| Identification | Back Directory | [Name]
10H-Phenothiazine, 10-[2-(4-morpholinyl)ethyl]- | [CAS]
4734-59-2 | [Synonyms]
J-3-54
LSD1-IN-24
10H-Phenothiazine, 10-[2-(4-morpholinyl)ethyl]- | [Molecular Formula]
C18H20N2OS | [MOL File]
4734-59-2.mol | [Molecular Weight]
312.43 |
| Chemical Properties | Back Directory | [Melting point ]
74.5-75.5 °C | [Boiling point ]
198-201 °C(Press: 0.5 Torr) | [density ]
1?+-.0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
6.68±0.10(Predicted) | [color ]
Pale purple to purple |
| Hazard Information | Back Directory | [Uses]
LSD1-IN-24(compound 3S) is a selective LSD1 inhibitor with IC50 = 0.247 μM. LSD1-IN-24 can mediate the expression of PD-L1, enhance T cell killing response, and can be used in cancer research[1]. | [in vivo]
LSD1-IN-24 (compound 3S) (0-50 mg/kg, oral gavage; daily for 2 weeks) inhibits in vivo MFC cell growth, tumor weight in a dose-dependent manner in a subcutaneous tumor model containing MFC cells Significantly decreased, tumor tissue Ki67 decreased significantly, and no obvious toxic effect on mice[1].
| Animal Model: | Male 615 mice with MFC cell[1] | | Dosage: | 0, 10, 25, and 50 mg/kg | | Administration: | Oral gavage; daily for 2 weeks | | Result: | Significantly decreased intratumoral PD-L1 expression, increased CD3+, CD4+, CD8+ cell numbers, interleukin-2 (IL2) and IFNγ mRNA and protein levels were also upregulated. |
| [References]
[1] Xing-Jie Dai, et al. Phenothiazine-Based LSD1 Inhibitor Promotes T-Cell Killing Response of Gastric Cancer Cells. J Med Chem. 2023 Mar 23;66(6):3896-3916. DOI:10.1021/acs.jmedchem.2c01593 |
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