| CAS |
65836-72-8 |
| Chinese Name |
2-氯-N-((3,4-二甲氧苯基)甲基)乙酰胺 |
| English Name |
(2-chloro-N) - 3, 4-dimethoxybenzyl acetamide |
| Synonyms |
DKM 2-93 |
| Molecular Formula |
C11H14ClNO3 |
| Molecular Weight |
243.69 |
| Solubility |
Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
| Purity |
≥98% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| 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 |
| Target Point |
UBA5 |
| Passage |
Ubiquitin |
| Background |
(2-chloro-N)-3,4-dimethoxybenzyl acetamide is a selective inhibitor of ubiquitin-like modifier activating enzyme 5 (UBA5). |
| Biological Activity |
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]. |
| Cell Experiment |
PaCa2 and Panc1 cells are treated with 0-1000 μM DKM 2-93 for 48 hours. Cell viability is assessed by Hoescht stain[1]. |
| Animal Experiment |
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]. |
| Data Literature Source |
[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. |
| Unit |
Bottle |
| Specification |
50mg |
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