1. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK Apoptosis
  2. Ribosomal S6 Kinase (RSK) DYRK Apoptosis
  3. MBM-55S

MBM-55S 是有效的 NIMA-related kinase 2 (Nek2) 抑制剂,IC50 值为 1 nM,是其他激酶选择性的 20 倍甚至更高,除了 RSK1 (IC50=5.4 nM) 和 DYRK1a (IC50=6.5 nM)。MBM-55S 通过诱导细胞周期停滞和凋亡 (apoptosis) 抑制癌细胞的增殖。具有抗肿瘤活性,且对小鼠没有明显的毒性。

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MBM-55S Chemical Structure

MBM-55S Chemical Structure

CAS No. : 2083624-07-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MBM-55S is a potent NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 1 nM. MBM-55S shows a 20-fold or greater selectivity in most kinases with the exception of RSK1 (IC50=5.4 nM) and DYRK1a (IC50=6.5 nM). MBM-55S effectively inhibits the proliferation of cancer cells by inducing cell cycle arrest and apoptosis. MBM-55S shows antitumor activities, and no obvious toxicity to mice[1].

IC50 & Target

RSK1

5.4 nM (IC50)

DYRK1A

6.5 nM (IC50)

体外研究
(In Vitro)

MBM-55S inhibits MGC-803, HCT-116, Bel-7402 cells proliferation with IC50s of 0.53, 0.84, 7.13 μM, respectively[1].
MBM-55S (0.5-1 μM; 24 hours) induces G2/M phase arrest and accumulation of cells with >4N content in HCT-116 cells[1].
MBM-55S (0.5-1 μM; 24 hours) causes cell apoptosis in a concentration-dependent manner in HCT-116 cells[1].

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

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1 μM
Incubation Time: 24 hours
Result: Induced G2/M phase arrest and accumulation of cells with >4N content.

Apoptosis Analysis[1]

Cell Line: HCT-116 cells
Concentration: 0.5, 1 μM
Incubation Time: 24 hours
Result: Caused cell apoptosis in a concentration-dependent manner.
体内研究
(In Vivo)

MBM-55S (20 mg/kg; i.p.; twice a day for 21 days) exhibits good antitumor activity and a well-tolerated dose schedule in nude mice bearing HCT-116 xenografts[1]. MBM-55S (1.0 mg/kg; i.v.) treatment shows the CL, Vss, T1/2, AUC0-t, and AUC0-∞ values of 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ng/h/mL, respectively[1].

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

Animal Model: Female BALB/c nu/nu mice (5-6 weeks, bearing HCT-116 xenografts)[1]
Dosage: 20 mg/kg
Administration: Intraperitoneal injection; twice a day for 21 days
Result: Significantly suppressed tumor growth.
Animal Model: Male Sprague Dawley (SD) rats[1]
Dosage: 1.0 mg/kg
Administration: IV injection (Pharmacokinetic Analysis)
Result: The CL, Vss, T1/2, AUC0-t, and AUC0-∞ values were 33.3 mL/min/kg, 2.53 L/kg, 1.72 hours, 495 ng/h/mL and 507 ml/min/kg, respectively.
分子量

734.73

Formula

C36H39FN6O10

CAS 号
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
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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.

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HY-101029A
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