dFKBP-1
CAS No. : 1799711-22-0
| Size | Price | Stock |
|---|---|---|
| 1mg | $550 | In-stock |
| 5mg | $1200 | In-stock |
| 10mg | $1860 | In-stock |
| 25mg | $3503 | In-stock |
| 50mg | $5430 | In-stock |
| 100mg | $8146 | In-stock |
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| 500 mg | Get quote | |
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| Cat. No. : | HY-103634 |
| M.Wt: | 1009.11 |
| Formula: | C53H64N6O14 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (ultrasonic) |
dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF (HY-114872) of FKBP12, the Thalidomide based Cereblon ligand and a linker[1]. In Vitro: dFKBP-1 potently decreases FKBP12 abundance in MV4;11 cells, leading to over 80% reduction of FKBP12 at 0.1 μM and 50% reduction at 0.01 μM. As with dBET1, destabilization of FKBP12 by dFKBP-1 is rescued by pre-treatment with Carfilzomib, MLN4924, free SLF or free Thalidomide. Cereblon (CRBN)-dependent degradation is established using previously published isogenic 293FT cell lines which are wild-type (293FT-WT) or deficient (293FT-CRBN / ) for CRBN. Treatment of 293FT-WT cells with dFKBP-1 induces potent, dose-dependent degradation of FKBP12, whereas 293FT-CRBN / are unaffected[1].
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