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製品番号: HY-190211

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EST1027

EST1027 is a CDK4 Molecular glue degrader. EST1027 degrades CDK4 by forming a CDK4-EST1027-RNF126 ternary complex. EST1027 can be used for research on cervical cancer.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号: 3036530-23-8
分子式: C₃₃H₃₅F₃N₈O₂
分子量:632.68

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

EST1027 構造式

CAS 番号: 3036530-23-8

価格（税別）

Amount: USD 0.00

* アイテムを追加する前、数量をご選択ください

Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性

製品説明

EST1027 is a CDK4 Molecular glue degrader. EST1027 degrades CDK4 by forming a CDK4-EST1027-RNF126 ternary complex. EST1027 can be used for research on cervical cancer^[1]^[2]^[3].

IC₅₀ & Target

^[1]

CDK4

RNF126

CDK アイソフォーム固有の製品をすべて表示 :

体外実験

Anti-cancerCell Cycle RegulationOthers

Anti-cancer

EST1027 engages RNF126 cysteine 32 in C33A cells with a control/EST1027 ratio of 2.0^[1].

Anti-cancer

Cell Cycle Regulation

EST1027 (3-5 μM; 24 h) induces proteasome- and RNF126-dependent CDK4 degradation in C33A cells, causing >50% CDK4 loss^[1].
EST1027 reduces CDK4 levels in C33A cells among >5000 quantified proteins, with 100 additional proteins affected^[1].

Others

EST1027 (0.1-50 μM) covalently engages recombinant RNF126 in a dose-dependent manner^[1].
EST1027 modifies cysteine 32 of RNF126^[1].

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

Western Blot Analysis^[1]

Cell Line:

C33A cells
Concentration:

3 μM (24 h); 5 μM (after 1 h BTZ pretreatment); 5 μM (24 h)
Incubation Time:

24 h (3 μM); 1 h (BTZ pretreatment for 5 μM); 24 h (5 μM)
Result:

Reduced CDK4 levels by >50% in C33A cells at 3 μM after 24 h but did not reduce CDK6.
At 5 μM for 24 h, CDK4 was also reduced.
BTZ pretreatment attenuated CDK4 degradation, indicating proteasome dependence.
RNF126 knockdown completely attenuated CDK4 degradation.
RNF126 levels were also reduced.

化学情報

CAS 番号 3036530-23-8
分子量 632.68
分子式 C₃₃H₃₅F₃N₈O₂
SMILES

O=C(C1=CC2=CN=C(NC3=NC=C(N4CCN(C(/C=C/C5=CC=C(C(F)(F)F)C=C5)=O)CC4)C=C3)N=C2N1C6CCCC6)N(C)C
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Toriki ES, et al. Rational Chemical Design of Molecular Glue Degraders. ACS central science. 2023 May 24;9(5):915-926. [Content Brief]

[2]. Hu Y, et al. Molecular glue degrader for tumor treatment. Frontiers in oncology. 2024;14:1512666. [Content Brief]

[3]. Schaefer D, et al. Recent Advances in Covalent Drug Discovery. Pharmaceuticals (Basel, Switzerland). 2023 Apr 28;16(5):663.

Calculators

モル濃度計算機

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

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

Minimum order quantity

100 mg

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Amount: USD 0.00

生物活性
- 製品説明
- IC₅₀ & Target
- 体外実験
化学情報
純度とドキュメンテーション
参考文献

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EST1027

CDK アイソフォーム固有の製品をすべて表示

生物活性

製品説明

IC50 & Target

体外実験

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

EST1027 関連分類

HY-190211 関連分類

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