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

HSND80 (Compound 1) 是一种有口服活性的 MNK/p70S6K 抑制剂，HSND80 对 MNK1 的 Kd 值为 44 nM，对 MNK2 的 Kd 值为 4 nM。HSND80 对 MNK1 和 MNK2 的靶点的停留时间分别为 45 分钟和 58 分钟。HSND80 在体外和体内均可抑制非小细胞肺癌 (NSCLC)，并且可以在体外抑制三阴性乳腺癌 (TNBC) 细胞生长。

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HSND80 Chemical Structure

HSND80 Chemical Structure

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HSND80 相关抗体

Top Publications Citing Use of Products

查看 MNK 亚型特异性产品:

查看所有亚型
MNK1 MNK2 MNK

查看 Ribosomal S6 Kinase (RSK) 亚型特异性产品:

查看所有亚型
p70S6K RSK1 RSK2 RSK3 RSK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

 

体外研究
(In Vitro)

HSND80 (0.1-104 nM，72小时) 抑制 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 细胞生长，IC50 分别为 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[1].
。 HSND80 (200 nM，30小时) 诱导MDA-MB-231 细胞 G1 停滞[1].
。 HSND80 (0.5-3 μM，4小时) 在MDA-MB-231细胞中可以下调 eIF4E (MNK1/2 靶点) 以及 S6 和 eIF4B（p70S6K 靶点）的磷酸化水平[1].
。

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

HSND80 相关抗体:

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).
体内研究
(In Vivo)

HSND80 (10 mg/kg；口服) 可提高口服生物利用度，HSND80 在雄性 CD1 小鼠中最大血浆浓度在 2 小时时为 176 ng/mL，在 24 小时时降至 2.5 ng/mL[1]。
HSND80 (15 mg/kg; 30 mg/kg；口服给药；给药5天，暂停2天，持续15天)， 可以减小 DBA/2 小鼠肿瘤体积[1]。

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.
分子量

632.68

Formula

C33H35F3N8O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

HSND80 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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