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Cat. No.: HY-189074

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JN210

JN210 is a dual inhibitor of DCN1 and HDAC, with an IC₅₀ of 94.26 nM against human DCN1. JN210 disrupts the UBE2M-DCN1 protein-protein interaction, blocks the neddylation modification of cullin-RING ligases, inhibits HDAC activity and induces histone hyperacetylation. JN210 impairs DNA damage repair function, induces cell apoptosis (apoptosis), exerts cytotoxicity and inhibits tumor growth. JN210 can be used for the research of non-small cell lung cancer.

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화학식: C₂₄H₃₀Cl₂N₄O₃
분자량:493.43

보관:

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

JN210 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
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

DCN1

94.26 nM (IC₅₀)

HDAC1

0.825 μM (IC₅₀)

HDAC2

2.369 μM (IC₅₀)

HDAC3

1.280 μM (IC₅₀)

HDAC6

0.253 μM (IC₅₀)

HDAC8

0.869 μM (IC₅₀)

HDAC11

2.894 μM (IC₅₀)

All HDAC Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC50	1.4 μM	Antiproliferative activity against human A549 nonsmall cell lung cancer cells assessed via cell proliferation inhibition assay. Antiproliferative activity against human A549 nonsmall cell lung cancer cells assessed via cell proliferation inhibition assay.	42593931
NCI-H1299	IC50	1.8 μM	Antiproliferative activity against human H1299 nonsmall cell lung cancer cells assessed via cell proliferation inhibition assay. Antiproliferative activity against human H1299 nonsmall cell lung cancer cells assessed via cell proliferation inhibition assay.	42593931
HepG2	IC50	2.3 μM	Antiproliferative activity against human HepG2 liver cancer cells assessed via cell proliferation inhibition assay. Antiproliferative activity against human HepG2 liver cancer cells assessed via cell proliferation inhibition assay.	42593931

In Vitro

JN210 potently inhibits the DCN1-UBE2M protein-protein interaction in a cell-free FP assay with an IC₅₀ of 94.26 nM^[1].
JN210 acts as a selective HDAC6 inhibitor in cell-free enzymatic assays, with an IC₅₀ of 0.253 μM, and exhibits moderate activity against most Class I HDACs, negligible activity against Class IIa HDACs, and weak activity against HDAC11^[1].
JN210 potently inhibits the proliferation of A549, H1299, and HepG2 cancer cells in vitro, with the highest potency in A549 cells (IC₅₀ = 1.4 μM)^[1].
JN210 (0.625-10 μM; 72 h) induces histone H3 and H4 hyperacetylation and upregulates Cullin1 and Cullin3 protein levels in A549 cells^[1].
JN210 (1.25-10 μM; 24 h) induces concentration-dependent accumulation of acetylated α-tubulin in A549 cells, confirming HDAC6 target engagement^[1].
JN210 (1.25-10 μM; 24 h) induces concentration-dependent upregulation of the p27 tumor suppressor in A549 cells, inhibiting Cullin3-mediated p27 degradation^[1].
JN210 (1.25-10 μM; 24 h) induces concentration-dependent DNA double-strand breaks in A549 cells, as measured by elevated γ-H2A.X levels^[1].
JN210 (3 μM; 24 h) alters global gene expression in A549 cells, with significant changes in genes related to cytoskeletal organization, cell cycle progression, protein degradation, and the PI3K/Akt signaling pathway^[1].
JN210 (5-20 μM; 48 h) induces concentration-dependent G1 phase cell cycle arrest in A549 cells^[1].
JN210 (5-10 μM; 48 h) induces concentration-dependent apoptosis in A549 cells, with greater efficacy at 10 μM than the equimolar physical combination of SAHA and NacM-OPT at a total concentration of 20 μM^[1].

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

Western Blot Analysis^[1]

Cell Line:

A549 nonsmall cell lung cancer cells
Concentration:

0.625-10 μM
Incubation Time:

72 h
Result:

Induced concentration-dependent hyperacetylation of histone H3 and histone H4.
Markedly upregulated Cullin1 and Cullin3 protein levels.
Exerted minimal effect on DCN1 expression.

Western Blot Analysis^[1]

Cell Line:

A549 nonsmall cell lung cancer cells
Concentration:

1.25-10 μM
Incubation Time:

24 h
Result:

Induced concentration-dependent accumulation of acetylated α-tubulin.\nInduced concentration-dependent upregulation of p27 protein levels, with a more pronounced effect than the parent DCN1 inhibitor NacM-OPT alone.\nInduced concentration-dependent increases in γ-H2A.X protein levels, a marker of DNA double-strand breaks.

Cell Cycle Analysis^[1]

Cell Line:

A549 nonsmall cell lung cancer cells
Concentration:

5-20 μM
Incubation Time:

48 h
Result:

Induced concentration-dependent G1 phase arrest.
Caused a corresponding decrease in the S-phase cell population.

Apoptosis Analysis^[1]

Cell Line:

A549 nonsmall cell lung cancer cells
Concentration:

5-10 μM
Incubation Time:

48 h
Result:

Induced concentration-dependent increases in apoptotic cells.
Induced apoptosis in over 60% of A549 cells at 10 μM.
Exerted a greater effect than the equimolar physical combination of SAHA and NacM-OPT (total 20 μM), which induced apoptosis in approximately 30% of cells.

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	MRT_0-t	MRT_0-∞
Mice^[1]	10 mg/kg	i.p.	3.45 h	0.12 h	4857.2 ng/mL	1064.7 ng·h/mL	1285.6 ng·h/mL	4.5 h	4.9 h

In Vivo

JN210 (10-30 mg/kg; i.p.; once daily; 15 days) exhibits dose-dependent in vivo antitumor efficacy in an A549 xenograft model, with a 68.6% tumor growth inhibition rate at 30 mg/kg once daily, and maintains a favorable safety profile^[1].

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

Animal Model:

Nude mice^[1]
Dosage:

10 mg/kg; 30 mg/kg
Administration:

i.p.; once daily; 15 days
Result:

Achieved a 44.6% tumor growth inhibition (TGI) rate at 10 mg/kg.
Achieved a 68.6% TGI rate at 30 mg/kg.
Caused no significant body weight loss at both doses.
Showed no obvious tissue damage via histopathological evaluation at both doses.

Chemical Information

분자량 493.43
화학식 C₂₄H₃₀Cl₂N₄O₃
SMILES

O=C(NO)C1=CC=C(CN(C2CCN(CCCC)CC2)C(NC3=CC=C(Cl)C(Cl)=C3)=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]. Zheng T, et al. Structure-Based Discovery of JN210 as a Potent Dual DCN1/HDAC Inhibitor for the Treatment of Nonsmall Cell Lung Cancer. Journal of medicinal chemistry. 2026 Aug 13;69(15):18076-18098.

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

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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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