Biochem/physiol Actions
Rapa*-3Z is a rapamycin analog that selectively targets FKBP12 with V55G mutation, while exhibiting reduced affinity toward the wild-type FKBP12 (mTOR FRB association induction EC50 = 11.8 nM/V55G vs 639 nM/wt FKBP12). Rapa*-3Z selectively inhibits the growth, the phosphorylation level of mTORC1 downstream pS6K/pS6 and mTORC2 downstream pAkt in 293 transfectants experssing the V55G FKBP12 mutant (mutant cells pS6K/pS6 IC50 = 1.0/1.3 nM vs. 76/121 nM in wt cells). Rapa*-3Z potently inhibits the larval development of transgenic flies that express human FKBP12 V55G (by 70%/75 μM and 100%/100 μM), but not those with wild-type human FKBP12.
- UPC:
- 51183702
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- SML3580-5MG
