MS8709 | G9a/GLP degrader | Probechem Biochemicals

Chemical Structure : MS8709

加入收藏

MS8709 (MS-8709)

货号: PC-22157Not For Human Use, Lab Use Only.

MS8709 is a potent, selective first-in-class G9a/GLP proteolysis targeting chimera (PROTAC) degrader with DC50 of 274/260 nM in 22Rv1 cells, respectively.

规格	价格	库存	数量
10 mg		Get quote
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

MS8709 is a potent, selective first-in-class G9a/GLP proteolysis targeting chimera (PROTAC) degrader with DC50 of 274/260 nM in 22Rv1 cells, respectively.
MS8709 potently inhibits 22Rv1 cell growth with GI50 of 4.1 uM, but not the parent inhibitor UNC0642.
MS8709 induces G9a/GLP protein degradation in a VHL- and UPS-dependent manner and is a bona fide G9a/GLP PROTAC degrader.
MS8709 does not induce the degradation of EZH2, PRMT7, and SET7/9, also shows no significant inhibition in a panel of 21 protein methyltransferases.
MS8709 (3 uM) effectively degrades G9a and GLP and displays superior antiproliferative activity in K562 and H1299 cells compared to UNC0642, inhibits cell growth H1299 cells with GI50 of 5 uM.
MS8709 has sufficient mouse PK properties and is suitable for in vivo efficacy studies.

物理化学性质&存储条件

分子量	1200.59
分子式	C64H95F2N11O7S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(2S,4R)-1-((S)-2-(12-(4-(4-((2-(4,4-Difluoropiperidin-1-yl)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazolin-4-yl)amino)piperidin-1-yl)butanamido)dodecanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

参考文献

1. Velez J, et al. Cancer Res (2024) 84 (6_Supplement): 4511.

2. Velez J, et al. J Med Chem. 2024 Apr 11. doi: 10.1021/acs.jmedchem.3c02394.

MS8709 (MS-8709)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

MS8709 (MS-8709)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.