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Cat. No.: HY-187458

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EST1140

EST1140 is a covalent molecular glue degrader targeting RNF126 for AR/AR-V7, with DC₅₀ values of 33 μM and 30 μM, respectively, in 22Rv1 cells. EST1140 covalently binds to the E3 ligase RNF126 to achieve targeted protein degradation. EST1140 can be used in the research of androgen-independent prostate cancer.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

CAS No.: 3105892-11-0
화학식: C₃₀H₃₂N₄O₆S
분자량:576.66

보관:

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

EST1140 Chemical Structure

CAS No.: 3105892-11-0

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
- Cellular Effect
- In Vitro
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
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Biological Activity

제품 설명

IC₅₀ & Target^[1]

AR-V7

RNF126

Cellular Effect

Cell Line	Type	Value	Description	References
22Rv1	DC₅₀	33 μM	50% degradation concentration of AR in human 22Rv1 androgen-independent prostate cancer cells after 24 h of treatment, assessed by Western blot assay. 50% degradation concentration of AR in human 22Rv1 androgen-independent prostate cancer cells after 24 h of treatment, assessed by Western blot assay.	41867716
22Rv1	DC₅₀	30 μM	50% degradation concentration of AR-V7 in human 22Rv1 androgen-independent prostate cancer cells after 24 h of treatment, assessed by Western blot assay. 50% degradation concentration of AR-V7 in human 22Rv1 androgen-independent prostate cancer cells after 24 h of treatment, assessed by Western blot assay.	41867716
22Rv1	EC₅₀	8 μM	Half-maximal effective concentration for inhibition of AR/AR-V7 transcriptional activity in human 22Rv1 androgen-independent prostate cancer cells after 12 h of treatment, assessed by luciferase reporter assay. Half-maximal effective concentration for inhibition of AR/AR-V7 transcriptional activity in human 22Rv1 androgen-independent prostate cancer cells after 12 h of treatment, assessed by luciferase reporter assay.	41867716

In Vitro

EST1140 (20 μM; 24 h)-mediated degradation of AR-V7 in 22Rv1 cells is dependent on the proteasome^[1].
Treatment with EST1140 (1-50 μM; 24 h) for 24 h induces dose-dependent degradation of AR (DC₅₀ = 33 μM) and AR-V7 (DC₅₀ = 30 μM) in 22Rv1 androgen-independent prostate cancer cells^[1].
EST1140 (8 μM; 12 h) potently inhibits the transcriptional activity of AR/AR-V7 in 22Rv1 cells, with an EC₅₀ of 8 μM^[1].
EST1140 (0.1-50 μM; 30 min) covalently binds to purified RNF126 protein in a dose-dependent manner in IA-rhodamine-labeled competition assays^[1].
The effect of EST1140 (20 μM; 24 h) on inducing FLAG-AR degradation in HEK293T cells is strictly dependent on RNF126^[1].

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

Western Blot Analysis^[1]

Cell Line:

22Rv1 androgen-independent prostate cancer cells
Concentration:

20 μM
Incubation Time:

24 h
Result:

Mediated degradation of AR-V7, which was attenuated by pre-treatment with proteasome inhibitor.

Western Blot Analysis^[1]

Cell Line:

22Rv1 androgen-independent prostate cancer cells
Concentration:

1, 5, 10, 20, 35, 50 μM
Incubation Time:

24 h
Result:

Induced dose-dependent degradation of both AR and AR-V7.
Achieved a 50% degradation concentration (DC₅₀) of 33 μM for AR.
Achieved a 50% degradation concentration (DC₅₀) of 30 μM for AR-V7.
Caused observable degradation as early as 4 h after treatment.

Western Blot Analysis^[1]

Cell Line:

FLAG-AR-expressing RNF126 wild-type (WT) and knockout (KO) HEK293T cells
Concentration:

20 μM
Incubation Time:

24 h
Result:

Significantly reduced FLAG-AR levels in RNF126 WT cells.
Abrogated FLAG-AR degradation in RNF126 KO cells.

Chemical Information

CAS No. 3105892-11-0
분자량 576.66
화학식 C₃₀H₃₂N₄O₆S
SMILES

COC1=CC=C(C(/C=C/C(N[C@@H]2C[C@@H](NC(COC3=CC=C(C4=CSC(N5CCOCC5)=N4)C=C3)=O)C2)=O)=O)C=C1
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]. Modi A, et al. An Optimized RNF126-Targeting Covalent Handle for Molecular Glue Degraders. bioRxiv [Preprint]. 2026 Mar 7:2026.03.06.709959.

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.

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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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Purity:
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EST1140

Biological Activity

Chemical Information

순도&문서

References

Calculators

Help & FAQs

EST1140 Related Classifications

HY-187458 Related Classifications

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