Bioactivity | Y-29794 tosylate is a selective, orally active inhibitor for non-peptide prolyl endopeptidase (PPCE), with an IC50 of 3 nM and a Ki of 0.95 nM. Y-29794 tosylate enhances the effect of thyrotropin-releasing hormone (TRH) on the release of ACh in the rat hippocampus, exhibits potential neuroprotective efficacy. Y-29794 tosylate exhibits anticancer activity through inhibition of the IRS1-AKT-mTORC1 pathway. Y-29794 tosylate penetrates the brain-blood barrier (BBB)[1][2]. |
Invitro | Y-29794 tosylate 抑制 TNBC 癌细胞 BT20、BT549、MDA453、DU4475、MDA 231、MDA468 和 SUM159PT 的增殖 (0-10 μM, 4 days), 在 G1/sub G1 期阻滞细胞周期 (0-10 μM, 48 h),诱导细胞死亡 (5-10 mM)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Y-29794 tosylate 相关抗体: Cell Proliferation Assay[1] Cell Line: |
In Vivo | Y-29794 tosylate (12.5-50 mg/kg,腹腔注射,每天,每周 5 天,持续 5 周) 在 NOD-SCID 小鼠模型中表现出对三阴性乳腺癌的抗肿瘤活性,且无明显毒性[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 143984-17-2 |
Formula | C30H42N2O4S3 |
Molar Mass | 590.86 |
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]. Perez RE, et al. Prolyl endopeptidase inhibitor Y-29794 blocks the IRS1-AKT-mTORC1 pathway and inhibits survival and in vivo tumor growth of triple-negative breast cancer. Cancer Biol Ther. 2020 Nov 1;21(11):1033-1040. [2]. Perez RE, et al., Prolyl endopeptidase inhibitor Y-29794 blocks the IRS1-AKT-mTORC1 pathway and inhibits survival and in vivo tumor growth of triple-negative breast cancer. Cancer Biol Ther. 2020 Nov 1;21(11):1033-1040. |