A selective inhibitor of SPHK2 (Ki = 6.4 µM; IC50s = 4.3 and >10 µM for human recombinant SPHK2 and SPHK1

K145 (hydrochloride) – 1 mg

Brand:
Cayman
CAS:
1449240-68-9
Storage:
-20
UN-No:
Non-Hazardous - /

K145 is a selective inhibitor of sphingosine kinase 2 (SPHK2; Ki = 6.4 µM) with IC50 values of 4.3 and >10 µM for human recombinant SPHK2 and SPHK1, respectively.{41106} It inhibits SPHK2, but not SPHK1, activity in U937 cells when used at a concentration of 10 µM. In vivo, K145 (15 mg/kg, i.p.) inhibits tumor growth in a U937 mouse xenograft model. It also improves glucose tolerance and regulates gluconeogenesis by stimulating insulin-dependent Akt/FoxO1 signaling in a mouse model of insulin resistance induced by dexamethasone (Item No. 11015) when administered at a dose of 30 mg/kg.{41107}  

 

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SKU: 11691 - 1 mg Category:

Description

A selective inhibitor of SPHK2 (Ki = 6.4 µM; IC50s = 4.3 and >10 µM for human recombinant SPHK2 and SPHK1, respectively); inhibits SPHK2 activity in U937 cells at 10 µM; inhibits tumor growth in a U937 mouse xenograft model at 15 mg/kg; improves glucose tolerance and regulates gluconeogenesis by stimulating insulin-dependent Akt/FoxO1 signaling in a mouse model of dexamethasone-induced insulin resistance at 30 mg/kg

Formal name: 3-(2-aminoethyl)-5Z-[3-(4-butoxyphenyl)propylidene]-2,4-thiazolidinedione, monohydrochloride

Synonyms: 

Molecular weight: 384.9

CAS: 1449240-68-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Lipid Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling||Research Area|Cell Biology|Cell Signaling|PI3K/Akt/mTOR Signaling||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Lipid Biochemistry|Sphingolipids

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