (AP21967) is a cell permeable ligand used to induce heterodimerization of two different fusion proteins, containing the DmrA and DmrC domains respectively. The A/C Heterodimerizer has been tested in vitro and in mice. It is non-toxic to cells at up to 1 µM concentrations and in mice at up to 30 mg/kg doses. We suggest testing various A/C Heterodimerizer concentrations within the recommended range (0.05 nM–500 nM for in vitro use) in order to obtain a complete dose-response profile. The A/C Heterodimerizer is identical to the AP21967 ligand, which was previously supplied by ARIAD Pharmaceuticals, Inc.
D/D Solubilizer—for use with the iDimerize Reverse Dimerization System
The D/D Solubilizer is a synthetic, cell-permeable ligand that can be used to disrupt oligomerization of fusion proteins containing the DmrD domain. The D/D Homodimerizer has been tested in vitro and in mice for applications including inducible secretion of proteins. It is nontoxic. We suggest testing various D/D Homodimerizer concentrations within the recommended range (10–500 nM) for different lengths of time (30 minutes to 12+ hours) in order to obtain a complete dose-response profile. The D/D Solubilizer performs the same function as the AP21998 ligand, which was previously supplied by ARIAD Pharmaceuticals, Inc. It is a different molecule than AP21998.
A/A Homodimerizer (AP1510)
AP1510 will be available from Clontech using the name A/A Homodimerizer for a limited transition period. This ligand can be used to induce homodimerization of a protein tagged with the DmrA domain. For short term studies, existing users who require AP1510 should purchase sufficient material to complete your studies. For longer term studies, you should consider converting your system to using B/B Homodimerizer (AP20187). AP1510 should not be used in vivo.
