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

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.

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

dFKBP-1 Chemical Structure

dFKBP-1 Chemical Structure

CAS No. : 1799711-22-0

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5 mg USD 1500 In-stock
10 mg USD 2400 In-stock
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Based on 1 publication(s) in Google Scholar

dFKBP-1 Related Antibodies

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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].

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

dFKBP-1 Related Antibodies
Molecular Weight

1009.11

Formula

C53H64N6O14
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C([C@H]1N(C(C(C(C)(C)CC)=O)=O)CCCC1)O[C@@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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 0.9910 mL 4.9549 mL 9.9097 mL 24.7743 mL
5 mM 0.1982 mL 0.9910 mL 1.9819 mL 4.9549 mL
10 mM 0.0991 mL 0.4955 mL 0.9910 mL 2.4774 mL
15 mM 0.0661 mL 0.3303 mL 0.6606 mL 1.6516 mL
20 mM 0.0495 mL 0.2477 mL 0.4955 mL 1.2387 mL
25 mM 0.0396 mL 0.1982 mL 0.3964 mL 0.9910 mL
30 mM 0.0330 mL 0.1652 mL 0.3303 mL 0.8258 mL
40 mM 0.0248 mL 0.1239 mL 0.2477 mL 0.6194 mL
50 mM 0.0198 mL 0.0991 mL 0.1982 mL 0.4955 mL
60 mM 0.0165 mL 0.0826 mL 0.1652 mL 0.4129 mL
80 mM 0.0124 mL 0.0619 mL 0.1239 mL 0.3097 mL
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dFKBP-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

dFKBP-11799711-22-0dFKBP1dFKBP 1PROTACsFKBPFK506-binding proteinPROTACBETdegraderFKBP12CereblonSLFInhibitorinhibitorinhibit

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