3060730-06-2
Chemical Structure
MS8709
- CAS No.: 3060730-06-2
- Formula:C64H95F2N11O7S
- Molecular Weight:1200.57
InChIKey: CLUWNSLFLMBFKA-RMCUFUCFSA-N
SMILES: O=C([C@H]1N(C([C@@H](NC(CCCCCCCCCCCNC(CCCN2CCC(NC3=C4C=C(OC)C(OCCCN5CCCC5)=CC4=NC(N6CCC(F)(F)CC6)=N3)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
Biological Activity: MS8709 is a PROTAC degrader that induces the degradation of G9a (EHMT2)/GLP (EHMT1) by recruiting VHL. MS8709 induces G9a/GLP protein degradation via a mechanism that simultaneously depends on G9a/GLP target protein binding, VHL recruitment, and the ubiquitin-proteasome system (UPS), while the mRNA levels of G9a and GLP do not show significant changes, indicating that the effect occurs primarily at the protein level rather than the transcriptional level. MS8709 retains the inhibitory effect on G9a/GLP methyltransferase activity and reduces H3K9me2 levels, thereby simultaneously affecting the catalytic and non-catalytic functions of G9a/GLP. MS8709 can be used for studies related to G9a/GLP biology, prostate cancer, lung cancer, and other relevant fields[1][2].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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MS8709 | 99.87% | MS8709 is a PROTAC degrader that induces the degradation of G9a (EHMT2)/GLP (EHMT1) by recruiting VHL. MS8709 induces G9a/GLP protein degradation via a mechanism that simultaneously depends on G9a/GLP target protein binding, VHL recruitment, and the ubiquitin-proteasome system (UPS), while the mRNA levels of G9a and GLP do not show significant changes, indicating that the effect occurs primarily at the protein level rather than the transcriptional level. MS8709 retains the inhibitory effect on G9a/GLP methyltransferase activity and reduces H3K9me2 levels, thereby simultaneously affecting the catalytic and non-catalytic functions of G9a/GLP. MS8709 can be used for studies related to G9a/GLP biology, prostate cancer, lung cancer, and other relevant fields. | ||||||||||||||||||||
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References
- [1]. Velez J, et al. Discovery of the First-in-Class G9a/GLP PROTAC Degrader. Journal of medicinal chemistry. 2024 Apr 25;67(8):6397-6409. [Content Brief]
- [2]. Mukherjee A, et al. A Novel PROTAC G9a/GLP Degrader that Inhibits, Similar to G9a siRNA, the Migration of MCF-7 Breast-Cancer Cells without Affecting Proliferation. Journal of medicinal chemistry. 2025 Sep 11;68(17):18258-18271. [Content Brief]
