TLK Inhibitor

UNC-CA2-103 is a TLK2 inhibitor with a human IC₅₀ of 18 nM, and it exhibits high selectivity over TLK1 and the vast majority of other kinases. UNC-CA2-103 can be used in research related to breast cancer, glioblastoma and gastric cancer.

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.

TLK1-IN-1 is a TLK1B inhibitor with a human IC₅₀ of 7.2 μM. TLK1-IN-1 causes accumulation of DNA damage and induces apoptotic cell death in cancer cells. TLK1-IN-1 can be used for the research of metastatic castration-resistant prostate cancer.