9-ING-41

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

9-ING-41 是一种糖原合成酶激酶 3 抑制剂。9-ING-41（2、4 μM；48 小时）可降低神经母细胞瘤细胞活力，诱导细胞凋亡。 9-ING-41 (0.1-1 μM) 抑制 GSK-3，导致 NF-κB 靶标 XIAP 表达降低，并导致神经母细胞瘤细胞显着凋亡，如细胞凋亡标记物 PARP 裂解所示。 9-ING-41 (0.5、1.0、1.5、2.0 μM) 浓度低至 1.0 mM 时即可抑制所有 TCL 和 MCL 细胞系的增殖率。

9-ING-41 is a glycogen synthase kinase-3 inhibitor.9-ING-41 (2, 4 μM; 48 hours) decreases neuroblastoma cell viability induces apoptosis. 9-ING-41 (0.1-1 μM) inhibits GSK-3 leading to a decreased expression of the NF-κB target XIAP and significant apoptosis in neuroblastoma cells as shown by PARP cleavage, an apoptosis marker. 9-ING-41 (0.5, 1.0, 1.5, 2.0 μM) inhibits the proliferation rate of all TCL and MCL lines with concentrations as low as 1.0 mM. 9-ING-41 (1, 2 μM; 24 hours) is a potent cell cycle-blocking agent for lymphoma cells[2].9-ING-41 (40 mg/kg/every other day; for 17 days) has single-agent antitumor activity in a mouse model of MCL.

Cell Viability Assay Cell Line:TCL and MCL lines Concentration:2, 4 μM Incubation Time:48 hours Result:Induced apoptosis.Cell Cycle Analysis Cell Line:Lymphoma cells (Jeko, Mino, and OCI-Ly cell lines) Concentration:1, 2 μM Incubation Time:24 hours Result:Led to cell cycle arrest in G2/M.Cell Autophagy Assay Cell Line:T24 cancer cells Concentration:25?μM Incubation Time:24?hours Result:Showed extensive vacuolation and formation of autophagosome like structures in the cytoplasm.Showed an increased expression of LC3, an autophagy marker.Western Blot Analysis Cell Line:SK-N-DZ and SK-N-BE neuroblastoma cells Concentration:0.1, 1 μM Incubation Time:48 hours Result:Inhibited GSK-3 leading to a decreased expression of the NF-κB target XIAP.

Animal Model:NSG (NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ) mice Dosage:40 mg/kg Administration:Every other day; for 17 days Result:Had single-agent antitumor activity in a mouse model of MCL.

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PI3K/Akt/mTOR signaling

GSK-3

GSK-3β

Others

Myelofibrosis

1034895-42-5

404.35

C22H13FN2O5

>98% (HPLC)

DMSO:97 mg/mL (239.89mM; Need ultrasonic)

Cn1cc(C2=C(C(=O)NC2=O)c2coc3ccc(F)cc23)c2cc3OCOc3cc12

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(-20℃)

With Ice Pack

≥ 2 years