MS-8709 is a G9a/GLP PROTAC Degrader (DC50 (G9a) = 274 nM; DC50 (GLP) = 260 nM). MS-8709 induces G9a/GLP degradation in a concentration-, time-, and ubiquitin-proteasome system (UPS)-dependent manner. Futhermore, MS-8709 does not alter the mRNA expression of G9a/ GLP and is selective for G9a/GLP over other methyltransferases. Moreover, MS-8709 displays superior cell growth inhibition to the parent G9a/GLP inhibitor UNC0642 in prostate, leukemia, and lung cancer cells and has suitable mouse pharmacokinetic properties for in vivo efficacy studies.
MedKoo Cat#: 126768
Name: MS-8709
CAS#: 3060730-06-2
Chemical Formula: C64H95F2N11O7S
Exact Mass: 1199.7105
Molecular Weight: 1200.59
Elemental Analysis: C, 64.03; H, 7.98; F, 3.16; N, 12.83; O, 9.33; S, 2.67
The following data is based on the product molecular weight 1,200.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
