Art. -Nr.: HY-10079

CHS-828

(Synonyms: GMX1778)

4 Cited Publications

Kundenbewertung

Based on 4 publication(s) in Google Scholar

CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC₅₀ less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD⁺ and exhibits a potent anticancer activity.

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Reinheit: 99.28%
CAS. Nr.: 200484-11-3
Formel: C₁₉H₂₂ClN₅O
Molecular Weight:371.86

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

CHS-828 Chemical Structure

CAS. Nr.: 200484-11-3

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC50: < 25 nM (NAMPT)^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
A2780	IC₅₀	0.001 μM Compound: 7; GMX1778	Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay Inhibition of NAMPT in human A2780 cells assessed as decrease in cell viability after 72 hrs by SRB assay	[PMID: 27541271]
A2780	IC₅₀	0.005 μM Compound: 1, GMX-1778	Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis Antiproliferative activity against human A2780 cells assessed as growth inhibition after 72 hrs by SRB-based microplate reader analysis	[PMID: 23859118]
A2780	IC₅₀	0.005 μM Compound: 1, GMX-1778, CHS828	Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay Antiproliferative activity against human A2780 cells after 72 hrs by sulforhodamine B assay	[PMID: 24405419]
A2780	IC₅₀	0.005 μM Compound: 2, GMX1778	Cytotoxicity against human A2780 cells after 72 hrs by SRB assay Cytotoxicity against human A2780 cells after 72 hrs by SRB assay	[PMID: 23617784]
A2780	IC₅₀	0.56 nM Compound: 2, CHS828	Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human A2780 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
B16	IC₅₀	280 nM Compound: 18	In vitro antiproliferative activity against B16 cell lines In vitro antiproliferative activity against B16 cell lines	10.1016/S0960-894X(97)10152-4
DLD-1	IC₅₀	2.315 μM Compound: CHS 828	Antiproliferative activity against human DLD-1 cells Antiproliferative activity against human DLD-1 cells	[PMID: 34655985]
DLD-1	IC₅₀	2315 nM Compound: CHS 828	Cytotoxicity against human DLD1 cells after 24 hrs by SRB assay Cytotoxicity against human DLD1 cells after 24 hrs by SRB assay	[PMID: 25147148]
DLD-1	IC₅₀	2315 nM Compound: CHS 828	Anticancer activity against human DLD-1 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human DLD-1 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
DLD-1	IC₅₀	2315 nM Compound: CHS 828	Cytotoxic activity against DLD1 colon cancer cell line Cytotoxic activity against DLD1 colon cancer cell line	[PMID: 14980658]
HA22T cell line	IC₅₀	2067 nM Compound: CHS 828	Cytotoxicity against human HA22T cells after 24 hrs by SRB assay Cytotoxicity against human HA22T cells after 24 hrs by SRB assay	[PMID: 25147148]
HA22T cell line	IC₅₀	2067 nM Compound: CHS 828	Anticancer activity against human HA22T cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HA22T cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
HA22T cell line	IC₅₀	2067 nM Compound: CHS 828	Cytotoxic activity against HA22T liver cancer cell line Cytotoxic activity against HA22T liver cancer cell line	[PMID: 14980658]
HeLa	IC₅₀	0.04 μM Compound: CHS 828	Antiproliferative activity against human HeLa cells Antiproliferative activity against human HeLa cells	[PMID: 34655985]
HepG2	IC₅₀	1245 nM Compound: CHS 828	Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay Cytotoxicity against human HepG2 cells after 24 hrs by SRB assay	[PMID: 25147148]
HepG2	IC₅₀	1245 nM Compound: CHS 828	Anticancer activity against human HepG2 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HepG2 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
HepG2	IC₅₀	1245 nM Compound: CHS 828	Cytotoxic activity against HepG2 liver cancer cell line Cytotoxic activity against HepG2 liver cancer cell line	[PMID: 14980658]
