2. PROTAC NF-κB
  3. PROTACs IKK
  4. PROTAC TBK1 degrader-2

PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM).

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

PROTAC TBK1 degrader-2 Chemical Structure

PROTAC TBK1 degrader-2 Chemical Structure

CAS No. : 2052306-13-3

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Based on 1 publication(s) in Google Scholar

PROTAC TBK1 degrader-2 Related Antibodies

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Description

PROTAC TBK1 degrader-2 is a Ligands for Target Protein for PROTAC. PROTAC TBK1 degrader-2 is a potent degrader based on the serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC50=15 nM; Kd=4.6 nM) with a maximum efficiency of 96%. PROTAC TBK1 degrader-2 also targets to IkB kinase IKKε (IC50=8.7 nM), with low selectivity over TBK1 (IC50=1.3 nM)[1].

IC50 & Target

IC50: 1.3 nM (TBK1), 8.7 nM (IKKε)[1]
In Vitro

PROTAC TBK1 degrader-2 (compound 3i) (100 nM) mediates degradation of TBK1 abrogated by VHL ligand 2 (10 μM) or proteasome inhibitor Carfilzomib (HY-10455) (100 nM)[1].
PROTAC TBK1 degrader-2 (0-3 μM) exhibits poor selectivity for TBK1 over IKKε (IC50 of 1.3 nM vs 8.7 nM), but has no effect on the levels of IKKε, at concentrations of more than 50-fold above its TBK1 DC50[1].
PROTAC TBK1 degrader-2 (100 nM; 300 M; 72 h) is not synthetically lethal in K-Ras mutant versus wild type cells[1].

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

PROTAC TBK1 degrader-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: K-Ras mutant cell lines (H23, A549, and H1792) and K-Rras wild type cell lines (H2110 and HCC827)
Concentration: 100 nM, 300 nM
Incubation Time: 72 hours
Result: Lacked synthetically lethality in K-Ras mutant versus wild type cells.
Molecular Weight

1093.18

Formula

C53H74BrN9O9S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NCC1=CC=C(C2=C(C)N=CS2)C=C1)[C@H]3N(C([C@H](C(C)(C)C)NC(COCCCOCCCCOCCCOC4=CC=C(NC5=NC=C(Br)C(NCCCN(C(C6CCC6)=O)C)=N5)C=C4)=O)=O)C[C@H](O)C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 110 mg/mL (100.62 mM; Need ultrasonic and warming; 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 0.9148 mL 4.5738 mL 9.1476 mL
5 mM 0.1830 mL 0.9148 mL 1.8295 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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. 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 0.9148 mL 4.5738 mL 9.1476 mL 22.8691 mL
5 mM 0.1830 mL 0.9148 mL 1.8295 mL 4.5738 mL
10 mM 0.0915 mL 0.4574 mL 0.9148 mL 2.2869 mL
15 mM 0.0610 mL 0.3049 mL 0.6098 mL 1.5246 mL
20 mM 0.0457 mL 0.2287 mL 0.4574 mL 1.1435 mL
25 mM 0.0366 mL 0.1830 mL 0.3659 mL 0.9148 mL
30 mM 0.0305 mL 0.1525 mL 0.3049 mL 0.7623 mL
40 mM 0.0229 mL 0.1143 mL 0.2287 mL 0.5717 mL
50 mM 0.0183 mL 0.0915 mL 0.1830 mL 0.4574 mL
60 mM 0.0152 mL 0.0762 mL 0.1525 mL 0.3812 mL
80 mM 0.0114 mL 0.0572 mL 0.1143 mL 0.2859 mL
100 mM 0.0091 mL 0.0457 mL 0.0915 mL 0.2287 mL
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PROTAC TBK1 degrader-2 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:

PROTAC TBK1 degrader-22052306-13-3PROTACsIKKIκB kinaseI kappa B kinaseInhibitorinhibitorinhibit

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