Bioactivity | Deltazinone 1, a pyrazolopyridazinone, is a highly selective PDEδ inhibitor with a KD of 8 nM. Deltazinone 1 inhibits the PDEδ-Ras interaction. Deltazinone 1 shows a dose-dependent inhibitory response on proliferation in oncogenic KRas-dependent cell lines[1][2]. |
Invitro | Deltazinone 1 (0.375-24 μM; 0-120 小时) 以剂量依赖性方式抑制细胞生长[1]。 Deltazinone 1 (20 μM; 1小时) 降低 KRas 依赖性 Panc-Tu-I 细胞中的 S6P 磷酸化[1]。 Deltazinone 1 (10μM) 显示致癌 KRas 依赖性 Panc-Tu-I 细胞死亡,但不显示致癌 KRas 非依赖性 PANC-1 细胞[1]。 Cell Viability Assay[1] Cell Line: |
Name | Deltazinone 1 |
CAS | 894554-89-3 |
Formula | C27H31N5O2 |
Molar Mass | 457.57 |
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]. Björn Papke, et al. Identification of pyrazolopyridazinones as PDEδ inhibitors. Nat Commun. 2016 Apr 20;7:11360. [2]. Pablo Martín-Gago, et al. Structure-based development of PDEδ inhibitors. Biol Chem. 2017 May 1;398(5-6):535-545. |