An ABHD12 inhibitor (IC50 = 11 nM); inhibits ABHD-dependent hydrolysis of lyso-PS in mouse brain membrane lysates (IC50 = 2.8 nM) and human THP-1 cells; increases levels of CCL3

DO264 – 10 mg

Brand:
Cayman
CAS:
2301866-59-9
Storage:
-20
UN-No:
Non-Hazardous - /

DO264 is an inhibitor of α/β-hydrolase domain-containing protein 12 (ABHD12; IC50 = 11 nM).{45704} It inhibits ABHD12-dependent hydrolysis of lysophosphatidylserine (lyso-PS) in mouse brain membrane lysates (IC50 = 2.8 nM) and human THP-1 cells.{45705} DO264 increases levels of chemokine (C-C motif) ligand 3 (CCL3), CCL4, TNF-α, and IL-1β in M1-polarized THP-1 macrophages. It potentiates ferroptotic cell death induced by the glutathione peroxidase 4 (GPX4) inhibitor RSL3 in HT1080 fibrosarcoma and SU-DHL-5 B cell lymphoma cells when used at a concentration of 1 μM.{45704,49606} In vivo, DO264 (30 mg/kg per day for four weeks) increases levels of 1-stearoyl-2-hydroxy-sn-glycero-3-PS, 1-arachidonoyl-2-hydroxy-sn-glycero-3-PS, 1-docosanoyl-2-hydroxy-sn-glycero-3-PS, 1-stearoyl-2-arachidonoyl-sn-glycero-3-PS, and 1-oleoyl-2-arachidonoyl-sn-glycero-3-PS in mouse brain.{45705} It increases levels of CCL2, CCL3, and CCL5 in bronchoalveolar lavage fluid (BALF) and decreases survival in a mouse model of infection with lymphocytic choriomeningitis virus (LCMV) clone 13 when administered at a dose of 30 mg/kg.  

 

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Description

An ABHD12 inhibitor (IC50 = 11 nM); inhibits ABHD-dependent hydrolysis of lyso-PS in mouse brain membrane lysates (IC50 = 2.8 nM) and human THP-1 cells; increases levels of CCL3, CCL4, TNF-α, and IL-1β in M1-polarized THP-1 macrophages; increases levels of 1-stearoyl-2-hydroxy-sn-glycero-3-PS, 1-arachidonoyl-2-hydroxy-sn-glycero-3-PS, 1-docosanoyl-2-hydroxy-sn-glycero-3-PS, 1-stearoyl-2-arachidonoyl-sn-glycero-3-PS, and 1-oleoyl-2-arachidonoyl-sn-glycero-3-PS in mouse brain at 30 mg/kg per day for four weeks; increases levels of CCL2, CCL3, and CCL5 in BALF and decreases survival in a mouse model of infection with LCMV clone 13 at 30 mg/kg

Formal name: N-[1-[3-chloro-4-[2-chloro-4-(trifluoromethoxy)phenoxy]-2-pyridinyl]-4-piperidinyl]-N′-3-pyridinyl-thiourea

Synonyms: 

Molecular weight: 558.4

CAS: 2301866-59-9

Purity: ≥98%

Formulation: A solid

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