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Product details

名称

GSK2879552

英文名称

GSK2879552

货号

G655930-1ml

包装规格

1ml

级别

Moligand™

浓度

10mM in DMSO

储存温度

-80℃储存

运输条件

超低温冰袋运输

产品介绍

GSK2879552 an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/ KDM1A) , with potential antineoplastic activity In Vitro GSK2879552 inhibits KDM1A histone demethylase activity, inducing differentiation of Sorafenib -resistant cells and attenuating stemness properties. GSK2879552 depresses the transcription of Wnt antagonists and downregulates β-catenin signaling activity in Sorafenib-resistant cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation Assay. Cell Line: 9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines. Concentration: 0-10000 nM. Incubation Time: 6 days. Result: Inhibited cell proliferation. RT-PCR. Cell Line: Resistant HCC cells (PLC/PRF/5 and Huh7). Concentration: 0, 1, 2 μM. Incubation Time: 24 h. Result: Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9,\nNanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4. In Vivo GSK2879552 (1.5 mg/kg, p.o.) treatment exhibits tumor growth inhibition in SCLC xenograft-bearing mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: NCI-H526 and NCI-H1417 xenografts. Dosage: 1.5 mg/kg. Administration: PO daily for 25-35 days. Result: There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice. IC50& Target:KDM1/LSD1

生化机理

GSK2879552 是一种具有潜在抗肿瘤活性的赖氨酸特异性去甲基化酶 1（LSD1/ KDM1A）口服活性、选择性和不可逆抑制剂。

CAS号

1401966-69-5(DMSO)

分子式

C23H28N2O2

分子量

364.5 g/mol

Smiles

C1CN(CCC1CNC2CC2C3=CC=CC=C3)CC4=CC=C(C=C4)C(=O)O

Reaxy-Rn

29487399

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

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「No related articles yet」

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