GSK-3685032是一种非时间依赖性、非共价、可逆的DNMT1选择性抑制剂,IC50为0.036 μM。GSK-3685032诱导DNA去甲基化、转录激活和抑制癌细胞生长。


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| 产品名称 | DNA Methyltransferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 6-Thioguanine | ✔ | 98% | |||||||||||||||||
| Zebularine | ✔ | 98% | |||||||||||||||||
| Procainamide HCl | ✔ | 99% | |||||||||||||||||
| 5-Azacytidine | ✔ | 95% | |||||||||||||||||
| Decitabine | ✔ | 99% | |||||||||||||||||
| SGI-1027 |
++
DNMT3A, IC50: 7.5 μM DNMT1, IC50: 6 μM |
99%+ | |||||||||||||||||
| RG108 |
+++
DNA methyltransferase, IC50: 115 nM |
99%+ | |||||||||||||||||
| Guadecitabine sodium | ✔ | 98% | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| Concentration | Treated Time | Description | References | |
| ES-2 | 100 nM, 500 nM, 1 μM, or 5 μM | 1, 2, or 4 days | To evaluate the effect of GSK-3685032 on ORF1p expression in ES-2 cells, results showed that GSK-3685032 robustly induced ORF1p expression within 4 days without appreciable DNA damage. | NPJ Precis Oncol. 2025 Mar 6;9(1):62 |
| 12Z | 100 nM, 500 nM, 1 μM, or 5 μM | 1, 2, or 4 days | To evaluate the effect of GSK-3685032 on ORF1p expression in 12Z cells, results showed that GSK-3685032 robustly induced ORF1p expression within 4 days without appreciable DNA damage. | NPJ Precis Oncol. 2025 Mar 6;9(1):62 |
| hEM3 | 100 nM, 500 nM, 1 μM, or 5 μM | 1, 2, or 4 days | To evaluate the effect of GSK-3685032 on ORF1p expression in hEM3 cells, results showed that GSK-3685032 robustly induced ORF1p expression within 4 days without appreciable DNA damage. | NPJ Precis Oncol. 2025 Mar 6;9(1):62 |
| KRAS mutant NSCLC cells | 10 nM | Evaluate the effect of DNMT1 inhibition on 3D growth, results showed similar to UHRF1 knockout, significantly inhibiting spheroid growth | Nat Commun. 2023 Jul 5;14(1):3966 | |
| MDS-L cells | 1 µM | 4 days | To assess the sensitivity of MDS-L cells to GSK-3685032, results showed no significant difference in sensitivity between TOPORS-edited and control cells. | Nat Commun. 2024 Aug 28;15(1):7360 |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | MV4–11 and SKM-1 subcutaneous xenograft models | Subcutaneous injection | 1 to 45 mg/kg | Twice daily for ≥4 weeks | To evaluate the in vivo efficacy and tolerability of GSK3685032 in AML models | Nat Cancer. 2021 Oct;2(10):1002-1017 |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.38mL 0.48mL 0.24mL |
11.89mL 2.38mL 1.19mL |
23.78mL 4.76mL 2.38mL |
|
| CAS号 | 2170137-61-6 |
| 分子式 | C22H24N6OS |
| 分子量 | 420.53 |
| SMILES Code | O=C(N)C(SC1=NC(N2CCC(N)CC2)=C(C#N)C(CC)=C1C#N)C3=CC=CC=C3 |
| MDL No. | N/A |
| 别名 | |
| 运输 | 蓝冰 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
DMSO: 25 mg/mL(59.45 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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