1. PROTAC
    Autophagy
    Apoptosis
    Immunology/Inflammation
  2. PROTAC
    FKBP
  3. dFKBP-1

dFKBP-1 

Cat. No.: HY-103634 Purity: 98.84%
Handling Instructions

dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF of FKBP12, the Thalidomide based cereblon ligand and a linker.

For research use only. We do not sell to patients.

dFKBP-1 Chemical Structure

dFKBP-1 Chemical Structure

CAS No. : 1799711-22-0

Size Price Stock Quantity
1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 2400 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF of FKBP12, the Thalidomide based cereblon ligand and a linker[1].

IC50 & Target[1]

Cereblon

 

FKBP

 

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].

Molecular Weight

1009.11

Formula

C₅₃H₆₄N₆O₁₄

CAS No.

1799711-22-0

SMILES

O=C([[email protected]]1N(C(C(C(C)(C)CC)=O)=O)CCCC1)O[[email protected]@H](C2=CC=CC(NC(CCC(NCCCCNC(COC3=CC=CC(C(N4C(CC5)C(NC5=O)=O)=O)=C3C4=O)=O)=O)=O)=C2)CCC6=CC=C(OC)C(OC)=C6

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (99.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9910 mL 4.9549 mL 9.9097 mL
5 mM 0.1982 mL 0.9910 mL 1.9819 mL
10 mM 0.0991 mL 0.4955 mL 0.9910 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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Keywords:

dFKBP-1dFKBP1dFKBP 1PROTACFKBPProteolysis-targeting chimeraFK506-binding proteinBETdegraderFKBP12CereblonSLFInhibitorinhibitorinhibit

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dFKBP-1
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