[CAS NO. 2079056-43-0] PROTACFKBPDegrader-3

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PRODUCTS SPECIFICATIONS [2079056-43-0]

Catelog

HY-135345

Brand

MCE

CAS

2079056-43-0

DESCRIPTION [2079056-43-0]

Overview

MDL	-
Molecular Weight	1295.54
Molecular Formula	C68H90N6O17S
SMILES	CC[C@H](C(N1[C@H](C(O[C@H](CCC2=CC=C(OC)C(OC)=C2)C3=CC=CC(OCC(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O)=C3)=O)CCCC1)=O)C7=CC(OC)=C(OC)C(OC)=C7

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

Summary

PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an von Hippel-Lindau binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader ^[1] .

IC50 & Target

VHL

FKBP

In Vitro

PROTAC treatment time courses demonstrated a notable increase in polyubiquitination of EGFP-FKBP in response to treatment with 250 nM of PROTAC FKBP Degrader-3 (compound 10) for VHL within the first hour. Upon recruiting endogenous VHL via PROTAC FKBP Degrader-3 (compound 10), only one EGFP background lysine (Lys158) is found to be ubiquitylated ^[1] .

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

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

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

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 19.30 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.7719 mL	3.8594 mL	7.7188 mL
5 mM	0.1544 mL	0.7719 mL	1.5438 mL
10 mM	0.0772 mL	0.3859 mL	0.7719 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 5 mg/mL (3.86 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (1.93 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (1.93 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Ottis P, et al. Assessing Different E3 Ligases for Small Molecule Induced Protein Ubiquitination and Degradation. ACS Chem Biol. 2017 Oct 20;12(10):2570-2578.