| 生物活性： |
靶点：UBA5
通路：Ubiquitin
背景说明：(2-chloro-N) - 3, 4-dimethoxybenzyl acetamide是一种泛素样修饰物激活酶5(UBA5)的选择性抑制剂。
生物活性：DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.[1]
IC50：IC50: 430μM(UBA5);90μM(PaCa2 cells);30μM(Panc1 cells)[1]
In Vitro：Ubiquitin-like modifier activating enzyme 5(UBA5)is a novel pancreatic cancer therapeutic target. DKM 2-93 impairs pancreatic cancer cell survival through covalently modifying the catalytic cysteine of UBA5，thereby inhibiting its activity as a protein that activates the ubiquitin-like protein UFM1 to UFMylate proteins. DKM 2-93 inhibits PaCa2 and Panc1 cells survival with IC50s of 90 and 30 μM，respectively[1].
In Vivo：DKM 2-93 daily treatment significantly impairs tumor growth of PaCa2 cells in vivo in tumor xenograft studies in immune-deficient mice without causing any weight loss or overt toxicity[1].
细胞实验：PaCa2 and Panc1 cells are treated with 0-1000 μM DKM 2-93 for 48 hours. Cell viability is assessed by Hoescht stain[1].
动物实验：Mice: Mice are subcutaneously injected with PaCa2 cells to initiate the tumor xenograft study and treatments of mice are initiated with vehicle or DKM 2-93(50 mg/kg ip，once per day)three days after injection of cancer cells[1].
数据来源文献：[1]. Roberts AM， et al. Chemoproteomic Screening of Covalent Ligands Reveals UBA5 As a Novel Pancreatic Cancer Target. ACS Chem Biol. 2017 Apr 21;12(4):899-904.
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| 其它标识： |
EC：EINECS 604-604-1
MDL：MFCD01733639
SMILES：O=C(NCC1=CC=C(OC)C(OC)=C1)CCl
InChIKey：CETPWRGZGWGPSV-UHFFFAOYSA-N
InChI：InChI=1S/C11H14ClNO3/c1-15-9-4-3-8(5-10(9)16-2)7-13-11(14)6-12/h3-5H,6-7H2,1-2H3,(H,13,14)
PubChem CID：2392259
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| 基本信息： |
CAS：65836-72-8
中文名称：2-氯-N-((3,4-二甲氧苯基)甲基)乙酰胺
英文名称：(2-chloro-N) - 3, 4-dimethoxybenzyl acetamide
别名：DKM 2-93
分子式：C11H14ClNO3
分子量：243.69
规格：50mg
溶解性：Soluble in DMSO ≥5mg/mL(Need ultrasonic)
纯度：≥98%
外观(性状)：White to off-white Solid
储存条件：Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
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| 靶点： |
UBA5 |
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