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Cat. No.: HY-190503

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CSN5-14

CSN5-14 is a CSN5 inhibitor (IC₅₀ 0.73 μM). CSN5-14 blocks the removal of NEDD8 from Cullin, leading to the accumulation of NEDD8-Cul1. CSN5-14 induces intracellular ROS accumulation. CSN5-14 induces cell cycle arrest and Apoptosis. CSN5-14 does not induce detectable cellular senescence. CSN5-14 exhibits anticancer activity against triple-negative breast cancer.

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화학식: C₂₉H₃₃N₅O₂
분자량:483.60

보관:

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

CSN5-14 Chemical Structure

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
- Cellular Effect
- In Vitro
- Parmacokinetics
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

Cellular Effect

Cell Line	Type	Value	Description	References
MDA-MB-231	IC50	8.1 μM	Cytotoxicity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Cytotoxicity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	42858571
MDA-MB-468	IC50	5.8 μM	Cytotoxicity against human MDA-MB-468 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Cytotoxicity against human MDA-MB-468 cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	42858571
MCF-10A	IC50	14.1 μM	Cytotoxicity against human MCF-10A cells assessed as viability reduction incubated 72 hrs by CCK-8 assay. Cytotoxicity against human MCF-10A cells assessed as viability reduction incubated 72 hrs by CCK-8 assay.	42858571

In Vitro

Anti-cancerApoptosisCell Cycle RegulationOxidative StressOthers

Anti-cancer

CSN5-14 (2.5-20 μM; 12 h) binds to CSN5 in MDA-MB-231 and MDA-MB-468 cells, increasing NEDD8-Cul1 starting from 2.5 μM without altering total CSN5 protein^[1].
CSN5-14 (0.39-100 μM; 72 h) reduces the viability of MDA-MB-231 and MDA-MB-468 cells, with an IC₅₀ of 8.1 μM in MDA-MB-231 and 5.8 μM in MDA-MB-468^[1].
CSN5-14 (5-20 μM; 24 h) dose-dependently inhibits DNA replication in MDA-MB-231 cells, with EdU incorporation decreasing to 34.1% at 5 μM and to below 10% at 10-20 μM^[1].
CSN5-14 (5-20 μM; 24 h exposure) impairs the long-term clonogenic survival of MDA-MB-231 and MDA-MB-468 cells, with almost complete inhibition at 20 μM^[1].
CSN5-14 (5-20 μM; 24 h) does not induce detectable cellular senescence in MDA-MB-231 cells^[1].
CSN5-14 (2.5-5 μM; 0-36 h) does not significantly affect MDA-MB-231 migration^[1].

Anti-cancer

Apoptosis

CSN5-14 (5-20 μM; 72 h) induces dose-dependent apoptosis in MDA-MB-468 cells, reaching approximately 45.6% at 20 μM, and produces approximately 32.8% apoptosis at 20 μM in MDA-MB-231 cells^[1].

Anti-cancer

Cell Cycle Regulation

CSN5-14 (2.5-20 μM; 24 h) induces concentration-dependent cell cycle redistribution in MDA-MB-231 cells, producing G0/G1 phase arrest at 2.5-10 μM and G2/M phase arrest at 20 μM^[1].

Anti-cancer

Oxidative Stress

CSN5-14 (5-20 μM; 24 h) causes only mild ROS changes at 5-10 μM, but significantly increases ROS-positive cells in MDA-MB-231 cells at 20 μM^[1].

Others

CSN5-14 (20 min pre-incubation; 60 min probe incubation) directly inhibits purified CSN5 in the FP assay, with an IC₅₀ of 0.73 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 and MDA-MB-468 cells
Concentration:

2.5, 5, 10, 20 μM (12 h); 20 μM (0, 2, 4, 8, 12, 24 h)
Incubation Time:

12 h (dose-dependent); 0, 2, 4, 8, 12, 24 h (20 μM time-course)
Result:

NEDD8-Cul1/Cul1 fold change was 1.45 at 2.5 μM, 1.84 at 5 μM, 2.29 at 10 μM, and 2.73 at 20 μM in MDA-MB-231 cells.
The ratios were 1.36, 1.83, 2.17, and 2.48 at 2.5, 5, 10, and 20 μM, respectively, in MDA-MB-468 cells.
NEDD8-Cul1 was detectable by 2 h, sustained through 12 h, and slightly decreased at 24 h.
Total CSN5 protein remained stable across dose groups.

Cell Viability Assay^[1]

Cell Line:

MDA-MB-231, MDA-MB-468, and MCF-10A cells
Concentration:

0.39-100 μM
Incubation Time:

72 h
Result:

IC50 was 8.1 μM in MDA-MB-231, 5.8 μM in MDA-MB-468, and 14.1 μM in MCF-10A cells.

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

5, 10, 20 μM
Incubation Time:

24 h
Result:

The EdU-positive rate was 34.1% at 5 μM and fell below 10% at 10 μM and 20 μM.

Cell Migration Assay^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

2.5, 5 μM
Incubation Time:

0, 12, 24, 36 h
Result:

No significant changes in migratory potential were detected between exposed and control groups over 36 h.

Cell Cycle Analysis^[1]

Cell Line:

MDA-MB-231 cells
Concentration:

2.5, 5, 10, 20 μM
Incubation Time:

24 h
Result:

G0/G1 fractions increased to 45.6%, 49.9%, and 56.8% at 2.5, 5, and 10 μM, respectively, with a concomitant decrease in S-phase cells.
At 20 μM, cells accumulated predominantly in G2/M, with the G2/M fraction reaching 66.9%.

Apoptosis Analysis^[1]

Cell Line:

MDA-MB-468 and MDA-MB-231 cells
Concentration:

5, 10, 20 μM
Incubation Time:

72 h
Result:

In MDA-MB-468 cells, total apoptotic rates were ~27.7% at 10 μM and ~45.6% at 20 μM.
In MDA-MB-231 cells, the total apoptotic rate was ~32.8% at 20 μM.

Related Protocols :

Parmacokinetics

Species	Dose	Route	T_max	C_max	AUC_0-24	AUC_0-∞	T_1/2	CL_z/F	V_z/F
Rat^[1]	10 mg/kg	i.p.	0.14 h	2950.76 μg/L	4105.63 μg/L·h	4106.12 μg/L·h	1.81 h	2.46 L/h/kg	6.31 L/kg

Chemical Information

분자량 483.60
화학식 C₂₉H₃₃N₅O₂
SMILES

O=C(NCCCNC1=C2C(NC(C3=CC=C(C)C=C3C4=CC=CC=C4)=C2)=NC=C1)CN5CCOCC5
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]. Yang Z, et al. Discovery of new 7-azaindole derivatives as CSN5 inhibitors with in vitro antitumor activity against triple-negative breast cancer. European journal of medicinal chemistry. 2026 Oct 09;321(Pt 1):119410.

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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Amount: USD 0.00

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

상품명:
Cat. No.:
수량:
MCE Japan Authorized Agent:

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CAS No.:
Species:
Purity:
수량:

CSN5-14

Biological Activity

제품 설명

Cellular Effect

In Vitro

Parmacokinetics

Chemical Information

순도&문서

References

Calculators

Help & FAQs

CSN5-14 Related Classifications

HY-190503 Related Classifications

Bioz

Keywords

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