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KLH45

KLH45 1632236-44-2
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产品信息
产品名称:KLH45 纯度:98% min
CAS NO:1632236-44-2 溶解度:
分子式:C24H25F3N4O2 包装:可按客户要求包装
分子量:458.476 贮存:-20 ℃
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备注说明

KLH45 is an inhibitor of the phospholipase DDHD domain containing 2 (DDHD2; IC50 = 1.3 nM). It is selective for DDHD2 over greater than 50 serine hydrolases, including DDHD1 and Sec23ip, but does inhibit α/β-hydrolase domain-containing protein 6 (ABHD6). It inhibits DDHD2 and ABHD6 in Neuro2A cells when used at a concentration of less than 10 nM and inhibits DDHD2 by greater than 95% at a concentration of 25 nM. KLH45 (2 µM) prevents increases in triacylglycerol (TAG) hydrolase activity in HEK293T cell lysates expressing recombinant DDHD2 and incubated with a radiolabeled TAG substrate. It decreases TAG levels in the CNS of mice when administered at a dose of 20 mg/kg twice per day for four days. KLH45 (2 µM) also reverses DDHD2-induced lipid droplet reduction in COS-7 cells expressing recombinant DDHD2 and loaded with oleic acid.

参考文献
1: Inloes JM, Hsu KL, Dix MM, Viader A, Masuda K, Takei T, Wood MR, Cravatt BF. 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. doi: 10.1073/pnas.1413706111. Epub 2014 Sep 29. PubMed PMID: 25267624; PubMed Central PMCID: PMC4205627.

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