HepG2	IC₅₀	18.3 nM Compound: 2, CHS828	Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis Inhibition of NAMPT in human HepG2 cells using [14C]-nicotinamide/PRPP as substrate assessed as formation of [14C]-nicotinamide mononucleotide after 1 hr by liquid scintillation counting analysis	[PMID: 24164086]
HONE1 cell line	IC₅₀	15 nM Compound: CHS 828	Cytotoxicity against human HONE1 cells after 24 hrs by SRB assay Cytotoxicity against human HONE1 cells after 24 hrs by SRB assay	[PMID: 25147148]
HONE1 cell line	IC₅₀	15 nM Compound: CHS 828	Anticancer activity against human HONE1 cell line assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human HONE1 cell line assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
HONE1 cell line	IC₅₀	15 nM Compound: CHS 828	Cytotoxic activity against HONE1 nasopharyngeal carcinoma cell line Cytotoxic activity against HONE1 nasopharyngeal carcinoma cell line	[PMID: 14980658]
Lewis lung carcinoma cell line	IC₅₀	560 nM Compound: 18	In vitro antiproliferative activity against Lewis cell lines In vitro antiproliferative activity against Lewis cell lines	10.1016/S0960-894X(97)10152-4
MCF7	IC₅₀	0.018 μM Compound: CHS 828	Antiproliferative activity against human MCF7 cells Antiproliferative activity against human MCF7 cells	[PMID: 34655985]
MCF7	IC₅₀	1.6 nM Compound: 2, CHS828	Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay Cytotoxicity against human MCF-7 cells assessed as growth inhibition after 72 hrs by WST-1 assay	[PMID: 24164086]
MCF7	IC₅₀	18 nM Compound: CHS 828	Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human MCF7 cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
MCF7	IC₅₀	18 nM Compound: CHS 828	Cytotoxic activity against MCF breast cancer cell line Cytotoxic activity against MCF breast cancer cell line	[PMID: 14980658]
MCF7	IC₅₀	31 nM Compound: 18	Evaluated in vitro for antiproliferative activity against MCF-7 cell lines model of hormone dependent breast cancer Evaluated in vitro for antiproliferative activity against MCF-7 cell lines model of hormone dependent breast cancer	10.1016/S0960-894X(97)10152-4
NCI-H460	IC₅₀	50 nM Compound: 18	Evaluated in vitro for antiproliferative activity against NIC-H460 cell lines derived from large cell carcinoma of the lung Evaluated in vitro for antiproliferative activity against NIC-H460 cell lines derived from large cell carcinoma of the lung	10.1016/S0960-894X(97)10152-4
NSCLC	IC₅₀	2.7 nM Compound: 18	Evaluated in vitro for antiproliferative activity against NYH cell lines derived from small cell lung cancer Evaluated in vitro for antiproliferative activity against NYH cell lines derived from small cell lung cancer	10.1016/S0960-894X(97)10152-4
NUGC	IC₅₀	25 nM Compound: CHS 828	Cytotoxicity against human NUGC cells after 24 hrs by SRB assay Cytotoxicity against human NUGC cells after 24 hrs by SRB assay	[PMID: 25147148]
NUGC	IC₅₀	25 nM Compound: CHS 828	Anticancer activity against human NUGC cells assessed as cell growth inhibition incubated for 24 hrs Anticancer activity against human NUGC cells assessed as cell growth inhibition incubated for 24 hrs	[PMID: 35694689]
NUGC	IC₅₀	25 nM Compound: CHS 828	Cytotoxic activity against NUGC gastric cancer cell line Cytotoxic activity against NUGC gastric cancer cell line	[PMID: 14980658]
PC-3	IC₅₀	4.4 nM Compound: 2; GMX1778	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 5 days by Cell-titer Glo reagent based assay	[PMID: 28610984]
WALKER	IC₅₀	500 nM Compound: 18	In vitro antiproliferative activity against Walker cell line In vitro antiproliferative activity against Walker cell line	10.1016/S0960-894X(97)10152-4
YOSHIDA	IC₅₀	140 nM Compound: 18	In vitro antiproliferative activity against Yoshida cell lines In vitro antiproliferative activity against Yoshida cell lines	10.1016/S0960-894X(97)10152-4

