SHMT2-IN-1 is a potent serine hydroxymethyltransferase 2 ( SHMT2 ) inhibitor with an IC50 of 1.21 μM and a K D of 10.6 μM. SHMT2-IN-1 binds to the folate binding site of SHMT2. SHMT2-IN-1 also inhibits SHMT1 with an IC50 of 1.83 μM. SHMT2-IN-1 can inhibit cancer cells proliferation, migration and invasion. SHMT2-IN-1 can induce cells apoptosis and ROS production and cause G2/M phase arrest. SHMT2-IN-1 can be used for the research of cancer, such as esophageal cancer [1].
In Vitro, SHMT2-IN-1 (0.1-10 μM, 24 h) exhibits potent antiproliferative activity against esophageal cancer cells KYSE-450 and KYSE-70 with IC50 values of 1.62 μM and 1.18 μM respectively[1]. SHMT2-IN-1 (2.5-10 μM, 24 h) dose-dependently inhibits the migration and invasion of KYSE-450 and KYSE-70 cells[1]. SHMT2-IN-1 (2.5-7.5 μM, 24-72 h) induces apoptosis, ROS production and cause G2/M phase arrest in KYSE-450 and KYSE-70 cells[1].
References:
[1]. Akram HMB, et al. Discovery of W478, a novel SHMT2 inhibitor for the treatment of esophageal carcinoma. Bioorg Chem. 2025 Oct;165:109028.
In Vitro, SHMT2-IN-1 (0.1-10 μM, 24 h) exhibits potent antiproliferative activity against esophageal cancer cells KYSE-450 and KYSE-70 with IC50 values of 1.62 μM and 1.18 μM respectively[1]. SHMT2-IN-1 (2.5-10 μM, 24 h) dose-dependently inhibits the migration and invasion of KYSE-450 and KYSE-70 cells[1]. SHMT2-IN-1 (2.5-7.5 μM, 24-72 h) induces apoptosis, ROS production and cause G2/M phase arrest in KYSE-450 and KYSE-70 cells[1].
References:
[1]. Akram HMB, et al. Discovery of W478, a novel SHMT2 inhibitor for the treatment of esophageal carcinoma. Bioorg Chem. 2025 Oct;165:109028.