L-778123 dihydrochloride
Based on 6 publication(s) in Google Scholar
L-778123 dihydrochloride is a dual FPTase and GGPTase-I inhibitor, with IC50s of 2 nM and 98 nM, respectively.
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- CAS. Nr.: 183499-56-1
- Formel: C22H22Cl3N5O
- Molecular Weight:478.80
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) L-778123 dihydrochloride
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Cell Proliferation/Viability Assay
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Flow Cytometry
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Histological Imaging/Staining
Biologische Aktivität
L-778123 dihydrochloride alone does not have obvious cytotoxicity on HT-29 and A549 cell lines (IC50: >100 μM), but can generate synergistic effects with Doxorubicin (HY-15142A), with the decreased IC50s of 1.72 and 1.52 μM respectively[2].
L-778123 dihydrochloride inhibits myeloid leukemia cell proliferation with IC50 values of 0.2 μM-1.8 μM for cell lines, and 0.1 μM-161.8 μM in primary samples[3].
L-778123 dihydrochloride (0-1 μM, 12 h; or 5 μM, 6 h) inhibits H-RAS prenylation in HL-60 cells, and inhibits phosphorylated MEK-1/2 level (5 μM, 24 h)[3].
L-778123 dihydrochloride (0-100 μM, 72 h) inhibits lymphocyte activation (marker: CD71 or CD25) and function in human PBMCs[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 183499-56-1
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Molecular Weight 478.80
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Formel C22H22Cl3N5O
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SMILES
N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1.[H]Cl.[H]Cl
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
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Journal Impact Factor
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Most Recent
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Cell
2026 Jan 8;189(1):23-33.e16. PMID: 41289993 -
Immunity
2024 May 14;57(5):1056-1070.e5. PMID: 38614091
L-778123 dihydrochloride purchased from MedChemExpress. Usage Cited in: Immunity. 2024 May 14;57(5):1056-1070.e5. [Abstract]
Confocal images of CFSE-labeled iIEMCs and CMT-93 cells cocultured in the presence of DMSO or 10 μM L-778123 and after 24 h, immunolabeled with DAPI, E-cadherin, and Mcpt1.
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Nat Commun
HMGCS1 drives cholesterol-dependent membrane repair and shields tumor cells from lymphocyte attack. [Abstract]2026 Jun 5. PMID: 42248910
L-778123 dihydrochloride purchased from MedChemExpress. Usage Cited in: Nat Commun. 2026 Jun 5. [Abstract]
HMGCS1-overexpressed A549-CD19 cells were pre-treated with or without 10 μM L778123 (L-778123) for 12 h before cocultured with CD19 CAR-T for 24 h. The L778123 treatment did not diminish the enhanced resistance to lymphocyte killing conferred by HMGCS1 overexpression.
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ACS Nano
M-Sec Overexpressed Stem Cells Growing Abundant Tunneling Nanotubes for Diverse Active Transferring. [Abstract]2025 Aug 12;19(31):28644-28659. PMID: 40743507
L-778123 dihydrochloride purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Aug 12;19(31):28644-28659. [Abstract]
Representative MitoSOX-Red and JC-1 staining of IL-1β chondrocytes cocultured with CeO2-MSCsM-sec in the presence of L-778123 (10 μM; 16 h). When TNT formation was inhibited using L-778123, CeO2-MSCsM-sec failed to effectively alleviate mitochondrial ROS levels of damaged chondrocytes.
L-778123 dihydrochloride purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Aug 12;19(31):28644-28659. [Abstract]
Quantification of intracellular ATP and ROS levels in IL-1β chondrocytes cocultured with CeO2-MSCsM-sec in the presence of L-778123 (10 μM; 16 h). adding L-778123 during the coculture process remarkably reduced the therapeutic effect of CeO2-MSCsM-sec, indicating the important role of TNTs as transport channels in the treatment process.
L-778123 dihydrochloride purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Aug 12;19(31):28644-28659. [Abstract]
Flow cytometry analysis showing the transfer of MitoTracker Green-labeled mitochondria and FITC-labeled CeO2 from CM-Dil-labeled MSCsM-sec to the cells isolated from the joint cavity. L-778123 (80 mg/kg; i.p.; single administration 3 days before cell injection) reduced the transfer of mitochondria and CeO2 to joint-cavity cells.
L-778123 dihydrochloride purchased from MedChemExpress. Usage Cited in: ACS Nano. 2025 Aug 12;19(31):28644-28659. [Abstract]
Safranin-O staining of knee-joint sections at week 8 in DMM osteoarthritis mice receiving CeO2-MSCsM-sec with L-778123 (80 mg/kg; i.p.; twice weekly for 4 weeks). Following TNT inhibition with L-778123, surface abrasion and disorganized chondrocytes remained, indicating reduced cartilage protection by CeO2-MSCsM-sec.
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bioRxiv
2023 Feb 8:2023.02.07.527548. PMID: 36798302
L-778123 dihydrochloride purchased from MedChemExpress. Usage Cited in: bioRxiv. 2023 Feb 8:2023.02.07.527548. [Abstract]
Western blot detection of specific protein markers in samples after tandem enrichment. GW4869 and L778123 (10 μM 12 h) are small-molecule inhibitors of exosome biogenesis and tunneling nanotube formation, respectively.
Reinheit & Dokumentation
Verweise
[1]. Lobell RB, et al. Preclinical and clinical pharmacodynamic assessment of L-778,123, a dual inhibitor of farnesyl:protein transferase and geranylgeranyl:protein transferase type-I. Mol Cancer Ther. 2002 Jul;1(9):747-758. [Content Brief]
[2]. Ghasemi S, et al. Comparison of Cytotoxic Activity of L778123 as a Farnesyltranferase Inhibitor and Doxorubicin against A549 and HT-29 Cell Lines. Adv Pharm Bull. 2013;3(1):73-77. [Content Brief]
[4]. Si MS, et al. Inhibition of lymphocyte activation and function by the prenylation inhibitor L-778,123. Invest New Drugs. 2005 Jan;23(1):21-9. [Content Brief]
Calculators
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