| Bioactivity | ERX-41 is an orally active and stereospecific small molecule targeting to lysosomal acid lipase A (LIPA). ERX-41 induces endoplasmic reticulum (ER) stress resulting in cell death, indicating a function independent of LIPA but dependent on its ER localization. ERX-41 involves in a targeted strategy for solid tumors[1]. |
| Target | Lysosomal acid lipase A (LIPA) |
| Invitro | ERX-41 (1 μM; 0-30 h) 诱导 MDA-MB-231 细胞死亡，对正常人乳腺上皮细胞 (HMECs) 无显著影响[1]。ERX-41 (1 μM; 2 h, 4 h) 在 4 h 内诱导内质网急剧扩张，并在 2 h 内导致外周内质网紊乱[1]。ERX-41 (1 μM; 0.5-4 h) 通过诱导 p-PERK 和 p-eIF2-α，诱导下游未折叠蛋白反应 (UPR) 通路[1]。 Cell Viability Assay[1] Cell Line: |
| In Vivo | ERX-41 (10 mg/kg; 口服或腹腔注射；单次剂量) 在口服或腹腔注射后，都能够在 1.5 h 内在肿瘤内被检测到[1]。ERX-41 (10 mg/kg; 口服; 单次剂量) 显著抑制 MDA-MB-231 异种移植小鼠模型中的肿瘤进展而不改变小鼠体重[1]。ERX-41 (10 mg/kg; 口服; 单次剂量) 显著抑制 D2A1 异种移植小鼠模型的疾病进展[1]。 Animal Model: |
| Name | ERX-41 |
| CAS | 2440087-54-5 |
| Formula | C38H48N4O9 |
| Molar Mass | 704.81 |
| 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]. Liu X, et al. Targeting LIPA independent of its lipase activity is a therapeutic strategy in solid tumors via induction of endoplasmic reticulum stress. Nat Cancer. 2022 Jul;3(7):866-884. |