[CAS NO. 2384184-40-9]  KB02-SLF

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PRODUCTS SPECIFICATIONS [2384184-40-9]

Catelog
HY-129610
Brand
MCE
CAS
2384184-40-9

DESCRIPTION [2384184-40-9]

Overview

MDL-
Molecular Weight949.52
Molecular FormulaC50H65ClN4O12
SMILESO=C([C@H]1N(C(C(C(C)(C)CC)=O)=O)CCCC1)O[C@@H](C2=CC=CC(NC(CCOCCOCCNC(COC3=CC4=C(N(C(CCl)=O)CCC4)C=C3)=O)=O)=C2)CCC5=CC=C(OC)C(OC)=C5

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

Summary

KB02-SLF is a PROTAC-based nuclear FKBP12 degrader (molecular glue). KB02-SLF promotes nuclear FKBP12 degradation by covalently modifying DCAF16 (E3 ligase) and can improve the durability of protein degradation in biological systems. SLF binds ubiquitin E3 ligase ligand KB02 via a linker to form KB02-SLF [1] .


IC50 & Target

FKBP12 [1]


In Vitro

KB02-SLF (2 µM; 4-72 hours; HEK293T cells) treatment promotes a substantial reduction in nuclear FKBP12 that is sustained across a 4-72 h time frame [1] .
Cell imaging studies confirms the selective loss of nuclear-localized FKBP12 in KB02-SLF-treated cells. KB02-SLF promotes the loss of FKBP12_NLS across a concentration of ~0.5-5µM, but shows varied reductions in activity at higher concentrations. The degradation of FKBP12_NLS induced by KB02-SLF is mediated by DCAF16 [1] .

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

Western Blot Analysis [1]

Cell Line: HEK293T cells
Concentration: 2 µM
Incubation Time: 4 hours, 8 hours, 24 hours, 48 hours, 72 hours
Result: Promoted a substantial reduction in nuclear FKBP12 that was sustained across a 4-72 h time frame.

Appearance

Solid


Shipping

Room temperature in continental US; may vary elsewhere.


Storage

4°C, sealed storage, away from moisture and light

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)


Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 105.32 mM ; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.0532 mL 5.2658 mL 10.5316 mL
5 mM 0.2106 mL 1.0532 mL 2.1063 mL
10 mM 0.1053 mL 0.5266 mL 1.0532 mL
* Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: 5 mg/mL (5.27 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: 5 mg/mL (5.27 mM); Suspended solution; Need ultrasonic

  • 3.

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

    Solubility: ≥ 5 mg/mL (5.27 mM); Clear solution

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