| Description | UCM-1336 (3,3′-(Octylimino)bis[N-phenylpropanamide]) is a potent ICMT inhibitor with an IC50 of 2 μM which is selective against the other enzymes involved in the post-translational modifications of Ras. |
| In vitro | UCM-1336显著降低了四种Ras亚型与膜的结合，导致Ras活性下降和Ras下游信号传导途径的抑制。UCM-1336在多种Ras突变的肿瘤细胞系中诱导细胞死亡，并在急性髓系白血病的活体模型中提高生存率。由于ICMT抑制剂不论激活突变如何都能降低四种Ras亚型的活性，UCM-1336克服了迄今所描述的可用Ras抑制剂的许多常见限制[2]。 |
| In vivo | UCM-1336 显著抑制了小鼠中的胶质母细胞瘤生长，且未引起毒性反应[1]。 |
| Target activity | ICMT:2 μM |
| Synonyms | 3,3′-(Octylimino)bis[N-phenylpropanamide] |
| molecular weight | 423.59 |
| Molecular formula | C26H37N3O2 |
| CAS | 1621535-90-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 11 mg/mL (25.97 mM) |
| References | 1. Wan W, et al. Isoprenylcysteine carboxyl methyltransferase is critical for glioblastoma growth and survival by activating Ras/Raf/Mek/Erk. Cancer Chemother Pharmacol. 2022 Mar;89(3):401-411. 2. Marín-Ramos NI, et al. A Potent Isoprenylcysteine Carboxylmethyltransferase (ICMT) Inhibitor Improves Survival in Ras-Driven Acute Myeloid Leukemia. J Med Chem. 2019 Jul 11;62(13):6035-6046. |