1240580-64-6
Chemical Structure
YL064
- CAS No.: 1240580-64-6
- Formula:C25H27NO4S
- Molecular Weight:437.55
InChIKey: DNCWZYWKEAGSRP-ZQJPODCASA-N
SMILES: CC(C=C1)=CC=C1S[C@@H]2C(C=CC(O)=C3O)=C3[C@@]4(CC(C(OC)=C5)=O)[C@]5([H])[C@@H]2N(CC4)C
Biological Activity: YL064 is a multi-target STAT3-c-MYC inhibitor that directly binds to ATXN3 and inhibits its deubiquitinating activity, thereby promoting the ubiquitination and proteasomal degradation of oncogenic substrates of ATXN3. YL064 inhibits the phosphorylation of STAT3-Tyr705 without altering the total protein level of STAT3; meanwhile, it directly binds to the SH2 domain of STAT3 to block the dimerization, nuclear translocation, and DNA-binding activity of STAT3. YL064 directly targets the C-terminal HLH-Zip domain of c-Myc, upregulates the phosphorylation of c-Myc at the Thr58 site, and induces the ubiquitination and proteasome-dependent degradation of c-Myc. YL064 suppresses tumor cell proliferation, induces G2/M cell cycle arrest, reduces cell migration and invasion capacities, and triggers cancer cell apoptosis. YL064 can be used in related research on breast cancer, prostate cancer, diffuse large B-cell lymphoma, and multiple myeloma[1][2][3].
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YL064 | YL064 is a multi-target STAT3-c-MYC inhibitor that directly binds to ATXN3 and inhibits its deubiquitinating activity, thereby promoting the ubiquitination and proteasomal degradation of oncogenic substrates of ATXN3. YL064 inhibits the phosphorylation of STAT3-Tyr705 without altering the total protein level of STAT3; meanwhile, it directly binds to the SH2 domain of STAT3 to block the dimerization, nuclear translocation, and DNA-binding activity of STAT3. YL064 directly targets the C-terminal HLH-Zip domain of c-Myc, upregulates the phosphorylation of c-Myc at the Thr58 site, and induces the ubiquitination and proteasome-dependent degradation of c-Myc. YL064 suppresses tumor cell proliferation, induces G2/M cell cycle arrest, reduces cell migration and invasion capacities, and triggers cancer cell apoptosis. YL064 can be used in related research on breast cancer, prostate cancer, diffuse large B-cell lymphoma, and multiple myeloma. | |||||||||||||||||||||
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References
- [1]. Zhang Z, et al. Identification of YL064 as a novel inhibitor of ATXN3 to suppress tumor growth and metastasis by promoting degradation of oncogenic substrates. Cell Death & Disease. August 6, 2026.
- [2]. Shan H, et al. YL064 activates proteasomal-dependent degradation of c-Myc and synergistically enhances the anti-tumor activity of ABT-199 in diffuse large B cell lymphoma. Signal Transduct Target Ther. 2020 Jul 6;5(1):116.
- [3]. Wang Y, et al. YL064 directly inhibits STAT3 activity to induce apoptosis of multiple myeloma cells. Cell death discovery. 2018;4:44.
