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Cat. No.: 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.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 3036530-23-8
화학식: C₃₃H₃₅F₃N₈O₂
분자량:632.68

보관:

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

EST1027 Chemical Structure

CAS No.: 3036530-23-8

Amount: USD 0.00

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Use of MCE Products

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

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

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

All CDK Isoforms :

In Vitro

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.

Chemical Information

CAS No. 3036530-23-8
분자량 632.68
화학식 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
선적

Room temperature in continental US; may vary elsewhere.
보관

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

순도&문서

Handling Instructions (2659 KB)

References

[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

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- IC₅₀ & Target
- In Vitro
Chemical Information
순도&문서
References

상품명:
Cat. No.:
수량:
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상품명:
CAS No.:
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Purity:
수량:

EST1027

All CDK Isoforms

Biological Activity

제품 설명

IC50 & Target

In Vitro

Chemical Information

순도&문서

References

Calculators

Help & FAQs

EST1027 Related Classifications

HY-190211 Related Classifications

Bioz

Keywords

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