Biochem/physiol Actions
Degradation tag (dTAG) system heterobifunctional degrader of FKBP12(F36V) fusions by bridging them with CRBN for ubiquitination.
dTAG-13 is a degradation tag (dTAG) system heterobifunctional degrader composed of an E3 ubiquitin ligase cereblon (CRBN)-binding thalidomide moiety and an FKBP12(F36V) mutant-specific ligand AP1867 void of affinity for endogenous (wild-type) FKBP12, allowing selective degradation of target proteins of interest when expressed as an FKBP12(F36V) in-frame fusion (by transgene expression or locus-specific knock-in) by bridging them with CRBN for ubiquitination. dTAG-13 is shown to potently degrade FKBP12F36V-MELK(sg3R) in MDA-MB-468 cells (100 nM for 4 hrs) as well as ENL-FKBP12F36V-HA, but not endogenous ENL, in MV4;1 cells (500 nM for 0.5-1 hrs).
Other Notes
Contains a mixture of diastereomers. This product has not been tested in cellular degradation assays.
Legal Information
Sold with permission under license from Dana Farber Cancer Institute.
| ligand | thalidomide |
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| color | white to beige |
| solubility | DMSO: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | O=C(O[C@@H](C1=C(C=CC=C1)OCC(NCCCCCCOC2=C(C3=CC=C2)C(N(C3=O)C4CCC(NC4=O)=O)=O)=O)CCC5=CC=C(C(OC)=C5)OC)[C@@H]6CCCCN6C([C@H](C7=CC(OC)=C(C(OC)=C7)OC)CC)=O |
| InChI | 1S/C57H68N4O15/c1-7-37(36-32-47(71-4)52(73-6)48(33-36)72-5)54(65)60-29-14-12-19-41(60)57(68)76-43(25-22-35-23-26-44(69-2)46(31-35)70-3)38-17-10-11-20-42(38)75-34-50(63)58-28-13-8-9-15-30-74-45-21-16-18-39-51(45)56(67)61(55(39)66)40-24-27-49(62)59-53(40)64 |
| InChI key | BJFBRLAWLPZOMJ-QHVFGHLPSA-N |