In Vitro

The phosphoribosyltransferase activity of recombinant NAMPT was sensitive to inhibition by CHS-828 (GMX1778) (IC50 < 25 nM) whereas the adenyltransferase activity of recombinant NMNAT1 was not. The Kd of recombinant NAMPT for GMX1778 labeled with a fluorescent tag (CHS-828 (GMX1778)-Alexa Fluor) was 120 nM. Overexpression of wild-type NAMPT was able to maintain a certain level of NAD+ under conditions of challenge with 3 nM GMX1778, but this effect was lost when cells were exposed to 300 nM CHS-828 (GMX1778)^[1]. CHS-828 (GMX1778) increases intracellular ROS in cancer cells by elevating the superoxide level while decreasing the intracellular NAD(+) level. Notably, CHS-828 (GMX1778) treatment does not induce ROS in normal cells. CHS-828 (GMX1778)-induced ROS can be diminished by adding nicotinic acid (NA) in a NA phosphoribosyltransferase 1 (NAPRT1)-dependent manner^[2].

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

In Vivo

A 4-h iv infusion of NA (120 mg/kg of body weight) did not adversely affect the antitumor activity of a 24-h iv infusion of CHS-828 (GMX1778) at a dose of 150 mg/kg or 650 mg/kg in the NAPRT1-deficient xenograft experiments. CHS-828 (GMX1778) at 650 mg/kg is above the maximum tolerated dose. The administration of NA as a 4-h iv infusion immediately following treatment with 750 mg/kg CHS-828 (GMX1778) reduced the mortality associated with toxic doses of GMX1777^[2].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 200484-11-3
Appearance Solid
Molecular Weight 371.86
Formel C₁₉H₂₂ClN₅O
Color White to off-white
SMILES

N#CN/C(NCCCCCCOC1=CC=C(C=C1)Cl)=N\C2=CC=NC=C2
Synonyms

GMX1778
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (4)

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Journal Impact Factor

Biochem Pharmacol

Scutellarein ameliorates pulmonary arterial hypertension via sirtuin 1 mediated deacetylation of nicotinamide nucleotide transhydrogenase. [Abstract]

2025 Apr 4:116932. PMID: 40189160
Clin Transl Sci

Computational drug discovery pipelines identify NAMPT as a therapeutic target in neuroendocrine prostate cancer. [Abstract]

2024 Sep;17(9):e70030. PMID: 39295559
bioRxiv

2024 Jul 25.
University of Minnesota

2024.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 39 mg/mL (104.88 mM; 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

2.6892 mL

13.4459 mL

26.8918 mL

5 mM

0.5378 mL

2.6892 mL

5.3784 mL

10 mM

0.2689 mL

1.3446 mL

2.6892 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.72 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, 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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 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]. Watson M, et al. The small molecule GMX1778 is a potent inhibitor of NAD+ biosynthesis: strategy for enhanced therapy in nicotinic acid phosphoribosyltransferase 1-deficient tumors. Mol Cell Biol. 2009 Nov;29(21):5872-88. [Content Brief]

[2]. Cerna D, et al. Inhibition of nicotinamide phosphoribosyltransferase (NAMPT) activity by small molecule GMX1778 regulates reactive oxygen species (ROS)-mediated cytotoxicity in a p53- and nicotinic acid phosphoribosyltransferase1 (NAPRT1)-dependent manner. J Biol Chem. 2012 Jun 22;287(26):22408-17. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6892 mL	13.4459 mL	26.8918 mL	67.2296 mL
	5 mM	0.5378 mL	2.6892 mL	5.3784 mL	13.4459 mL
	10 mM	0.2689 mL	1.3446 mL	2.6892 mL	6.7230 mL
	15 mM	0.1793 mL	0.8964 mL	1.7928 mL	4.4820 mL
	20 mM	0.1345 mL	0.6723 mL	1.3446 mL	3.3615 mL
	25 mM	0.1076 mL	0.5378 mL	1.0757 mL	2.6892 mL
	30 mM	0.0896 mL	0.4482 mL	0.8964 mL	2.2410 mL
	40 mM	0.0672 mL	0.3361 mL	0.6723 mL	1.6807 mL
	50 mM	0.0538 mL	0.2689 mL	0.5378 mL	1.3446 mL
	60 mM	0.0448 mL	0.2241 mL	0.4482 mL	1.1205 mL
	80 mM	0.0336 mL	0.1681 mL	0.3361 mL	0.8404 mL
	100 mM	0.0269 mL	0.1345 mL	0.2689 mL	0.6723 mL

Keywords

CHS-828

4 Cited Publications

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CHS-828

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Covalent Screening Library

Human Metabolite Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) CHS-828

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CHS-828

Apoptosis Compound Library

Metabolism/Protease Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Covalent Screening Library

Human Metabolite Library

Heterocyclic Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) CHS-828

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CHS-828 Related Classifications

Art. -Nr.: HY-10079