| Bioactivity | KLH45 is a potent and selective DDHD2 inhibitor, with an IC50 of 1.3 nM[1]. | ||||||||||||
| Invitro | KLH45 (25 nM, 4 h) completely inactivats DDHD2 (>95% inhibition) in Neuro2A cells and shows no cross-reactivity with any of the other 40+ detected serine hydrolases with the exception of ABHD6[1].KLH45 (2 μM) increases LD formation in fatty acid-supplemented DDHD2-expressing cells[2]. Cell Viability Assay[2] Cell Line: | ||||||||||||
| In Vivo | KLH45 (20 mg/kg; administered every 12 h) for a total of 4 d exhibits significant elevations in several of the TAGs that accumulated in the brains of DDHD2−/− mice[1]. Animal Model: | ||||||||||||
| Name | KLH45 | ||||||||||||
| CAS | 1632236-44-2 | ||||||||||||
| Formula | C24H25F3N4O2 | ||||||||||||
| Molar Mass | 458.48 | ||||||||||||
| Appearance | Solid-liquid mixture | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Jordon M Inloes, et al. The hereditary spastic paraplegia-related enzyme DDHD2 is a principal brain triglyceride lipase. Proc Natl Acad Sci U S A. 2014 Oct 14;111(41):14924-9. [2]. Jordon M Inloes, et al. Functional Contribution of the Spastic Paraplegia-Related Triglyceride Hydrolase DDHD2 to the Formation and Content of Lipid Droplets. Biochemistry. 2018 Feb 6;57(5):827-838. |