| Identification | Back Directory | [Name]
4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide | [CAS]
695207-56-8 | [Synonyms]
BC-LI-0186
3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide
4-(2,3-dimethyl-5-oxo-4-propan-2-ylpyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide
4-(4-Isopropyl-2,3-dimethyl-5-oxo-2,5-dihydro-1H-pyrazol-1-yl)-N-(2-phenoxyethyl)benzenesulfonamide
Aminoacyl-tRNA Synthetase,RagD,rapamycin-resistant,BCLI0186,tRNA Synthetase, aaRS,H460,KRAS G12D,A549,lung cancer,BC LI 0186,inhibit,Inhibitor,Leucyl-tRNA synthetase | [Molecular Formula]
C22H27N3O4S | [MDL Number]
MFCD05259468 | [MOL File]
695207-56-8.mol | [Molecular Weight]
429.53 |
| Chemical Properties | Back Directory | [Boiling point ]
582.9±60.0 °C(Predicted) | [density ]
1.232±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
10.68±0.50(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Biological Activity]
BC-LI-0186 is a selective blocker of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50 = 46.11 nM) by competing against RagD for LRS VC domain binding (KD = 42.1 nM) without affecting LRS-Vps34LRS-EPRSRagB-RagD associationmTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 inhibits Leu-dependent LRS lysosomal membrane localization (10 μM)RagD GTPase and mTORC1 activation (IC50 = 81.4 nM against Leu-induced S6K phosphorylation)but not ARF1 activationAKT S473 phosphorylationGlu- or Arg-dependent S6K phosphorylationnor the cytosolic and mitochondrial LRS catalytic activities. BC-LI-0186 effectively suppresses the growth of rapamycin-resistant MCT116 MM cancer cells with mTOR-S2035I mutation both in cultures (GI50 = 42.03) and in mice in vivo (by 40% in 2 wks; 20 mg/kg/day i.p.). | [storage]
Store at -20°C |
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