LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1[1].
IC50 & Target
IC50: 123 nM (LSD1)[1]
分子量
349.18
Formula
C15H13BrN2O3
CAS 号
2035912-43-5
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.
参考文献
[1]. Duan YC, et al. Discovery of resveratrol derivatives as novel LSD1 inhibitors: Design, synthesis and their biological evaluation. Eur J Med Chem. 2017 Jan 27;126:246-258.
LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1[1].
IC50 & Target
IC50: 121 nM (LSD1)[1]
分子量
349.18
Formula
C15H13BrN2O3
CAS 号
2035912-55-9
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.
参考文献
[1]. Duan YC, et al. Discovery of resveratrol derivatives as novel LSD1 inhibitors: Design, synthesis and their biological evaluation. Eur J Med Chem. 2017 Jan 27;126:246-258.
GSK-LSD1 dihydrochloride is a potent, selective and irreversible lysine specific demethylase 1 (LSD1) inhibitor with an IC50 of 16 nM.
IC50 & Target
IC50: 16 nM (LSD1)[1]
体外研究 (In Vitro)
GSK-LSD1 shows more than 1000 fold selectivity over other closely related FAD utilizing enzymes including LSD2, and monoamine oxidases MAO-A, MAO-B[1]. GSK-LSD1 can inhibit KDM1A/LSD1 enzyme activity. GSK-LSD1 induces the formation of LC3-II in U2OS cells. The electronic microscopy shows the formation of autophagosome with GSK-LSD1 treatment. GSK-LSD1 potently inhibits proliferation of varies cancer cell lines by changing gene expression patterns[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
289.24
Formula
C14H22Cl2N2
CAS 号
2102933-95-7
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Purich D. The Inhibitor Index A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads. ISBN 9781138739215
[2]. Wang Z, et al. Inhibition of H3K4 demethylation induces autophagy in cancer cell lines. Biochim Biophys Acta. 2017 Aug 8;1864(12):2428-2437.
LSD1/HDAC6-IN-1 is an orally active dual inhibitor of lysine specific demethylase 1(LSD1)/Histone deacetylase 6 (HDAC6), with anti-tumor activity. LSD1/HDAC6-IN-1 can be used for the research of multiple myeloma (MM)[1].
体外研究 (In Vitro)
LSD1/HDAC6-IN-1 shows superior potency in multiple MM lines[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
LSD1/HDAC6-IN-1 is efficacy in the MM.1S xenograft model[1].
Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量
407.55
Formula
C50H66N6O4
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.
参考文献
[1]. M Naveen Sadhu, et al. Novel dual LSD1/HDAC6 inhibitors for the treatment of multiple myeloma. Bioorg Med Chem Lett. 2020 Dec 24;34:127763.