2. MAPK/ERK Pathway
  3. MNK Ribosomal S6 Kinase (RSK)
  4. HSND80

HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with Kd values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro.

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HSND80 Chemical Structure

HSND80 Chemical Structure

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HSND80 Related Antibodies

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MNK1 MNK2 MNK

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p70S6K RSK1 RSK2 RSK3 RSK4

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Description

HSND80 (Compound 1) is an orally active inhibitor of MNK/p70S6K, with Kd values of 44 nM against MNK1 and 4 nM against MNK2. HSND80 has a longer target residence time of 45 mins and 58 mins against MNK1 and MNK2 respectively. HSND80 can suppress non-small cell lung cancer (NSCLC) both in vitro and in vivo, and suppress Triple-Negative Breast Cancer (TNBC) in vitro[1].

IC50 & Target[1]

MNK1

44 nM (Kd)

MNK2

4 nM (Kd)

p70S6K

 

In Vitro

HSND80 (0.1-104nM, 72 h) inhibits cells growth of MDA-MB-23, MDA-MB-468, 4T1, T47D, MCF-7, HOP-92, NCI-H226, NCI-H522, EKVX, NCI-H322M, A549, NCI-H23, NCI-H460, HOP-62, KLN205 with IC50 values of 8.8 nM, 18.3 nM, 0.93 nM, 84.2 nM, 18.5 nM, 27 nM, 29.5 nM, 31.6 nM, 38 nM, 57.5 nM, 79.4 nM, 107.2 nM, 107.2 nM, 144.5 nM, 360 nM, respectively[1].
. HSND80 (200 nM, 30 h) induces G1 arrest[1].
. HSND80 (0.5-3 μM, 4 h) downregulates phosphorylation levels of eIF4E (MNK1/2 target), along with S6 and eIF4B (p70S6K targets)[1].
.

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

HSND80 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-23, MDA-MB-468, 4T1, T47D, MCF-7, HOP-92, NCI-H226, NCI-H522, EKVX, NCI-H322M, A549, NCI-H23, NCI-H460, HOP-62, KLN205
Concentration: 0.1-104 nM
Incubation Time: 72 h
Result: Reduced cell viability.

Cell Cycle Analysis[1]

Cell Line: MDA-MB-231
Concentration: 200 nM
Incubation Time: 30 h
Result: Induced G1 arrest.

Western Blot Analysis[1]

Cell Line: MDA-MB-231
Concentration: 0.5 μM, 1 μM, 3 μM
Incubation Time: 4 h
Result: Downregulated phosphorylation levels of eIF4E (MNK1/2 target), along with S6 and eIF4B (p70S6K targets).
In Vivo

HSND80 (10 mg/kg; p.o.) improves oral bioavailability, the maximum plasma concentration of HSND80 in male CD1 mice is 176 ng/mL at 2 h, which diminish to 2.5 ng/mL at 24 h[1].
HSND80 (15 mg/kg, 30 mg/kg; p.o.; 5 days on, 2 days off, 15 days) leads to a reduction in tumor volumes in DBA/2 mice [1].

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

Animal Model: DBA/2 mice (6-8 weeks) were subcutaneously injected with 0.7 x 106 KLN 205 cells per 100 μL, administrated after 6 months [1]
Dosage: 15 or 30 mg/kg
Administration: Oral gavage (p.o.); 5 days on, 2 days off; total 15 days.
Result: Led to a reduction in tumor volumes.
Animal Model: Male CD1 mice[1]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.) and blood sampling was done between 0.25-24 h.
Result: Improved oral bioavailability, the maximum plasma concentration was 176 ng/mL at 2 h, which diminished to 2.5 ng/mL at 24 h.
Molecular Weight

632.68

Formula

C33H35F3N8O2
SMILES

O=C(NC1=CC=C(CN2CCN(C)CC2)C(C(F)(F)F)=C1)C3=CN=CC(C#CC4=CN=C5C=CC(N6C[C@H](C)O[C@H](C)C6)=NN54)=C3
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HSND80 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HSND80HSND 80HSND-80MNKRibosomal S6 Kinase (RSK)Mitogen activated protein kinase interacting kinaseMAP kinase interacting kinaseMAPK interacting kinaseS6KAnticancerbreast cancerlung cancerdual MNK/p70S6K inhibitorssyngeneic NSCLC modeloral bioavailabilityMDA-MB-231MCF-7Inhibitorinhibitorinhibit

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