PROTAC TBK1 degrader-2

Name: PROTAC TBK1 degrader-2
Brand: MedChemExpress
SKU: HY-112557
Rating: 4.5 (1 reviews)

製品番号: HY-112557 純度: 98.2%: Data Sheet SDS COA 取扱説明書
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PROTAC TBK1 degrader-2 is a potent PROTAC degrader of serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC₅₀=15 nM; K_d=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).
(Pink: TBK1 Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker).

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PROTAC TBK1 degrader-2 構造式

CAS 番号 : 2052306-13-3

容量	価格（税別）	在庫状況	数量
1 mg	$345	在庫あり	Estimated Time of Arrival: December 31
5 mg	$1034	お問い合わせ
10 mg		お問い合わせ
50 mg		お問い合わせ

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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

顧客検証

•Res Sq. 2026 Mar 12.

PROTACs アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

IKK アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

IKK-α IKK-β IKK IKKε TBK1

生物活性
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

PROTAC TBK1 degrader-2 is a potent PROTAC degrader of serine/threonine kinase TANK-binding kinase 1 (TBK1) (DC₅₀=15 nM; K_d=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]. (Pink: TBK1 Target protein ligand; Blue: VHL ligand (HY-125845); Black: linker).

IC₅₀ & Target

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

体外実験

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.

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.

分子量

1093.18

分子式

C₅₃H₇₄BrN₉O₉S

CAS 番号

2052306-13-3

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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
10 mM	0.0915 mL	0.4574 mL	0.9148 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.

Molarity Calculator
Dilution Calculator

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

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

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

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

純度とドキュメンテーション

純度: 98.2%

Select Batch:

データシート (270 KB) SDS (251 KB)

COA (244 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Crew AP, et al. Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1. J Med Chem. 2018 Jan 25;61(2):583-598. [Content Brief]

Complete Stock Solution Preparation Table

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