(+)SHIN2 

(+)SHIN2 is a serine hydroxymethyltransferase (SHMT) inhibitor, whose target can be traced with ¹³C-serine. (+)SHIN2 increases survival in NOTCH1-driven mouse primary acute lymphoblastic leukemia (T-ALL) in vivo with a synergistic effect with Methotrexate (HY-14519)^[1]. (+)SHIN2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Serine hydroxymethyltransferase (SHMT)^[1]

(+)SHIN2 (0-10 μM; 24 h) blocks proliferation of HCT116 Ras-driven colon cancer cells, in a stereoselective manner with an IC₅₀ value of 300 nM^[1].
(+)SHIN2 (0-100 μM; 48 h) achieves a nearly complete blockade of SHMT activity as evidenced by the decrease in M+1 and M+2 serine, M+2 glycine, and the incorporation of serine-derived glycine and 1C units into ATP, GTP, and dTTP (M+1-M+4 ATP and GTP and M+1 dTTP), and inhibits human T-ALL cell line Molt4 growth with a IC₅₀ value of 89 nM^[1].
(+)SHIN2 (2 μM; 24 h) arrests cell cycle at S phase^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

(+)SHIN2 (200 mg/kg; i.p.; single dose) shows therapeutic activity in mouse primary T-ALL in vivo^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

406.48

C₂₃H₂₆N₄O₃

固体

White to light yellow

Room temperature in continental US; may vary elsewhere.

• [1]. García-Cañaveras JC, et al. SHMT inhibition is effective and synergizes with methotrexate in T-cell acute lymphoblastic leukemia. Leukemia. 2021 Feb;35(2):377-388.  [Content Brief]