Cat. No.: HY-16273

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L-778123

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC₅₀s of 2 nM and 98 nM respectively.

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Pureté: 99.92%
CAS No.: 183499-57-2
Formule: C₂₂H₂₀ClN₅O
Masse moléculaire:405.88

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

L-778123 Chemical Structure

CAS No.: 183499-57-2

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (6)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

L-778123 is a dual FPTase and GGPTase-I inhibitor, with IC₅₀s of 2 nM and 98 nM respectively^[1]^[2].

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	1.72 μM Compound: 51; L-788,123	Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay	[PMID: 33228976]
A549	IC₅₀	100.72 μM Compound: 51; L-788,123	Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 33228976]
Cancer cell lines	IC₅₀	2280 nM Compound: 51; L-788,123	Antiproliferative activity against human cancer cell lines harboring KRAS mutation assessed as reduction in cell viability Antiproliferative activity against human cancer cell lines harboring KRAS mutation assessed as reduction in cell viability	[PMID: 33228976]
Cancer cell lines	IC₅₀	70 nM Compound: 51; L-788,123	Antiproliferative activity against human cancer cell lines harboring wild type RAS mutation assessed as reduction in cell viability Antiproliferative activity against human cancer cell lines harboring wild type RAS mutation assessed as reduction in cell viability	[PMID: 33228976]
HT-29	IC₅₀	1.52 μM Compound: 51; L-788,123	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs in presence of doxorubicin by MTT assay	[PMID: 33228976]
HT-29	IC₅₀	125.78 μM Compound: 51; L-788,123	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 33228976]
PSN1	EC₅₀	6300 nM Compound: 1	Effective dose required for half-maximal inhibition of prenylation in PSN-1 cells (Ki-Ras) Effective dose required for half-maximal inhibition of prenylation in PSN-1 cells (Ki-Ras)	[PMID: 14741259]
PSN1	EC₅₀	6760 nM Compound: 1	Effective dose required for half-maximal inhibition of geranylgeranylated protein (Rap1a) in PSN-1 cells Effective dose required for half-maximal inhibition of geranylgeranylated protein (Rap1a) in PSN-1 cells	[PMID: 14741259]
PSN1	EC₅₀	92 nM Compound: 1	Effective dose required for half-maximal inhibition of farnesylated protein (HDJ2) in PSN-1 cells Effective dose required for half-maximal inhibition of farnesylated protein (HDJ2) in PSN-1 cells	[PMID: 14741259]
Rat1	IC₅₀	3 nM Compound: 1	Concentration required to displace 50% of a radiolabeled farnesyltransferase inhibitor from FPTase in cultured Ha-Ras transformed RAT1 cells Concentration required to displace 50% of a radiolabeled farnesyltransferase inhibitor from FPTase in cultured Ha-Ras transformed RAT1 cells	[PMID: 11378366]
Rat1	IC₅₀	3.6 nM Compound: 1	Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells. Displacement of radiolabeled FTI from Farnesyltransferase in cultured Ha-ras transformed RAT1 cells.	[PMID: 14741259]
Rat1	IC₅₀	95 nM Compound: 1	Displacement of radiolabeled FTI from Farnesyltransferase in v-Ha-ras-transformed Rat1 cells. Displacement of radiolabeled FTI from Farnesyltransferase in v-Ha-ras-transformed Rat1 cells.	[PMID: 11965368]

In Vitro

L-778123 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 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) 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) 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) 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 No. 183499-57-2
Appearance Solid
Masse moléculaire 405.88
Formule C₂₂H₂₀ClN₅O
Color White to off-white
SMILES

N#CC1=CC=C(CN2C(CN3CC(N(C4=CC=CC(Cl)=C4)CC3)=O)=CN=C2)C=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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 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 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 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 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 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 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 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.

Solvant et solubilité

In Vitro:

1 M HCl : ≥ 100 mg/mL (246.38 mM)

DMSO : 20 mg/mL (49.28 mM; ultrasonic and adjust pH to 2 with 1 M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" 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

2.4638 mL

12.3189 mL

24.6378 mL

5 mM

0.4928 mL

2.4638 mL

4.9276 mL

10 mM

0.2464 mL

1.2319 mL

2.4638 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 90% Corn Oil

Solubility: ≥ 2.22 mg/mL (5.47 mM); Clear solution

This protocol yields a clear solution of ≥ 2.22 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 (22.2 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 2

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

Solubility: ≥ 2 mg/mL (4.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 3

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

Solubility: ≥ 2 mg/mL (4.93 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

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.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (393 KB)
- English - EN (393 KB)
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- Deutsch - DE (393 KB)
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- 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)
Instruction de manipulation (2659 KB)

Références

[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

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO / 1 M HCl	1 mM	2.4638 mL	12.3189 mL	24.6378 mL	61.5946 mL
	5 mM	0.4928 mL	2.4638 mL	4.9276 mL	12.3189 mL
	10 mM	0.2464 mL	1.2319 mL	2.4638 mL	6.1595 mL
	15 mM	0.1643 mL	0.8213 mL	1.6425 mL	4.1063 mL
	20 mM	0.1232 mL	0.6159 mL	1.2319 mL	3.0797 mL
	25 mM	0.0986 mL	0.4928 mL	0.9855 mL	2.4638 mL
	30 mM	0.0821 mL	0.4106 mL	0.8213 mL	2.0532 mL
	40 mM	0.0616 mL	0.3080 mL	0.6159 mL	1.5399 mL
1 M HCl	50 mM	0.0493 mL	0.2464 mL	0.4928 mL	1.2319 mL
	60 mM	0.0411 mL	0.2053 mL	0.4106 mL	1.0266 mL
	80 mM	0.0308 mL	0.1540 mL	0.3080 mL	0.7699 mL
	100 mM	0.0246 mL	0.1232 mL	0.2464 mL	0.6159 mL

Keywords

L-778123

6 Cited Publications

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L-778123

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) L-778123

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

L-778123

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) L-778123

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

L-778123 Related Classifications

HY-16273 Related Classifications