Bioactivity | PPI-GIT1/β-Pix interaction-IN-1 is a potent and orally active GIT1/β-Pix protein-protein interaction (PPI) inhibitor with a KD value of 7.7 µM. PPI-GIT1/β-Pix interaction-IN-1 disrupts the GIT/PIX interaction can impact the activation of the downstream Rho GTPase Rac1 and Cdc42. PPI-GIT1/β-Pix interaction-IN-1 inhibits metastasis of gastric cancer[1]. |
Invitro | PPI-GIT1/β-Pix interaction-IN-1 (compound 14-5-18; 0-50 μM) 抑制活细胞中 GIT1 和 β-Pix 之间的相互作用[1]。PPI-GIT1/β-Pix interaction-IN-1 (0-50 μM; 24 小时; MGC803 细胞和 MKN45 细胞) 以剂量依赖的方式抑制胃癌细胞侵袭,破坏 GIT/PIX 相互作用可影响下游 Rho GTPase Rac1 和 Cdc42[1]。 Western Blot Analysis[1] Cell Line: |
In Vivo | PPI-GIT1/β-Pix interaction-IN-1 (compound 14-5-18; 10 and 30 mg/kg; i.g.; 24 h) 抑制 MGC803 异种移植雌性裸鼠胃癌细胞侵袭[1] 。 Animal Model: |
Name | PPI-GIT1/β-Pix interaction-IN-1 |
Formula | C23H21NO5 |
Molar Mass | 391.42 |
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]. Gu J, et, al. Construction of a synthetic methodology-based library and its application in identifying a GIT/PIX protein-protein interaction inhibitor. Nat Commun. 2022 Nov 23;13(1):7176. |