2098621-17-9
Chemical Structure
TPC-144
- CAS No.: 2098621-17-9
- Formula:C31H31F2N3O2
- Molecular Weight:515.59
IUPAC Name: 5'-((1R,3r,5S)-3-amino-8-azabicyclo[3.2.1]octane-8-carbonyl)-2'',3-difluoro-4''-(2-hydroxy-2-methylpropyl)-[1,1':2',1''-terphenyl]-4-carbonitrile
InChIKey: NPMWAUQVRAYSDP-BKFWDETESA-N
SMILES: N[C@H]1C[C@H]2CC[C@@H](C1)N2C(C3=CC(C4=CC=C(C(F)=C4)C#N)=C(C=C3)C5=CC=C(C=C5F)CC(O)(C)C)=O
Biological Activity: TPC-144 is a LSD1/KDM1A inhibitor. TPC-144 inhibits LSD1, and leads to a decrease in the protein level of DNMT1, causing low methylation of the LINE-1 element. TPC-144 can also produce a synergistic effect with Decitabine (HY-A0004) (a DNMT inhibitor), jointly promoting DNA demethylation and thereby inducing differentiation and apoptosis of leukemia cells. TPC-144 has also demonstrated anti-tumor efficacy in acute myeloid leukemia (AML) models. TPC-144 can be used for the study of AML[1][2].
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TPC-144 | TPC-144 is a LSD1/KDM1A inhibitor. TPC-144 inhibits LSD1, and leads to a decrease in the protein level of DNMT1, causing low methylation of the LINE-1 element. TPC-144 can also produce a synergistic effect with Decitabine (HY-A0004) (a DNMT inhibitor), jointly promoting DNA demethylation and thereby inducing differentiation and apoptosis of leukemia cells. TPC-144 has also demonstrated anti-tumor efficacy in acute myeloid leukemia (AML) models. TPC-144 can be used for the study of AML. | |||||||||||||||||||||
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References
- [1]. Osada A, et al. Abstract A169: Combination of TPC-144, a reversible LSD1 inhibitor, and a hypomethylating agent resulted in synergistic antitumor efficacy in preclinical models of AML. Molecular Cancer Therapeutics. 2018 Jan 1;17(1_Supplement):A169-.
- [2]. Pandey MR, Wang ES. What potential is there for LSD1 inhibitors to reach approval for AML?. Expert opinion on emerging drugs. 2019 Oct 2;24(4):205-12.
