2716909-84-9
Chemical Structure
AP-4-139B
- CAS No.: 2716909-84-9
- Formula:C34H33BrN3PS
- Molecular Weight:626.59
InChIKey: DVNFYDQLZWXBCJ-UHFFFAOYSA-M
SMILES: C1([P+](C2=CC=CC=C2)(C3=CC=CC=C3)CCCCCCC4=NN5C=C(N=C5S4)C6=CC=CC=C6)=CC=CC=C1.[Br-]
Biological Activity: AP-4-139B is a blood-brain barrier-permeable HSP70 inhibitor with a IC50 of 180 nM against hHSP70. AP-4-139B binds directly to HSP70 and inhibits its ATPase activity. AP-4-139B promotes Autophagy by increasing the phosphorylation of Beclin-1. AP-4-139B exerts antitumor effects in preclinical models of colorectal cancer and pancreatic ductal adenocarcinoma[1][2].
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AP-4-139B | 98.87% | AP-4-139B is a blood-brain barrier-permeable HSP70 inhibitor with a IC50 of 180 nM against hHSP70. AP-4-139B binds directly to HSP70 and inhibits its ATPase activity. AP-4-139B promotes Autophagy by increasing the phosphorylation of Beclin-1. AP-4-139B exerts antitumor effects in preclinical models of colorectal cancer and pancreatic ductal adenocarcinoma. | ||||||||||||||||||||
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- [1]. Barnoud T, et al. A Novel Inhibitor of HSP70 Induces Mitochondrial Toxicity and Immune Cell Recruitment in Tumors. Cancer Res. 2020;80(23):5270-5281. [Content Brief]
- [2]. Ferretti GDS, et al. HSP70-mediated mitochondrial dynamics and autophagy represent a novel vulnerability in pancreatic cancer. Cell Death Differ. 2024;31(7):881-896. [Content Brief]
Keywords
