| Description | Zt-12-037-01 is a ATP competitive STK19 inhibitor（IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N),respectively). |
| In vitro | ZT-12-037-01 显著抑制突变型NRAS-STK19驱动的黑色素细胞群体形成和增殖。 |
| In vivo | ZT-12-037-01 作为一种特异性的 STK19 靶向抑制剂，能有效阻断致癌的 NRAS 驱动的黑色素细胞恶性转化和体内的黑色素瘤生长。 |
| Animal experiments | ZT-12-037-01 (injection subcutaneously; 25-50 mg/kg; once daily; 21 days) inhibits growth of SK-MEL-2 xenograft melanoma and the sections of tumors indicates induction of apoptosis by increasing cleaved caspase-3. |
| Target activity | STK19 (WT):23.96 nM , STK19 (D89N):27.94 nM |
| molecular weight | 385.5 |
| Molecular formula | C21H31N5O2 |
| CAS | 2328073-61-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 41 mg/mL (106.36 mM) |
| References | 1. Yin C, Zhu B, Zhang T, et al.Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis[J].Cell. 2019 Feb 21;176(5):1113-1127. |