Art. -Nr.: HY-16273A

L-778123 hydrochloride

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC₅₀ values of 2 nM and 98 nM respectively.

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Reinheit: 99.85%
CAS. Nr.: 253863-00-2
Formel: C₂₂H₂₁Cl₂N₅O
Molecular Weight:442.34

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

L-778123 hydrochloride Chemical Structure

CAS. Nr.: 253863-00-2

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Biologische Aktivität
- Beschreibung
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

L-778123 hydrochloride is a dual inhibitor of FPTase and GGPTase-I, with IC₅₀ values of 2 nM and 98 nM respectively.

In Vitro

L-778123 hydrochloride 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 hydrochloride 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 (0-1 μM, 12 h; or 5 μM, 6 h) hydrochloride inhibits H-RAS prenylation in HL-60 cells, and inhibits phosphorylated MEK-1/2 level (5 μM, 24 h)^[3].
L-778123 (0-100 μM, 72 h) hydrochloride 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.

In Vivo

L-778123 (50 mg/kg/day, infusion, 7 days) hydrochloride inhibits both HDJ2 and Rap1A prenylation in PBMCs of dogs, but without inhibition in Ki-Ras prenylation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 253863-00-2
Appearance Solid
Molecular Weight 442.34
Formel C₂₂H₂₁Cl₂N₅O
Color White to off-white
SMILES

N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1.[H]Cl
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (6)

All IFWBCell Proliferation/Viability AssayCell Imaging/StainingBio/Physico-chemical AssayFlow CytometryHistological Imaging/Staining

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Journal Impact Factor

Cell

RNA innate immunity constitutes a barrier for interspecies chimerism. [Abstract]

2026 Jan 8;189(1):23-33.e16. PMID: 41289993
Immunity

Intraepithelial mast cells drive gasdermin C-mediated type 2 immunity. [Abstract]

2024 May 14;57(5):1056-1070.e5. PMID: 38614091

L-778123 hydrochloride 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.
Nat Commun

HMGCS1 drives cholesterol-dependent membrane repair and shields tumor cells from lymphocyte attack. [Abstract]

2026 Jun 5. PMID: 42248910

L-778123 hydrochloride 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.
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 hydrochloride 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-MSCs^M-sec in the presence of L-778123 (10 μM; 16 h). When TNT formation was inhibited using L-778123, CeO₂-MSCs^M-sec failed to effectively alleviate mitochondrial ROS levels of damaged chondrocytes.

L-778123 hydrochloride 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-MSCs^M-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-MSCs^M-sec, indicating the important role of TNTs as transport channels in the treatment process.

L-778123 hydrochloride 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 MSCs^M-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 hydrochloride 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-MSCs^M-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-MSCs^M-sec.
bioRxiv

2025 Jul 29.
bioRxiv

Dynamic mapping of proteome trafficking within and between living cells by TransitID. [Abstract]

2023 Feb 8:2023.02.07.527548. PMID: 36798302

L-778123 hydrochloride 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.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 25 mg/mL (56.52 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 25 mg/mL (56.52 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2607 mL

11.3035 mL

22.6070 mL

5 mM

0.4521 mL

2.2607 mL

4.5214 mL

10 mM

0.2261 mL

1.1304 mL

2.2607 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.25 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.25 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.25 mg/mL (5.09 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS

Solubility: 100 mg/mL (226.07 mM); Suspended solution; Need ultrasonic and adjust pH to 5 with 1M HCl

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact

MedChemExpress (MCE) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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]

[3]. Fredrick O. Onono, et al. The Farnesyltransferase Inhibitor (FTI) L-778,123 Displays Promising Anti-Leukemia Activity. Blood (2008); 112 (11): 2627.

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / H₂O	1 mM	2.2607 mL	11.3035 mL	22.6070 mL	56.5176 mL
	5 mM	0.4521 mL	2.2607 mL	4.5214 mL	11.3035 mL
	10 mM	0.2261 mL	1.1304 mL	2.2607 mL	5.6518 mL
	15 mM	0.1507 mL	0.7536 mL	1.5071 mL	3.7678 mL
	20 mM	0.1130 mL	0.5652 mL	1.1304 mL	2.8259 mL
	25 mM	0.0904 mL	0.4521 mL	0.9043 mL	2.2607 mL
	30 mM	0.0754 mL	0.3768 mL	0.7536 mL	1.8839 mL
	40 mM	0.0565 mL	0.2826 mL	0.5652 mL	1.4129 mL
	50 mM	0.0452 mL	0.2261 mL	0.4521 mL	1.1304 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

L-778123 hydrochloride

6 Cited Publications

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L-778123 hydrochloride

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Publications Citing Use of MedChemExpress (MCE) L-778123 hydrochloride

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

L-778123 hydrochloride

Bioactive Compound Library Max

Bioactive Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Targeted Diversity Library

Metabolic Enzyme Compound Library

Anti-Hematopathy Compound Library

MCE Bioactive Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) L-778123 hydrochloride

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

L-778123 hydrochloride Related Classifications

HY-16273A Related Classifications