4734-59-2
Chemical Structure
LSD1/TLK1-IN-1
Synonym(s): J54; J3-54
- CAS No.: 4734-59-2
- Formula:C18H20N2OS
- Molecular Weight:312.43
IUPAC Name: 4-(2-(10H-phenothiazin-10-yl)ethyl)morpholine
InChIKey: VJQXIWLVJMDRGV-UHFFFAOYSA-N
SMILES: N1(CCN2C3=C(SC4=C2C=CC=C4)C=CC=C3)CCOCC1
Biological Activity: LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer[1][2].
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LSD1/TLK1-IN-1 | 99.20% | LSD1/TLK1-IN-1 is an orally active LSD1, TLK1, TLK2, TTK inhibitor with an LSD1 IC50 of 0.247 μM. LSD1/TLK1-IN-1 suppresses phosphorylation of Nek1 at T141 and Rad9 at S328, abrogates the TLK1>Nek1>ATR>Chk1 axis, protects H3K4me1/2 from demethylation, and does not affect LSD2, MAO-A, or MAO-B. LSD1/TLK1-IN-1 induces apoptosis, bypasses cell-cycle arrest, suppresses tumor growth, downregulates PD-L1 expression, enhances T-cell killing response, inhibits gastric cancer cell proliferation. LSD1/TLK1-IN-1 can be used for the research of prostate cancer and gastric cancer. | ||||||||||||||||||||
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- [1]. Singh V, et al. Generation of Phenothiazine with Potent Anti-TLK1 Activity for Prostate Cancer Therapy. iScience. 2020;23(9):101474. Published 2020 Aug 20. [Content Brief]
- [2]. Dai XJ, et al. Phenothiazine-Based LSD1 Inhibitor Promotes T-Cell Killing Response of Gastric Cancer Cells. J Med Chem. 2023;66(6):3896-3916. [Content Brief]
Keywords
