An inhibitor of SPHK2 (Ki = 9.8 µM); inhibits SPHK2 (IC50 = 60 μM) without affecting SPHK1 activity up to 100 μM but does reduce SPHK1a protein levels in cells via an SPHK1-indirect proteasomal-dependent mechanism at 5-25 µM; inactive against a panel of 20 lipid-regulated kinases at 50 μM; inhibits proliferation of a variety of human cancer cell lines (IC50s = 6

ABC294640 – 25 mg

Brand:
Cayman
CAS:
915385-81-8
Storage:
-20
UN-No:
Non-Hazardous - /

ABC294640 is an inhibitor of sphingosine kinase 2 (SPHK2; Ki = 9.8 μM).{18506} It inhibits SPHK2 (IC50 = 60 μM) without affecting SPHK1 activity up to 100 μM but does reduce SPHK1 isoform a (SPHK1a) protein levels in androgen-independent LNCaP (LNCaP-AI) cells via an SPHK1-indirect, proteasomal-dependent mechanism when used at concentrations ranging from 5 to 25 µM.{56206} ABC294640 is inactive against a panel of 20 lipid-regulated kinases at 50 μM.{18506} It decreases sphingosine-1-phosphate (S1P) production in MDA-MB-231 cells in a concentration-dependent manner. ABC294640 inhibits proliferation of a variety of cancer cells, including HepG2 liver, A-498 kidney, PANC-1 pancreas, and HT-29 colon cells (IC50s = 6, 12.2, 32.8, and 48.1 µM, respectively). It reduces actin filament polymerization in, and cell migration of, A-498 cells in a scratch assay. Oral administration of ABC294640 (35 and 100 mg/kg every other day) reduces tumor growth in a mouse syngeneic model of mammary adenocarcinoma. It also reduces colonic inflammation in mouse and rat models of Crohn’s disease induced by trinitrobenzene sulfonic acid (TNBS).{37136}  

 

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SKU: 10587 - 25 mg Category:

Description

An inhibitor of SPHK2 (Ki = 9.8 µM); inhibits SPHK2 (IC50 = 60 μM) without affecting SPHK1 activity up to 100 μM but does reduce SPHK1a protein levels in cells via an SPHK1-indirect proteasomal-dependent mechanism at 5-25 µM; inactive against a panel of 20 lipid-regulated kinases at 50 μM; inhibits proliferation of a variety of human cancer cell lines (IC50s = 6, 12.2, 32.8, and 48.1 µM, respectively); reduces tumor growth in a mouse syngeneic model of mammary adenocarcinoma at 35 and 100 mg/kg every other day; reduces colonic inflammation in mouse and rat models of Crohn’s disease

Formal name: 3-(4-chlorophenyl)-N-(4-pyridinylmethyl)-tricyclo[3.3.1.13,7]decane-1-carboxamide

Synonyms: 

Molecular weight: 380.9

CAS: 915385-81-8

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 Migration & Metastasis||Research Area|Cancer|Cell Signaling||Research Area|Immunology & Inflammation|Gastric Disease|Crohn’s Disease||Research Area|Lipid Biochemistry|Sphingolipids

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