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Cat. No.: HY-182939

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MNK1/2-IN-10

MNK1/2-IN-10 is an orally active, selective MNK1/MNK2 inhibitor, with an IC₅₀ of 10.84 nM for MNK1 and an IC₅₀ of 12.81 nM for MNK2. MNK1/2-IN-10 inhibits eIF4E phosphorylation, the NF-κB signaling pathway, macrophage polarization, oxidative stress and the production of pro-inflammatory cytokines. MNK1/2-IN-10 alleviates kidney and spleen damage in LPS (HY-D1056)-induced inflammatory mouse models. Anti-inflammatory agent 115 is applicable for research related to acute inflammation.

연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.

화학식: C₂₅H₂₄N₆O₃S₂
분자량:520.63

보관:

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

MNK1/2-IN-10 Chemical Structure

Amount: USD 0.00

* 장바구니에 담기 전 물품의 수량을 선택해 주십시오.

Use of MCE Products

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

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

Biological Activity

제품 설명

IC₅₀ & Target

^[1]

MNK1

10.84 nM (IC₅₀)

MNK2

12.81 nM (IC₅₀)

All MNK Isoforms :

All NF-κB Isoforms :

In Vitro

MNK1/2-IN-10 (Compound 13) (48 h) shows low cytotoxicity in RAW 264.7, HEK293T, HUVECs and AML-12 cell lines, with IC₅₀ values ranging from 24.25 to 77.56 μM after 48 h of incubation^[1].
MNK1/2-IN-10 (1.25-10 μM; 24 h) inhibits LPS-induced expression of p-eIF4E and iNOS in RAW 264.7 cells in a concentration-dependent manner^[1].
MNK1/2-IN-10 (1.25-10 μM; 4 h) concentration-dependently inhibits the LPS-induced expression of p-eIF4E in RAW 264.7 cells^[1].
MNK1/2-IN-10 (1.25-10 μM; 24 h) inhibits LPS-induced release of IL-6, TNF-α and MCP-1 in RAW 264.7 cells in a concentration-dependent manner^[1].
MNK1/2-IN-10 (1.25-10 μM; 24 h) inhibits lipopolysaccharide (LPS)-induced nitric oxide release in RAW 264.7 cells in a concentration-dependent manner, with the maximum inhibitory effect observed at 10 μM^[1].
MNK1/2-IN-10 (10 μM; 24 h) inhibits LPS-induced iNOS expression in RAW 264.7 cells^[1].
MNK1/2-IN-10 (1.25-10 μM; 12 h) inhibits LPS-induced activation of the NF-κB pathway in RAW 264.7 cells in a concentration-dependent manner in vitro^[1].
MNK1/2-IN-10 (10 μM; 24 h) inhibits LPS-induced nuclear translocation of P65 in RAW 264.7 cells^[1].
MNK1/2-IN-10 (2.5-10 μM; 13 h) reduces LPS-induced ROS production in RAW 264.7 cells in a concentration-dependent manner^[1].
MNK1/2-IN-10 (10 μM; 14 h) inhibits LPS-induced ROS production in RAW 264.7 cells^[1].
MNK1/2-IN-10 (2.5-10 μM; 24 h) restores GSH levels and enhances SOD activity in LPS-stimulated RAW 264.7 cells in a concentration-dependent manner in vitro^[1].

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

Western Blot Analysis^[1]

Cell Line:

RAW 264.7
Concentration:

10 μM, 5 μM, 2.5 μM, 1.25 μM
Incubation Time:

24 h
Result:

Suppressed LPS-induced phosphorylation of eIF4E in a concentration-dependent manner, with maximal suppression at 10 μM.
Suppressed LPS-induced expression of iNOS in a concentration-dependent manner, with maximal suppression at 10 μM.

Immunofluorescence^[1]

Cell Line:

RAW 264.7
Concentration:

10 μM, 5 μM, 2.5 μM, 1.25 μM
Incubation Time:

2 h (pretreatment); 2 h (LPS stimulation)
Result:

Inhibited LPS-induced p-eIF4E expression in a concentration-dependent manner, as shown by reduced green fluorescence intensity.

ELISA Assay^[1]

Cell Line:

RAW 264.7
Concentration:

10 μM, 5 μM, 2.5 μM, 1.25 μM
Incubation Time:

24 h
Result:

Inhibited LPS-induced secretion of IL-6 in a dose-dependent manner.
Inhibited LPS-induced secretion of TNF-α in a dose-dependent manner.
Inhibited LPS-induced secretion of MCP-1 in a dose-dependent manner.

