DKM 2-93

Cas No.:	65836-72-8
Chemical Name:	2-Chloro-N-(3,4-dimethoxybenzyl)acetamide
Synonyms:	2-Chloro-N-(3,4-dimethoxybenzyl)acetamide;2-chloro-N-[(3,4-dimethoxyphenyl)methyl]acetamide;2-Chloro-N-((3,4-dimethoxyphenyl)methyl)acetamide;Acetamide,2-chloro-N-((3,4-dimethoxyphenyl)methyl);C-Chlor-N-veratryl-acetamid;Chlor-essigsaeure-veratrylamid;chloro-acetic acid veratrylamide;N-(3.4-Dimethoxy-benzyl)-chloracetamid;N-(Dimethoxy-3,4 benzyl)-chloroacetamide [French];N-Chloracetyl-(3,4-dimethoxyphenyl)methylamin;N-chloroacetyl-3,4-dimethoxybenzylamine;DKM 2-93
SMILES:	O=C(NCC1=CC=C(OC)C(OC)=C1)CCl
Formula:	C11H14NO3Cl
M.Wt:	243.68676
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
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].
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].
Cell Assay:	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 Administration:	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].
References:	[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.