65836-72-8

65836-72-8 structure

Name	2-chloro-N-[(3,4-dimethoxyphenyl)methyl]acetamide
Synonyms	Chlor-essigsaeure-veratrylamid N-chloroacetyl-3,4-dimethoxybenzylamine C-Chlor-N-veratryl-acetamid 2-chloro-N-(3,4-dimethoxybenzyl)acetamide chloro-acetic acid veratrylamide N-(3.4-Dimethoxy-benzyl)-chloracetamid 2-Chloro-N-((3,4-dimethoxyphenyl)methyl)acetamide N-(Dimethoxy-3,4 benzyl)-chloroacetamide [French] Acetamide,2-chloro-N-((3,4-dimethoxyphenyl)methyl) N-Chloracetyl-(3,4-dimethoxyphenyl)methylamin DKM 2-93

Description	DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
Related Catalog	Signaling Pathways >> Metabolic Enzyme/Protease >> E1/E2/E3 Enzyme Research Areas >> Cancer
Target	IC50: 430 μM (UBA5), 90 μM (PaCa2 cells), 30 μM (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 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 Admin	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.

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: APFRAD Annales Pharmaceutiques Francaises. (SPPIF, B.P.22, F-41353 Vineuil, France) V.1- 1943- Volume(issue)/page/year: 41,457,1983

Hazard Codes	Xi
HS Code	2924299090

5763-61-1

79-04-9

~87%

65836-72-8

5763-61-1

79-11-8

65836-72-8

Literature: Quevedo, Rodolfo; Baquero, Edwin; Rodriguez, Mario Tetrahedron Letters, 2010 , vol. 51, # 13 p. 1774 - 1778

53527-20-1

77-78-1

65836-72-8

Literature: Jacobs; Heidelberger Journal of Biological Chemistry, 1915 , vol. 20, p. 674

91-16-7

2832-19-1

65836-72-8

Literature: Monti Gazzetta Chimica Italiana, 1930 , vol. 60, p. 777,778

HS Code	2924299090
Summary	2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%