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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-DF-A7
DF-A7

Chemical Structure : DF-A7

CAS No.: 105580-96-9

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DF-A7 (YTHDF2 inhibitor DF-A7)

货号: PC-22438Not For Human Use, Lab Use Only.

DF-A7 a specific small-molecule degrader/inhibitor of m6A reader YTHDF2 with IC50 of 50 nM in immunoblotting assays (HEK 293T cells), induces degradation of YTHDF2 without affecting the degradation of YTHDF1 and YTHDF3.

规格 价格 库存 数量
5 mg ￥2580 In stock
10 mg ￥3980 In stock
25 mg ￥5980 In stock
50 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

DF-A7 a specific small-molecule degrader/inhibitor of m6A reader YTHDF2 with IC50 of 50 nM in immunoblotting assays (HEK 293T cells), induces degradation of YTHDF2 without affecting the degradation of YTHDF1 and YTHDF3.
DF-A7 predictively binds to the YTHDF2 protein at the K416, G463, K521, N518, and R527 sites, forming a total of seven hydrogen bonds.
DF-A7 increases the mRNA expression of Cx3cl1 and PRR5 after degrading YTHDF2.
DF-A7 (12.5 mg/kg) significantly inhibited tumor growth compared with vehicle control in both MC38 and B16-OVA tumor models, significantly prolonged the survival of mice.
DF-A7 inhibits tumor growth and improves antitumor efficacy when in combination with PD-1/PD-L1 blockade therapy.

物理化学性质&存储条件

分子量 446.50
分子式 C22H30N4O6
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

5,8-bis((2-((2-hydroxyethyl)amino)ethyl)amino)anthracene-1,4,9,10-tetraol

参考文献

1. Xiao S, et al. Sci Immunol. 2024 May 31;9(95):eadl2171.

2. Durand M, et al. J Exp Clin Cancer Res. 2024 May 22;43(1):148.

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