LAF-153 

LAF-153 is a Methionine Aminopeptidase-2 (MetAP-2) inhibitor with human IC₅₀ values of 0.074 μM and 0.16 μM.LAF-153 has a t-butyl group extending into the innermost portion of the MetAP-2 cleft, a lactam ring coordinated in the enzyme’s shallow surface pocket, and three hydroxyl groups coordinating to the two cobalt ions in the enzyme’s active site^[1].

LAF-153 reversibly binds to human MetAP-2 via coordination of its hydroxyl groups to the enzyme's cobalt ions, with its t-butyl group and lactam ring occupying distinct pockets in the enzyme cleft^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

388.46

C₁₈H₃₂N₂O₇

661482-39-9

CC(C)(C)/C=C/[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC)C(N[C@@H]1C(NC[C@@H](CC1)O)=O)=O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Heinrich T, et al. Discovery and structure-based optimization of next-generation reversible methionine aminopeptidase-2 (MetAP-2) inhibitors[J]. Journal of medicinal chemistry, 2019, 62(10): 5025-5039.  [Content Brief]