DTAGV-1

• Target:

  Others

• Related Pathways:

  Others

• Bioactivity:

  Degrader targeting mutant FKBP12F36V fusion proteins. Comprises a ligand selective for F36V single-point mutated FKBP12, a linker and a von Hippel-Lindau (VHL) -binding ligand. Induces potent and selective degradation of FKBP12F36V fusion proteins in vitro and in vivo. Selectively degrades FKBP12F36V-EWS/FLI fusion proteins and inhibits cell proliferation in FKBP12F36V-EWS/FLI-expressing Ewing sarcoma cells. Hydrochloride salt available; suitable for in vivo use. Negative control dTAGV-1-NEG also available. FKBP12F36V can be expressed as a fusion with a target protein of interest using genome engineering techniques, via transgene expression or CRISPR-mediated locus-specific knock-in. Custom knock-in cell lines for the dTAG and aTAG platforms are available from our sister brand R&D Systems. Email [email protected] to enquire. Plasmid vectors for the lentiviral expression and CRISPR-mediated knock-in of FKBP12F36V are available from Addgene.

• Smiles:

  CC[C@@H](C1=CC(OC)=C(C(OC)=C1)OC)C(N2CCCC[C@H]2C(O[C@H](CCC3=CC(OC)=C(C=C3)OC)C4=CC=CC=C4OCC(NCCCCCCC(N[C@H](C(N5C[C@@H](C[C@H]5C(N[C@@H](C)C6=CC=C(C=C6)C7=C(N=CS7)C)=O)O)=O)C(C)(C)C)=O)=O)=O)=O

• Molecular Formula:

  C68H90N6O14S

• Molecular Weight:

  1247.54

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2451573-86-5