SML3893
LCL521 dihydrochlroide
≥95% (HPLC)
동의어(들):
(1R,2R)-2-N-(Tetradecanoylamino)-1-(40-nitrophenyl)-propyl-1,3-O,O-di-(N,N-dimethylamino) acetate dihydrochloride, 1,3-DMG-B13, 1,3-O,O-DMG-B13•2HCl, 1,3-di-DMG-B13, B13: (1R,2R)-2-(tetradecanoylamino)-1-(4′-nitrophenyl)-1,3-propandiol), LCL 521, LCL-521
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크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C31H52N4O7·2HCl
CAS 번호:
Molecular Weight:
665.69
UNSPSC Code:
51111800
MDL number:
NACRES:
NA.21
SMILES string
CN(C)CC(O[C@H](C1=CC=C(C=C1)[N+]([O-])=O)[C@@H](COC(CN(C)C)=O)NC(CCCCCCCCCCCCC)=O)=O.[2HCl]
assay
≥95% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
N,N-dimethyl glycine (DMG) diester prodrug form of the selective acid ceramidase (ACDase) inhibitor B13 for enhanced lysosomal delivery and cellular potency.
LCL521 is the N,N-dimethyl glycine (DMG) diester prodrug form of the selective acid ceramidase (ACDase) inhibitor B13 (no inhibition against NCDase/ASAH2 or AlkCDase/ACER2). The DMG enables efficient and targeted B13 lysosomal delivery, resulting in enhanced cellular ACDase inhibitory potency (by 70% vs 12% in MCF7, respectively, post 1h treatment by 1 μM LCL521 or 10 μM B13) and effective blockage of ceramide (Cer) to sphingosine (Sph) processing (80% vs 0% Sph level drop in MCF7, respectively, post 1h treatment by 1 μM LCL521 or 10 μM B13).
LCL521 is the N,N-dimethyl glycine (DMG) diester prodrug form of the selective acid ceramidase (ACDase) inhibitor B13 (no inhibition against NCDase/ASAH2 or AlkCDase/ACER2). The DMG enables efficient and targeted B13 lysosomal delivery, resulting in enhanced cellular ACDase inhibitory potency (by 70% vs 12% in MCF7, respectively, post 1h treatment by 1 μM LCL521 or 10 μM B13) and effective blockage of ceramide (Cer) to sphingosine (Sph) processing (80% vs 0% Sph level drop in MCF7, respectively, post 1h treatment by 1 μM LCL521 or 10 μM B13).
Disclaimer
Hygroscopic
저장 등급
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Shai White-Gilbertson et al.
Journal of lipid research, 60(7), 1225-1235 (2019-04-17)
Radiation treatment failure or relapse after initial response to chemotherapy presents significant clinical challenges in cancer patients. Escape from initial courses of treatment can involve reactivation of embryonic developmental stages, with the formation of polynuclear giant cancer cells (PGCCs). This
Mladen Korbelik et al.
International journal of cancer, 139(6), 1372-1378 (2016-05-04)
Acid ceramidase has been identified as a promising target for cancer therapy. One of its most effective inhibitors, LCL521, was examined as adjuvant to photodynamic therapy (PDT) using mouse squamous cell carcinoma SCCVII model of head and neck cancer. Lethal
Shai White-Gilbertson et al.
Cancer medicine, 9(9), 3142-3152 (2020-03-07)
Polyploid giant cancer cells (PGCC) represent a poorly understood, small subpopulation of tumor cells that are increasingly being recognized for their critical role in therapy resistance, metastasis, and cancer recurrence. PGCC have the potential to generate progeny through primitive or
Rachael E Clifford et al.
Cells, 9(12) (2020-12-19)
Previous work utilizing proteomic and immunohistochemical analyses has identified that high levels of acid ceramidase (AC) expression confers a poorer response to neoadjuvant treatment in locally advanced rectal cancer. We aimed to assess the radiosensitising effect of biological and pharmacological
Anticancer actions of lysosomally targeted inhibitor, LCL521, of acid ceramidase
PLoS ONE, 12(6) (2017)
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