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[1][2].

Product Specifications

CAS Number

[2098621-17-9]

UNSPSC

12352005

Target

Apoptosis; Histone Demethylase

Related Pathways

Apoptosis; Epigenetics

Field of Research

Cancer

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

Molecular Formula

C31H31F2N3O2

Molecular Weight

515.59

References & Citations

[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.