| 产品描述: | (+)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 . (+)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. |
| 靶点: |
Serine hydroxymethyltransferase (SHMT) |
| 体外研究: |
(+)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. (+)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. (+)SHIN2 (2 μM; 24 h) arrests cell cycle at S phase. |
| 体内研究: |
(+)SHIN2 (200 mg/kg; i.p.; single dose) shows therapeutic activity in mouse primary T-ALL in vivo. |
| 参考文献: |
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.
|
| 保存条件: |
-20°C |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.46 ml |
12.301 ml |
24.601 ml |
| 5 mM |
0.492 ml |
2.46 ml |
4.92 ml |
| 10 mM |
0.246 ml |
1.23 ml |
2.46 ml |
| 50 mM |
0.049 ml |
0.246 ml |
0.492 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |