| Bioactivity | (+)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]. |
| Target | Serine hydroxymethyltransferase (SHMT) |
| Invitro | (+)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]. |
| In Vivo | (+)SHIN2 (200 mg/kg; i.p.; single dose) shows therapeutic activity in mouse primary T-ALL in vivo[1]. Animal Model: |
| Name | (+)SHIN2 |
| Formula | C23H26N4O3 |
| Molar Mass | 406.48 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |