| Description | SHIN1 (RZ-2994) is an inhibitor of human serine hydroxymethyltransferse 1(SHMT1) with IC50 of 5 nM and human serine hydroxymethyltransferse 2 (SHMT2) with an IC50 of 13 nM. |
| In vitro | SHIN1 inhibits the growth of SHMT2 deletion HCT-116 cells (IC50: 10 nM). SHIN1 inhibits SHMT1/2 in HCT-116 cells. SHIN1 is particularly active against B-cell malignancies. SHIN1 blocks cell growth through a progressive depletion of purines, leading to loss of nucleotide triphosphates [1]. |
| Target activity | SHMT1:5 nM, SHMT2:13 nM |
| Synonyms | RZ-2994 |
| molecular weight | 400.47 |
| Molecular formula | C24H24N4O2 |
| CAS | 2146095-85-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 50 mg/mL (124.85 mM) |
| References | 1. Ducker GS, et al. Human SHMT inhibitors reveal defective glycine import as a targetable metabolic vulnerability of diffuse large B-cell lymphoma. Proc Natl Acad Sci U S A. 2017 Oct 24;114(43):11404-11409. |
| Citations | 1. Liufu T, Zhao X, Yu M, et al.Multiomics analysis reveals serine catabolism as a potential therapeutic target for MELAS.The FASEB Journal.2024, 38(12): e23742. |