Immunofluorescence^[1]

Cell Line:

RAW 264.7
Concentration:

10 μM
Incubation Time:

24 h
Result:

Diminished iNOS signal in the cytoplasm of LPS-stimulated cells.

Western Blot Analysis^[1]

Cell Line:

RAW 264.7
Concentration:

10 μM, 5 μM, 2.5 μM, 1.25 μM
Incubation Time:

12 h
Result:

Inhibited LPS-induced phosphorylation of P65 in a concentration-dependent manner.
Inhibited LPS-induced phosphorylation of IκBα in a concentration-dependent manner.

Immunofluorescence^[1]

Cell Line:

RAW 264.7
Concentration:

10 μM
Incubation Time:

12 h (pretreatment); 12 h (LPS stimulation)
Result:

Blocked LPS-triggered nuclear translocation of P65, with significantly reduced fluorescence intensity in the nucleus.

Parmacokinetics

Species	Dose	Route	C_max	T_max	T_1/2	AUC_0-t	Bioavailability
Rat^[1]	10 mg/kg	i.v.	17403.000 ng/mL	1.389 h	10.090 h	82007.297 ng·h/mL	/
Rat^[1]	200 mg/kg	p.o.	5833.000 ng/mL	2.167 h	15.951 h	107535.552 ng·h/mL	6.6 %

In Vivo

MNK1/2-IN-10 (Compound 13) (25-100 mg/kg; p.o.; daily; 16 days) potently alleviates LPS-induced acute inflammation and organ damage in male C57BL/6J mice, with the 100 mg/kg dose demonstrating the strongest efficacy in reducing pro-inflammatory cytokines, suppressing p-eIF4E and iNOS expression, restoring antioxidant function, and improving tissue pathology^[1].

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

Animal Model:

C57BL/6J (male, 6−8 weeks old, 18−21 g, LPS-induced)^[1]
Dosage:

25 mg/kg; 50 mg/kg; 100 mg/kg
Administration:

p.o.; daily; 16 days
Result:

Significantly reduced LPS-induced kidney and spleen indices, with the 100 mg/kg dose showing the strongest effect.
Improved renal function, reducing serum creatinine and urea nitrogen levels; the 50 and 100 mg/kg doses showed greater improvement than the positive control dexamethasone.
Mitigated LPS-induced kidney pathological changes (tubular dilation, brush border necrosis, vacuolization, structural disruption) and spleen pathological changes (nuclear swelling, cellular edema, inflammatory infiltration, microcirculatory dysfunction).
Significantly reduced serum levels of pro-inflammatory cytokines TNF-α, IL-6, MCP-1, and IL-1β, with the 100 mg/kg dose showing the strongest suppression.
Significantly suppressed p-eIF4E expression and downregulated the M1 macrophage marker iNOS in kidney and spleen tissues, with the 100 mg/kg dose showing the strongest effect.
Restored antioxidant capacity by increasing glutathione and superoxide dismutase levels, and reduced lipid peroxidation by lowering malondialdehyde levels in tissues.

Related Protocols :

Chemical Information

분자량 520.63
화학식 C₂₅H₂₄N₆O₃S₂
SMILES

O=C(N1CCN(S(CCC)(=O)=O)CC1)C2=CC=C(C3=NN4C(S3)=NC=C4C5=CC=C(C#N)C=C5)C=C2
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]. Li H, et al. Discovery of Imidazo[2,1-b][1,3,4]thiadiazole-Based MNK Inhibitors with Anti-inflammatory Efficacy via Dual Suppression of eIF4E Phosphorylation and NF-κB Signaling. J Med Chem. 2026 Apr 7.
[Content Brief]

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

견적 받기

Amount: USD 0.00

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

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

상품명:
CAS No.:
Species:
Purity:
수량:

MNK1/2-IN-10

All MNK Isoforms

All NF-κB Isoforms

Biological Activity

제품 설명

IC50 & Target

In Vitro

Parmacokinetics

In Vivo

Chemical Information

순도&문서

References

Calculators

Help & FAQs

MNK1/2-IN-10 Related Classifications

HY-182939 Related Classifications

Bioz

Keywords

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