DO264
- CAS NO.:2301866-59-9
- Empirical Formula: C23H20Cl2F3N5O2S
- Molecular Weight: 558.4
- MDL number: MFCD31812603
- EINECS: 604-604-1
- Update Date: 2023-06-08 09:03:01
What is DO264?
Description
DO264 is an inhibitor of α/β-hydrolase domain-containing protein 12 (ABHD12; IC50 = 11 nM). It inhibits ABHD12-dependent hydrolysis of lysophosphatidylserine (lyso-PS) in mouse brain membrane lysates (IC50 = 2.8 nM) and human THP-1 cells. 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. 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. 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.
The Uses of DO264
DO264 is a potent inhibitor of ABHD12 (α/β-hydrolase domain-containing 12) which shows negligible interaction with other serine hydrolases as determined by activity-based protein profiling.
References
1) Ogasawara?et al.?(2019),?Discovery and Optimization of Selective and in Vivo Active Inhibitors of the Lysophosphatidylserine Lipase α/β-Hydrolase Domain-Containing 12 (ABHD12); J. Med. Chem.,?62?1643 2) Ogasawara?et al.?(2018),?Selective Blockade of the Lyso-PS Lipase ABHD12 Stimulates Immune Responses In Vivo; Nat. Chem. Biol.,?14?1099
Properties of DO264
Boiling point: | 601.5±65.0 °C(Predicted) |
Density | 1.52±0.1 g/cm3(Predicted) |
storage temp. | under inert gas (nitrogen or Argon) at 2–8 °C |
solubility | Soluble in DMSO (up to 30 mg/ml). |
form | solid |
pka | 11.53±0.70(Predicted) |
color | Pale yellow |
Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month. |
Safety information for DO264
Signal word | Warning |
Pictogram(s) |
Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H302:Acute toxicity,oral H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for DO264
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