1. MAPK/ERK Pathway JAK/STAT Signaling Apoptosis Cell Cycle/DNA Damage Epigenetics
  2. MNK Pim Apoptosis Caspase Eukaryotic Initiation Factor (eIF) PARP c-Myc
  3. MNK/PIM-IN-2

MNK/PIM-IN-2 是一种 Mnk/Pim 激酶抑制剂,其 Mnk1 IC50 为 32 nM,Mnk2 IC50 为 3 nM,Pim1 IC50 为 37 nM。MNK/PIM-IN-2 可降低 p-eIF4Ep-4EBP1 的水平。MNK/PIM-IN-2 可诱导白血病细胞发生细胞周期阻滞、凋亡 (apoptosis) 并产生抗增殖作用。MNK/PIM-IN-2 可用于白血病的相关研究。

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MNK/PIM-IN-2

MNK/PIM-IN-2 Chemical Structure

CAS No. : 3081482-46-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MNK/PIM-IN-2 is a Mnk/Pim kinase inhibitor with an IC50 of 32 nM for Mnk1, 3 nM for Mnk2, and 37 nM for Pim1. MNK/PIM-IN-2 reduces the levels of p-eIF4E and p-4EBP1. MNK/PIM-IN-2 induces cell cycle arrest, apoptosis (apoptosis) and exerts antiproliferative effects in leukemia cells. MNK/PIM-IN-2 can be used in studies related to leukemia[1].

体外研究
(In Vitro)

MNK/PIM-IN-2 (compound 2j) (72 h) 可抑制人白血病细胞系 MOLM-13、THP-1、U937 和 K562 的增殖[1]
MNK/PIM-IN-2 (1-2 μM; 12-24 h) 可诱导人白血病细胞 MOLM-13 和 K562 发生 G0/G1 期阻滞[1]
MNK/PIM-IN-2 (1-2 μM; 12-24 h) 可诱导人白血病细胞系 MOLM-13 发生凋亡,但对人白血病细胞系 K562 未诱导出显著的凋亡效应[1]
MNK/PIM-IN-2 (2 μM; 12-24 h) 可抑制人白血病细胞 MOLM-13 和 K562 中的 Pim/Mnk 信号通路,降低 p-eIF4E 和 p-4EBP1 水平,下调 Mcl-1c-Myc 的表达,并诱导 MOLM-13 细胞中的 PARP 裂解[1]

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

Cell Proliferation Assay[1]

Cell Line: Human leukemia cell lines (MOLM-13, THP-1, U937, K562)
Concentration: /
Incubation Time: 72 h
Result: Exhibited potent antiproliferative activity against MOLM-13 cells with a GI50 value of 0.19 μM.
Exhibited potent antiproliferative activity against THP-1 cells with a GI50 value of 1.04 μM.
Exhibited potent antiproliferative activity against U937 cells with a GI50 value of 0.59 μM.
Exhibited potent antiproliferative activity against K562 cells with a GI50 value of 0.70 μM.

Cell Cycle Analysis[1]

Cell Line: Human leukemia cell lines (MOLM-13, K562)
Concentration: 1, 2 μM
Incubation Time: 12 h (MOLM-13); 24 h (K562)
Result: Induced G0/G1 phase arrest in MOLM-13 cells at 1 μM for 12 h, with 65.32% of cells in G0/G1.
Caused substantial accumulation in the sub-G1 phase in MOLM-13 cells at 2 μM for 12 h, with 40.44% of cells in sub-G1.
Induced G0/G1 phase arrest in K562 cells at 1 μM for 24 h.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax T1/2 AUC0-last Bioavailability
Rat[1] 2 mg/kg i.v. 247 ng/mL 5.23 h 500 ng·h/mL /
Rat[1] 10 mg/kg i.p. 357 ng/mL 5.36 h 2235 ng·h/mL 90.31 %
体内研究
(In Vivo)

MNK/PIM-IN-2 (10-20 mg/kg,持续 2 周) 在 MOLM-13 异种移植模型中展现出强效的体内抗白血病活性,且未观察到急性毒性[1]

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

Animal Model: Balb-c/nu (female) with subcutaneous MOLM‑13 cell inoculation to establish leukemia xenografts[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: daily; 2 weeks
Result: Suppressed tumor growth with an inhibition rate of 57.1%.
Suppressed tumor growth with an inhibition rate of 72.6%.
Reduced Ki67 expression in tumor tissues.
Upregulated cleaved-caspase 3 levels in tumor tissues.
Caused no significant changes in mouse body weight during administration.
Showed no abnormal changes in major organs via pathological analysis.
分子量

489.54

Formula

C26H28FN7O2

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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  • 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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MNK/PIM-IN-2
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HY-182957
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