DKM 2-93

• CAT Number: I013660
• CAS Number: 65836-72-8
• Molecular Formula: C11H14ClNO3
• Molecular Weight: 243.69
• Purity: ≥95%
• Synonyms: 2-chloro-N-[(3,4-dimethoxyphenyl)methyl]acetamide
• 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)
• InChIKey: CETPWRGZGWGPSV-UHFFFAOYSA-N
• SMILES: COC1=C(C=C(C=C1)CNC(=O)CCl)OC

DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
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].
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].

Reference

[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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